Bronaugh R L, Tabak J, Ohashi T, Goldstein M
Psychopharmacol Commun. 1975;1(5):501-10.
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.
研究了布他拉莫的两种对映体以及几种抗精神病药物对阿扑吗啡引起的突触体酪氨酸羟化酶活性抑制的影响。布他拉莫的(+)对映体而非(-)对映体可逆转阿扑吗啡引起的酶抑制作用。(+)布他拉莫比其他受试抗精神病药物更有效。所有受试抗精神病药物均可逆转阿扑吗啡引起的酶抑制作用,但其相对效力有所不同。使用两个标准,即最大程度或25%逆转酶抑制作用所需的抗精神病药物浓度,效力递减顺序如下:(+)布他拉莫、氟奋乃静、氟哌啶醇、匹莫齐特、氯丙嗪。结果表明,阿扑吗啡引起的突触体酪氨酸羟化酶活性抑制的逆转是筛选抗精神病药物的有效测试模型。