人类大脑皮层中释放调节性多巴胺自身受体。
Release-regulating dopamine autoreceptors in human cerebral cortex.
作者信息
Fedele E, Andrioli G C, Ruelle A, Raiteri M
机构信息
Institute of Pharmacology and Pharmacognosy, University of Genova, Italy.
出版信息
Br J Pharmacol. 1993 Sep;110(1):20-2. doi: 10.1111/j.1476-5381.1993.tb13765.x.
Abstract
Slices from fresh specimens of human neocortex which had to be removed during neurosurgery to reach subcortical tumours were labelled with [3H]-dopamine and stimulated electrically. Quinpirole, a selective dopamine D2 receptor agonist, inhibited the stimulated tritium overflow (EC50 = 25 nM; maximal inhibition: about 80% at 10 microM). The selective D1 receptor agonist, SKF 38393, was inactive up to 10 microM. Quinpirole was antagonized by the D2 receptor antagonist (-)-sulpiride (apparent pA2 = 8.26). Thus dopaminergic axon terminals in the human mesocortical pathway possess autoreceptors of the D2 type.
摘要
为了切除皮质下肿瘤而在神经外科手术中必须切除的人类新皮质新鲜标本切片，用[3H] - 多巴胺进行标记并电刺激。喹吡罗，一种选择性多巴胺D2受体激动剂，抑制刺激后的氚溢出（EC50 = 25 nM；最大抑制：在10 microM时约为80%）。选择性D1受体激动剂SKF 38393在高达10 microM时无活性。喹吡罗被D2受体拮抗剂（-）-舒必利拮抗（表观pA2 = 8.26）。因此，人类中皮质通路中的多巴胺能轴突终末具有D2型自身受体。
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