The effect of butaclamol and of other neuroleptic agents on the apomorphine-elicited inhibition of synaptosomal tyrosine hydroxylase activity.

Psychopharmacology communications Pub Date : 1975-01-01
R L Bronaugh, J Tabak, T Ohashi, M Goldstein
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Abstract

The effects of the two enantiomers of butaclamol and of several neuroleptics on the apomorphine-elicited inhibition of synaptosomal tyrosine hydroxylase activity was investigated. The (+) but not the (-) enantiomer of butaclamol reverses the apomorphine-elicited enzyme inhibition. (+) Butaclamol is more potent than the other tested neuroleptics. All the tested neuroleptics reverse the apomorphine-elicited enzyme inhibition but their relative potency differs. Using two criteria, namely the concentrations of neuroleptics required to reverse enzyme inhibition maximally or by 25%, the order of decreasing potency is as follows: (+) butaclamol, fluphenazine, haloperidol, pimozide, chlorpromazine. The results suggest that the reversal of apomorphine-elicited inhibition of synaptosomal tyrosine hydroxylase activity is a valid test model for screening antipsychotic drugs.

丁他卡莫和其他抗精神病药物对阿吗啡引起的突触体酪氨酸羟化酶活性抑制的影响。
研究了丁他卡醇的两种对映体和几种抗精神病药对阿吗啡引起的突触体酪氨酸羟化酶活性的抑制作用。丁他卡莫的(+)对映体而不是(-)对映体逆转阿吗啡引起的酶抑制作用。(+)布他卡摩比其他测试的抗精神病药更有效。所有的抗精神病药都能逆转阿吗啡引起的酶抑制,但它们的相对效力不同。使用两个标准,即最大限度地逆转酶抑制或25%所需的神经抑制剂浓度,降低效力的顺序如下:(+)丁他卡莫、氟非那嗪、氟哌啶醇、吡莫胺、氯丙嗪。结果表明,逆转阿吗啡引起的突触体酪氨酸羟化酶活性抑制是筛选抗精神病药物的有效试验模型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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