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Journal articles on the topic 'Imidazoline receptors agonists'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

Maltsev, A. V., та Y. M. Kokoz. "Non-Central Influences of α2-Adrenergic and Imidazoline Agonist Interactions in Isolated ardiomyocytes Cardiac Cells". Kardiologiia 59, № 4 (2019): 52–63. http://dx.doi.org/10.18087/cardio.2019.4.10241.

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Aim: to investigate the functional interaction of α2-adrenergic and imidazoline receptors recently identified on the sarcolemma of isolated cardiomyocytes for regulation of the intracellular calcium and the production of the signal molecule of nitric oxide (NO).Materials and methods:experiments were performed on isolated left ventricular cardiomyocytes of Wistar rats. Potential-dependent Ca2+-currents were measured from the whole-cell by the patch-clamp method in “perforated-patch” configuration. The intracellular calcium and the production of nitric oxide were estimated from the changes in fl

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2

Nikolic, Katarina, and Danica Agbaba. "Imidazoline receptors ligands." Chemical Industry 66, no. 5 (2012): 619–35. http://dx.doi.org/10.2298/hemind120221037n.

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Extensive biochemical and pharmacological studies have determined three different subtypes of imidazoline receptors: I1-imidazoline receptors (I1-IR) involved in central inhibition of sympathicus that produce hypotensive effect; I2-imidazoline receptors (I2-IR) modulate monoamine oxidase B activity (MAO-B); I3-imidazoline receptors (I3-IR) regulate insulin secretion from pancreatic ?-cells. Therefore, the I1/I2/I3 imidazoline receptors are selected as new, interesting targets for drug design and discovery. Novel selective I1/I2/I3 agonists and antagonists have been recently developed. In the p

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Kagawa, Kiyokazu, Tadanori Mammoto, Yukio Hayashi, Takahiko Kamibayashi, Takashi Mashimo та Ikuto Yoshiya. "The Effect of Imidazoline Receptors and α2-adrenoceptors on the Anesthetic Requirement (MAC) for Halothane in Rats". Anesthesiology 87, № 4 (1997): 963–67. http://dx.doi.org/10.1097/00000542-199710000-00032.

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Background Recent evidences have documented that several pharmacologic actions of alpha2-adrenoceptor agonists are mediated via activation of not only alpha2-adrenoceptors, but also by imidazoline receptors, which are nonadrenergic receptors in the central nervous system. However, the effect of imidazoline receptors on the anesthesia is not well known, and it is important to clarify the effects of both receptors on anesthesia. Methods Seventy-two rats were anesthetized with halothane, and the anesthetic requirement for halothane was evaluated as minimum alveolar concentration (MAC). The MAC fo

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Ernsberger, Paul, and Musa A. Haxhiu. "The I1-imidazoline-binding site is a functional receptor mediating vasodepression via the ventral medulla." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 273, no. 5 (1997): R1572—R1579. http://dx.doi.org/10.1152/ajpregu.1997.273.5.r1572.

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I1-imidazoline-binding sites fulfill all essential criteria for identification as receptors, including specificity of binding, association with physiological functions, appropriate anatomic and cellular and subcellular localization, and specific cell signaling pathways. Moreover, binding affinities correlate with functional drug responses. The evidence linking I1 receptors to vasodepression includes expression in RVLM and consistent correlations between vasodepressor potency in humans and animals and I1 binding affinity. Some I1 agonists are antagonists at α2-adrenergic receptors (α2AR), and t

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5

Prichard, Brian N., and Barrie R. Graham. "I1 Imidazoline Agonists. General Clinical Pharmacology of Imidazoline Receptors." Drugs & Aging 17, no. 2 (2000): 133–59. http://dx.doi.org/10.2165/00002512-200017020-00005.

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6

Soldatov, Vladislav O., Elena A. Shmykova, Marina A. Pershina, et al. "Imidazoline receptors agonists: possible mechanisms of endothelioprotection." Research Results in Pharmacology 4, no. 2 (2018): 11–19. http://dx.doi.org/10.3897/rrpharmacology.4.27221.

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Imidazoline receptor agonists are one of the groups of contemporary antihypertensive drugs with the pleiotropic cardiovascular effects. In this review, the historical, physiological, pathophysiological aspects concerning imidazoline receptor agonists and possible mechanisms for their participation in endothelioprotection were considered. Illuminated the molecular biology of each subtype of imidazoline receptors and their significance in the pharmacological correction of cardiovascular disease. IR type 1 are localized in the brain nucleus, carrying out the descending tonic control of sympatheti

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7

Soldatov, Vladislav O., Elena A. Shmykova, Marina A. Pershina, et al. "Imidazoline receptors agonists: possible mechanisms of endothelioprotection." Research Results in Pharmacology 4, no. (2) (2018): 11–18. https://doi.org/10.3897/rrpharmacology.4.27221.

