多巴胺受体拮抗剂对离体蟑螂唾液腺分泌反应的作用。

The action of dopamine receptor antagonists on the secretory response of the cockroach salivary gland in vitro.

Evans A M, Green K L

Department of Pharmacology, University of Edinburgh, U.K.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1990;97(2):283-6. doi: 10.1016/0742-8413(90)90142-v.

Abstract

A study has been made of the potency of a number of dopamine antagonists to inhibit dopamine-induced secretion from the cockroach salivary gland in vitro. 2. Chlorpromazine (0.5-5 microM), SCH23390 (10-100 microM), haloperidol (10-100 microM) and metoclopramide (2 mM) competitively inhibited the secretory response to dopamine. In contrast (+/-)sulpiride (1-100 microM) and domperidone (1-100 microM) had no effect on either basal or dopamine-induced secretion. 3. Apparent dissociation constants (KDapp) were obtained using a 'three point assay'. The rank order of potency (KDapp in parentheses) was as follows: chlorpromazine (0.2 microM) greater than SCH23390 (2.2 microM) greater than haloperidol (17.5 microM) much greater than metoclopramide (1.2 mM). 4. It is concluded that the receptor mediating dopamine-induced secretion in the cockroach salivary gland is similar to the D1/DA1 dopamine receptor and distinct from the D2/DA2 receptor found in mammalian systems.

摘要

已对多种多巴胺拮抗剂在体外抑制蟑螂唾液腺多巴胺诱导分泌的效力进行了研究。2. 氯丙嗪（0.5 - 5微摩尔）、SCH23390（10 - 100微摩尔）、氟哌啶醇（10 - 100微摩尔）和甲氧氯普胺（2毫摩尔）竞争性抑制对多巴胺的分泌反应。相比之下，（±）舒必利（1 - 100微摩尔）和多潘立酮（1 - 100微摩尔）对基础分泌或多巴胺诱导的分泌均无影响。3. 使用“三点测定法”获得了表观解离常数（KDapp）。效力顺序（括号内为KDapp）如下：氯丙嗪（0.2微摩尔）＞SCH23390（2.2微摩尔）＞氟哌啶醇（17.5微摩尔）远大于甲氧氯普胺（1.2毫摩尔）。4. 得出的结论是，介导蟑螂唾液腺多巴胺诱导分泌的受体类似于D1/DA1多巴胺受体，与在哺乳动物系统中发现的D2/DA2受体不同。