Schächter M, Geaney D P, Grahame-Smith D G, Cowen P J, Elliott J M
Br J Clin Pharmacol. 1985 Apr;19(4):453-7. doi: 10.1111/j.1365-2125.1985.tb02670.x.
Using a [3H]-lysergic acid diethylamide [( 3H]-LSD) binding technique, platelet 5-hydroxytryptamine (5-HT) receptor number and affinity were compared in schizophrenics treated with depot thioxanthenes and phenothiazines and controls. There was an approximately 30% increase in platelet receptor number (Bmax) in the patient group. There was a decrease in affinity (increase in Kd) of about 30% in the patient group. This was probably due to the persistence of the neuroleptic in the platelet membrane preparation. There was a weak positive correlation between receptor number and total neuroleptic dosage. The increased number of 5-HT receptors is consistent with the previously reported enhancement of 5-HT-induced platelet aggregation in patients treated with long-term phenothiazines and thioxanthenes. Our findings are compatible with 5-HT up-regulation in human platelets produced by depot neuroleptic therapy. It is not known whether parallel changes may be occurring in brain 5-HT receptors.
采用[3H]-麦角酸二乙酰胺([3H]-LSD)结合技术,对接受长效硫杂蒽类和吩噻嗪类药物治疗的精神分裂症患者及对照组的血小板5-羟色胺(5-HT)受体数量和亲和力进行了比较。患者组血小板受体数量(Bmax)增加了约30%。患者组亲和力下降(Kd增加)约30%。这可能是由于血小板膜制剂中抗精神病药物的持续存在。受体数量与抗精神病药物总剂量之间存在弱正相关。5-HT受体数量增加与先前报道的长期使用吩噻嗪类和硫杂蒽类药物治疗的患者中5-HT诱导的血小板聚集增强一致。我们的研究结果与长效抗精神病药物治疗导致人血小板中5-HT上调相符。尚不清楚脑5-HT受体是否可能发生平行变化。