Journal articles: 'Drugs acting on the central nervous system'

1

Gupta, S. P. "QSAR studies on drugs acting at the central nervous system." Chemical Reviews 89, no. 8 (December 1989): 1765–800. http://dx.doi.org/10.1021/cr00098a007.

Full text

APA, Harvard, Vancouver, ISO, and other styles

2

Samsam, Mohtashem. "Central Nervous System Acting Drugs in Treatment of Migraine Headache." Central Nervous System Agents in Medicinal Chemistry 12, no. 3 (August 1, 2012): 158–72. http://dx.doi.org/10.2174/187152412802430147.

Full text

APA, Harvard, Vancouver, ISO, and other styles

3

Zhu, Xing-Zu. "Development of natural products as drugs acting on central nervous system." Memórias do Instituto Oswaldo Cruz 86, suppl 2 (1991): 173–75. http://dx.doi.org/10.1590/s0074-02761991000600039.

Full text

APA, Harvard, Vancouver, ISO, and other styles

4

ALMEIDA, SEBASTIÃO S., JOHN TONKISS, and JANINA R. GALLER. "Malnutrition and Reactivity to Drugs Acting in the Central Nervous System." Neuroscience & Biobehavioral Reviews 20, no. 3 (January 1996): 389–402. http://dx.doi.org/10.1016/0149-7634(95)00054-2.

Full text

APA, Harvard, Vancouver, ISO, and other styles

5

Jann, Michael W., and Sara R. Grimsley. "Pharmacogenetics of Agents Acting on the Central Nervous System." Journal of Pharmacy Practice 6, no. 1 (February 1993): 2–16. http://dx.doi.org/10.1177/089719009300600103.

Full text

Abstract:

This article will review the various agents affecting the central nervous system (CNS) such as the analgesics, antidepressants, anticonvulsants, antipsychotics, and benzodiazepines. Most of the research in pharmacogenetics with the CNS agents have been conducted in the antidepressants. The cytochrome 450 IID6 isozyme system has been shown to influence the disposition of the antidepressants and antipsychotics. Amitriptyline metabolism to nortriptyline and nortriptyline conversion to its 10-OH metabolite were shown to be influenced by the IID6 isozyme. Interestingly, imipramine metabolism to desipramine is only partially related to the IID6 isozyme. Biotransformation of imipramine to its 2-OH metabolite was shown to be affected by the IID6 isozyme, but its metabolism to the 10-OH remains to be investigated. Of the antipsychotic drugs, haloperidol and thioridazine are two agents most studied. Haloperidol is converted to a reduced metabolite via a ketone reductase enzyme. The reduced metabolite is oxidized back to Haloperidol. This oxidation pathway was reported to be affected by the IID6 isozyme. Thioridazine metabolism to mesoridazine and conversion of codeine to morphine appear to be also influenced by CP-450 IID6. Other 450 isozymes are reported to be involved with other CNS agents.

APA, Harvard, Vancouver, ISO, and other styles

6

Monzani, Agar, Gianfranco Gamberini, Daniela Braghiroli, Maria Di Bella, Lina Raffa, and Maurizio Sandrini. "Sulfonamides Acting on the Central Nervous System, VI." Archiv der Pharmazie 318, no. 4 (1985): 299–304. http://dx.doi.org/10.1002/ardp.19853180404.

Full text

APA, Harvard, Vancouver, ISO, and other styles

7

Kharkar, Prashant S. "Drugs acting on central nervous system (CNS) targets as leads for non-CNS targets." F1000Research 3 (March 21, 2014): 40. http://dx.doi.org/10.12688/f1000research.3-40.v2.

Full text

Abstract:

Innovative drug discovery approaches are currently needed to rejuvenate the shrinking product pipelines of the pharmaceutical companies across the globe. Here a theme is presented – the use of central nervous system (CNS) drugs as leads for non-CNS targets. The approach is related to the use of existing drugs for new indications. Suitable chemical modifications of the CNS drugs abolish their CNS penetration. These novel analogs may then be screened for activity against non-CNS targets. Careful selection of the appropriate structural modifications remains the key to success.

APA, Harvard, Vancouver, ISO, and other styles

8

Garattini, Silvio, and Vittorio Bertele'. "Efficacy, safety and cost of new drugs acting on the central nervous system." European Journal of Clinical Pharmacology 59, no. 1 (March 22, 2003): 79–84. http://dx.doi.org/10.1007/s00228-003-0569-3.

Full text

APA, Harvard, Vancouver, ISO, and other styles

9

Saganuwan, Saganuwan Alhaji. "Chirality of Central Nervous System (CNS) Acting Drugs: A Formidable Therapeutic Hurdle Against CNS Diseases." Central Nervous System Agents in Medicinal Chemistry 19, no. 3 (October 31, 2019): 171–79. http://dx.doi.org/10.2174/1871524919666190624150214.

Full text

Abstract:

Background: Over fifty percent of drugs being used clinically are chiral and 90% of them are racemates. Unfortunately, they have both adverse and beneficial effects on body systems. Methods: Because of the erratic effects of chiral compounds on body functional systems, literature search was carried out with a view to identify CNS chiral drugs, their clinical advantages and disadvantages, unique physicochemical properties and structural modifications into safer drugs. Results: Findings have shown that majority of CNS and non-CNS acting drugs have chiral functional groups that may occur as either dextrorotatory (clockwise) or levorotatory (anticlockwise) or racemates which are inert. Sometimes, the enantiomers (optical isomers) could undergo keto-enol tautomerism, appearing in either acidic or basic or inert form. Chiral CNS acting drugs have agonistic and antagonistic effects, clinical advantages, disadvantages, and special clinical applications, possible modifications for better therapeutic effects and possible synthesis of more potent drugs from racemates. Clockwise chirality may be more effective and safer than the drugs with anticlockwise chirality. When chiral drugs are in racemate state they become inert and may be safer than when they are single. Also, diastereoisomers may be more dangerous than stereoisomers. Conclusion: Therefore, chiral compounds should be adequately studied in lab rodents and primates, and their mechanisms of actions should be comprehensively understood before being used in clinical setting. Since many of them are toxic, their use should be based on principle of individualized medicine. Their molecular weights, functional groups, metabolites, polymers and stereoisomers could be valuable tools for their modifications.

APA, Harvard, Vancouver, ISO, and other styles

10

KONTANI, Hitoshi, Mikiko NAKAGAWA, and Takeshi SAKAI. "Effects of Central Nervous System-Acting Drugs on Urinary Bladder Contraction in Unanesthetized Rats." Japanese Journal of Pharmacology 50, no. 3 (1989): 327–32. http://dx.doi.org/10.1016/s0021-5198(19)42447-5.

