关于氯氮平对肾上腺素能神经元的作用机制。
On the mechanism of action of clozapine on the adrenergic neurone.
作者信息
Dorris R L, Shore P A
出版信息
Br J Pharmacol. 1976 Mar;56(3):279-83. doi: 10.1111/j.1476-5381.1976.tb07639.x.
1 The antipsychotic drug, clozapine, lowered noradrenaline and metaraminol (MA) concentrations in the rat heart. This action was blocked by the presence of a ganglionic blocking drug. 2 Other alpha-adrenoceptor blocking drugs (phenoxybenzamine, phentolamine) did not significantly lower heart amine concentrations. An inhibitor of neuronal amine uptake (desipramine) caused only a slight lowering. The combination of phentolamine and desipramine showed considerable activity, and this action was blocked by ganglionic blockade. 3 Clozapine had little or no action in blocking amine uptake, yet greatly potentiated amine release caused by the phentolamine-desipramine combination. 4 Other antipsychotic drugs (haloperidol, chlorpromazine, thioridazine) or other agents (propranolol, atropine) did not share this action of clozapine. 5 Ganglionic blockade markedly delayed amine release induced by reserpine administration. 6 It is suggested that clozapine may have an incomplete reserpine-like effect specifically on the adrenergic neurone, facilitating impulse-induced amine release.
抗精神病药物氯氮平可降低大鼠心脏中去甲肾上腺素和间羟胺（MA）的浓度。这种作用可被神经节阻断药物所阻断。
其他α-肾上腺素受体阻断药物（酚苄明、酚妥拉明）并未显著降低心脏胺类浓度。神经元胺摄取抑制剂（地昔帕明）仅引起轻微降低。酚妥拉明和地昔帕明的组合显示出相当大的活性，且这种作用可被神经节阻断所阻断。
氯氮平在阻断胺摄取方面几乎没有作用，但却极大地增强了酚妥拉明-地昔帕明组合所引起的胺释放。
其他抗精神病药物（氟哌啶醇、氯丙嗪、硫利达嗪）或其他药物（普萘洛尔、阿托品）并不具有氯氮平的这种作用。
神经节阻断显著延迟了利血平给药所诱导的胺释放。
提示氯氮平可能对肾上腺素能神经元具有不完全的类似利血平的作用，促进冲动诱导的胺释放。
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