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Journal articles on the topic 'Piperazine Piperazine Drugs Rats Rats'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Delon, Annie, Serge Bouquet, Francois Huguet, Valerie Brunet, Philippe Courtois, and William Couet. "Pharmacokinetic-Pharmacodynamic Contributions to the Convulsant Activity of Fluoroquinolones in Rats." Antimicrobial Agents and Chemotherapy 43, no. 6 (1999): 1511–15. http://dx.doi.org/10.1128/aac.43.6.1511.

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ABSTRACT The in vivo convulsant activities in rats of five representative fluoroquinolones (FQs), norfloxacin, enoxacin, sparfloxacin, fleroxacin, and pefloxacin, were compared. The experimental approach allowed distinction between the drugs’ ability to reach the pharmacological receptors at the level of the central nervous system (pharmacokinetic contribution) and their ability to interact with these receptors (pharmacodynamic contribution). The presence of a methyl group on the piperazine moiety decreased the pharmacodynamic contribution to the convulsant activity by severalfold, and the rat

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Васина, Е. Ю., С. Г. Чефу, and Н. Н. Петрищев. "The effect of Notrombel on FeCl3-induced carotid artery thrombosis in rats." ZHurnal «Patologicheskaia fiziologiia i eksperimental`naia terapiia», no. 2() (May 27, 2019): 50–55. http://dx.doi.org/10.25557/0031-2991.2019.02.50-55.

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Цель работы - изучение влияния Нотромбела (ЗАО «Вертекс», Санкт-Петербург, РФ) на развитие экспериментального тромбоза. Методика. Опыты выполнены на крысах-самцах Вистар массой 250-270 г. Нотромбел вводили внутривенно и интрагастрально в течение 10 сут (курсовая доза 25, 50 и 100 мг/кг). В качестве препаратов сравнения использовали ацетилсалициловую кислоту (АСК) и Клопидогрел (курсовая доза 10,5 и 20 мг/кг соответственно). Тромбоз сонной артерии вызывали 60-секундной аппликацией 20% FeCl3. Кровоток регистрировали методом высокочастотной ультразвуковой допплерографии («Минимакс-Допплер-К» Санк

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Kubacka, Monika, Szczepan Mogilski, Monika Zadrożna та ін. "MH-76, a Novel Non-Quinazoline α1-Adrenoceptor Antagonist, but Not Prazosin Reduces Inflammation and Improves Insulin Signaling in Adipose Tissue of Fructose-Fed Rats". Pharmaceuticals 14, № 5 (2021): 477. http://dx.doi.org/10.3390/ph14050477.

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Background: Quinazoline α1-adrenoceptors antagonists have been shown to exert moderately favorable effects on the metabolic profile in hypertensive patients. However, based on AntiHypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) results, they are no longer recommended as a first line therapy of hypertension. Recent studies have shown that quinazoline-based α1-adrenoceptors antagonists (prazosin, doxazosin) induce the apoptosis and necrosis, which may be responsible for ALLHAT outcomes; however, these effects were proven to be independent of α1-adrenoceptor block

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van Lookeren Campagne, Menno, Jeroen B. Verheul, Klaas Nicolay, and Robert Balázs. "Early Evolution and Recovery from Excitotoxic Injury in the Neonatal Rat Brain: A Study Combining Magnetic Resonance Imaging, Electrical Impedance, and Histology." Journal of Cerebral Blood Flow & Metabolism 14, no. 6 (1994): 1011–23. http://dx.doi.org/10.1038/jcbfm.1994.133.