Full text

APA, Harvard, Vancouver, ISO, and other styles

11

Saganuwan, Saganuwan A. "Conversion of Benzimidazoles, Imidazothiazoles and Imidazoles into more Potent Central Nervous System Acting Drugs." Central Nervous System Agents in Medicinal Chemistry 20, no. 1 (March 3, 2020): 3–12. http://dx.doi.org/10.2174/1871524919666190621160323.

Full text

Abstract:

Background: Benzimidazole (albendazole), imidazothiazole (levamisole) and imidazole (euconazole) are used in chemotherapy of helminthosis and mycosis respectively, with central nervous system (CNS) side effects. But only a limited number of azole groups are used clinically in the treatment of CNS diseases, which are on increase and could not be cured permanently. Due to increased incidence of more challenging new CNS diseases, there is a need for the synthesis of more potent CNS drugs. Methods: Hence, literature studies were carried out for the identification of common pathways for the synthesis of the three groups of compounds, their CNS properties and the possibility of modifying them to potent CNS drugs. Results: Findings have shown that gloxal with formaldehyde in the presence of ammonia can be converted into imidazole, imidazothiazole and benzimidazole via distillation, condensation, alkylation, acylation, oxidation, cyclization, sulphation and amidation. However, agents such as phosphorus pentoxide, ethanolic potassium hydroxide, sodium hypochlorite, sodium hexafluroaluminate, aniline, calcium acetate, calcium benzoate, sodium hydroxide, aromatic aldehydes, bromoketones, alpha dicarbonyl compounds among others are used as reagents. The furan ring(s) may have a strong capability of penetrating CNS for the treatment of neurological disorders. The products from the three groups have agonistic, antagonistic, mixed agonistic and mixed antagonistic depressant and stimulant activities due to the presence of heteroatoms such as nitrogen, oxygen and sulphur. Imidazole may be the most potent with best characteristics of CNS penetrability and activity followed by imidazothiazole and benzimidazole. Conclusion: Azole group is common to all the three classes and may be responsible for some of their CNS effects. The resultant compounds could act via all neurotransmitters, voltage and ligand-gated ion channels and may be chiral.

APA, Harvard, Vancouver, ISO, and other styles

12

KONTANI, Hitoshi, Mikiko NAKAGAWA, and Takeshi SAKAI. "Effects of central nervous system-acting drugs on urinary bladder contraction in unanesthetized rats." Japanese Journal of Pharmacology 50, no. 3 (1989): 327–32. http://dx.doi.org/10.1254/jjp.50.327.

Full text

APA, Harvard, Vancouver, ISO, and other styles

13

Saganuwan, Saganuwan Alhaji. "Chemistry and Effects of Brainstem Acting Drugs." Central Nervous System Agents in Medicinal Chemistry 19, no. 3 (October 31, 2019): 180–86. http://dx.doi.org/10.2174/1871524919666190620164355.

Full text

Abstract:

Background: Brain is the most sensitive organ, whereas brainstem is the most important part of Central Nervous System (CNS). It connects the brain and the spinal cord. However, a myriad of drugs and chemicals affects CNS with severe resultant effects on the brainstem. Methods: In view of this, a number of literature were assessed for information on the most sensitive part of brain, drugs and chemicals that act on the brainstem and clinical benefit and risk assessment of such drugs and chemicals. Results: Findings have shown that brainstem regulates heartbeat, respiration and because it connects the brain and spinal cord, all the drugs that act on the spinal cord may overall affect the systems controlled by the spinal cord and brain. The message is sent and received by temporal lobe, occipital lobe, frontal lobe, parietal lobe and cerebellum. Conclusion: Hence, the chemical functional groups of the brainstem and drugs acting on brainstem are complementary, and may produce either stimulation or depression of CNS.

APA, Harvard, Vancouver, ISO, and other styles

14

Dinis-Oliveira, Ricardo Jorge. "Usos Lícito e Ilícito dos Fármacos." Acta Médica Portuguesa 27, no. 6 (December 30, 2014): 755. http://dx.doi.org/10.20344/amp.5215.

Full text

Abstract:

Drugs of abuse are a heterogeneous group of xenobiotics or endobiotics that alter synaptic organization in the central nervous system in a transient or permanent basis, often leading to a compulsively use. What unites its members is that they confer pleasure (hedonism) to the abusers, namely by their action in the mesolimbic dopamine system. To exert its effects, different drugs of abuse will act on receptors and neurotransmitter transporters, modeling neurotransmitter release into the synaptic cleft. Besides acting on presynaptic<br />neurons also function in neurotransmitter receptors and ion channels in postsynaptic neurons, thereby modifying the signaling pathways. In this work, the pharmacodynamic and the potential of some psychoactive substances that are typically subjected to abuse in Portugal, is reviewed. With this approach it was also possible a discussion of drugs of abuse that exhibit very different toxicological effects such as stimulants, depressants and hallucinogens. Particularly, the potential to induce dependence and addition, as well as to undergo illicit and licit uses, of central nervous system depressants, stimulants, anticholinergic antiparkinson drugs, opioids, cannabinoids and hallucinogens, is discussed.<br /><strong>Keywords: </strong>Antiparkinson Agents; Central Nervous System Depressants; Cholinergic Antagonists; Analgesics, Opioid; Hallucinogens; Central Nervous System Stimulants.

APA, Harvard, Vancouver, ISO, and other styles

15

Hobara, Norio, Akiharu Watanabe, and Hideo Nagashima. "Effect of Various Central Nervous System-Acting Drugs on Ethanol and Acetaldehyde Metabolism in Rats." Pharmacology 30, no. 6 (1985): 333–38. http://dx.doi.org/10.1159/000138087.

Full text

APA, Harvard, Vancouver, ISO, and other styles

16

Gogol, M., H. Hartmann, S. Wustmann, and A. Simm. "Influence of central nervous system-acting drugs on results of cognitive testing in geriatric inpatients." Zeitschrift für Gerontologie und Geriatrie 47, no. 4 (June 2014): 279–84. http://dx.doi.org/10.1007/s00391-014-0654-5.

Full text

APA, Harvard, Vancouver, ISO, and other styles

17

Borthwick, Mark. "Pharmacology and Pharmacokinetics of Sedative Agents." Journal of the Intensive Care Society 9, no. 3 (October 2008): 253–54. http://dx.doi.org/10.1177/175114370800900315.

Full text

Abstract:

Our understanding of the pharmacology and pharmacokinetics of agents acting on the central nervous system has made considerable advances. This article describes the actions of the drugs most commonly used in critical care units for sedation of critically ill patients.