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Imidazoline receptor agonists are one of the groups of contemporary antihypertensive drugs with the pleiotropic cardiovascular effects. In this review, the historical, physiological, pathophysiological aspects concerning imidazoline receptor agonists and possible mechanisms for their participation in endothelioprotection were considered. Illuminated the molecular biology of each subtype of imidazoline receptors and their significance in the pharmacological correction of cardiovascular disease. IR type 1 are localized in the brain nucleus, carrying out the descending tonic control of sympatheti

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8

Dovgan, A. P., S. V. Povetkin, G. A. Batishcheva, A. A. Dolzhikov, M. V. Pokrovsky, and Z. S. Urozhevskaya. "Possible ways of pharmacological correction of ischemic liver damages using agonist of peripheral imidazoline receptors c7070." I.P. Pavlov Russian Medical Biological Herald 26, no. 1 (2018): 21–35. http://dx.doi.org/10.23888/pavlovj2018121-35.

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A comorbid condition both in diabetes mellitus and in metabolic syndrome is fatty dystrophy of the liver that further progresses to hepatic necrosis. In the article variants of pharmacological correction of ischemia-reperfusion of the liver with agonists of imidazoline receptor are proposed. Materials and Methods. The experiment was conducted on 70 rats of both sexes divided into 7 groups (n=10): intact group; pseudo-operated animals (incision of the abdominal wall without ligation of hepatic vessels); animals subject to ischemia/reperfusion without drug correction; animals subject to is

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Dovgan, A. P., S. V. Povetkin, G. A. Batishcheva, A. A. Dolzhikov, M. V. Pokrovsky, and Z. S. Urozhevskaya. "Possible ways of pharmacological correction of ischemic liver damages using agonist of peripheral imidazoline receptors c7070." I.P. Pavlov Russian Medical Biological Herald 26, no. 1 (2018): 21–35. http://dx.doi.org/10.23888/pavlovj201826121-35.

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A comorbid condition both in diabetes mellitus and in metabolic syndrome is fatty dystrophy of the liver that further progresses to hepatic necrosis. In the article variants of pharmacological correction of ischemia-reperfusion of the liver with agonists of imidazoline receptor are proposed. Materials and Methods. The experiment was conducted on 70 rats of both sexes divided into 7 groups (n=10): intact group; pseudo-operated animals (incision of the abdominal wall without ligation of hepatic vessels); animals subject to ischemia/reperfusion without drug correction; animals subject to is

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10

Shetty, Sadanand, Anil Bhoraskar, J. C. Mohan, et al. "Selective imidazoline receptor agonists: redefining role of centrally acting agents in role of centrally acting agents in management of hypertension." International Journal of Advances in Medicine 6, no. 5 (2019): 1688. http://dx.doi.org/10.18203/2349-3933.ijam20194234.

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Hypertension, often referred to as ‘The silent killer’, is christened so, as it is seldom preceded by any warning signs or symptoms. With the new ACC/AHA guidelines lowering the Blood Pressure (BP) threshold values, it has resulted in a 140% relative increase in the hypertension prevalence in India, which is 3 times higher than that of in United States. Imidazoline receptor agonists control BP effectively with minimal adverse effects of sedation and mental depression that are usually associated with centrally acting antihypertensives. While having a low affinity to the α2-adrenergic receptors,

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Hu, Liaoyuan A., Tian Zhou, Jinwoo Ahn, et al. "Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands." Biochemical Journal 424, no. 1 (2009): 39–45. http://dx.doi.org/10.1042/bj20090998.

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TAARs (trace amine-associated receptors) are G-protein-coupled receptors that respond to low abundance, endogenous amines such as tyramine and tryptamine, and represent potential targets for neuropsychiatric diseases. However, some members of this receptor subfamily either have no ligand identified or remain difficult to express and characterize using recombinant systems. In the present paper we report the successful expression of human and mouse TAAR1, and the characterization of their responses to various natural and synthetic agonists. In HEK (human embryonic kidney)-293/CRE-bla cells, mous

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Karpushkina, Ekaterina S., Olga A. Zhdanova, Galina A. Batishcheva, and Yulia A. Petukhova. "Pathogenetic features of acute naphazoline poisoning in children." Research Results in Pharmacology 7, no. 3 (2021): 93–100. http://dx.doi.org/10.3897/rrpharmacology.7.70242.

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Introduction: Acute poisoning by nasal decongestants is an important issue in pediatrics due to physiological and anatomical characteristics of the child’s body and pharmacokinetics of drugs in early childhood. Epidemiology: The number of poisonings by this group of drugs ranged from 4% to 39% during the period from 2000 to 2018. All the studies reported that the most severe degree of intoxication was observed in children aged 1–3 years. Mechanism of action of nasal decongestants: The peculiarity of selective alpha2-adrenergic agonists is that when taken orally, misused or overdosed, they lose

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Karpushkina, Ekaterina S., Olga A. Zhdanova, Galina A. Batishcheva, and Yulia A. Petukhova. "Pathogenetic features of acute naphazoline poisoning in children." Research Results in Pharmacology 7, no. (3) (2021): 93–100. https://doi.org/10.3897/rrpharmacology.7.70242.