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We explored the therapeutic potentials of two N-methyl-d-aspartate (NMDA) receptor antagonists in vivo using different techniques. NMDA injected into the striatum of neonatal rats (20 nmol/0.5 μl) induced a rapid increase in the diffusion-weighted (DW) image intensity, spreading over a large part of the ipsilateral hemisphere. Subcutaneous injection of the NMDA receptor antagonist MK-801 (1 mg/kg) or d-( E)-4-(3-phosphono-2-prop-enyl)-2-piperazine-carboxylic acid (D-CPPene; 1.5 mg/kg) reversed both the volume and the grading of the NMDA-induced hyperintensity of DW images, the reversal by MK-8

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Jiang, Xiaomei, Xiaomei Ling, Fangbin Han, Runtao Li, and Jingrong Cui. "Studies on the metabolism of 4-methyl-piperazine-1-carbodithioc acid 3-cyano-3,3-diphenylpropyl ester hydrochloride in rats by high-performance liquid chromatography/electrospray ionization tandem mass spectrometry." Journal of Pharmaceutical and Biomedical Analysis 44, no. 5 (2007): 1127–32. http://dx.doi.org/10.1016/j.jpba.2007.05.026.

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6

Manzini, Stefano, Francesca Perretti, Paola Boni, Gabriele Barbanti, Damiano Turini, and Carlo Alberto Maggi. "In vitro and in vivo studies on the effects of the alpha-adrenoceptor blocker IP/66 (1-(2-ethoxy-2-(3? -pyridyl)ethyl)-4-(2?-methoxy-phenyl)piperazine) on urethral tone in rats." Drug Development Research 23, no. 1 (1991): 35–46. http://dx.doi.org/10.1002/ddr.430230104.

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Ismail, Djauhar, Utomo Utomo, Sugeng Yuwono, and Noerhayati S. "The Use of Anthelmintics in the Treatmenlt of Ascariasis." Paediatrica Indonesiana 16, no. 9-10 (2019): 391–5. http://dx.doi.org/10.14238/pi16.9-10.1976.391-5.

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Ninety-seven children with Ascariasis were treated at randomly with Piperazine, Tetramisole, and Pyrantel pamoate in a single dose with cure rates of 59%, 62%, and 88%, respectively. In the children who were not cured, a reduction in egg count of nearly 80% was found in all three treatment groups. The results of this study showed that Pyrantel pamoate is the most effective of the three drugs.

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8

Zenner, Lionel. "Effective eradication of pinworms (Syphacia muris, Syphacia obvelata and Aspiculuris tetraptera) from a rodent breeding colony by oral anthelmintic therapy." Laboratory Animals 32, no. 3 (1998): 337–42. http://dx.doi.org/10.1258/002367798780559202.

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An oral combination of piperazine and ivermectin was used over a 6-week period for treating three different colonies of mice or rats infested with Syphacia obvelata, Syphacia muris or Aspiculuris tetraptera. No acute toxic effect was found in transgenic lines of mice or rats with these products in a preliminary trial. The colonies were treated with piperazine, 2.1 mg/ml in tap water for 2 weeks, then with ivermectin, 0.007 mg/ml, in tap water for the third and fourth weeks, and finally with piperazine for two further weeks. Hygiene measures such as a complete cage change, thorough disinfection

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Sasamori, Hitomi, Naoya Nishitani, Yu Ohmura, and Mitsuhiro Yoshioka. "Blonanserin and 1-(2-Pyriidinyl)-piperazine suppress impulsive action in rats." Proceedings for Annual Meeting of The Japanese Pharmacological Society 94 (2021): 3—P1–25. http://dx.doi.org/10.1254/jpssuppl.94.0_3-p1-25.

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Kim, Eun-Yeong, Keewon Yu, Kyungmi Choi, Hyung Eun Yu, Soo Jin Oh, and Kiho Lee. "Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats." Biological & Pharmaceutical Bulletin 38, no. 8 (2015): 1161–68. http://dx.doi.org/10.1248/bpb.b15-00044.

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11

Gorokhova, Larisa G., Nadezhda N. Mikhailova, Anna G. Zhukova, and Tatyana D. Logunova. "Pre-clinical evaluation of metabolic and morphological changes in the body induced by 4-chlorobenzhydryl pip." Hygiene and sanitation 99, no. 7 (2020): 745–49. http://dx.doi.org/10.47470/0016-9900-2020-99-7-745-749.

