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Journal articles on the topic 'Imidazoline receptor type I'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

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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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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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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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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Demidova, T. U., A. S. Ametov, and L. V. Smagina. "Moxinidine in the correction of metabolic disturbancis and endothelial dysfunction in patients with diabetes mellitus associated with arterial hypertension." "Arterial’naya Gipertenziya" ("Arterial Hypertension") 10, no. 2 (2004): 104–9. http://dx.doi.org/10.18705/1607-419x-2004-10-2-104-109.

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The paper presents the results of a follow-up and treatment of 30 patients with arterial hypertension (AH) accompanied by the persistent blood pressure elevation that requires continuous antihypertensive therapy and that is associated with type 2 diabetes mellitus. It shows the antihypersensive effect of the imidazoline-receptor agonist moxonidine and its positive action on metabolic parameters and a risk for cardiovascular events in this group of patients.

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Gaponova, N. I., and V. R. Abdrakhmanov. "Theory and practice of selective imidazoline receptor agonist use in Russia." Rational Pharmacotherapy in Cardiology 20, no. 3 (2024): 340–48. http://dx.doi.org/10.20996/1819-6446-2024-3058.

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Activation of the sympathetic nervous system plays an important role in arterial hypertension (AH) development. Antihypertensive drugs of central action contribute to the elimination of sympathetic activation. The selective imidazoline receptor agonist moxonidine has been successfully used in the treatment of patients with hypertension. The review article presents data on the antihypertensive efficacy of moxonidine, the possibility of its use in combination therapy to reduce elevated blood pressure (BP). The effectiveness of moxonidine in overweight patients, metabolic syndrome, diabetes melli

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7

Zhernakova, Yu V., G. H. Sharipova, and I. E. Chazova. "Patients with arterial hypertension associated with metabolic disorders: characteristics and therapeutic approach." Systemic Hypertension 12, no. 1 (2015): 52–57. http://dx.doi.org/10.26442/sg29094.

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Arterial hypertension (AH) is associated with metabolic disorders in approximately 80% of cases. There is a pandemic of so-called new risk factors, such as insulin resistance and association with systemic type of hyperinsulinemia, abdominal obesity, hyperinsulinemia and a special type of dislipidemy, nowadays. Patients with AH associated with such metabolic disorders are at a higher risk of developing cardiovascular disease and diabetes. However, it is very difficult to achieve the target level of blood pressure in this category of patients. Usually, these patients should be treated using comb

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8

Kim, Young-Hwan, Ji-Hyun Jeong, Duck-Sun Ahn, and Seungsoo Chung. "Agmatine suppresses peripheral sympathetic tone by inhibiting N-type Ca2+ channel activity via imidazoline I2 receptor activation." Biochemical and Biophysical Research Communications 477, no. 3 (2016): 406–12. http://dx.doi.org/10.1016/j.bbrc.2016.06.086.

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9

Dahmani, Souhayl, Andrea Paris, Virginie Jannier та ін. "Dexmedetomidine Increases Hippocampal Phosphorylated Extracellular Signal–regulated Protein Kinase 1 and 2 Content by an α2-Adrenoceptor–independent Mechanism". Anesthesiology 108, № 3 (2008): 457–66. http://dx.doi.org/10.1097/aln.0b013e318164ca81.

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Background Dexmedetomidine is a potent and selective alpha2-adrenoceptor (alpha2AR) agonist that exhibits a broad pattern of actions, including sedation, analgesia, and neuroprotection. Recent studies have emphasized the role of phosphorylated extracellular signal-regulated protein kinases (pERK1 and 2) in coupling rapid events such as neurotransmitter release and receptor stimulation long-lasting changes in synaptic plasticity and cell survival. Here, the authors hypothesized that dexmedetomidine increases pERK1 and 2 content and examined the mechanisms involved in this effect. Methods The ef

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10

Moore, Graham J., Harry Ridgway, Laura Kate Gadanec, Vasso Apostolopoulos, Anthony Zulli, and John M. Matsoukas. "Gating Mechanism for Biased Agonism at Angiotensin II Type 1 Receptors." Molecules 30, no. 11 (2025): 2399. https://doi.org/10.3390/molecules30112399.