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Introduction: Acute poisoning by nasal decongestants is an important issue in pediatrics due to physiological and anatomical characteristics of the child's body and pharmacokinetics of drugs in early childhood. Epidemiology: The number of poisonings by this group of drugs ranged from 4% to 39% during the period from 2000 to 2018. All the studies reported that the most severe degree of intoxication was observed in children aged 1–3 years. Mechanism of action of nasal decongestants: The peculiarity of selective alpha2-adrenergic agonists is that when taken orally, misused or overdosed, they lose

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14

Dovgan, Anton, Zhanna Urozhevskaya, and Anatolii Khavanskii. "POSSIBLE WAYS OF PHARMACOLOGICAL CORRECTION OF ISCHEMIC DAMAGE TO THE LIVER WITH THE AGONIST OF PERIPHERAL IMIDAZOLINE RECEPTORS C7070." Research Results in Pharmacology 3, no. (3) (2017): 3–8. https://doi.org/10.18413/2313-8971-2017-3-3-3-8.

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Introduction: We glad to introduce several variants of pharmacological correction of ischemic hepatic injury by imidazoline I2 receptor agonistС7070. Materials and methods: The experiment was carried out on 70 rats of both sexes, divided into 7 groups (n = 10): an intact group; Pseudo-operated animals (autopsy of the abdominal wall without ligation of the liver vessels); Ischemia / reperfusion group without drug correction; Animals undergoing ischemia / liver reperfusion + Metformin (50 mg / kg); Animals undergoing ischemia / liver reperfusion + Moxonidine (1 μg / kg); Animals undergoing ische

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Coupry, Isabelle, Valérie Lachaud, René-Alexandre Podevin, Elisabeth Koenig та Angelo Parini. "Different Affinities of α2-Agonists for Imidazoline and α2-Adrenergic Receptors". American Journal of Hypertension 2, № 6_Pt_1 (1989): 468–70. http://dx.doi.org/10.1093/ajh/2.6.468.

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16

Chen, Mei-Fen, Jo-Ting Tsai, Li-Jen Chen, et al. "Antihypertensive Action of Allantoin in Animals." BioMed Research International 2014 (2014): 1–6. http://dx.doi.org/10.1155/2014/690135.

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The agonists of imidazoline I-1 receptors (I-1R) are widely used to lower blood pressure. It has been indicated that guanidinium derivatives show an ability to activate imidazoline receptors. Also, allantoin has a chemical stricture similar to guanidinium derivatives. Thus, it is of special interest to characterize the effect of allantoin on I-1R. In conscious male spontaneous hypertensive rats (SHRs), mean blood pressure (MBP) was recorded using the tail-cuff method. Furthermore, the hemodynamic analyses in catheterized rats were applied to measure the actions of allantoin in vivo. Allantoin

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17

Setzer, Kayla, Nicholas Baldwin, Tracey Mersfelder, and Matthew Kelly. "Profound hypotension following concomitant administration of tizanidine and lisinopril." BMJ Case Reports 18, no. 2 (2025): e262982. https://doi.org/10.1136/bcr-2024-262982.

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Tizanidine, a muscle relaxant, exerts its mechanism as a centrally acting alpha-2 adrenergic receptor agonist and binds to imidazoline receptors. Bradycardia and hypotension are adverse effects associated with alpha-2 adrenergic receptor agonists. A man in his 50s with a medical history of hypertension and chronic back pain presented with chest pain and hypertension. Pertinent medication history included metoprolol tartrate, lisinopril, hydralazine, hydrochlorothiazide and tizanidine and was continued. Following medication administration, the patient was hypotensive. Further episodes occurred

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Lazareva, G. A., A. P. Dovgan, S. B. Nikolaev, and N. I. Zhernokova. "METHODS OF PHARMACOLOGICAL CORRECTION OF ISCHEMIC DAMAGES INSULATED LEATHER TISSUE BY AGONISTS OF IMIDAZOLINE RECEPTORS." Belgorod State University Scientific bulletin Medicine Pharmacy 41, no. 1 (2018): 188–97. http://dx.doi.org/10.18413/2075-4728-2018-41-1-188-197.

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Contino, Marialessandra, Antonio Carrieri, Francesco Berardi, et al. "Guinea-pig ileum as ex vivo model useful to characterize ligands displaying Imidazoline I2 and Adrenergic alpha2 mixed activity: a preliminary study." Drugs and Therapy Studies 3, no. 1 (2013): 1. http://dx.doi.org/10.4081/dts.2013.e1.

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The lack of an effective analgesic treatment makes pain a clinical challenge and the need of a novel approach to identify new agents is urgent. In this scenario I2-ligands can be considered an alternative strategy in pain therapy. The development of an <em>ex vivo</em> model useful for the evaluation of functional activities at both a2 and I2-IBs (imidazoline binding sites) is an important task in pharmacological sciences since several I2 ligands display activity also towards a receptors. The present study aims to develop an <em>ex vivo</em> model for estimating the act

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Giorgioni, Gianfabio, Dario Ambrosini, Cristian Vesprini, et al. "Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI." Bioorganic & Medicinal Chemistry 18, no. 19 (2010): 7085–91. http://dx.doi.org/10.1016/j.bmc.2010.08.005.