APA, Harvard, Vancouver, ISO, and other styles

18

2 Versha Parcha, Sukanya Chetri and Shikha Saxena, Versha Parcha. "Evaluation of Central Nervous System Acting Effects of Citrus Peel Essential Oils Extracted Using Enzyme Technology on Rodent Models." Universities' Journal of Phytochemistry and Ayurvedic Heights 1, no. 30 (June 26, 2021): 12–17. http://dx.doi.org/10.51129/ujpah-june2021-30-1(2).

Full text

Abstract:

Abstract-There is growing evidence of measurable effects of essential oils in animal brains and so more clinical research is required to validate their influence on the human central nervous system. This will enable us to discover essential oil-based drugs for treatment of mental illnesses such as depression, anxiety etc. Several methods have been developed to obtain oil from oil-rich plant materials using aqueous enzymatic methods. By using enzymes to mediate the extraction, it is possible to maintain mild conditions and effect superior extraction. The enzymes such as cellulase, hemicellulase, pectinase and protease are the most favourable enzymes for degrading the cell wall in oilseeds to loosen oil sacs embedded in the seed structures. Reduced equipment costs and energy consumption are also potentially possible, since oil and protein may be recovered simultaneously Therefore, the present study is proposed on quality and quantity enhancement of essential oils from citrus peel waste through enzymatic intervention and evaluates their effect on the central nervous system in Rodent Models. As an attempt to obtain the essential oil through hydro distillation HD and hydro distillation enzyme assisted HDEA was carried out. Several experiments have been conducted to determine the optimal process parameters for both methods, i.e., substrate to solvent ratio, extraction temperature, extraction time, enzyme loading, and incubation time etc. to Obtain essential oil from citrus peel collected from the local market of Dehradun. Total yield and physical characteristics like specific Gravity, viscosity, refractive index, acid, Saponification, iodine no etc. were compared. Both samples of oil CA-1 and CA-2 were further screened for their effect on Central Nervous System on the rodent model. Result indicated HDEAnot only improved yield but also has sustainably stimulant effect on the central nervous system as compared to HD. Keywords: Essential oil, Enzymes, Central nervons system.

APA, Harvard, Vancouver, ISO, and other styles

19

Neumaier, Felix, Boris D. Zlatopolskiy, and Bernd Neumaier. "Drug Penetration into the Central Nervous System: Pharmacokinetic Concepts and In Vitro Model Systems." Pharmaceutics 13, no. 10 (September 23, 2021): 1542. http://dx.doi.org/10.3390/pharmaceutics13101542.

Full text

Abstract:

Delivery of most drugs into the central nervous system (CNS) is restricted by the blood–brain barrier (BBB), which remains a significant bottleneck for development of novel CNS-targeted therapeutics or molecular tracers for neuroimaging. Consistent failure to reliably predict drug efficiency based on single measures for the rate or extent of brain penetration has led to the emergence of a more holistic framework that integrates data from various in vivo, in situ and in vitro assays to obtain a comprehensive description of drug delivery to and distribution within the brain. Coupled with ongoing development of suitable in vitro BBB models, this integrated approach promises to reduce the incidence of costly late-stage failures in CNS drug development, and could help to overcome some of the technical, economic and ethical issues associated with in vivo studies in animal models. Here, we provide an overview of BBB structure and function in vivo, and a summary of the pharmacokinetic parameters that can be used to determine and predict the rate and extent of drug penetration into the brain. We also review different in vitro models with regard to their inherent shortcomings and potential usefulness for development of fast-acting drugs or neurotracers labeled with short-lived radionuclides. In this regard, a special focus has been set on those systems that are sufficiently well established to be used in laboratories without significant bioengineering expertise.

APA, Harvard, Vancouver, ISO, and other styles

20

Sá, Matheus Malta de, Kerly Fernanda Mesquita Pasqualoto, and Carlota de Oliveira Rangel-Yagui. "A 2D-QSPR approach to predict blood-brain barrier penetration of drugs acting on the central nervous system." Brazilian Journal of Pharmaceutical Sciences 46, no. 4 (December 2010): 741–51. http://dx.doi.org/10.1590/s1984-82502010000400016.

Full text

Abstract:

Drugs acting on the central nervous system (CNS) have to cross the blood-brain barrier (BBB) in order to perform their pharmacological actions. Passive BBB diffusion can be partially expressed by the blood/brain partition coefficient (logBB). As the experimental evaluation of logBB is time and cost consuming, theoretical methods such as quantitative structure-property relationships (QSPR) can be useful to predict logBB values. In this study, a 2D-QSPR approach was applied to a set of 28 drugs acting on the CNS, using the logBB property as biological data. The best QSPR model [n = 21, r = 0.94 (r² = 0.88), s = 0.28, and Q² = 0.82] presented three molecular descriptors: calculated n-octanol/water partition coefficient (ClogP), polar surface area (PSA), and polarizability (α). Six out of the seven compounds from the test set were well predicted, which corresponds to good external predictability (85.7%). These findings can be helpful to guide future approaches regarding those molecular descriptors which must be considered for estimating the logBB property, and also for predicting the BBB crossing ability for molecules structurally related to the investigated set.

APA, Harvard, Vancouver, ISO, and other styles

21

Farah, Daniela, and Marcelo Cunio Machado Fonseca. "Short-term Evidence in Adults of Anorexigenic Drugs Acting in the Central Nervous System: A Meta-Analysis." Clinical Therapeutics 41, no. 9 (September 2019): 1798–815. http://dx.doi.org/10.1016/j.clinthera.2019.06.005.

Full text

APA, Harvard, Vancouver, ISO, and other styles

22

Abe, Masamitsu, Kazuo Tabuchi, Shin Tanaka, Akira Hodozuka, Katsuzo Kunishio, Naohiko Kubo, and Yukimasa Nishimura. "Capillary hemangioma of the central nervous system." Journal of Neurosurgery 101, no. 1 (July 2004): 73–81. http://dx.doi.org/10.3171/jns.2004.101.1.0073.

