Autoradiography of 3H-pirenzepine and 3H-AFDX-384 in Mouse Brain Regions: Possible Insights into M1, M2, and M4 Muscarinic Receptors Distribution [PDF]
Frontiers in Pharmacology, 2018 Autoradiography helps to determine the distribution and density of muscarinic receptor (MR) binding sites in the brain. However, it relies on the selectivity of radioligands toward their target.
Paulina Valuskova +4 more
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Unexpected scaffold rearrangement product of pirenzepine found in commercial samples [PDF]
Scientific Reports, 2021 Pharmacovigilance aims at a better understanding of the molecular events triggered by medications to prevent adverse effects, which despite significant advances in our analytical repertoire plague the use of drugs until today. In this study, we find that
Marius Ozenil +10 more
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Prevention of HIV-1 TAT Protein-Induced Peripheral Neuropathy and Mitochondrial Disruption by the Antimuscarinic Pirenzepine [PDF]
Frontiers in Neurology, 2021 HIV-associated distal sensory polyneuropathy (HIV-DSP) affects about one third of people with HIV and is characterized by distal degeneration of axons. The pathogenesis of HIV-DSP is not known and there is currently no FDA-approved treatment.
May Madi Han +5 more
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Pirenzepine Promotes the Dimerization of Muscarinic M1 Receptors through a Three-step Binding Process* [PDF]
Journal of Biological Chemistry, 2009 Ligand binding to G protein-coupled receptors is a complex process that involves sequential receptor conformational changes, ligand translocation, and possibly ligand-induced receptor oligomerization.
B. Ilien +8 more
semanticscholar +2 more sources
Pirenzepine Binding Sites in the Brain of the Honeybee Apis mellifera: Localization and Involvement in Non-Associative Learning [PDF]
Insects, 2022 Muscarinic acetylcholine receptors (mAChRs) play a central role in learning and memory in mammals as in honeybees. The results obtained in the honeybee Apis mellifera are based on the detrimental effects of the mAChR antagonists, atropine and scopolamine,
Chaïma Messikh +2 more
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Muscarinic acetylcholine receptor activated effectors in principal neurons of the rat basolateral amygdala [PDF]
Frontiers in Cellular NeuroscienceThe basolateral amygdala (BLA) plays a crucial role in context-specific learning and memory by integrating valence-specific stimuli with internal physiological states.
Todd J. Sahagian +7 more
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GDM enhanced acetylcholine induced vasoconstriction in human umbilical vein via CHRM3 and CACNA1C upregulation linked to promoter hypomethylation [PDF]
Scientific ReportsIntrauterine exposure to hyperglycemia increases the risk of hypertension disorders in the offspring. Vascular dysfunction has a critical role in hypertension development.
Yun He +6 more
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Poly (ADP-Ribose) Polymerase-1 (PARP1) Deficiency and Pharmacological Inhibition by Pirenzepine Protects From Cisplatin-Induced Ototoxicity Without Affecting Antitumor Efficacy [PDF]
Frontiers in Cellular Neuroscience, 2019 Cisplatin remains an indispensable drug for the systemic treatment of many solid tumors. However, a major dose-limiting side-effect is ototoxicity. In some scenarios, such as treatment of germ cell tumors or adjuvant therapy of non-small cell lung cancer,
Anke Tropitzsch +7 more
doaj +2 more sources
Translating Basic Science to Clinical Applications: A Narrative Review of Repurposed Pharmacological Agents in Preclinical Models of Diabetic Neuropathy [PDF]
BiomedicinesDiabetic neuropathy (DN) remains a major clinical burden, characterized by progressive sensory dysfunction, pain, and impaired quality of life. Despite the available symptomatic treatments, there is a pressing need for disease-modifying therapies.
Corina Andrei +3 more
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Identification of Antagonistic Action of Pyrrolizidine Alkaloids in Muscarinic Acetylcholine Receptor M1 by Computational Target Prediction Analysis [PDF]
PharmaceuticalsPyrrolizidine alkaloids (PAs) are one of the largest distributed classes of toxins in nature. They have a wide range of toxicity, such as hepatotoxicity, pulmonary toxicity, neuronal toxicity, and carcinogenesis.
Sara Abdalfattah +7 more
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