产品描述:
Pinaverium is an inhibitor of L-type voltage-gated calcium channels (Cav; IC50 = 1.5 µM in a patch-clamp assay using isolated rabbit jejunal smooth muscle cells).{66736,66737} It binds to CHO cells expressing the Cav1.2 α1C-a or α1C-b subunits (Kis = 1.5 and 2.92 µM, respectively).{66736} Pinaverium inhibits contractions induced by acetylcholine (ACh; Item No. 23829) or potassium chloride in colonic circular muscle strips isolated from non-stressed or cold-restraint-stressed rats (IC50s = 0.91 and 1.66 µM for ACh, respectively, and 3.8 and 8.13 µM for potassium chloride, respectively) in a model of stress-induced smooth muscle contractility disorder.{66738} It increases survival and decreases pulmonary neutrophil infiltration in a mouse model of LPS-induced septic shock when administered at doses ranging from 1 to 10 mg/kg.{66739} Formulations containing pinaverium have been used in the treatment of irritable bowel syndrome (IBS).