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被哌仑西平区分的毒蕈碱受体参与大鼠伏隔核中神经递质释放的调节。

Muscarinic receptors discriminated by pirenzepine are involved in the regulation of neurotransmitter release in rat nucleus accumbens.

作者信息

de Belleroche J, Gardiner I M

出版信息

Br J Pharmacol. 1985 Oct;86(2):505-8. doi: 10.1111/j.1476-5381.1985.tb08921.x.

Abstract

The effect of pirenzepine, a selective muscarinic antagonist, was tested on the oxotremorine facilitation of the K+-evoked release of [14C]-dopamine from tissue slices of rat nucleus accumbens. The effect of pirenzepine was compared with that of scopolamine and other antagonists which show no heterogeneity in their action on muscarinic receptors in order to determine whether a selective action at a single receptor subtype, M1 or M2, could be distinguished. Pirenzepine and scopolamine both antagonized the oxotremorine-induced (EC50 = 3 X 10(-7) M) facilitation of [14C]-dopamine release with pA2 values of 7.5 and 8.9 respectively. This result indicated that the high affinity pirenzepine receptor (M1) was involved in this response. Low concentrations of 3-quinuclidinyl benzilate (3 X 10(-10) M), N-methylscopolamine (3 X 10(-9) M) and methyl atropine (10(-8) M) also abolished this facilitatory effect of oxotremorine.

摘要

对选择性毒蕈碱拮抗剂哌仑西平,就氧化震颤素对大鼠伏隔核组织切片中钾离子诱发的[14C] - 多巴胺释放的促进作用进行了测试。将哌仑西平的作用与东莨菪碱及其他对毒蕈碱受体作用无异质性的拮抗剂的作用进行比较,以确定是否能区分对单一受体亚型M1或M2的选择性作用。哌仑西平和东莨菪碱均拮抗氧化震颤素诱导的(EC50 = 3×10(-7) M)[14C] - 多巴胺释放,其pA2值分别为7.5和8.9。该结果表明高亲和力的哌仑西平受体(M1)参与了此反应。低浓度的3 - 喹核醇基苯甲酸酯(3×10(-10) M)、N - 甲基东莨菪碱(3×10(-9) M)和甲基阿托品(10(-8) M)也消除了氧化震颤素的这种促进作用。

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1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.

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