Full text

Abstract:

Object. Capillary hemangiomas are benign tumors or tumorlike lesions that originate from blood vessels and have rarely been reported to develop in the brain or spinal cord. The authors summarize the clinical and histological features of capillary hemangiomas of the central nervous system (CNS). Methods. The clinical features, imaging characteristics, and outcomes in 10 patients with CNS capillary hemangiomas were reviewed. Histological studies included immunostaining with CD31, α-smooth muscle actin, vascular endothelial growth factor, and Ki-67 antigen. Three patients with lesions in the brain presented with symptoms of increased intracranial pressure or seizures. Seven patients with lesions in the spinal cord presented with progressive sensorimotor disturbances of the lower limbs. Computerized tomography and magnetic resonance imaging demonstrated well-defined, enhancing lesions associated with marked perifocal edema. Angiography demonstrated hypervascular lesions, which have not recurred after resection. In two cases, multiple satellite lesions resolved after the systemic administration of steroid drugs or interferon-α. Histologically, all lesions were consistent with findings of capillary hemangioma of the skin or soft tissues. The CNS lesions differed significantly from other vascular neoplasms, such as hemangioendotheliomas, hemangiopericytomas, and hemangioblastomas. Conclusions. Capillary hemangiomas of the CNS are benign lesions that can be surgically removed and cured without adjuvant therapy.

APA, Harvard, Vancouver, ISO, and other styles

23

Khan, M. A., Prikuls V. F. Prikuls V.F., N. A. Mikitchenko, O. Yu Smotrina, and Filatova E. V. Filatova E.V. "Physical rehabilitation of children with perinatal lesion of the central nervous system." Fizioterapevt (Physiotherapist), no. 3 (May 25, 2021): 29–39. http://dx.doi.org/10.33920/med-14-2106-04.

Full text

Abstract:

The article is dedicated to non-pharmacological rehabilitation of children with perinatal lesions of the central nervous system. Currently, the main methodological principles of the staged medical rehabilitation of newborns, mainly children with consequences of perinatal damage to the nervous system, have been determined. Special attention should be paid to the issue of the minimum use of drugs in children with perinatal pathology. In this regard, an important task is to develop and scientifically substantiate new non-drug technologies for medical rehabilitation, especially in children under 1 year of age. Medical rehabilitation has the following aims: stimulation of blood circulation in the tissues of the brain, improvement of muscle tone by acting on the central nervous system and the peripheral nervous system, activation of the processes of neuromuscular transmission and improvement of the psychomotor development of a child with perinatal pathology of the central nervous system. Medical rehabilitation of children with perinatal lesions of the central nervous system begins at the earliest possible date and is carried out by specialists of a multidisciplinary rehabilitation team based on an individual medical rehabilitation program. At present, a wide range of non-drug technologies for medical rehabilitation of children with the consequences of perinatal damage to the central nervous system is used: therapeutic gymnastics, massage, kinesitherapy with a neuroreflex component according to the V. Vojta’s method, Bobath therapy. The analysis of publications presented in the review has shown that the inclusion of modern technologies of kinesitherapy and massage in the complex of rehabilitation measures in children with perinatal lesions can increase the effectiveness of rehabilitation measures, reduce the severity of movement disorders, and decrease the incidence of cerebral palsy.

APA, Harvard, Vancouver, ISO, and other styles

24

Trifiro, Gianluca, and Edoardo Spina. "Age-related Changes in Pharmacodynamics: Focus on Drugs Acting on Central Nervous and Cardiovascular Systems." Current Drug Metabolism 12, no. 7 (September 1, 2011): 611–20. http://dx.doi.org/10.2174/138920011796504473.

Full text

APA, Harvard, Vancouver, ISO, and other styles

25

Sagheddu, Claudia, Miriam Melis, Anna Lisa Muntoni, and Marco Pistis. "Repurposing Peroxisome Proliferator-Activated Receptor Agonists in Neurological and Psychiatric Disorders." Pharmaceuticals 14, no. 10 (October 8, 2021): 1025. http://dx.doi.org/10.3390/ph14101025.

Full text

Abstract:

Common pathophysiological mechanisms have emerged for different neurological and neuropsychiatric conditions. In particular, mechanisms of oxidative stress, immuno-inflammation, and altered metabolic pathways converge and cause neuronal and non-neuronal maladaptative phenomena, which underlie multifaceted brain disorders. The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors modulating, among others, anti-inflammatory and neuroprotective genes in diverse tissues. Both endogenous and synthetic PPAR agonists are approved treatments for metabolic and systemic disorders, such as diabetes, fatty liver disease, and dyslipidemia(s), showing high tolerability and safety profiles. Considering that some PPAR-acting drugs permeate through the blood–brain barrier, the possibility to extend their scope from the periphery to central nervous system has gained interest in recent years. Here, we review preclinical and clinical evidence that PPARs possibly exert a neuroprotective role, thereby providing a rationale for repurposing PPAR-targeting drugs to counteract several diseases affecting the central nervous system.

APA, Harvard, Vancouver, ISO, and other styles

26

Fukusumi, Hayato, Yukako Handa, Tomoko Shofuda, and Yonehiro Kanemura. "Small-scale screening of anticancer drugs acting specifically on neural stem/progenitor cells derived from human-induced pluripotent stem cells using a time-course cytotoxicity test." PeerJ 6 (January 4, 2018): e4187. http://dx.doi.org/10.7717/peerj.4187.

Full text

Abstract:

Since the development of human-induced pluripotent stem cells (hiPSCs), various types of hiPSC-derived cells have been established for regenerative medicine and drug development. Neural stem/progenitor cells (NSPCs) derived from hiPSCs (hiPSC-NSPCs) have shown benefits for regenerative therapy of the central nervous system. However, owing to their intrinsic proliferative potential, therapies using transplanted hiPSC-NSPCs carry an inherent risk of undesired growth in vivo. Therefore, it is important to find cytotoxic drugs that can specifically target overproliferative transplanted hiPSC-NSPCs without damaging the intrinsic in vivo stem-cell system. Here, we examined the chemosensitivity of hiPSC-NSPCs and human neural tissue—derived NSPCs (hN-NSPCs) to the general anticancer drugs cisplatin, etoposide, mercaptopurine, and methotrexate. A time-course analysis of neurospheres in a microsphere array identified cisplatin and etoposide as fast-acting drugs, and mercaptopurine and methotrexate as slow-acting drugs. Notably, the slow-acting drugs were eventually cytotoxic to hiPSC-NSPCs but not to hN-NSPCs, a phenomenon not evident in the conventional endpoint assay on day 2 of treatment. Our results indicate that slow-acting drugs can distinguish hiPSC-NSPCs from hN-NSPCs and may provide an effective backup safety measure in stem-cell transplant therapies.

APA, Harvard, Vancouver, ISO, and other styles

27

El-Ragehy, N. A., A. M. El-Kosasy, S. S. Abbas, and S. Z. El-Khateeb. "Polymeric membrane electrodes for selective determination of the central nervous system acting drugs fluphenazine hydrochloride and nortriptyline hydrochloride." Analytica Chimica Acta 418, no. 1 (August 2000): 93–100. http://dx.doi.org/10.1016/s0003-2670(00)00941-7.