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El-Mas, Mahmoud M., та Abdel A. Abdel-Rahman. "Differential modulation by estrogen of α2-adrenergic and I1-imidazoline receptor-mediated hypotension in female rats". Journal of Applied Physiology 97, № 4 (2004): 1237–44. http://dx.doi.org/10.1152/japplphysiol.00401.2004.

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We have recently shown that estrogen negatively modulates the hypotensive effect of clonidine (mixed α2-/I1-receptor agonist) in female rats and implicates the cardiovascular autonomic control in this interaction. The present study investigated whether this effect of estrogen involves interaction with α2- and/or I1-receptors. Changes evoked by a single intraperitoneal injection of rilmenidine (600 μg/kg) or α-methyldopa (100 mg/kg), selective I1- and α2-receptor agonists, respectively, in blood pressure, hemodynamic variability, and locomotor activity were assessed in radiotelemetered sham-ope

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Orer, H. S., S. Zhong, S. M. Barman, and G. L. Gebber. "Central catecholaminergic neurons are involved in expression of the 10-Hz rhythm in SND." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 270, no. 2 (1996): R333—R341. http://dx.doi.org/10.1152/ajpregu.1996.270.2.r333.

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We studied the effects of adrenoceptor agonists and antagonists on sympathetic nerve discharge (SND) of urethan-anesthetized, baroreceptor-denervated cats. In cats in which a 10-Hz rhythm coexisted with irregular 2- to 6-Hz oscillations in SND, intravenous clonidine, an alpha 2-adrenoceptor agonist, blocked the 10-Hz rhythm without affecting power at lower frequencies. In contrast, power at frequencies < or = 6 Hz was depressed by clonidine in cats in which the 10-Hz rhythm was absent. These effects were reversed by intravenous administration of alpha 2-adrenoceptor antagonists, idazoxan an

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Aguado, Andreina, John Boulos, Anladys Carreras, Angelica Montoya, and Judith Rodriquez. "Synthesis of furanyl and oxazolyl N-substituted piperidine and imidazoline salts as potential agonists of M1 muscarinic receptors." Journal of Heterocyclic Chemistry 44, no. 6 (2007): 1517–20. http://dx.doi.org/10.1002/jhet.5570440644.

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Duflo, Frédéric, Dawn Conklin, Xinhui Li, and James C. Eisenach. "Spinal Adrenergic and Cholinergic Receptor Interactions Activated by Clonidine in Postincisional Pain." Anesthesiology 98, no. 5 (2003): 1237–42. http://dx.doi.org/10.1097/00000542-200305000-00028.

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Background Previous pharmacologic and molecular studies suggest that the alpha(2)-adrenoceptor subtype A is the target for spinally administered alpha(2)-adrenergic agonists, i.e., clonidine, for pain relief. However, intrathecally administered alpha(2) C antisense oligodeoxynucleotide was recently reported to decrease antinociception induced by clonidine in the rat, suggesting non-A sites may be important as well. The current study sought to determine the subtype of alpha(2) adrenoceptors activated by clonidine in a rodent model for human postoperative pain, and to examine its interaction wit

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Petrusewicz, Jacek, and Roman Kaliszan. "Effect of Imidazoline Drugs on Human Blood Platelet Aggregation." Thrombosis and Haemostasis 54, no. 04 (1985): 784–87. http://dx.doi.org/10.1055/s-0038-1660133.

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SummaryThe effect of seven commonly used in therapy imidazoline derivatives on human blood platelet aggregation was studied. Three of the agents, i.e. clonidine, antazoline and tetryzoline were classified as partial agonists of the receptor responsible for aggregation. Two other drugs, i.e. phentolamine and tolazoline act as competitive antagonists of relatively high receptor affinity. The remaining imidazolines: xylometazoline and naphazoline effectively inhibit the platelet receptor in a non-competitive manner. The last two compounds seem to be selective alpha2-adrenoceptor antagonists.

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Cao, Chunhua, Chang Won Kang, Sung Zoo Kim, and Suhn Hee Kim. "Augmentation of moxonidine-induced increase in ANP release by atrial hypertrophy." American Journal of Physiology-Heart and Circulatory Physiology 287, no. 1 (2004): H150—H156. http://dx.doi.org/10.1152/ajpheart.00977.2003.

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Imidazoline receptors are divided into I1 and I2 subtypes. I1-imidazoline receptors are distributed in the heart and are upregulated during hypertension or heart failure. The aim of this study was to define the possible role of I1-imidazoline receptors in the regulation of atrial natriuretic peptide (ANP) release in hypertrophied atria. Experiments were performed on isolated, perfused, hypertrophied atria from remnant-kidney hypertensive rats. The relatively selective I1-imidazoline receptor agonist moxonidine caused a decrease in pulse pressure. Moxonidine (3, 10, and 30 μmol/l) also caused d

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Konradi, Alexandra O., Nadezhda E. Zvartau, Irina E. Chazova, Juliya V. Zhernakova, Aletta E. Schutte, and Markus P. Schlaich. "Features of antihypertensive therapy and real-world prescription of selective imidazoline receptor agonists in Russia vs other countries: STRAIGHT study data analysis." Terapevticheskii arkhiv 93, no. 4 (2021): 440–48. http://dx.doi.org/10.26442/00403660.2021.04.200818.