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For the interaction of angiotensin II (AngII) with AngII type 1 receptors (AT1R), two potential proton hopping pathways have been identified, each associated with distinct physiological outcomes. The octapeptide AngII (Asp1-Arg2-Val3-Tyr4-Ile5-His6-Pro7-Phe8) appears to form a charge relay system (CRS) in solution in which the C-terminal carboxylate abstracts a proton from the His6 imidazole group, which, in turn, abstracts a proton from the Tyr4 hydroxyl (OH) group, creating a tyrosinate anion. When AngII binds to the AT1R, the CRS can be reconstituted with D281 of the receptor taking up the

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Pallottini, Valentina, Maria Marino, and Paolo Ascenzi. "Clonidine Displacement from Type 1 Imidazoline Receptor by p -Aminobenzamidine, the Prototype of Trypsin-Like Serine Protease Inhibitors." IUBMB Life (International Union of Biochemistry and Molecular Biology: Life) 54, no. 5 (2002): 301–4. http://dx.doi.org/10.1080/15216540215672.

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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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Kim, Young-Hwan, Taick-Sang Nam, Duck-Sun Ahn, and Seungsoo Chung. "Modulation of N-type Ca2+ currents by moxonidine via imidazoline I1 receptor activation in rat superior cervical ganglion neurons." Biochemical and Biophysical Research Communications 409, no. 4 (2011): 645–50. http://dx.doi.org/10.1016/j.bbrc.2011.05.058.

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14

ULIBARRI, ISABEL, JOHANKA SOTO, JAVIER RUIZ, JAVIER BALLESTEROS, JOSE V. JAUREGUI, and J. JAVIER MEANA. "I2-Imidazoline Receptors in Platelets of Patients with Parkinson's Disease and Alzheimer's Type Dementiaa." Annals of the New York Academy of Sciences 881, no. 1 IMIDAZOLINE R (1999): 199–202. http://dx.doi.org/10.1111/j.1749-6632.1999.tb09360.x.

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15

Salazar-Bookaman, M. M., D. D. Miller, and P. N. Patil. "Antagonism by imidazoline - type drugs of muscarinic and other receptors in the guinea-pig ileum." Autonomic and Autacoid Pharmacology 26, no. 3 (2006): 267–73. http://dx.doi.org/10.1111/j.1474-8673.2006.00355.x.

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Maltsev, A. V., E. V. Evdokimovskii, O. Yu Pimenov, M. N. Nenov, and Yu M. Kokoz. "Regulation of potential-dependent L-type Ca2+ currents by agmatine. Imidazoline receptors in isolated cardiomyocytes." Biochemistry (Moscow) Supplement Series A: Membrane and Cell Biology 6, no. 4 (2012): 279–87. http://dx.doi.org/10.1134/s1990747812040058.

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Chang, Chin-Hong, Pin-Chun Chao, Ho-Shan Niu, Gin-Chi Huang, Li-Jen Chen, and Juei-Tang Cheng. "Canavanine activates imidazoline I-2 receptors to reduce hyperglycemia in type 1-like diabetic rats." Chemico-Biological Interactions 240 (October 2015): 304–9. http://dx.doi.org/10.1016/j.cbi.2015.08.019.

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Chung, Seungsoo, Duck-Sun Ahn, Young-Hwan Kim, Yoon-Suk Kim, Ji-Hyun Joeng, and Taick-Sang Nam. "Experimental Physiology -Research Paper: Modulation of N-type calcium currents by presynaptic imidazoline receptor activation in rat superior cervical ganglion neurons." Experimental Physiology 95, no. 10 (2010): 982–93. http://dx.doi.org/10.1113/expphysiol.2010.053355.

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Peresypkina, Anna A. "A comparative evaluation of the efficacy of dimethylaminoethanol derivative 7–16, C7070 and picamilon in correction of experimental hypertensive neuroretinopathy." Research Results in Pharmacology 4, no. (3) (2018): 1–8. https://doi.org/10.3897/rrpharmacology.4.29388.