Full text

APA, Harvard, Vancouver, ISO, and other styles

28

Woollard, A., N. Waters, S. Waters, J. Kullingsjö, P. Svensson, T. Andreasson, and C. Sonesson. "Q06 Multivariate classification of central nervous system-acting drugs based on in vivo response patterns – profile of pridopidine." Journal of Neurology, Neurosurgery & Psychiatry 83, Suppl 1 (August 29, 2012): A56.2—A56. http://dx.doi.org/10.1136/jnnp-2012-303524.176.

Full text

APA, Harvard, Vancouver, ISO, and other styles

29

Barbui, Corrado, and Silvio Garattini. "Regulatory policies on medicines for psychiatric disorders: is Europe on target?" British Journal of Psychiatry 190, no. 2 (February 2007): 91–93. http://dx.doi.org/10.1192/bjp.bp.106.024794.

Full text

Abstract:

SummaryThe European Medicines Agency (EMEA) is the regulatory body that provides the institutions of the European Community with the best possible scientific advice on the quality, safety and efficacy of medicinal products. Drugs approved by the EMEA are automatically marketable in all the European member states. Since the beginning of the EMEA's activities a number of drugs acting on the central nervous system obtained marketing authorisation. This editorial highlights some aspects of the EMEA rules that may negatively affect the evaluation of medicines for psychiatric disorders.

APA, Harvard, Vancouver, ISO, and other styles

30

Urmila, Aswar, Patil Rashmi, Ghag Nilam, and Bodhankar Subhash. "Recent Advances in the Endogenous Brain Renin-Angiotensin System and Drugs Acting on It." Journal of the Renin-Angiotensin-Aldosterone System 2021 (November 30, 2021): 1–21. http://dx.doi.org/10.1155/2021/9293553.

Full text

Abstract:

The RAS (renin-angiotensin system) is the part of the endocrine system that plays a prime role in the control of essential hypertension. Since the discovery of brain RAS in the seventies, continuous efforts have been put by the scientific committee to explore it more. The brain has shown the presence of various components of brain RAS such as angiotensinogen (AGT), converting enzymes, angiotensin (Ang), and specific receptors (ATR). AGT acts as the precursor molecule for Ang peptides—I, II, III, and IV—while the enzymes such as prorenin, ACE, and aminopeptidases A and N synthesize it. AT1, AT2, AT4, and mitochondrial assembly receptor (MasR) are found to be plentiful in the brain. The brain RAS system exhibits pleiotropic properties such as neuroprotection and cognition along with regulation of blood pressure, CVS homeostasis, thirst and salt appetite, stress, depression, alcohol addiction, and pain modulation. The molecules acting through RAS predominantly ARBs and ACEI are found to be effective in various ongoing and completed clinical trials related to cognition, memory, Alzheimer’s disease (AD), and pain. The review summarizes the recent advances in the brain RAS system highlighting its significance in pathophysiology and treatment of the central nervous system-related disorders.

APA, Harvard, Vancouver, ISO, and other styles

31

Sicras, Antoni, and Ramón Morillo Verdugo. "Concomitant use of direct-acting antivirals (DDAs) and central nervous system drugs in current chronic hepatitis C patient profile." Journal of Hepatology 73 (August 2020): S332. http://dx.doi.org/10.1016/s0168-8278(20)31167-3.

Full text

APA, Harvard, Vancouver, ISO, and other styles

32

El-Gendy, A. E., M. G. El-Bardicyy, H. M. Loutfy, and M. F. El-Tarras. "Flow Injection Analysis of Pharmaceutical Compounds. VI. Determination of Some Central Nervous System Acting Drugs by UV-Spectrophotometric Detection." Spectroscopy Letters 26, no. 9 (November 1993): 1649–60. http://dx.doi.org/10.1080/00387019308010764.

Full text

APA, Harvard, Vancouver, ISO, and other styles

33

Nagahama, Masahiro, and Jun Sakurai. "Effect of drugs acting on the central nervous system on the lethality in mice of Clostridium perfringens epsilon toxin." Toxicon 31, no. 4 (April 1993): 427–35. http://dx.doi.org/10.1016/0041-0101(93)90178-l.

Full text

APA, Harvard, Vancouver, ISO, and other styles

34

Abdel-Rahman, Abdel A., Robert G. Carroll, and Mahmoud M. El-Mas. "Role of the sympathetic nervous system in the alcohol–guanabenz hemodynamic interaction." Canadian Journal of Physiology and Pharmacology 70, no. 9 (September 1, 1992): 1217–24. http://dx.doi.org/10.1139/y92-169.

Full text

Abstract:

The present study evaluated the contribution of the sympathetic nervous system to the adverse hemodynamic action of ethanol on hypotensive responses in conscious unrestrained spontaneously hypertensive rats. Ethanol caused a dose-related attenuation of the hypotensive effect of guanabenz. An equivalent hypotensive response to sodium nitroprusside was not influenced by ethanol, which indicates a potential specific interaction between ethanol and guanabenz. Alternatively, it is possible that a preexisting high sympathetic nervous system activity, which occurred during nitroprusside infusion, may mask a sympathoexcitatory action of ethanol. Further, ethanol (1 g/kg) failed to reverse the hypotensive effect of the ganglionic blocker hexamethonium. This suggests that a centrally mediated sympathoexcitatory action of ethanol is involved, at least partly, in the reversal of hypotension. In addition, the antagonistic interaction between ethanol and guanabenz seems to take place within the central nervous system and involves opposite effects on central sympathetic tone. Finally, changes in plasma catecholamines provide supportive evidence for the involvement of the sympathetic nervous system in this interaction. In a separate group of conscious spontaneously hypertensive rats, ethanol (1 g/kg) reversed the guanabenz-evoked decreases in blood pressure and plasma catecholamine levels. It is concluded that (i) ethanol adversely interacts with centrally acting antihypertensive drugs through a mechanism that involves a directionally opposite effect on sympathetic activity, and (ii) a sympathetically mediated pressor effect of ethanol is enhanced in the presence of an inhibited central sympathetic tone.Key words: spontaneously hypertensive rats, ethanol, catecholamines, guanabenz, hexamethonium.

APA, Harvard, Vancouver, ISO, and other styles

35

Kontani, Hitoshi, and Ryozo Koshiura. "The effects of drugs acting on central nervous systems on the rat urinary bladder contraction in vivo." Japanese Journal of Pharmacology 39 (1985): 358. http://dx.doi.org/10.1016/s0021-5198(19)63880-1.

