α-氟哌噻吨：一种昆虫唾液腺制剂中多巴胺诱发的液体分泌的拮抗剂。
alpha-Flupenthixol: an antagonist of dopamine-evoked fluid secretion by an insect salivary gland preparation.
作者信息
Breward J, House C R, Smith R K
出版信息
Br J Pharmacol. 1980 May;69(1):123-9. doi: 10.1111/j.1476-5381.1980.tb10891.x.
1 We have demonstrated inhibition of secretory responses of cockroach salivary glands to dopamine, adrenaline, noradrenaline and neurotransmitter by alpha-flupenthixol. This inhibition was slow in onset (60 min) and in reversal (greater than 2 h). 2 Inhibition of responses to adrenaline and noradrenaline was non-competitive, since the maxima and slopes of dose-response curves of these agonists were reduced. 3 Although at low concentrations (less than 3 microM) the antagonism of responses to dopamine showed some characteristics of competitive inhibition, at higher doses non-competitive inhibition was clearly demonstrated. 4 These results are explained in terms of different efficacies of the agonists for the receptors antagonized by alpha-flupenthixol. 5 beta-Flupenthixol was shown to antagonize responses to dopamine; however it was 10 to 100 times less potent than alpha-flupenthixol.
1 我们已经证明，α-氟奋乃静可抑制蟑螂唾液腺对多巴胺、肾上腺素、去甲肾上腺素和神经递质的分泌反应。这种抑制起效缓慢（60分钟），逆转也缓慢（超过2小时）。2 对肾上腺素和去甲肾上腺素反应的抑制是非竞争性的，因为这些激动剂剂量-反应曲线的最大值和斜率降低了。3 尽管在低浓度（小于3微摩尔）时，对多巴胺反应的拮抗表现出一些竞争性抑制的特征，但在高剂量时，非竞争性抑制得到了明确证明。4 这些结果可以根据激动剂对被α-氟奋乃静拮抗的受体的不同效力来解释。5 已表明β-氟奋乃静可拮抗对多巴胺的反应；然而，其效力比α-氟奋乃静低10至100倍。
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