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Introduction. The efficacy of dimethylaminoethanol (DMAE) derivative 7–16, substance C7070 in comparison with picamylon in hypertensive neuroretinopathy model in white laboratory rats was evaluated. Materials and methods. For measuring the blood pressure, a system of noninvasive blood pressure measurement in small animals NIBP200 was used. Ophthalmoscopy was performed by using Bx a Neitz ophthalmoscope (Japan) and Osher MaxField 78D lens, OI-78M model. Electroretinography (ERG) was recorded in response to a single stimulation. Biopotentials were presented graphically on the screen with the hel

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20

Baranova, E. I., V. Ionin, and O. P. Rotar. "Personalized approach to the treatment of patients with arterial hypertension: focus on imidazoline receptor agonists. Opinion on the problem." Cardiovascular Therapy and Prevention 24, no. 2 (2025): 4342. https://doi.org/10.15829/1728-8800-2025-4342.

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Hypertension (HTN) remains one of the most pressing problems of modern healthcare. Morbidity and mortality associated with HTN continue to increase, despite a wide range of available antihypertensive agents and regular updates of related clinical guidelines. In October 2024, an annual forum was held to discuss the optimization of approaches to the treatment of HTN. During the discussion, special attention was paid to personalized therapy of patients, which should be based on modern concepts of the disease pathogenesis and individual risk factors. In addition, the validity of prescribing imidaz

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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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Lee, J. P., W. Chen, H. T. Wu, K. C. Lin, and J. T. Cheng. "Metformin can Activate Imidazoline I-2 Receptors to Lower Plasma Glucose in Type 1-like Diabetic Rats." Hormone and Metabolic Research 43, no. 01 (2010): 26–30. http://dx.doi.org/10.1055/s-0030-1267169.

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23

Soto, J., I. Ulibarri, J. V. Jauregui, J. Ballesteros, and J. J. Meana. "Dissociation between I2-imidazoline receptors and MAO-B activity in platelets of patients with Alzheimers type dementia." Journal of Psychiatric Research 33, no. 3 (1999): 251–57. http://dx.doi.org/10.1016/s0022-3956(98)00065-x.

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24

Su, Chin-Hui, I. Min Liu, Hsien-Hui Chung, and Juei-Tang Cheng. "Activation of I2-imidazoline receptors by agmatine improved insulin sensitivity through two mechanisms in type-2 diabetic rats." Neuroscience Letters 457, no. 3 (2009): 125–28. http://dx.doi.org/10.1016/j.neulet.2009.03.093.

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Hsu, Chia-Chen, Mang Lin, Juei-Tang Cheng, and Ming Wu. "Diosmin, a Citrus Nutrient, Activates Imidazoline Receptors to Alleviate Blood Glucose and Lipids in Type 1-Like Diabetic Rats." Nutrients 9, no. 7 (2017): 684. http://dx.doi.org/10.3390/nu9070684.

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Li, Guanguan, Amanda N. Nieman, Md Yeunus Mian, et al. "A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABAA Receptor." Molecules 25, no. 17 (2020): 3864. http://dx.doi.org/10.3390/molecules25173864.

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Analgesic and anti-inflammatory properties mediated by the κ opioid receptor (KOR) have been reported for oxadiazole imidazodiazepines. Affinities determined by radioligand competition assays of more than seventy imidazodiazepines using cell homogenates from HEK293 cells that overexpress KOR, µ opioid receptor (MOR), and δ opioid receptor (DOR) are presented. Affinities to synaptic, benzodiazepine-sensitive receptors (BZR) were determined with rat brain extract. The highest affinity for KOR was recorded for GL-I-30 (Ki of 27 nM) and G-protein recruitment was observed with an EC50 of 32 nM. Aff

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Ugedo, Luisa, Joseba Pineda, José A. Ruiz-Ortega, and Raúl Martín-Ruiz. "Stimulation of locus coeruleus neurons by non-I1 /I2 -type imidazoline receptors: an in vivo and in vitro electrophysiological study." British Journal of Pharmacology 125, no. 8 (1998): 1685–94. http://dx.doi.org/10.1038/sj.bjp.0702255.