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Analysis of routine clinical practice of hypertensive patient management represents one of the important tools in the search for further ways to minimize hypertension-associated cardiovascular and renal adverse outcomes. Aim. To compare the strategies for hypertension management and features of clinical use of I1-imidazoline receptor (I1-IR) agonists in the Russian Federation and other countries where the STRAIGHT (Selective imidazoline receptor agonists Treatment Recommendation and Action In Global management of HyperTension) study was conducted. Materials and methods. It was a cr

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Takamatsu, Isao, Ayano Iwase, Makoto Ozaki, Tomiei Kazama, Keiji Wada, and Masayuki Sekiguchi. "Dexmedetomidine Reduces Long-term Potentiation in Mouse Hippocampus." Anesthesiology 108, no. 1 (2008): 94–102. http://dx.doi.org/10.1097/01.anes.0000296076.04510.e1.

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Background Dexmedetomidine (Precedex; Abbott Laboratories, Abbott Park, IL) is a selective alpha2-adrenergic agonist that also has affinity for imidazoline receptors. In clinical studies, dexmedetomidine has sedative effects and impairs memory, but the action of dexmedetomidine on synaptic plasticity in the brain has yet to be established. In the present study, the authors investigated the effects of dexmedetomidine on two forms of synaptic plasticity-long-term potentiation (LTP) and paired-pulse facilitation-in the CA1 region of mouse hippocampal slices. Methods The authors recorded Schaffer

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Schwaner, I., R. Seifert, and G. Schultz. "Receptor-mediated increases in cytosolic Ca2+ in the human erythroleukaemia cell line involve pertussis toxin-sensitive and -insensitive pathways." Biochemical Journal 281, no. 2 (1992): 301–7. http://dx.doi.org/10.1042/bj2810301.

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The pluripotent human erythroleukaemia cell line, HEL, possesses erythrocytic, megakaryocytic and macrophage-like properties. With respect to signal transduction, HEL cells have been used as a model system for platelets, but little attention has been paid to their phagocytic properties. We studied the effects of various receptor agonists on the intracellular free Ca2+ concentration ([Ca2+]i) in HEL cells. Thrombin, platelet-activating factor (PAF), ATP, UTP, prostaglandins E1 and E2 (PGE1 and PGE2), the PGE2 analogue sulprostone and the stable PGI2 analogues iloprost and cicaprost increased [C

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Nebieridze, D. V., and A. S. Safaryan. "Place of imidazoline receptor agonists in the treatment of hypertension." Cardiovascular Therapy and Prevention 20, no. 8 (2022): 3129. http://dx.doi.org/10.15829/1728-8800-2021-3129.

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The review is devoted to selective I1-imidazoline-receptor agonists. An analysis of Russian and foreign studies is presented, the results of which indicate that this drug class not only provides adequate and long-term control of blood pressure, but also has a number of favorable metabolic effects. Therefore, it contributes to reducing insulin resistance (weight loss) and has organ protective properties (endothelial function improvement, left ventricular hypertrophy regression, microalbuminuria reduction). At the same time, selective I1-imidazoline-receptor agonists are much less likely to caus

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Ren, Yu Jie, Fan Hong Wu, Chun Feng Shu, and Ma Liu. "Synthesis and Potent Biological Activity of 1-Sulfonyl Substituted Imidazole and Benzo[d]imidazole Compounds." Advanced Materials Research 236-238 (May 2011): 2570–73. http://dx.doi.org/10.4028/www.scientific.net/amr.236-238.2570.

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A new series of 1-sulfonly substituted imidazole compounds (containing 19 compounds) were synthesized and characterized by1HNMR,13CNMR and HRMS. 2d, 2e, 2h, 2i showed promising activities in animal test (in rats) for anti-inflammation. 2k - 2t were used in Chemokine Receptors CXCR4 receptor agonist Calcium assay showed no activities.

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Bozdagi, O., X. B. Wang, G. P. Martinelli, et al. "Imidazoleacetic acid-ribotide induces depression of synaptic responses in hippocampus through activation of imidazoline receptors." Journal of Neurophysiology 105, no. 3 (2011): 1266–75. http://dx.doi.org/10.1152/jn.00263.2010.

