Pirenzepine (LS 519 free base) is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits gastric acid secretion and reduces muscle spasm, making it a valuable compound for investigating peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative activity against 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]. Cell Proliferation Assay [2] Cell Line: PC-3 cells Concentration: 100-140 μg/mL Incubation Time: 24 hours Result: Inhibited PC-3 cell proliferation in a concentration-dependent manner. Cell Migration Assay [2] Cell Line: PC-3 and A549 cells Concentration: 110 μg/mL Incubation Time: 24 hours Result: Inhibited the migration of PC-3 and A549 cell lines (P=0.014). Western Blot Analysis [2] Cell Line: PC-3 cells Concentration: 110 μg/mL Incubation Time: 0-24 hours Result: Inhibited the expression of GLI1 and PTCH1. RT-PCR [2] Cell Line: PC-3 cell Concentration: 100-130 μg/mL Incubation Time: 24 hours Result: Suppressed GLI1 mRNA expression in PC-3 cells. Increased PTCH1 mRNA level but not reach statistical significance. Showed no SHH mRNA expression level change.

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock [3]. Animal Model: Male C57BL/6 mice with experimental endotoxemia [3] Dosage: 0.3 mg/kg Administration: Intraperitoneal injection; 0.3 mg/kg; once Result: Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.