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Renouard, Anne, Peter S. Widdowson, and Alex Cordi. "[3H]-idazoxan binding to rabbit cerebral cortex recognises multiple imidazoline I2-type receptors: pharmacological characterization and relationship to monoamine oxidase." British Journal of Pharmacology 109, no. 3 (1993): 625–31. http://dx.doi.org/10.1111/j.1476-5381.1993.tb13618.x.

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Lukasiewicz, Peter D., and Colleen R. Shields. "Different Combinations of GABAA and GABAC Receptors Confer Distinct Temporal Properties to Retinal Synaptic Responses." Journal of Neurophysiology 79, no. 6 (1998): 3157–67. http://dx.doi.org/10.1152/jn.1998.79.6.3157.

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Lukasiewicz, Peter D. and Colleen R. Shields. Different combinations of GABAA and GABAC receptors confer distinct temporal properties to retinal synaptic responses. J. Neurophysiol. 79:3157–3167, 1998. This study addresses how γ-aminobutyric acid-A(GABAA) and GABAC receptors confer distinct temporal properties to neuronal synaptic responses. The retina is a model system for the study of postsynaptic contributions to synaptic responses because GABAergic amacrine cells synapse onto neurons, which have different combinations of GABAA and GABAC receptors. It is not known, however, how GABAA versus

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Du, Jiu-Lin, and Xiong-Li Yang. "Subcellular Localization and Complements of GABAA and GABAC Receptors on Bullfrog Retinal Bipolar Cells." Journal of Neurophysiology 84, no. 2 (2000): 666–76. http://dx.doi.org/10.1152/jn.2000.84.2.666.

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γ-Aminobutyric acid (GABA) receptors on retinal bipolar cells (BCs) are highly relevant to spatial and temporal integration of visual signals in the outer and inner retina. In the present work, subcellular localization and complements of GABAA and GABACreceptors on BCs were investigated by whole cell recordings and local drug application via multi-barreled puff pipettes in the bullfrog retinal slice preparation. Four types of the BCs (types 1–4) were identified morphologically by injection of Lucifer yellow. According to the ramification levels of the axon terminals and the responses of these

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Zhernakova, Yu V. "Modern ideas about the consequences of sympathoadrenal hyperactivation in hypertensive patients with metabolic disorders: modulation possibilities." Russian Journal of Cardiology 28, no. 12 (2023): 5681. http://dx.doi.org/10.15829/1560-4071-2023-5681.

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The prevalence of hypertension (HTN) in the Russian Federation and the world continues to grow. This is largely due to the epidemic of obesity and related conditions — metabolic syndrome and type 2 diabetes. The most common and proven hypothesis of the relationship between hypertension and obesity is the activation of the sympathetic nervous system. However, modern research shows that the consequences of sympathetic hyperactivation are not limited only to hemodynamic effects, but extend to many organs and systems. Long-term sympathetic hyperactivation can lead to insulin resistance and type 2

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Liu, Zhenxing, Shuan Zhao, Shuaishuai Wu, Jingyou Zhang, Zunyang Nie, and Shenming Zeng. "A novel role of transient receptor potential mucolipin1 (TRPML1) in protecting against imidazole-induced cytotoxicity." Biochemistry and Cell Biology 92, no. 4 (2014): 279–86. http://dx.doi.org/10.1139/bcb-2014-0044.

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Lysosomotropic amines cause serious side effects such as cytoplasmic vacuolation and cell death. TRPML1 (also known as mucolipin1), a member of the transient receptor potential (TRP) protein family, may regulate fusion/fission of vesicles along the endocytic pathway and some aspects of lysosomal ion homeostasis. Nevertheless, it is still unknown whether TRPML1 is involved in death of mammalian cells induced by lysosomotropic agents. In this study, imidazole was used as a model to investigate the role of TRPML1 in the cytotoxicity of lysosomotropic agents. Overexpression of wild-type TRPML1 inh

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BENSON, JACK A. "A Novel Gaba Receptor in the Heart of a Primitive Arthropod, Limulus Polyphemus." Journal of Experimental Biology 147, no. 1 (1989): 421–38. http://dx.doi.org/10.1242/jeb.147.1.421.