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Introduction. A significant medical and social challenge in occupational health poses a risk of chemical intoxication in the industrial synthesis of new drug compounds.The aim of the work was a pre-clinical study of metabolic and morphological changes in acute and subchronic exposure of 4-chlorobenzhydryl piperazine on the body, which will allow early diagnosis of health problems in workers in workshops where the reaction synthesis of piperazine compounds are used and carried out.Material and methods. A complex of toxic-hygienic and biochemical studies was carried out. The object of the resear

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12

Lee, Jaeok, Song Wha Chae, A. Reum Oh, et al. "Effects of Piperazine Derivative on Paclitaxel Pharmacokinetics." Pharmaceutics 11, no. 1 (2019): 23. http://dx.doi.org/10.3390/pharmaceutics11010023.

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Paclitaxel (PTX) is an anticancer agent that is used to treat many cancers but it has a very low oral bioavailability due, at least in part, to the drug efflux transporter, P-glycoprotein (P-gp). Therefore, this study was performed to enhance oral bioavailability of PTX. In this study, we investigated the effects of several piperazine derivatives on P-gp function in vitro. Compound 4 was selected as the most potent P-gp inhibitor from the in vitro results for examining the pharmacokinetic (PK) changes of PTX in rats. Compound 4 increased the AUCinf of PTX without alterations in the Cmax value.

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Monti, Martina, Valerio Ciccone, Aurora Pacini, et al. "Anti-hypertensive property of a nickel-piperazine/NO donor in spontaneously hypertensive rats." Pharmacological Research 107 (May 2016): 352–59. http://dx.doi.org/10.1016/j.phrs.2016.03.033.

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Shrivastava, Alpa, Ajaya Kumar Singh, Neerja Sachdev, Dilip R. Shrivastava, and Surendra Prasad. "Micellar oxidative transformation of ciprofloxacin: a kinetic investigation." Environmental Chemistry 14, no. 4 (2017): 231. http://dx.doi.org/10.1071/en17034.

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Environmental contextPollution of the aquatic environment by drugs results not only during their manufacture, but also from the excretion of drug residues and the discharge of expired drugs by households and hospitals. The transformation of ciprofloxacin, one of the leading antibiotic drugs, in the presence of surfactants has been investigated. The results provide a better understanding of how ciprofloxacin degrades in aquatic environments by considering the effect of omnipresent surfactants. AbstractThe kinetics of the oxidative transformation, i.e. oxidative degradation, of ciprofloxacin (CI

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15

Sullivan, Dexter W., Shayne C. Gad, Bryan Laulicht, Sasha Bakhru, and Solomon Steiner. "Nonclinical Safety Assessment of PER977." International Journal of Toxicology 34, no. 4 (2015): 308–17. http://dx.doi.org/10.1177/1091581815590667.

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A new molecular entity, PER977 (di-arginine piperazine), is in clinical development as an anticoagulant reversal agent for new oral anticoagulants and heparins. The good laboratory practices (GLP)-compliant studies were conducted to evaluate the toxicity of PER977 and its primary metabolite, 1,4-bis(3-aminopropyl)piperazine (BAP). PER977 and BAP were negative for systemic toxicity in dogs and rats. PER977 was rapidly eliminated from the blood with little to no accumulation. PER977 was negative for genotoxicity and did not alter neurological, respiratory, or cardiovascular function. Maximum tol

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Senda, Toshihiko, Kiyoshi Matsuno, and Shiro Mita. "The suppression of potassium cyanide-induced mortality by the increase of extracellular acetylcholine level in the brain." Canadian Journal of Physiology and Pharmacology 78, no. 8 (2000): 645–48. http://dx.doi.org/10.1139/y00-034.

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We examined whether potassium cyanide (KCN)-induced mortality in mice was regulated by acetylcholine transmission in the brain. Our novel compound, (±)-1-(1,2-diphenyl)ethyl-4-[2-(3,4-dimethoxyphenyl)ethyl]piperazine dihydrochloride (SA3251), suppressed KCN-induced mortality in mice. In parallel, SA3251 increased the cortical and hippocampal extracellular acetylcholine level in conscious, freely-moving rats. Interestingly, the time course patterns of these two events induced by SA3251 correlated. These results suggest that the central cholinergic system plays an important role in the suppressi

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17

Marjanović, S. Đorđe, Danica Bogunović, Mirjana Milovanović, et al. "Antihelminic Activity of Carvacrol, Thymol, Cinnamaldehyde and P-Cymen Against the Free-Living Nematode Caenorhabditis elegans and Rat Pinworm Syphacia muris." Acta Veterinaria 68, no. 4 (2018): 445–56. http://dx.doi.org/10.2478/acve-2018-0036.