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Imidazole-4-acetic acid-ribotide (IAA-RP), an endogenous agonist at imidazoline receptors (I-Rs), is a putative neurotransmitter/regulator in mammalian brain. We studied the effects of IAA-RP on excitatory transmission by performing extracellular and whole cell recordings at Schaffer collateral-CA1 synapses in rat hippocampal slices. Bath-applied IAA-RP induced a concentration-dependent depression of synaptic transmission that, after washout, returned to baseline within 20 min. Maximal decrease occurred with 10 μM IAA-RP, which reduced the slope of field extracellular postsynaptic potentials (

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Crider, A. M., S. Liu, C. Tang, B. Ho, M. Ankersen, and C. E. Stidsen. "2-Pyridylthioureas: Novel Nonpeptide Somatostatin Agonists with SST4 Selectivity." Current Pharmaceutical Design 5, no. 4 (1999): 255–63. http://dx.doi.org/10.2174/1381612805666230109213422.

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Somatostatin [somatotropin release-inhibiting factor (SRIF)] is a cyclic tetradecapcptiJc that is a potent inhibitor of growth hormone (GH) secretion from the anterior pituitary. In addition to the inhibitory effects on GH-release, SRIF-14 and SRJF-28, a 28-amino acid form of SRIF extended from the N-terminal end, inhibit the release of a variety of other peptides including glucagon, insulin, and gastriri, and both peptides act as neurotransmitters and neuromodulators in the central nervous system and the periphery. SRIF exerts its potent inhibitory effects following binding to high affinity S

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Sun, Shiyang, Pengyun Li, Jiaqi Wang та ін. "Novel Scaffold Agonists of the α2A Adrenergic Receptor Identified via Ensemble-Based Strategy". Molecules 29, № 5 (2024): 1097. http://dx.doi.org/10.3390/molecules29051097.

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The α2A adrenergic receptor (α2A-AR) serves as a critical molecular target for sedatives and analgesics. However, α2A-AR ligands with an imidazole ring also interact with an imidazoline receptor as well as other proteins and lead to undesirable effects, motivating us to develop more novel scaffold α2A-AR ligands. For this purpose, we employed an ensemble-based ligand discovery strategy, integrating long-term molecular dynamics (MD) simulations and virtual screening, to identify new potential α2A-AR agonists with novel scaffold. Our results showed that compounds SY-15 and SY-17 exhibited signif

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Boxwalla, Mustufa, George Matwyshyn, Bhagya L. Puppala, Shridhar V. Andurkar, and Anil Gulati. "Involvement of imidazoline and opioid receptors in the enhancement of clonidine-induced analgesia by sulfisoxazole." Canadian Journal of Physiology and Pharmacology 88, no. 5 (2010): 541–52. http://dx.doi.org/10.1139/y10-007.

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Clonidine, an α2-adrenergic agonist, has been demonstrated to produce significant analgesia and potentiate morphine analgesia. Endothelin (ETA) receptor antagonists have also been found to potentiate the antinociceptive response to morphine. Clonidine and ET have been reported to have cardiovascular interactions involving the sympathetic nervous system, but it is not known whether ETA receptor antagonist affects clonidine analgesia. This study examined the influence of sulfisoxazole (ETA receptor antagonist) on clonidine analgesia. Male Swiss Webster mice were used to determine antinociceptive

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Moore, Graham J., Harry Ridgway, Konstantinos Kelaidonis, et al. "Actions of Novel Angiotensin Receptor Blocking Drugs, Bisartans, Relevant for COVID-19 Therapy: Biased Agonism at Angiotensin Receptors and the Beneficial Effects of Neprilysin in the Renin Angiotensin System." Molecules 27, no. 15 (2022): 4854. http://dx.doi.org/10.3390/molecules27154854.

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Angiotensin receptor blockers (ARBs) used in the treatment of hypertension and potentially in SARS-CoV-2 infection exhibit inverse agonist effects at angiotensin AR1 receptors, suggesting the receptor may have evolved to accommodate naturally occurring angiotensin ‘antipeptides’. Screening of the human genome has identified a peptide (EGVYVHPV) encoded by mRNA, complementary to that encoding ANG II itself, which is an inverse agonist. Thus, opposite strands of DNA encode peptides with opposite effects at AR1 receptors. Agonism and inverse agonism at AR1 receptors can be explained by a receptor

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Cho, Analia Young Hwa, Hery Chung, Javier Romero-Parra, et al. "Motifs in Natural Products as Useful Scaffolds to Obtain Novel Benzo[d]imidazole-Based Cannabinoid Type 2 (CB2) Receptor Agonists." International Journal of Molecular Sciences 24, no. 13 (2023): 10918. http://dx.doi.org/10.3390/ijms241310918.

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The endocannabinoid system (ECS) constitutes a broad-spectrum modulator of homeostasis in mammals, providing therapeutic opportunities for several pathologies. Its two main receptors, cannabinoid type 1 (CB1) and type 2 (CB2) receptors, mediate anti-inflammatory responses; however, their differing patterns of expression make the development of CB2-selective ligands therapeutically more attractive. The benzo[d]imidazole ring is considered to be a privileged scaffold in drug discovery and has demonstrated its versatility in the development of molecules with varied pharmacologic properties. On th

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Zhainazarov, A. B., M. Wachowiak, A. Boettcher, S. Elenes, and B. W. Ache. "Ionotropic GABA Receptor From Lobster Olfactory Projection Neurons." Journal of Neurophysiology 77, no. 5 (1997): 2235–51. http://dx.doi.org/10.1152/jn.1997.77.5.2235.

