Nicolau M, Lapa A J, Valle J R
Arch Int Pharmacodyn Ther. 1978 Nov;236(1):131-6.
To analyse the influence of delta9-Tetrahydrocannabinol (THC) on the effects induced by sympathomimetic, parasympathomimetic and direct spasmogenic drugs, the isolated rat vas deferens preparation was chosen. Instead of the usual emulsifying agents, we have used 1% ethanol (ET-OH) to keep the cannabinoids in homogeneous dispersion in the bath. THC exerted a non-competitive inhibition of noradrenaline and of acetylcholine responses but no synergistic action nor competitive antagonism was seen on the dose range used. BaCl2 was potentiated by ethanol and this effect was abolished by THC. The water soluble derivative SP 111 showed actions similar to those of THC on noradrenaline and acetylcholine responses. It did not affect BaCl2 contractions, indicating that the cannabinoid might act by depressing early events of membrane activation.
为分析δ9-四氢大麻酚(THC)对拟交感神经药、拟副交感神经药和直接致痉药所诱导效应的影响,选用了离体大鼠输精管制备物。我们使用1%乙醇(ET-OH)替代常用乳化剂,以使大麻素在浴槽中保持均匀分散。THC对去甲肾上腺素和乙酰胆碱反应产生非竞争性抑制,但在所使用的剂量范围内未观察到协同作用或竞争性拮抗作用。乙醇增强了BaCl2的作用,而THC消除了这种效应。水溶性衍生物SP 111对去甲肾上腺素和乙酰胆碱反应表现出与THC相似的作用。它不影响BaCl2引起的收缩,这表明大麻素可能通过抑制膜激活的早期事件发挥作用。