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Abstract In the present study we tested the dose andh time dependence of the antinematodal effects of carvacrol and tyhmol on Caenorabditis elegans, and the efficacy of carvacrol, thymol, p-cymene and cinnamaldehyde,which were administrated in the drinking water of rats naturally infected with the pinworm Syphacia muris. The control treatment of the infected rats was carried out with piperazine. Thymol caused a dose and time-dependent mortality in adult C. elegans. The value of the Median Lethal Concentration (LC50) of thymol was 117.9nM after 24h and 62.89 nM after 48h of exposure. Carvacrol

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18

Ghasi, S., AU Mbah, PU Nze, E. Nwobodo, AO Ogbonna, and G. Onuaguluchi. "Interventional role of piperazine citrate in barium chloride induced ventricular arrhythmias in anaesthetized rats." Biomedical Research - India 20, no. 3 (2009): 186. http://dx.doi.org/10.4103/0970-938x.54839.

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19

Zuideveld, Klaas P., Jasna Rusiç-Pavletiç, Hugo J. Maas, Lambertus A. Peletier, Piet H. Van der Graaf, and Meindert Danhof. "Pharmacokinetic-Pharmacodynamic Modeling of Buspirone and Its Metabolite 1-(2-Pyrimidinyl)-piperazine in Rats." Journal of Pharmacology and Experimental Therapeutics 303, no. 3 (2002): 1130–37. http://dx.doi.org/10.1124/jpet.102.036798.

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20

Broqua, Pierre, Véronique Baudrie, Marie-Thérèse Bluet-Pajot, and Francis Chaouloff. "Buspirone, ipsapirone and 1-(2-pyrimidinyl)-piperazine decrease cold-induced thyrotropin secretion in rats." European Journal of Pharmacology 204, no. 2 (1991): 141–47. http://dx.doi.org/10.1016/0014-2999(91)90698-p.

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21

Lijinsky, William, and Robert M. Kovatch. "Carcinogenic effects in rats of nitrosopiperazines administered intravesically: possible implications for the use of piperazine." Cancer Letters 74, no. 1-2 (1993): 101–3. http://dx.doi.org/10.1016/0304-3835(93)90050-j.

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22

Sugimoto, Yumi, Jun Yamada, Tomoko Yoshikawa, and Kazuyoshi Horisaka. "Effects of the receptor agonist 1-(3-chlorophenyl)piperazine on plasma glucose levels of rats." European Journal of Pharmacology 307, no. 1 (1996): 75–80. http://dx.doi.org/10.1016/0014-2999(96)00189-6.

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23

Rowland, Neil E., Jonathan D. Roth, Megan R. McMullen, Aashish Patel, and Anna T. Cespedes. "Dexfenfluramine and norfenfluramine: comparison of mechanism of action in feeding and brain Fos-ir studies." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 278, no. 2 (2000): R390—R399. http://dx.doi.org/10.1152/ajpregu.2000.278.2.r390.

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Dexfenfluramine (dF) and dexnorfenfluramine (dNF), its metabolite, are anorectic agents that release serotonin (5-HT) and may have a direct postsynaptic action. The effects on the anorectic effects of dF and dNF of either acute ( p-chlorophenylalanine, PCPA) or chronic (5,7-dihydroxytryptamine, 5,7-DHT) brain 5-HT depletions were studied in rats and compared with the actions of a 5-HT uptake inhibitor (fluoxetine) and 5-HT1B/2C receptor agonists [1-(3-trifluoromethyl-phenyl)-piperazine and 1-(3-chlorophenyl) piperazine]. The anorexia caused by these agonists was enhanced in rats with 5,7-DHT l

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24

Demir Özkay, Ümide, Özgür Devrim Can, Begüm Nurpelin Sağlık, and Nazlı Turan. "A benzothiazole/piperazine derivative with acetylcholinesterase inhibitory activity: Improvement in streptozotocin-induced cognitive deficits in rats." Pharmacological Reports 69, no. 6 (2017): 1349–56. http://dx.doi.org/10.1016/j.pharep.2017.06.009.