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1. The isolated, intact heart of the marine arachnid Limulus polyphemus continues to beat in vitro for many hours. Application of γaminobutyric acid (GABA) decreased the heart beat frequency with a threshold of 3xlO−7 moll−1 and an EC50 of 2.0±0.6xlO−5 moll−1 (mean±s.D., N = 8). At lO−4moll−1 and above the heart beat was completely and reversibly inhibited. 2. The agonist potency profile of the Limulus heart chronotropic GABA receptor was very similar to that of the vertebrate GABAA receptor: muscimol &gt; ZAPA&gt;GABA=⋍TACA&gt;isoguvacine&gt;THIP&gt;3-aminopropane sulphoni

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Pan, Wen, Wen-Yuan Wu, Yan-Hua Bing, Chun-Ping Chu, Ri Jin, and De-Lai Qiu. "Mechanisms of Etomidate-Mediated Decrease of Spontaneous Spike Activity of Mouse Cerebellar Purkinje Cells in vivo." Pharmacology 103, no. 1-2 (2018): 82–92. http://dx.doi.org/10.1159/000494980.

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Etomidate is an imidazole, nonbarbiturate hypnotic agent that is increasingly used in procedural sedation. However, the effects of etomidate on the spontaneous activity of cerebellar Purkinje cells (PCs) in living mouse have not been fully understood. In this study, we investigated the effects of etomidate on the spontaneous simple spike (SS) activity of PCs in urethane-anesthetized mice by cell-attached recording and pharmacological methods. Cerebellar surface application of etomidate (50 μmol\L) reduced the SS firing rate in a concentration-dependent manner (IC50: 43.4 µmol\L). Application o

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Avsar, Timucin, Berfu Nur Yigit, Gizem Turan, et al. "Development of imidazolone based angiotensin II receptor type I inhibitor small molecule as a chemotherapeutic agent for cell cycle inhibition." All Life 14, no. 1 (2021): 678–90. http://dx.doi.org/10.1080/26895293.2021.1954098.

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Cotten, Joseph F., S. Shaukat Husain, Stuart A. Forman, et al. "Methoxycarbonyl-etomidate." Anesthesiology 111, no. 2 (2009): 240–49. http://dx.doi.org/10.1097/aln.0b013e3181ae63d1.

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Background Etomidate is a rapidly acting sedative-hypnotic that provides hemodynamic stability. It causes prolonged suppression of adrenocortical steroid synthesis; therefore, its clinical utility and safety are limited. The authors describe the results of studies to define the pharmacology of (R)-3-methoxy-3-oxopropyl1-(1-phenylethyl)-1H-imidazole-5-carboxylate (MOC-etomidate), the first etomidate analogue designed to be susceptible to ultra-rapid metabolism. Methods The gamma-aminobutyric acid type A receptor activities of MOC-etomidate and etomidate were compared by using electrophysiologic

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Shin, Soona, Nobunao Wakabayashi, Vikas Misra, et al. "NRF2 Modulates Aryl Hydrocarbon Receptor Signaling: Influence on Adipogenesis." Molecular and Cellular Biology 27, no. 20 (2007): 7188–97. http://dx.doi.org/10.1128/mcb.00915-07.

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ABSTRACT The NF-E2 p45-related factor 2 (NRF2) and the aryl hydrocarbon receptor (AHR) are transcription factors controlling pathways modulating xenobiotic metabolism. AHR has recently been shown to affect Nrf2 expression. Conversely, this study demonstrates that NRF2 regulates expression of Ahr and subsequently modulates several downstream events of the AHR signaling cascade, including (i) transcriptional control of the xenobiotic metabolism genes Cyp1a1 and Cyp1b1 and (ii) inhibition of adipogenesis in mouse embryonic fibroblasts (MEFs). Constitutive expression of AHR was affected by Nrf2 ge

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Brusina, M. A., L. G. Kubarskaya, V. V. Iljin, D. N. Nikolaev, and L. B. Piotrovskiy. "DESIGN OF COMPOUNDS WITH ANTICONVULSANT ACTIVITY AMONG NMDA-RECEPTOR LIGANDS." Medical academic journal 19, no. 1S (2019): 225–26. http://dx.doi.org/10.17816/maj191s1225-226.

