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多巴胺D3受体激动剂7-羟基-DPAT会导致狗呕吐。

A dopamine D3 receptor agonist, 7-OH-DPAT, causes vomiting in the dog.

作者信息

Yoshida N, Yoshikawa T, Hosoki K

机构信息

Department of Pharmacology, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

Life Sci. 1995;57(21):PL347-50. doi: 10.1016/0024-3205(95)02186-m.

Abstract

R(+)7-hydroxy-N,N-di-n-propyl-2-aminotetralin (R(+)-7-OH-DPAT), a selective dopamine D3 receptor agonist, (0.03-0.3 mg/kg, s.c.) dose-relatedly caused emesis, whereas S (-)-7-OH-DPAT at even 1 mg/kg did not induce emesis in dogs. Apomorphine (0.03-0.3 mg/kg, s.c.) or quinpirole (0.03-0.1 mg/kg, s.c.) also caused emesis in a dose-dependent manner. The potency of R(+)-7-OH-DPAT in inducing emesis was the same as that of apomorphine and quinpirole. On the other hand, SKF-38393 (1 and 3 mg/kg, s.c.), a selective D1 receptor agonist, failed to induce emesis in dogs. The emesis induced by R(+)-7-OH-DPAT (0.3 mg/kg, s.c.) was inhibited by S(-)-eticlopride (0.01-0.1 mg/kg, s.c.), a potent D2 and D3 receptor antagonist but not by SCH-23390 (1 mg/kg, s.c.), a selective D1 receptor antagonist or clozapine (1 mg/kg, s.c.), a D4 receptor antagonist. These results indicate that dopamine D3 receptors play an important role in the genesis of emesis in dogs.

摘要

R(+)7-羟基-N,N-二正丙基-2-氨基四氢萘(R(+)-7-OH-DPAT),一种选择性多巴胺D3受体激动剂,(0.03 - 0.3毫克/千克,皮下注射)剂量依赖性地引起呕吐,而即使是1毫克/千克的S(-)-7-OH-DPAT在犬中也不诱发呕吐。阿扑吗啡(0.03 - 0.3毫克/千克,皮下注射)或喹吡罗(0.03 - 0.1毫克/千克,皮下注射)也以剂量依赖性方式引起呕吐。R(+)-7-OH-DPAT诱发呕吐的效力与阿扑吗啡和喹吡罗相同。另一方面,选择性D1受体激动剂SKF-38393(1和3毫克/千克,皮下注射)未能在犬中诱发呕吐。R(+)-7-OH-DPAT(0.3毫克/千克,皮下注射)诱发的呕吐被强效D2和D3受体拮抗剂S(-)-依托必利(0.01 - 0.1毫克/千克,皮下注射)抑制,但不被选择性D1受体拮抗剂SCH-23390(1毫克/千克,皮下注射)或D4受体拮抗剂氯氮平(1毫克/千克,皮下注射)抑制。这些结果表明多巴胺D3受体在犬呕吐的发生中起重要作用。

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