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25

Haleem, Darakhshan J. "Function specific supersensitivity of m-chlorophenyl piperazine-induced serotonergic neurotransmission in female compared to male rats." Life Sciences 52, no. 25 (1993): PL279—PL284. http://dx.doi.org/10.1016/0024-3205(93)90693-w.

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26

Zhou, Qi, Zhongchuan Tan, Desen Yang, et al. "Improving the Solubility of Aripiprazole by Multicomponent Crystallization." Crystals 11, no. 4 (2021): 343. http://dx.doi.org/10.3390/cryst11040343.

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Aripiprazole (ARI) is a third-generation antipsychotic with few side effects but a poor solubility. Salt formation, as one common form of multicomponent crystals, is an effective strategy to improve pharmacokinetic profiles. In this work, a new ARI salt with adipic acid (ADI) and its acetone hemisolvate were obtained successfully, along with a known ARI salt with salicylic acid (SAL). Their comprehensive characterizations were conducted using X-ray diffraction and differential scanning calorimetry. The crystal structures of the ARI-ADI salt acetone hemisolvate and ARI-SAL salt were elucidated

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Righi, Mohamed, and Gilles Gauthier. "Natural infection by intestinal cestodes: variability and effect on growth in Greater Snow Goose goslings (Chen caerulescens atlantica)." Canadian Journal of Zoology 80, no. 6 (2002): 1077–83. http://dx.doi.org/10.1139/z02-089.

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We determined the species of intestinal helminths in Greater Snow Goose (Chen caerulescens atlantica) goslings and examined annual variability in infection levels over a 5-year period on Bylot Island, Nunavut. The intestines of 112 wild goslings collected when near fledging were examined. We also evaluated the effect of intestinal parasites on growth and behaviour of captive goslings in a controlled experiment. In 2000, one group (n = 11) was treated with anthelmintic drugs (Piperazine 52 for nematodes and Droncit® for cestodes) and the other (n = 14) was used as a control. Four hymenolepidid

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28

Dolan, Sean B., Ritu A. Shetty, Michael J. Forster, and Michael B. Gatch. "Impure but not inactive: Behavioral pharmacology of dibenzylpiperazine, a common by-product of benzylpiperazine synthesis." Journal of Psychopharmacology 32, no. 7 (2018): 802–10. http://dx.doi.org/10.1177/0269881118780613.

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Background: Substituted piperazines comprise a substantial proportion of the novel psychoactive substance market. Among the most widely abused piperazine compounds are meta-chlorophenylpiperazine (mCPP), tri-fluoromethylphenylpiperazine (TFMPP), and, especially, benzylpiperazine (BZP), which are commonly incorporated, either alone or in combination, in illicit “party pills” or “ecstasy” formulations. Illicit synthesis of BZP often results in production of an impure by-product dibenzylpiperazine (DBZP), which frequently appears alongside BZP in these formulations; however, despite its ubiquity,

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29

Ghasi, S. I., I. K. Umana, A. O. Ogbonna, M. O. Nwokike, and S. Ufelle. "Cardioprotective effects of animal grade piperazine citrate on isoproterenol induced myocardial infarction in wistar rats: Biochemical and histopathological evaluation." African Journal of Pharmacy and Pharmacology 14, no. 8 (2020): 285–93. http://dx.doi.org/10.5897/ajpp2020.5164.

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Salga, Muhammad Saleh, Hapipah Mohd Ali, Mahmood Ameen Abdulla, and Siddig Ibrahim Abdelwahab. "Acute Oral Toxicity Evaluations of Some Zinc(II) Complexes Derived from 1-(2-Salicylaldiminoethyl)piperazine Schiff Bases in Rats." International Journal of Molecular Sciences 13, no. 2 (2012): 1393–404. http://dx.doi.org/10.3390/ijms13021393.