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Zhainazarov, A. B., M. Wachowiak, A. Boettcher, S. Elenes, and B. W. Ache. Ionotropic GABA receptor from lobster olfactory projection neurons. J. Neurophysiol. 77: 2235–2251, 1997. This study reports an ionotropic GABA (γ-aminobutyric acid) receptor in projection neurons acutely dissociated from the olfactory lobe of the brain of the spiny lobster and analyzed by whole cell and cell-free patch-clamp recording. GABA evokes a macroscopic current in the cells that is linear from −100 to +100 mV, reverses at the imposed chloride equilibrium potential, has a permeability sequence of Cl− > acetat

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Diaz, Alvaro, Soraya Mayet, and Anthony H. Dickenson. "BU-224 produces spinal antinociception as an agonist at imidazoline I2 receptors." European Journal of Pharmacology 333, no. 1 (1997): 9–15. http://dx.doi.org/10.1016/s0014-2999(97)01118-7.

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Guyenet, Patrice G. "Is the hypotensive effect of clonidine and related drugs due to imidazoline binding sites?" American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 273, no. 5 (1997): R1580—R1584. http://dx.doi.org/10.1152/ajpregu.1997.273.5.r1580.

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Clonidine and related α2-adrenergic receptor (α2AR) agonists lower arterial pressure primarily by an action within the central nervous system. These drugs also have varying degrees of affinity for other cellular components called nonadrenergic imidazoline binding sites (NAIBS). For over 20 years, the α2AR agonist activity of clonidine-like drugs was thought to account for their therapeutic effects (α2 theory). However, several groups have recently proposed a competing “imidazoline theory” according to which the hypotensive effect of clonidine-like drugs would in fact owe more to their affinity

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Kukes, V. G., G. S. Anikin, E. M. Andreevskaya, and E. A. Ashurkova. "Treatment of hypertension in overweight patients." Systemic Hypertension 12, no. 3 (2015): 46–49. http://dx.doi.org/10.26442/sg29105.

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The aim of the treatment of hypertension in patients with overweight is not only normalization of blood pressure, but also improvement of endothelial function, reduction of insulin resistance and lipid metabolism. Some of the drugs with a broad therapeutic spectrum and huge evidential base, - I1-imidazoline-receptor agonists can be applied in both monotherapy and as a part of the combined therapy in overweight patients.

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Abasova, L. I., R. L. Dashdamirov, and A. B. Bakhshaliev. "Arterial hypertension and metabolic syndrome: specifics of antihypertensive therapy." Cardiovascular Therapy and Prevention 10, no. 4 (2011): 107–9. http://dx.doi.org/10.15829/1728-8800-2011-4-107-109.

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This review summarizes the literature evidence on humoral disturbances in arterial hypertension (AH), as well as on AH interrelationship with individual components of metabolic syndrome (MS). Based on the results of multi-centre randomised trials, the rationale for the use of antihypertensive agents with favourable metabolic profile is demonstrated, in particular, for antagonists of slow calcium channels, angiotensin-converting enzyme inhibitors, and selective imidazoline receptor agonists.

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Nakamura, K., H. Kariyazono, T. Shinkawal, et al. "Inhibitory effects of H2-receptor antagonists on platelet function in vitro." Human & Experimental Toxicology 18, no. 8 (1999): 487–92. http://dx.doi.org/10.1191/096032799678847069.

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1 To evaluate in vitro inhibitory effects of four types of histamine H2-receptor antagonist (H2-receptor antagonists), famotidine, roxatidine, cimetidine and ranitidine, on platelet function, we examined aggregating potency and P-selectin levels with agonist-induced aggregation. Ranitidine and cimetidine inhibited, in concentration of 0.35 mM, the secondary aggregation induced by 5 pM adenosine diphosphate (ADP), the aggregation induced by 1,g/mL collagen and 3 gM arachidonic acid. All of H2-receptor antagonists inhibited, in concentration of 1.4 mm, the aggregation induced by ADP, collagen an

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Grahovac, Jelena, Kristina Živić, Marijana Pavlović, et al. "Abstract 2476: Nischarin is a potential druggable target in both epithelial and stromal compartments of pancreatic ductal adenocarcinoma." Cancer Research 83, no. 7_Supplement (2023): 2476. http://dx.doi.org/10.1158/1538-7445.am2023-2476.

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Abstract Nischarin is a scaffolding protein involved in the regulation of cell cytoskeletal organization and metabolic homeostasis. In breast and ovarian cancers, nischarin has been demonstrated to have tumor suppressive functions. We have found that nischarin was expressed in both the epithelial and stromal compartments of the PDAC patient tissue, in cancer cell lines and patient-derived stellate cells. Of interest, nischarin is a functional imidazoline 1 receptor for which there are several FDA-approved agonists used for treatment of hypertension. The aim of this study was to examine the eff

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Finta, Ervin. "A rilmenidinterápia hatása a szívfrekvencia- és a vérnyomás-variabilitásra, a baroreflex-szenzitivitásra." Hypertonia és Nephrologia 28, no. 2 (2024): 93–95. http://dx.doi.org/10.33668/hn.28.006.

