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激动剂和拮抗剂对多巴胺D1和D2受体的选择性

Dopamine D1 and D2 receptor selectivities of agonists and antagonists.

作者信息

Seeman P, Ulpian C

机构信息

Department of Pharmacology, University of Toronto, Canada.

出版信息

Adv Exp Med Biol. 1988;235:55-63. doi: 10.1007/978-1-4899-2723-1_5.

Abstract

The selectivities of various dopamine agonists and antagonists for dopamine D1 and D2 receptors were obtained by comparing their relative dissociation constants for inhibiting the binding of [3H]SCH 23390 at D1 receptors (calf caudate nucleus) and at D2 receptors (pig anterior pituitary tissue). The most selective agonists were SK&F 38393 (for D1) and (+)-PHNO (for D2), while the most selective antagonists were SCH 23390 (for D1) and raclopride or eticlopride (for D2).

摘要

通过比较各种多巴胺激动剂和拮抗剂抑制[³H]SCH 23390在D1受体(小牛尾状核)和D2受体(猪垂体前叶组织)上结合的相对解离常数,得出它们对多巴胺D1和D2受体的选择性。选择性最高的激动剂是SK&F 38393(针对D1)和(+)-PHNO(针对D2),而选择性最高的拮抗剂是SCH 23390(针对D1)和雷氯必利或依替必利(针对D2)。

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