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31

Amano, Manabu, Arata Goto, Atsuko Sakai, et al. "Comparison of the Anticonflict Effect of Buspirone and Its Major Metabolite l-(2-Pyrimidinyl)-Piperazine (1-PP) in Rats." Japanese Journal of Pharmacology 62, no. 2 (1993): 199–202. http://dx.doi.org/10.1254/jjp.62.199.

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32

De Simoni, Maria Grazia, Luca Imeri, Ada De Luigi, Fabio Fodritto, and Silvio Garattini. "Effect of buspirone and its metabolite 1-(2-Pyrimydinyl)-piperazine on hippocampal serotoninergic system, studied in freely moving rats." Life Sciences 46, no. 3 (1990): 197–205. http://dx.doi.org/10.1016/0024-3205(90)90105-z.

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AWATA, Norio, Tsuneo KAWASHIMA, Osamu SATOMI, et al. "Placental Transfer and Mammary Excretion of 1-(Bis(4-fluorophenyl)-methyl)-4-(2,3,4-trimethoxybenzyl)piperazine Dihydrochloride(KB-2796) in Rats." Drug Metabolism and Pharmacokinetics 9, no. 4 (1994): 536–46. http://dx.doi.org/10.2133/dmpk.9.536.

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Martin, P. "1-(2-Pyrimidinyl)-piperazine may alter the effects of the 5-HT1A agonists in the learned helplessness paradigm in rats." Psychopharmacology 104, no. 2 (1991): 275–78. http://dx.doi.org/10.1007/bf02244191.

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Rauhala, P., J. J. Idanpaan-Heikkila, A. Lang, R. K. Tuominen, and P. T. Mannisto. "Cold exposure attenuates effects of secretagogues on serum prolactin and growth hormone levels in male rats." American Journal of Physiology-Endocrinology and Metabolism 268, no. 4 (1995): E758—E765. http://dx.doi.org/10.1152/ajpendo.1995.268.4.e758.

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The stimulatory effect of morphine, dexmedetomidine (an alpha 2-adrenoceptor agonist), 1-(3-chlorophenyl)-piperazine (m-CPP, a 5-HT1B agonist), U-50488H (a kappa-opioid receptor agonist), pimozide (a dopamine antagonist), and restraint stress on prolactin and growth hormone (GH) secretion was compared during cold exposure (4 degrees C) and under basal conditions (30 degrees C) in male rats. Rectal temperature was also measured. The stimulatory effect of morphine, dexmedetomidine, m-CPP, and partially U-50488H on prolactin secretion was attenuated in rats kept at 4 degrees C. Cold exposure did

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Dhevaraj, J., S. Vembu, S. Pazhamalai, and M. Gopalakrishnan. "“Design and Synthesis of Some Cyclic Carbohydrates with Norfloxacin as Surface moiety. A Study of Sustained Relax of Drugs”." Oriental Journal of Chemistry 35, no. 2 (2019): 577–90. http://dx.doi.org/10.13005/ojc/350211.

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Biocompatible and biodegradable sustained drug delivery system has been constructed from reaction between norfloxacin and cyclodextrin through secondary amine of piperazine ring and hydroxyl group of the carbohydrate. Covalent bond polymeric structure is designed by the help of chloroacetyl chloride, target dendrimer formed by removing two hydrochloride molecules. The development of cyclodextrin core drug delivery system with twenty one norfloxacin surface moiety has been synthesized by only two steps. The synthesized polymeric structure was thoroughly studied by NMR, FT-IR, MALDI and UV- spec

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De Deurwaerdère, Philippe, and Marie-Françoise Chesselet. "Nigrostriatal Lesions Alter Oral Dyskinesia and c-Fos Expression Induced by the Serotonin Agonist 1-(m-Chlorophenyl)piperazine in Adult Rats." Journal of Neuroscience 20, no. 13 (2000): 5170–78. http://dx.doi.org/10.1523/jneurosci.20-13-05170.2000.

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Shi, Huiyan, Chenzhi Hou, Liqiang Gu, et al. "Influence of pretreatment of piperazine ferulate on pharmacokinetic parameters of methotrexate in methotrexate-induced renal injury model rats by HPLC-MS." Asian Journal of Pharmaceutical Sciences 12, no. 2 (2017): 202–8. http://dx.doi.org/10.1016/j.ajps.2016.08.010.

