SELECTIVE ACTIVATION OF 5HT1A RECEPTORS INDUCES LOWER LIP RETRACTION IN THE RAT
SELECTIVE ACTIVATION OF 5HT1A RECEPTORS INDUCES LOWER LIP RETRACTION IN THE RAT
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DOI：
10.1016/0091-3057(89)90477-2
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发表时间：
1989-08-01
影响因子：
3.6
通讯作者：
BROEKKAMP, CLE
中科院分区：
文献类型：
--
作者：
BERENDSEN, HHG;JENCK, F;BROEKKAMP, CLE
研究了5 -羟色胺能（5HT）化合物对下唇收缩（LLR）的诱导作用、化合物对LLR的拮抗作用以及通过多种受体系统作用的化合物对LLR的拮抗作用。皮下注射8-羟基-2-（二正丙胺）-四萘林（8-OH-DPAT）、丁螺环酮、ipsapione或ru24969均可诱导LLR。推测的5HT1B无活性。1C激动剂1-（3”-氯苯基）-哌嗪（mCCP）， 5HT2.1C激动剂(dl)-（2,5-二甲氧基-4-碘苯基）-2-氨基丙烷（DOI）， 5HT再摄取抑制剂西酞普兰和帕罗西汀以及5HT释放化合物对氯安非他明（PCA）和芬氟拉明。5-甲氧基- n， n -二甲基色胺（5-MeODMT）经美高林、赛庚啶或利坦色林预处理后可诱导下唇收缩，但不单独作用。8- oh - dpat诱导的LLR可被直接和间接5HT激动剂mCPP、DOI、5-MeODMT、PCA、芬氟拉明和大剂量帕罗西汀拮抗，但不能被5HT拮抗剂美戈林、甲基塞吉特、mesulergine、GR38032F、木胺嘧啶或哌烯酮拮抗。多巴胺激动剂阿波啡和培高利特可拮抗8- oh - dpat诱导的LLR，而SKF 38393的活性较弱。多巴胺拮抗剂氟哌啶醇和spiperone未发现明显的拮抗作用。2激动剂可乐定和。1拮抗剂哌唑嗪和。2拮抗剂咪唑嗪。抗组胺药甲胺、抗胆碱能药阿托品、阿片类拮抗剂纳洛酮和抗焦虑药氯二氮环氧化物也无活性。结果表明，在体内，各种5HT受体之间发生功能相互作用。讨论了下唇收缩是由化合物直接选择性刺激5HT1A受体引起的假说。
The induction of lower lip retraction (LLR) by serotonergic (5HT) compounds and antagonism of LLR by compounds and antagonism of LLR by compounds acting via a variety of receptor systems was investigated. LLR could be induced by subcutaneous injection of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), buspirone, ipsapirone or RU 24969. Inactive were the putative 5HT1B.1C agonist 1-(3''-chlorophenyl)-piperazine (mCCP), the 5HT2.1C agonist (dl)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), the 5HT reuptake inhibitors citalopram and paroxetine and the 5HT-releasing compounds parachloroamphetamine (PCA) and fenfluramine. 5-Methoxy-N,N-dimethyltryptamine (5-MeODMT) induced lower lip retraction after pretreatment with metergoline, cyproheptadine or ritanserin but not by itself. 8-OH-DPAT-induced LLR could be antagonised by the direct and indirect 5HT agonists mCPP, DOI, 5-MeODMT, PCA, fenfluramine and high doses of paroxetine, but not by the 5HT antogonists metergoline, methysergide, mesulergine, GR38032F, xylamidine or pirenperone. The dopamine agonists apomorphine and pergolide antagonised 8-OH-DPAT-induced LLR, whereas SKF 38393 was weakly active. No significant antagonism was found with the dopamine antagonists haloperidol and spiperone, the .alpha.2 agonist clonidine and the .alpha.1 antagonist prazosin and the .alpha.2 antagonist idazoxan. Also inactive were the antihistaminic mepyramine, the anticholinergic atropine, the opiate antagonist naloxone and the anxiolytic chlordiazepoxide. The results suggest that, in vivo, functional interactions take place between the various 5HT receptors. The hypothesis that lower lip retraction is induced by compounds directly and selectively stimulating 5HT1A receptors is discussed.