Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].
Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity[2].Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration[2].Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells[2].
Pirenzepine (intraperitoneal injection; 0.3?mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock[3].
References:
[1]. Carmine AA, et al. Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases. Drugs. 1985 Aug;30(2):85-126.
[2]. Yin QQ, et al. Muscarinic acetylcholine receptor M1 mediates prostate cancer cell migration and invasion through hedgehog signaling. Asian J Androl. 2018 Nov-Dec;20(6):608-614.
[3]. Yabuki Y, et al. The T-type calcium channel enhancer SAK3 inhibits neuronal death following transient brain ischemia via nicotinic acetylcholine receptor stimulation. Neurochem Int. 2017 Sep;108:272-281.