Juneja R, Gupta I, Wali A, Chakravarti R N, Majumdar S
Department of Obstetrics and Gynecology, Postgraduate Institute of Medical Education and Research, Chandigarh, India.
Contraception. 1990 Apr;41(4):419-29. doi: 10.1016/0010-7824(90)90041-s.
Verapamil, a potent calcium channel blocker, was administered orally at three different doses to guinea pigs for both short- (4 weeks) and long-term (12 weeks) effects. The drug treatment stimulated Ca(++)-transport and Ca(++)-activated ATPase in isolated plasma membrane vesicles of guinea pig spermatozoa. Ca(++)-uptake studies exhibited partial to complete restoration of stimulated Ca(++)-transport during recovery period, whereas the CA(++)-activated ATPase system remained stimulated even after 4 and 6 weeks of withdrawal of the drug treatment. The lack of inhibitory effect of verapamil on Ca(++)-uptake ruled out the involvement of calcium channels in spermatozoal calcium uptake in guinea pigs. The stimulatory effect of the drug on CA(++)-uptake, on the other hand, might indicate the possible capability of this lipophilic compound to induce favourable changes in the lipid microenvironment of the membrane, wherein the integral membrane proteins operate.
维拉帕米是一种强效钙通道阻滞剂，以三种不同剂量口服给予豚鼠，以研究短期（4周）和长期（12周）效应。药物治疗刺激了豚鼠精子分离质膜囊泡中的Ca(++)转运和Ca(++)激活的ATP酶。Ca(++)摄取研究显示，在恢复期，刺激的Ca(++)转运部分至完全恢复，而即使在停药治疗4周和6周后，Ca(++)激活的ATP酶系统仍受到刺激。维拉帕米对Ca(++)摄取缺乏抑制作用，排除了钙通道参与豚鼠精子钙摄取的可能性。另一方面，该药物对Ca(++)摄取的刺激作用可能表明这种亲脂性化合物可能有能力在膜的脂质微环境中诱导有利变化，而膜整合蛋白在该微环境中发挥作用。