Full text

APA, Harvard, Vancouver, ISO, and other styles

36

Matsuda, Hiromi, Hiroo Shimura, Yasuo Watanabe, Hiroyuki Matsunaga, Nobuyuki Imanishi, Hiroko Tsuji, Megumi Izumisawa, and Takeshi Shibuya. "Relation between endocrinologic status and behavior in female animals under the influence of drugs acting on the central nervous system." Japanese Journal of Pharmacology 43 (1987): 222. http://dx.doi.org/10.1016/s0021-5198(19)58468-2.

Full text

APA, Harvard, Vancouver, ISO, and other styles

37

Dass, Ervilla. "A study of clinical information of various package inserts: an approach to encourage adverse drug reaction reporting and emphasis on black box warning." International Journal of Basic & Clinical Pharmacology 7, no. 7 (June 22, 2018): 1232. http://dx.doi.org/10.18203/2319-2003.ijbcp20182424.

Full text

Abstract:

Background: The package insert (PI) is important for providing accurate and reliable product information which is essential for the safe and effective use of medications.Methods: A total number of 115 PIs from pharmacological drug class such as antibiotics, drugs acting on central nervous system and drugs acting on endocrine system were collected from pharmacy store. Contents and presentation of the PIs was critically evaluated by comparing the information as listed in the Drugs and Cosmetics Rules, 1945.Results: The results were expressed under headings as listed in the Drugs and Cosmetics Rules, 1945. The information in the package inserts was inadequate in many aspects; for example, adverse drug reactions were not mentioned completely, information for special population and guidelines for use of the drugs also was lacking. Moreover, black box warning was seen only in few PI. For PI of antibiotics; legibility 80%, use in special populations 76.66%, undesirable effects 46.66%. For PI of CNS of legibility 60%, use in special populations 73.33%, undesirable effects 70%. For PI of endocrine system of legibility 70%, use in special populations 70%, undesirable effects 36.66%.Conclusions: The results reveal that, information relevant to the safe and effective use of medication was not mentioned in the analyzed package inserts. It is, therefore, recommended to update the existing package inserts based on criteria mentioned in the Schedule D of Drug and Cosmetic Act, 1945.

APA, Harvard, Vancouver, ISO, and other styles

38

R., Bauer, Lauer R., Linz B., Pittner F., Peschek G.A., Ecker G.F., Friedl P., and Noe C.R. "An in vitro Model for Blood Brain Barrier Permeation." Scientia Pharmaceutica 70, no. 4 (November 22, 2002): 317–22. http://dx.doi.org/10.3797/scipharm.aut-02-30.

Full text

Abstract:

The ability to permeate accross the blood brain barrier (BBB) is essential for drugs acting on the central nervous system (CNS). Thus, systems that allow rapid and inexpensive screening of the BBB-permeability properties of novel lead compounds are of great importance for speeding up the drug discovery process in the CNS-area. We used immortalized porcine brain microvessel endothelial cells (PBMECICl-2) to develop a model for measurement of blood-brain barrier permeation of CNS active drugs. Investigation of different cell culture conditions showed, that a system using C6 astrocyte glioma conditioned medium and addition of a cyclic AMP analog in combination with a type IV phosphodiesterase inhibitor (R020-1724) leads to cell layers with transendothelial electrical resistance values up to 300 Ω.cm2. Permeability studies with U-[14C]sucroseg ave a permeability coefficient Pe of 3.24 + 0.14 × 10−4 cm/min, which is in good agreement to published values and thus indicates the formation of tight junctions in vitro.

APA, Harvard, Vancouver, ISO, and other styles

39

Finnerup, Nanna Brix, Rohini Kuner, and Troels Staehelin Jensen. "Neuropathic Pain: From Mechanisms to Treatment." Physiological Reviews 101, no. 1 (January 1, 2021): 259–301. http://dx.doi.org/10.1152/physrev.00045.2019.

Full text

Abstract:

Neuropathic pain caused by a lesion or disease of the somatosensory nervous system is a common chronic pain condition with major impact on quality of life. Examples include trigeminal neuralgia, painful polyneuropathy, postherpetic neuralgia, and central poststroke pain. Most patients complain of an ongoing or intermittent spontaneous pain of, for example, burning, pricking, squeezing quality, which may be accompanied by evoked pain, particular to light touch and cold. Ectopic activity in, for example, nerve-end neuroma, compressed nerves or nerve roots, dorsal root ganglia, and the thalamus may in different conditions underlie the spontaneous pain. Evoked pain may spread to neighboring areas, and the underlying pathophysiology involves peripheral and central sensitization. Maladaptive structural changes and a number of cell-cell interactions and molecular signaling underlie the sensitization of nociceptive pathways. These include alteration in ion channels, activation of immune cells, glial-derived mediators, and epigenetic regulation. The major classes of therapeutics include drugs acting on α2δ subunits of calcium channels, sodium channels, and descending modulatory inhibitory pathways.

APA, Harvard, Vancouver, ISO, and other styles

40

Raevsky, O. A., S. L. Solodova, O. E. Raevskaya, Y. V. Liplavskiy, and R. M. Mannhold. "Computer classification models on the relationship between chemical structures of compounds and drugs with their blood brain barrier penetration." Biomeditsinskaya Khimiya 58, no. 3 (2012): 246–56. http://dx.doi.org/10.18097/pbmc20125803246.

Full text

Abstract:

Ability of drugs to cross blood-brain barrier (BBB) (BBB+ for BBB-penetrating and BBB- for non-penetrating compounds) is one of the most important properties of chemicals acting on the central nervous system (CNS). This work presents the results of modelling of the relationship between chemicals structure and BBB-crossing ability. The data set included 1513 compounds BBB+/- (1276 BBB+ and 237 BBB-). Computer modelling of structure-activity relationship was realized by two directions: using the "read-across" method and linear discriminant analysis (LDA) based on physico-chemical descriptors. It was found that a sum of donor-acceptor factors is the principal parameter, which define BBB penetration.

APA, Harvard, Vancouver, ISO, and other styles

41

Monteiro, Cristina, Beatriz Dias, and Maria Vaz-Patto. "Headache as an Adverse Reaction to the Use of Medication in the Elderly: A Pharmacovigilance Study." International Journal of Environmental Research and Public Health 18, no. 5 (March 7, 2021): 2674. http://dx.doi.org/10.3390/ijerph18052674.