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Zhang, Hao, Rong Sun, Xin-Yong Liu, et al. "A Tetramethylpyrazine Piperazine Derivate CXC137 Prevents Cell Injury in SH-SY5Y Cells and Improves Memory Dysfunction of Rats with Vascular Dementia." Neurochemical Research 39, no. 2 (2013): 276–86. http://dx.doi.org/10.1007/s11064-013-1219-5.

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40

Jumani, R. S., K. Bessoff, M. S. Love, et al. "A Novel Piperazine-Based Drug Lead for Cryptosporidiosis from the Medicines for Malaria Venture Open-Access Malaria Box." Antimicrobial Agents and Chemotherapy 62, no. 4 (2018): e01505-17. http://dx.doi.org/10.1128/aac.01505-17.

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ABSTRACTCryptosporidiosis causes life-threatening diarrhea in children under the age of 5 years and prolonged diarrhea in immunodeficient people, especially AIDS patients. The standard of care, nitazoxanide, is modestly effective in children and ineffective in immunocompromised individuals. In addition to the need for new drugs, better knowledge of drug properties that drivein vivoefficacy is needed to facilitate drug development. We report the identification of a piperazine-based lead compound forCryptosporidiumdrug development, MMV665917, and a new pharmacodynamic method used for its charact

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SHIMOHARA, Koichi, Hiromichi NIIDA, and Susumu OKABE. "Effects of KB-5492, 1-(3,4,5-Trimethoxybenzyl)-4-((4-Methoxyphenyl)oxycarbonylmethyl)piperazine Monofumarate Monohydrate, on Gastric Lesions and Gastric Secretion in Rats." Japanese Journal of Pharmacology 53, no. 2 (1990): 275–79. http://dx.doi.org/10.1254/jjp.53.275.

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Kong, Detao, Siting Wang, Xiaomei Ling, Runtao Li, and Jingrong Cui. "Determination of Anti-Tumor Agent TM208, 4-Methyl-piperazine-1-carbodithioc Acid 3-Cyano-3,3-diphenylpropyl Ester Hydrochloride, in Rats by LC." Chromatographia 70, no. 11-12 (2009): 1721–25. http://dx.doi.org/10.1365/s10337-009-1402-7.

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Protiva, Miroslav, Antonín Dlabač, Martin Valchář, Stanislav Wildt, Irena Červená, and Zdeněk Šedivý. "Potential noncataleptic neuroleptic agents; 2,6-Dichloro-, 2,7-dichloro- and 2,8-dichloro-10-piperazino-10,11-dihydrodibenzo[b,f]thiepins." Collection of Czechoslovak Chemical Communications 51, no. 1 (1986): 156–66. http://dx.doi.org/10.1135/cccc19860156.

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Substitution reactions of 2,6,10-trichloro-, 2,7,10-trichloro- and 2,8,10-trichloro-10,11-dihydrodibenzo[b,f]thiepin (Vabc) with 1-(2-hydroxyethyl)piperazine, 1-methylpiperazine and 1-benzylpiperazine gave the title compounds IIabc, IIIab and IVab. The new chloro compounds Va and Vb were obtained in 6 steps starting from reactions of 2,5-dichloroacetophenone with 2-chlorothiophenol or 3-chlorothiophenol. Compounds IIabc are 6-chloro, 7-chloro and 8-chloro derivatives of the noncataleptic neuroleptic agent docloxythepin (I). They are almost devoid of cataleptic activity and do not inhibit the a

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KAWASHIMA, Tsuneo, Norio AWATA, Osamu SATOMI, et al. "Absorption, distribution and excretion of 1-(bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl) piperazine dihydrochloride (KB-2796) after single oral administration in rats." Drug Metabolism and Pharmacokinetics 5, no. 5 (1990): 723–37. http://dx.doi.org/10.2133/dmpk.5.723.