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A szimpatikus idegrendszer fontos és széles körben tanulmányozott szerepet játszik a hypertoniában és a társuló kórfolyamatokban. A különböző típusú antihipertenzív szerek között, amelyekkel lehetséges a túlzott szimpatikus aktivitás mérséklése, a centrális hatású szerek kiemelt szerepet játszanak. Az imidazolin I1-receptor-agonista rilmenidin néhány speciális tulajdonsága kerül áttekintésre az összefoglalóban.

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Podzolkov, V. I., E. A. Gladysheva, and A. E. Bragina. "Moxonidin in combined therapy of metabolic syndrome." "Arterial’naya Gipertenziya" ("Arterial Hypertension") 13, no. 4 (2007): 246–49. http://dx.doi.org/10.18705/1607-419x-2007-13-4-246-249.

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The paper presents the results of 24-weeks follow-up and treatment patients with metabolic syndrome. It shows antihypertensive effect of imidazoline-receptor agonist moxonidine and hypolipidemic effect of micronized fenofibrate in patients with metabolic syndrome. The combination demonstrate synergic action on carbohydrate and uric acid metabolism. Thus, it can significantly decrease the level of cardio-vascular risk (SCORE) in patients with metabolic syndrome.

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Levkova, Elena A., Anton L. Pazhinsky, Sergey S. Lugovskoy, et al. "Correction of retinal ischemic injuries by using non-selective imidazoline receptor agonists in the experiment." Research Results in Pharmacology 5, no. (4) (2019): 7–17. https://doi.org/10.3897/rrpharmacology.5.38498.

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Introduction: Retinoprotective effects of non-selective imidazoline receptor agonists: potassium salt of С7070; sodium salt of С7070; С7070 processed with CO<sub>2</sub> – were investigated in comparison with C7070 on the retinal ischemia-reperfusion model in rats. Materials and methods: The protective effects of the substances were evaluated by using ophthalmoscopy, laser Doppler flowmetry, electroretinography, histological and morphometric studies of retinal layers. Results and discussion: The most pronounced retinoprotective effect was observed in potassium salt of C7070 at a dose of 10 mg/

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Ruffolo, Robert R. "Relative agonist potency as a means of differentiating α-adrenoceptors and α-adrenergic mechanisms". Clinical Science 68, s10 (1985): 9s—15s. http://dx.doi.org/10.1042/cs068s009.

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1. Relative potencies (ED50), affinities (assessed as dissociation constants) and efficacies (i.e. ability to activate the receptor) of agonists are useful in subclassifying and differentiating α-adrenoceptors. 2. The postsynaptic α-adrenoceptor of rat aorta is of the α1-subtype, but may differ from the α1-adrenoceptor of rabbit and guinea pig aortae, based on comparison of relative potencies of selected agonists. 3. By evaluating the relative potency of agonists, qualitative and quantitative species differences between α1-adrenoceptors in rat and guinea pig are observed in a variety of test s

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Huang, Rong, Ye Chen, A. C. H. Yu, and Leif Hertz. "Dexmedetomidine-Induced Stimulation of Glutamine Oxidation in Astrocytes: A Possible Mechanism for its Neuroprotective Activity." Journal of Cerebral Blood Flow & Metabolism 20, no. 6 (2000): 895–98. http://dx.doi.org/10.1097/00004647-200006000-00001.

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Dexmedetomidine is a highly specific α2-adrenergic agonist, which is used clinically as an anesthetic adjuvant and in animal experiments has a neuroprotective effect during ischemia. The current study showed that dexmedetomidine enhances glutamine disposal by oxidative metabolism in astrocytes. This effect occurs at pharmacologically relevant concentrations. It is exerted on α2-adrenergic receptors and not on imidazoline-preferring sites, and it is large enough to reduce the availability of glutamine as a precursor of neurotoxic glutamate.

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Nebieridze, D. V., A. S. Safaryan, E. I. Ivanova, and E. A. Poddubskaya. "Place of imidazoline receptor agonists in the treatment of arterial hypertension." Rational Pharmacotherapy in Cardiology 19, no. 6 (2023): 603–6. http://dx.doi.org/10.20996/1819-6446-2023-2943.

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The review is devoted to one of the most controversial issues of modern antihypertensive therapy — the role of new generation sympatholytics — selective I1-imidazoline receptor agonists (AIRs). In modern European recommendations, AIR (moxonidine rilmenidine), along with other centrally acting drugs (reserpine, alpha-methyldopa, clonidine), are mainly intended for additional therapy in rare cases of resistant hypertension, when other treatment options have been ineffective. Nevertheless, AIR invariably finds its place in Russian recommendations for the treatment of arterial hypertension (AH). T

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