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NMDA receptors play an important role in the development of immune responses. Therefore, the design of NMDAergic compounds presents great interest in various areas, including immunology. We have previously shown that some imidazole-4,5-dicarboxylic acid (IDA) derivatives are ligands of these receptors, and can exhibit both agonistic and antagonistic activities. In continuation of these studies and in attempt to establish the main structural parameters that determine the type of the activity, we developed a general method for synthesis of 1-, 2-mono and 1,2-disubstituted IDA derivatives. To est

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Ernsberger, Paul, Jacob E. Friedman, and Richard J. Koletsky. "The I1-imidazoline receptor." Journal of Hypertension 15 (1997): S9—S23. http://dx.doi.org/10.1097/00004872-199715011-00002.

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Lehmann, John, Elisabeth Koenig-Bérard, and Philippe Vitou. "The imidazoline-preferring receptor." Life Sciences 45, no. 18 (1989): 1609–15. http://dx.doi.org/10.1016/0024-3205(89)90270-1.

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Bousquet, P., J. Feldman, and L. Monassier. "Imidazoline receptor ligands:cardiovascular applications." Emerging Drugs 3, no. 1 (1998): 113–20. http://dx.doi.org/10.1517/14728214.3.1.113.

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ZHU, H. "Relationship between Platelet Imidazoline Receptor-Binding Peptides and Candidate Imidazoline-1 Receptor, IRAS." Annals of the New York Academy of Sciences 1009, no. 1 (2003): 439–46. http://dx.doi.org/10.1196/annals.1304.058.

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Wang, Gang, Oleg S. Gorbatyuk, S. Regunathan, Govindan Dayanithi, Teresa A. Milner, and Donald J. Reis. "Agmatine Is an Autocrine/Paracrine Inhibitor of Pre-Synaptic Ca ⁺⁺ Channels and Vasopressin Release in Vasopressinergic Neurons of the Hypothalamo-Hypophyseal Tract." Hypertension 36, suppl_1 (2000): 681. http://dx.doi.org/10.1161/hyp.36.suppl_1.681-c.

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20 Agmatine (decarboxylated arginine), an organic cation, endogenous ligand at imidazoline (I-) and α 2 -adrenergic receptors, antagonist of NMDA receptors and inhibitor of nitric oxide synthase, may be a novel neurotransmitter in mammalian CNS (Reis and Regunathan, TIPS, 2000). To further establish a cellular function of agmatine we investigated whether it is expressed in, and regulates the function of, magnocellular neurons of the hypothalamic paraventricular (PVH)/supraoptic (SON) nuclei in rat. By LM, agmatine-like immunoreactivity (Ag-LI) was present in virtually all magnocellular PVH and

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Miyamoto, Masahiko, Naohiko Onozato, Dakshnamurthy Selvakumar, Tetsuya Kimura, Yasuhiro Furuichi, and Tadazumi Komiyama. "The role of the histidine-35 residue in the cytocidal action of HM-1 killer toxin." Microbiology 152, no. 10 (2006): 2951–58. http://dx.doi.org/10.1099/mic.0.29100-0.

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Diethylpyrocarbonate modification and site-directed mutagenesis studies of histidine-35 in HM-1 killer toxin (HM-1) have shown that a specific feature, the imidazole side chain of histidine-35, is essential for the expression of the killing activity. In subcellular localization experiments, wild-type HM-1 was in the membrane fraction of Saccharomyces cerevisiae BJ1824, but not the HM-1 analogue in which histidine-35 was replaced by alanine (H35A HM-1). Neither wild-type nor H35A HM-1 was detected in cellular fractions of HM-1-resistant yeast S. cerevisiae BJ1824 rhk1Δ : : URA3 and HM-1-insensi

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Demaurex, N., A. Monod, D. P. Lew, and K. H. Krause. "Characterization of receptor-mediated and store-regulated Ca2+ influx in human neutrophils." Biochemical Journal 297, no. 3 (1994): 595–601. http://dx.doi.org/10.1042/bj2970595.