Full text

Abstract:

There is a consensus that elderly individuals are quite vulnerable to adverse drug reactions (ADRs), and headaches are one of the most frequent clinical presentations of central nervous system problems in the general population, which can be an ADR. The purpose of our work was to analyze reports of “headache” associated ADRs in the elderly sent to the Portuguese Pharmacovigilance System (PPS), and also which drugs were more frequently associated with this adverse reaction. A retrospective analysis of suspected ADR reports involving patients aged 65 years or older received by the PPS in the last 10 years was conducted. A search of all the terms associated with the High Level Term “headache” was performed. All duplicate reports were excluded from the analysis. A total of 155 ADRs reports were included, in which 15 reported isolated “headache” as suspected ADR, while the remaining 140 ADRs reports reported “headache” together with several other adverse reactions. Most reports of “headache” ADR occurred in women (74.8%; n = 116). About half (46.5%; n = 72) of the ADR reports were considered serious. Anti-viral medication, anti-depressants, anti-dyslipidemic agents and central nervous system-acting analgesics were the most frequent drugs associated with “headache” ADR reports in this population. In elderly patients, most ADR reports involving headaches occurred in women and a high percentage (46.5%) were considered serious. Thus, it is important that healthcare professionals pay more attention to headaches reported as ADRs in the elderly and drugs suspected to cause them, in order to increase knowledge about this type of reaction and contribute towards safely using drugs in this age group.

APA, Harvard, Vancouver, ISO, and other styles

42

NAKAJIMA, Masaharu, Tomoko OHTA, Nozomi KAWAKAMI, Susumu YAMATO, Kenji SHIMADA, Hiroshi MIYAZAKI, Akira HONDA, et al. "DETERMINATION OF VALPROIC ACID IN TEAR BY GCQ -ASSESSEMENT OF THE CONCENTRATIONS OF DRUGS ACTING ON THE CENTRAL NERVOUS SYSTEM IN TEAR-." Drug Metabolism and Pharmacokinetics 13, supplement (1998): 120–21. http://dx.doi.org/10.2133/dmpk.13.supplement_120.

Full text

APA, Harvard, Vancouver, ISO, and other styles

43

NAKASHIMA, EMI, MASAMI TAKEDA, JUNKO ISHIZAKI, KOICHI YOKOGAWA, RYO MATSUSHITA, and FUJIO ICHIMURA. "Development of Radioreceptor Assay for Microdetermination of Drugs Acting on the Central Nervous System and its Application to a Pharmacokinetics in Rats." Japanese Journal of Hospital Pharmacy 19, no. 2 (1993): 111–18. http://dx.doi.org/10.5649/jjphcs1975.19.111.

Full text

APA, Harvard, Vancouver, ISO, and other styles

44

Billard, Valerie. "Pharmacokinetic-pharmacodynamic relationship of anesthetic drugs: from modeling to clinical use." F1000Research 4 (November 18, 2015): 1289. http://dx.doi.org/10.12688/f1000research.6601.1.

Full text

Abstract:

Anesthesia is a combination of unconsciousness, amnesia, and analgesia, expressed in sleeping patients by limited reaction to noxious stimulations. It is achieved by several classes of drugs, acting mainly on central nervous system. Compared to other therapeutic families, the anesthetic drugs, administered by intravenous or pulmonary route, are quickly distributed in the blood and induce in a few minutes effects that are fully reversible within minutes or hours. These effects change in parallel with the concentration of the drug, and the concentration time course of the drug follows with a reasonable precision mathematical models based on the Fick principle.Therefore, understanding concentration time course allows adjusting the dosing delivery scheme in order to control the effects. The purpose of this short review is to describe the basis of pharmacokinetics and modeling, the concentration-effects relationship, and drug interactions modeling to offer to anesthesiologists and non-anesthesiologists an overview of the rules to follow to optimize anesthetic drug delivery.

APA, Harvard, Vancouver, ISO, and other styles

45

Filatova, E. S., Sh F. Erdes, and E. G. Filatova. "Central regulation of pain in patients with joint disease and approaches to therapy." Terapevticheskii arkhiv 88, no. 12 (December 15, 2016): 159–64. http://dx.doi.org/10.17116/terarkh20168812159-164.

Full text

Abstract:

The paper reviews investigations studies that have demonstrated that chronic pain syndrome is mixed in rheumatic diseases. The nervous system is involved in its pathogenesis with different frequency and different mechanisms. Under the influence of afferent pain impulses from damaged joints, there are changes in the excitability of spinal cord neurons, which is called central sensitization (CS). A number of patients have enhanced CS and clinical manifestations as neuropathic sensitive phenomena. The mixed model of the development of chronic pain in joint diseases and its presence along with nociceptive (inflammatory) and neuropathic pain components may explain the discrepancy between joint inflammatory and structural changes and pain intensity, the presence of distant pain and sensitive disorders in the areas outside the joint, and sometimes the efficiency of anti-inflammatory therapy. The presence of the neuropathic pain component serves as a rationale for combined therapy by adding centrally acting drugs, such as anticonvulsants.

APA, Harvard, Vancouver, ISO, and other styles

46

Marlier, Didier. "Doping in Racing Pigeons (Columba livia domestica): A Review and Actual Situation in Belgium, a Leading Country in This Field." Veterinary Sciences 9, no. 2 (January 22, 2022): 42. http://dx.doi.org/10.3390/vetsci9020042.

Full text

Abstract:

Pigeon racing is a sport in which trained homing pigeons (Columba livia domestica) are released between 60 and 1200 km from their loft and then have to return home as quickly as possible. The first race was held in 1818 in Belgium and since then, Belgium has led the world in pigeon breeding. Unfortunately, as in other sports, doping has become a major issue and doping controls have been implemented. This review provides information about pigeon racing, rules from the Royal Federation Colombophile of Belgium, and laws applicable in Belgium as doping control issues cannot be understood without including them as part of pigeon racing. The main pharmacological data concerning corticoids, non-steroidal anti-inflammatory drugs, anabolic steroids, pain relievers and narcotic analgesics, bronchodilators and β-agonists, drugs acting on the central nervous system and other performance-enhancing drugs, in addition to methods relevant to doping in pigeons are presented. Moreover, the chosen matrix and analytical methods are described.

APA, Harvard, Vancouver, ISO, and other styles

47

Dabiré, Hubert, and Christine Richer. "Implication of the Central Nervous System in the Systemic and Regional Hemodynamics of Two Centrally Acting Hypotensive Drugs, Flesinoxan and Clonidine, in the Rat." Journal of Cardiovascular Pharmacology 18, no. 4 (October 1991): 605–13. http://dx.doi.org/10.1097/00005344-199110000-00018.

Full text

APA, Harvard, Vancouver, ISO, and other styles

48

Yadav, Yogesh C., Kamla Pathak, and Devender Pathak. "Review on Preclinical and Clinical Evidence of Food (Beverages, Fruits and Vegetables) and Drug Interactions: Mechanism and Safety." Current Drug Therapy 15, no. 1 (January 14, 2020): 12–27. http://dx.doi.org/10.2174/1574885514666190126141424.

