Imidazoline-preferring receptors are important in the pathophysiology of hypertension. The selective l1-receptor agonists are moxonidine, cimetidine and rilmenidine. Some clinical studies indicate the usefulness of moxonidine therapy in hypertension, arrhythmias and acute myocardial infarction.
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Agmatine diminishes behavioral and endocrine alterations in a rat model of post-traumatic stress disorder.
Neurosci Lett
January 2025
Division of Neuroscience, Smt. Kishoritai Bhoyar College of Pharmacy, Kamptee, Nagpur, Maharashtra 441002, India. Electronic address:
Post-traumatic stress disorder (PTSD), is a severe anxiety disorder characterized by associative fear conditioning. Single prolonged stress (SPS) is a widely accepted reliable animal model to stimulate PTSD. Agmatine is an endogenous neuromodulator of stress; however, its effect on PTSD remains to be investigated.
View Article and Find Full Text PDFModelling of chromatographic and electrophoretic behaviour of imidazoline and alpha adrenergic receptors ligands under different acid-base conditions.
ADMET DMPK
May 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11000 Belgrade, Serbia.
Background And Purpose: The ligands of the imidazoline and α-adrenergic receptors are mainly imidazoline and guanidine derivatives, known as centrally-acting antihypertensives and compounds with potential use in various neurological disorders. The extent of their ionisation has a major influence on their behaviour in the different analytical systems. The main objective of this work was to compare the mechanism of chromatographic retention and electrophoretic mobility under acidic, neutral and basic conditions.
View Article and Find Full Text PDFExploring the reactivity of bicyclic α-iminophosphonates to access new imidazoline I receptor ligands.
Bioorg Chem
October 2023
Laboratory of Medicinal Chemistry (Associated Unit to CSIC), Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, and Institute of Biomedicine (IBUB), University of Barcelona, Av. Joan XXIII, 27-31, E-08028 Barcelona, Spain. Electronic address:
Recent studies pointed out the modulation of imidazoline I receptors (I-IR) by selective ligands as a putative strategy to face neurodegenerative diseases. Foregoing the classical 2-imidazoline/imidazole-containing I-IR ligands, we report a family of bicyclic α-iminophosphonates endowed with high affinity and selectivity upon I-IR and we advanced a representative compound B06 in preclinical phases. In this paper, we describe the synthetic possibilities of bicyclic α-iminophosphonates by exploring its ambivalent reactivity, leading to unprecedented molecules that showed promising activities as I-IR ligands in human brain tissues and good BBB permeation capabilities.
View Article and Find Full Text PDF2-BFI protects against ischemic stroke by selectively acting on NR2B-containing NMDA receptors.
Brain Res
December 2024
Department of Neurology, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China. Electronic address:
Background And Purpose: The intricate roles of NMDA receptors, specifically those containing the NR2A or NR2B subunit, in ischemic stroke pathology necessitate targeted therapeutic investigations. Building on our prior discovery showcasing the neuroprotective potential of 2-(benzofuran-2-yl)-2-imidazoline (2-BFI), an imidazoline I2 receptor ligand, in inhibiting NMDA receptor currents during ischemic stroke, this study aims to elucidate the specific impact of 2-BFI on NR2A- and NR2B-containing NMDARs.
Experimental Approach: Through whole-cell patch-clamp techniques, we observed an inhibition by 2-BFI on NR2A-containing NMDAR currents (IC50 = 238.
Indirect involvement of α-adrenoceptors in the mechanical antihypersensitivity effect induced by the spinally administered imidazoline I receptor ligand LNP599 in a rat model of experimental neuropathy.
Brain Res Bull
October 2024
Department of Physiology, Faculty of Medicine, University of Helsinki, Helsinki, Finland. Electronic address:
Here we assess whether neuropathic pain hypersensitivity is attenuated by spinal administration of the imidazoline I-receptor agonist LNP599 and whether the attenuation involves co-activation of α-adrenoceptors. Spared nerve injury (SNI) model of neuropathy was used to induce mechanical hypersensitivity in male and female rats with a chronic catheter for intrathecal drug administrations. Mechanical sensitivity and heat nociception were assessed behaviorally in the injured limb.
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