Topical application of the antimuscarinic pirenzepine increased lower limb nerve fibre density in a phase 2a study in type 2 patients with diabetes with peripheral neuropathyResearch in context [PDF]
EBioMedicineSummary: Background: There is no effective definitive treatment for diabetic peripheral neuropathy (DPN). Strategies that target nerve pathology, limit nerve degeneration, and promote axon regeneration can potentially be beneficial.
Ajith Sivadasan +12 more
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Mechanisms of Pilocarpine‐Induced Nitric Oxide and Prostaglandin Production in Porcine Ciliary Muscle [PDF]
FASEB BioAdvancesPilocarpine, a muscarinic receptor agonist, is clinically used to reduce intraocular pressure via ciliary muscle contraction. However, the intracellular signaling pathways mediating pilocarpine‐induced nitric oxide (NO) and prostaglandin E2 (PGE2 ...
Giovanna Benozzi +3 more
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Pirenzepine exhibits anti-prostate cancer activity and enhances checkpoint inhibitor-based immunotherapy by targeting STING [PDF]
European Journal of Medical ResearchPurpose Therapeutic options targeting programmed cell death protein 1 (PD-1) and programmed death ligand-1 (PD-L1) have been approved for use in human malignancies, showing clinical benefits.
Jinge Xu +3 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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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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Cholinergic Signaling Mediated by Muscarinic Receptors Triggers the Ultraviolet-Induced Release of Melanosome in Cultured Melanoma Cells. [PDF]
Pigment Cell Melanoma ResSchematic diagram illustrating the role of mAChRs in UVB‐mediated melanosome release. Under UVB irradiation, the epidermal keratinocytes and melanocytes release ACh. ACh stimulates M1/M3 mAChRs and leads to activation of PLC, which thereafter increases the levels of IP3 and DAG, as well as the intracellular Ca2+ and PKC. In addition, the expressions of
Guo MS +8 more
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Evaluation of the Alterations in Central Cholinergic Neurotransmission in Aging and Amyloid Precursor Protein Knock-In Mice. [PDF]
J NeurochemIn Alzheimer's disease, reduced release of ACh is linked more to Aβ pathology than to age‐related change, highlighting an early sign of disease. ABSTRACT A progressive decline in cognitive function occurs as a result of aging and Alzheimer's disease (AD) and is primarily associated with diminished cholinergic neurotransmission.
Nagai-Arakawa I +14 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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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
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