Full text

Abstract:

Background:The therapeutic potency and efficacy of drugs can be affected by a patient’s dietary habit. The food composition and their nutritional value interact with drugs that lead to alteration of the therapeutic response of drugs in patients.Objective:This present review is an attempt to illustrate clinical reports of food-drug interaction. Further, it also highlights specific interaction mechanism(s) and the safety thereof.Methods:Through the search engine “Scopus”; literature on recent advances in food and drug interactions includes almost all therapeutic categories such as antimicrobials, antiviral, antifungal, antihistamines, anticoagulants, non-steroidal anti-inflammatory drugs, and drugs acting on the central nervous system and cardiovascular system.Results:Preclinical and clinical studies that have been conducted by various researchers affirm significant drug-food interactions across the various therapeutic categories of drugs. Preclinical studies have documented the effects of food, milk products, alcohols, fruit and vegetables on the drug absorption, metabolizing enzymes and drug transporters. The clinical studies on fruits/vegetables and drugs interactions report significant alteration in therapeutic response.Conclusion:Based on the preclinical and clinical reports, it can be concluded that the interaction of food with drug(s) significantly alters their therapeutic potential. The inputs from clinical practitioners to elucidate potential risk of food-drug interaction need to be intensified in order to prevent adverse clinical consequences.

APA, Harvard, Vancouver, ISO, and other styles

49

AMANITI (Ε.Μ. ΑΜΑΝΙΤΗ), E. M., I. SAVVAS (Ι. ΣΑΒΒΑΣ), and N. DIAKAKIS (Ν. ΔΙΑΚΑΚΗΣ). "Pain assessment and treatment in equines." Journal of the Hellenic Veterinary Medical Society 61, no. 2 (March 22, 2018): 134. http://dx.doi.org/10.12681/jhvms.14882.

Full text

Abstract:

Current concepts in pain on animals suggest that -at least- mammals perceive and experience pain like humans do. Pain receptors are the free nerve endings. Qualitative analysis and interpretation is done in brain cortex (somatosensory area), while nociception may be done in lower centres. Pain may be physiological or clinical. In physiological pain, short acting noxious stimuli act on nociceptors and produce pain, but without any neurophysiological modification. In clinical pain, mostly intense noxious stimuli bring alterations in neuronal physiology, in central nervous system (central sensitization), as well as in peripheral nervous system (peripheral sensitization). Eventually, pain threshold is reduced and hyperalgesia is established. Clinical pain may be inflammatory or neuropathic. According to its origin, it may be somatic (skin, bones, joints, muscles), which is acute and may be accurately localized, or visceral (from the abdominal and thoracic organs), which is blunt and diffuse. Post-operative pain mayprolong hospitalization and increase morbidity. Pain management is mandatory for humane, legal and medical reasons. The latter include elimination of side effects of catecholamine production, facilitation of healing and restoration of the animal's normal functions (diet, self-care, etc.), which in general reduce the response to stress. Moreover, organ function is improved and morbidity is reduced. As a result, peri-operative analgesia may improve health, as long as most analgesic techniques improve organ function post-operatively. The first indication of pain in animals is behavioural alteration. In chronic pain, metabolic disturbances may alsooccur. In normal equines, it seems that there are variations among individuals. In general, it is easier to diagnose an acute abdominal pain than a chronic pain in joints, tendons or bones. In acute pain, the horse develops special facial expression. The animal looksbackwards and kicks the ground. Peripheral somatic pain may produce acute signs. Pain is definitely treated only after diagnosing itscause. However, it may also be treated symptomatically with analgesics and local denervations. Additionally, trans-cutaneous electrical nerve stimulation (TENS) of peripheral nerves or other sights of central nervous system may alleviate pain (electroanalgesia). Finally,acupuncture maybe applied. Among the analgesic drugs, in equines, opioids (morphine, methadone, pethidine, butorphanile) produce very good analgesia and mild sedation. Respiratory and intestinal contractility depression is common side effect. Central nervous system excitations maybe seen, especially after morphine administration. Local anaesthetics produce excellent analgesia and maybe used pre- (pre-emptive analgesia), intra- (to reduce general anaesthetic dose rates) and post-operatively. a2-Adrenergic agonists produce analgesia, mainly visceral. They are very good analgesics in cases of colics, whereas their sedative effects reduce the incidence of self-trauma. Their major disadvantage is cardiovascular depression. Non-steroidal anti-inflammatory drugs (NSAIDs) have very good anti-inflammatory properties. They are used in cases of acute pain, traumatic or surgical, as well as in chronic pain.

APA, Harvard, Vancouver, ISO, and other styles

50

Kocsis, Pál, István Gyertyán, János Éles, Judit Laszy, Nikolett Hegedüs, Dávid Gajári, Levente Deli, Zsófia Pozsgay, Szabolcs Dávid, and Károly Tihanyi. "Vascular Action as the Primary Mechanism of Cognitive Effects of Cholinergic, CNS-Acting Drugs, a Rat phMRI BOLD Study." Journal of Cerebral Blood Flow & Metabolism 34, no. 6 (March 19, 2014): 995–1000. http://dx.doi.org/10.1038/jcbfm.2014.47.

Full text

Abstract:

Concordant results of functional magnetic resonance imaging (fMRI) and behavioral tests prove that some non-blood-brain barrier-penetrating drugs produce robust central nervous system (CNS) effects. The anticholinergic scopolamine interferes with learning when tested in rats, which coincides with a negative blood-oxygen-level-dependent (BOLD) change in the prefrontal cortex (PFC) as demonstrated by fMRI. The peripherally acting butylscopolamine also evokes a learning deficit in a water-labyrinth test and provokes a negative BOLD signal in the PFC. Donepezil—a highly CNS-penetrating Cholinesterase inhibitor—prevents the negative BOLD and cognitive deficits regardless whether the provoking agent is scopolamine or butylscopolamine. Interestingly, the non-BBB-penetrating Cholinesterase inhibitor neostigmine also prevents or substantially inhibits those cognitive and fMRI changes. Intact cerebral blood flow and optimal metabolism are crucial for the normal functioning of neurons and other cells in the brain. Drugs that are not BBB penetrating yet act on the CNS highlight the importance of unimpaired circulation, and point to the cerebral vasculature as a primary target for drug action in diseases where impaired circulation and consequently suboptimal energy metabolism are followed by upstream pathologic events.

APA, Harvard, Vancouver, ISO, and other styles

Journal articles on the topic 'Drugs acting on the central nervous system'

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles