Pinaverium (bromide)

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). It binds to CHO cells expressing the Cav1.2 alpha1C-a or alpha1C-b subunits (Kis = 1.5 and 2.92 µM, respectively). Pinaverium inhibits contractions induced by acetylcholine (ACh, Cay-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. 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. Formulations containing pinaverium have been used in the treatment of irritable bowel syndrome (IBS).Formal Name: 4-[(2-bromo-4,5-dimethoxyphenyl)methyl]-4-[2-[2-(6,6-dimethylbicyclo[3.1.1]hept-2-yl)ethoxy]ethyl]-morpholinium, monobromide. CAS Number: 53251-94-8. Synonyms: PVB. Molecular Formula: C26H41BrNO4 . Br. Formula Weight: 591.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml, PBS (pH 7.2): Soluble: >10 mg/ml. SMILES: CC1(C2C(CCOCC[N+]3(CC4=C(Br)C=C(OC)C(OC)=C4)CCOCC3)CCC1C2)C.[Br-]. InChi Code: InChI=1S/C26H41BrNO4.BrH/c1-26(2)21-6-5-19(22(26)16-21)7-11-31-12-8-28(9-13-32-14-10-28)18-20-15-24(29-3)25(30-4)17-23(20)27,/h15,17,19,21-22H,5-14,16,18H2,1-4H3,1H/q+1,/p-1. InChi Key: IKGXLCMLVINENI-UHFFFAOYSA-M.