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1. It is not known to what extent the emptying of intracellular Ca2+ stores participates in the mediation of chemoattractant-induced Ca2+ influx in human neutrophils. To study this question, we compared the properties of bivalent-cation influx in response to the chemoattractant N-formyl-L-methionyl-L-leucyl-L-phenyl-alanine (f-MLP) and to the microsomal Ca(2+)-ATPase inhibitor thapsigargin. 2. The influx pathway activated by f-MLP and thapsigargin had identical properties of permeation. Mn2+ influx became saturated at around 1 mM extracellular Mn2+, whereas Ca2+ influx did not become saturated

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Sasmal, Pujan, Shyamal Kumar Biswas, Akash Koley, Rimpa Jana, and Jagrity Biswas. "DESIGN AND DISCOVERY OF LOPHINE DERIVATIVES AS MULTI-TARGETING AGENTS BY MOLECULAR DOCKING, ADMET, MD SIMULATION AND PHARMACOPHORE ANALYSIS: A COMPUTATIONAL APPROACH." Turkish Computational and Theoretical Chemistry 9, no. 3 (2024): 1–24. https://doi.org/10.33435/tcandtc.1531766.

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Background Lophine is one of the new core moiety with substitution of three phenyl rings at 2nd, 4th, and 5th position of the imidazole. Lophine is not explored in development of drug molecules. In this research, we have designed 30 lophine derivatives with different substituted functional groups. The designed compounds were evaluated through different In-silico tools and softwares to check their properties for different biological receptors. Methods Molecular docking study was carried out on different receptors i.e. EGFR for anti-cancer, COX-1, and COX-2 for anti-inflammatory, fungal oxidored

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Chen, Mei-Fen, Jo-Ting Tsai, Li-Jen Chen, et al. "Characterization of Imidazoline Receptors in Blood Vessels for the Development of Antihypertensive Agents." BioMed Research International 2014 (2014): 1–7. http://dx.doi.org/10.1155/2014/182846.

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It has been indicated that activation of peripheral imidazoline I2-receptor (I-2R) may reduce the blood pressure in spontaneously hypertensive rats (SHRs). Also, guanidinium derivatives show the ability to activate imidazoline receptors. Thus, it is of special interest to characterize the I-2R using guanidinium derivatives in blood vessels for development of antihypertensive agent(s). Six guanidinium derivatives including agmatine, amiloride, aminoguanidine, allantoin, canavanine, and metformin were applied in this study. Western blot analysis was used for detecting the expression of imidazoli

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Atlas, Daphne, Sophia Diamant, and Ruth Zonnenschein. "Is Imidazoline Site a Unique Receptor?" American Journal of Hypertension 5, no. 4_Pt_2 (1992): 83S—90S. http://dx.doi.org/10.1093/ajh/5.4.83s.

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van Zwieten, P. A. "Centrally Acting Imidazoline I1-Receptor Agonists." American Journal of Cardiovascular Drugs 1, no. 5 (2001): 321–26. http://dx.doi.org/10.2165/00129784-200101050-00002.

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Forman, Stuart A., and David S. Warner. "Clinical and Molecular Pharmacology of Etomidate." Anesthesiology 114, no. 3 (2011): 695–707. http://dx.doi.org/10.1097/aln.0b013e3181ff72b5.

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This review focuses on the unique clinical and molecular pharmacologic features of etomidate. Among general anesthesia induction drugs, etomidate is the only imidazole, and it has the most favorable therapeutic index for single-bolus administration. It also produces a unique toxicity among anesthetic drugs: inhibition of adrenal steroid synthesis that far outlasts its hypnotic action and that may reduce survival of critically ill patients. The major molecular targets mediating anesthetic effects of etomidate in the central nervous system are specific γ-aminobutyric acid type A receptor subtype

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