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选择性D1和D2多巴胺激动剂对离体蟑螂唾液腺腺泡细胞的影响。

Effects of selective D1 and D2 dopamine agonists on cockroach salivary gland acinar cells in vitro.

作者信息

Evans A M, Green K L

机构信息

Department of Pharmacology, University of Edinburgh.

出版信息

Br J Pharmacol. 1991 Dec;104(4):787-92. doi: 10.1111/j.1476-5381.1991.tb12507.x.

Abstract
  1. The ability of the selective dopamine receptor agonists, fenoldopam and SKF38393 (D1) and quinpirole and LY163502 (D2), to mimic the effect of dopamine on cockroach salivary gland acinar cells has been investigated. 2. Intracellular recordings of the membrane potential established that all the agonists mimicked dopamine (i.e. they induced a hyperpolarization which was occasionally followed by a depolarization), whether applied by addition to the superfusate or locally by pressure ejection. 3. The rank order of potency of the agonists to induce a hyperpolarization was (equipotent molar ratio relative to dopamine in parentheses): dopamine (1) much much greater than fenoldopam (1000) greater than SKF38393 (3500) greater than LY163502 (13750) greater than quinpirole (35000). 4. The agonists also elicited secretion from the salivary gland when superfused onto the preparation. SKF38393 and quinpirole did not induce the same maximum rate of secretion as dopamine. The rank order of potency of the agonists was (minimum effective concentration in parentheses): dopamine (0.03 microM) much much greater than fenoldopam (4.8 microM) greater than SKF38393 (40.8 microM) greater than quinpirole (132 microM). 5. Both the hyperpolarizing and secretory responses to all the agonists were antagonized by the selective D1 antagonist, (+)-SCH23390, but not the selective D2 antagonist, (+/-)-sulpiride. 6. These results support the idea that the same receptors mediate both the hyperpolarizing and secretory responses, and that they are similar to the mammalian D1 receptor.
摘要
  1. 已研究了选择性多巴胺受体激动剂非诺多泮和SKF38393(D1)以及喹吡罗和LY163502(D2)模拟多巴胺对蟑螂唾液腺腺泡细胞作用的能力。2. 对膜电位进行的细胞内记录表明,所有激动剂均能模拟多巴胺(即它们诱导超极化,偶尔随后出现去极化),无论是添加到灌流液中还是通过压力喷射局部应用。3. 激动剂诱导超极化的效价顺序为(相对于多巴胺的等效摩尔比,括号内):多巴胺(1)远大于非诺多泮(1000)大于SKF38393(3500)大于LY163502(13750)大于喹吡罗(35000)。4. 当将激动剂灌流到标本上时,它们也能引起唾液腺分泌。SKF38393和喹吡罗诱导的最大分泌速率与多巴胺不同。激动剂的效价顺序为(括号内为最小有效浓度):多巴胺(0.03微摩尔)远大于非诺多泮(4.8微摩尔)大于SKF38393(40.8微摩尔)大于喹吡罗(132微摩尔)。5. 对所有激动剂的超极化和分泌反应均被选择性D1拮抗剂(+)-SCH23390拮抗,但未被选择性D2拮抗剂(+/-)-舒必利拮抗。6. 这些结果支持这样的观点,即相同的受体介导超极化和分泌反应,并且它们与哺乳动物D1受体相似。

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SCH 23390 - the first selective dopamine D-1 antagonist.SCH 23390——首个选择性多巴胺D-1拮抗剂。
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