Seeman P, Guan H C
Department of Pharmacology, University of Toronto, Canada.
Mol Pharmacol. 1987 Dec;32(6):760-3.
The protonated form of apomorphine was found to be active at the high affinity state of dopamine D1 and D2 receptors in canine striatum, since pH reduction from 7.4 to 6.4 enhanced the apomorphine potency 3-fold at both these sites without affecting the potency of the permanently charged apomorphine methiodide. It was estimated that the protonated form of apomorphine was approximately 20-fold more potent than the uncharged form of apomorphine at both the D1 and the D2 receptors.
阿扑吗啡的质子化形式在犬纹状体中多巴胺D1和D2受体的高亲和力状态下具有活性,因为pH值从7.4降至6.4可使阿扑吗啡在这两个位点的效力增强3倍,而不影响永久带电的阿扑吗啡甲碘化物的效力。据估计,阿扑吗啡的质子化形式在D1和D2受体上的效力比不带电的阿扑吗啡形式大约强20倍。