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Tsutsumi, H., M. Katagi, A. Miki, et al. "Isolation, identification and excretion profile of the principal urinary metabolite of the recently banned designer drug 1-(3-trifluoromethylphenyl)piperazine (TFMPP) in rats." Xenobiotica 35, no. 1 (2005): 107–16. http://dx.doi.org/10.1080/00498250400020335.

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Jiang, X., Y. Bai, X. Ling, F. Han, R. Li, and J. Cui. "Simultaneous Determination of 4-Methyl-Piperazine-1-Carbodithioc Acid 3-Cyano-3,3-Diphenylpropyl Ester Hydrochloride and its Major Metabolite in Rats by HPLC." Journal of Chromatographic Science 48, no. 2 (2010): 125–29. http://dx.doi.org/10.1093/chromsci/48.2.125.

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Sauer, Dirk, Edgar Weber, Guido Lüönd, Fernando Da Silva, and Peter R. Allegrini. "The Competitive NMDA Antagonist CGP 40116 Permanently Reduces Brain Damage after Middle Cerebral Artery Occlusion in Rats." Journal of Cerebral Blood Flow & Metabolism 15, no. 4 (1995): 602–10. http://dx.doi.org/10.1038/jcbfm.1995.74.

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In this study we evaluated the effect of the competitive N-methyl-d-aspartate (NMDA) antagonist d-(E)-4-(3-phosphonoprop-2-enyl)piperazine-2-carboxylic acid (CGP 40116) on both early (2 days) and late (28 days) ischemic brain damage in a rodent model of focal cerebral ischemia by means of magnetic resonance imaging (MRI) and conventional histology. Immediately after occlusion of the left middle cerebral artery (MCA), rats received either CGP 40116 (20 mg/kg i.p.) or isotonic saline. Two MRI scans were performed in each animal 2 and 28 days after MCA occlusion. After the second scan, rats were

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Rhoades, R. W., C. A. Bennett-Clarke, M. Y. Shi, and R. D. Mooney. "Effects of 5-HT on thalamocortical synaptic transmission in the developing rat." Journal of Neurophysiology 72, no. 5 (1994): 2438–50. http://dx.doi.org/10.1152/jn.1994.72.5.2438.

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1. Recent immunocytochemical and receptor binding data have demonstrated a transient somatotopic patterning of serotonin (5-HT)-immunoreactive fibers in the primary somatosensory cortex of developing rats and a transient expression of 5-HT1B receptors on thalamocortical axons from the ventral posteromedial thalamic nucleus (VPM). 2. These results suggest that 5-HT should strongly modulate thalamocortical synaptic transmission for a limited time during postnatal development. This hypothesis was tested in intracellular recording experiments carried out in thalamocortical slice preparations that

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Horan, Bryan, Eliot L. Gardner, Stephen L. Dewey, Jonathan D. Brodie та Charles R. Ashby. "The selective σ1 receptor agonist, 1-(3,4-dimethoxyphenethyl)-4-(phenylpropyl)piperazine (SA4503), blocks the acquisition of the conditioned place preference response to (−)-nicotine in rats". European Journal of Pharmacology 426, № 1-2 (2001): R1—R2. http://dx.doi.org/10.1016/s0014-2999(01)01229-8.

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Kido, Kanta, Norika Katagiri, Hiromasa Kawana, Shigekazu Sugino, Masanori Yamauchi, and Eiji Masaki. "Nociceptive Sensitization by Activation of Protease-Activated Receptor 2 in a Rat Model of Incisional Pain." Brain Sciences 11, no. 2 (2021): 144. http://dx.doi.org/10.3390/brainsci11020144.

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Postoperative pain and consequent inflammatory responses after tissue incision adversely affects many surgical patients due to complicated mechanisms. In this study, we examined whether activation of protease-activated receptor 2 (PAR-2), which is stimulated by tryptase from mast cells, elicits nociception and whether the PAR-2 antagonist could reduce incisional nociceptive responses in vivo and in vitro. The effects of a selective PAR-2 antagonist, N3-methylbutyryl-N-6-aminohexanoyl-piperazine (ENMD-1068), pretreatment on pain behaviors were assessed after plantar incision in rats. The effect

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