Araki K, Ohashi T, Gomi Y
J Pharmacobiodyn. 1983 Apr;6(4):254-60. doi: 10.1248/bpb1978.6.254.
Effects of tripelennamine, N,N-dimethyl-N',N'-dibenzylethylenediamine (DBED) and N,N-dibenzyl-N',N'-dimethyl-1,2-propanediamine (DBPD) on the isotonic contractions of isolated vas deferens of intact and reserpinized guinea pigs to acetylcholine were examined. Increase in sensitivity to acetylcholine induced by tripelennamine, DBED and DBPD was attenuated remarkably by reserpine. Tripelennamine- and DBED-induced increases in Ca2+-contractions were not affected by reserpine. Acetylcholine-contractions in Ca2+-free Tyrode solution were inhibited by reserpine, but K+-contractions in Ca2+-free Tyrode solution were not affected by reserpine. Tripelennamine- and DBED-induced increases in acetylcholine- and K+-contractions in Ca2+-free Tyrode solution were attenuated or abolished by reserpine. DBPD decreased cholinesterase activity of vas deferens of guinea pig, but DBED did not. These results suggest that, although the Ca2+-storage site utilized for acetylcholine-contraction is different from that for K+-contraction, tripelennamine- and DBED-induced increase in Ca2+-release from superficial Ca2+-binding sites induced by acetylcholine and K+ is inhibited by reserpine. It is also estimated that DBPD-induced supersensitivity to acetylcholine might be due to the inhibition of cholinesterase activity. However, the mechanism of inhibition of DBPD-induced supersensitivity by reserpine remained obscure.
研究了曲吡那敏、N,N-二甲基-N',N'-二苄基乙二胺（DBED）和N,N-二苄基-N',N'-二甲基-1,2-丙二胺（DBPD）对完整和利血平化豚鼠离体输精管对乙酰胆碱等张收缩的影响。利血平显著减弱了曲吡那敏、DBED和DBPD所诱导的对乙酰胆碱敏感性的增加。曲吡那敏和DBED所诱导的Ca²⁺收缩增加不受利血平影响。在无Ca²⁺的台氏液中，利血平抑制乙酰胆碱收缩，但不影响无Ca²⁺台氏液中的K⁺收缩。在无Ca²⁺台氏液中，曲吡那敏和DBED所诱导的乙酰胆碱和K⁺收缩增加被利血平减弱或消除。DBPD降低豚鼠输精管的胆碱酯酶活性，但DBED没有。这些结果表明，虽然用于乙酰胆碱收缩的Ca²⁺储存位点与用于K⁺收缩的不同，但曲吡那敏和DBED所诱导的由乙酰胆碱和K⁺引起的浅表Ca²⁺结合位点Ca²⁺释放增加被利血平抑制。还估计DBPD所诱导的对乙酰胆碱超敏反应可能是由于胆碱酯酶活性的抑制。然而，利血平抑制DBPD所诱导的超敏反应的机制仍不清楚。
