Kennett G A, Curzon G
Institute of Neurology, Queen Square, London, UK.
Psychopharmacology (Berl). 1988;96(1):93-100. doi: 10.1007/BF02431539.
Male Sprague-Dawley rats deprived of food for 18 h were injected with the 5-HT agonists RU 24969, 1-(3-chlorophenyl)piperazine (mCPP) or 1-[3-(trifluoromethyl)phenyl)]piperazine (TFMPP) and 20 min later presented with their normal diet. Food intake was determined 1, 2 and 4 h later. All three drugs reduced intake over 1 and 2 h. Three out of four drugs with high affinity for 5-HT1C receptors (metergoline, mianserin, and mesulergine but not cyproheptadine) opposed hypophagia caused by mCPP. Another drug reported to have high affinity for the 5-HT1C site, 1-naphthyl-piperazine (1-NP), also blocked the hypophagic response to mCPP at doses which attenuated mCPP-induced hypolocomotion. Only one of the above drugs (metergoline) which also has high affinity for other 5-HT sites opposed hypophagia caused by RU 24969. Two out of three 5-HT1B receptor antagonists [(+/-) cyanopindolol, (-) propranolol, but not (-) pindolol)] which oppose hypophagia caused by RU 24969 (Kennett et al. 1987) also opposed hypophagia caused by mCPP. The 5-HT2 antagonists ketanserin and ritanserin, the 5-HT3 antagonist ICS 205-930 and the alpha 2 adrenoceptor antagonist idazoxan did not oppose the hypophagic effect of mCPP. In agreement with results for mCPP, hypophagia caused by TFMPP was opposed by both, mianserin and (+/-) cyanopindolol. Given alone, mianserin 1-NP and cyproheptadine but not ICS 205-930 increased food consumption of normally fed rats. The results suggest that RU 24969-induced hypophagia depends on 5-HT1B receptors but not on 5-HT1C receptors, while mCPP (and TFMPP)-induced hypophagia may depend on both receptors.(ABSTRACT TRUNCATED AT 250 WORDS)
将禁食18小时的雄性斯普拉格-道利大鼠注射5-羟色胺(5-HT)激动剂RU 24969、1-(3-氯苯基)哌嗪(mCPP)或1-[3-(三氟甲基)苯基]哌嗪(TFMPP),20分钟后给予其正常饮食。分别在1小时、2小时和4小时后测定食物摄入量。所有三种药物在1小时和2小时内均减少了食物摄入量。对5-HT1C受体具有高亲和力的四种药物中的三种(美替拉酮、米安色林和甲磺ergine,但不是赛庚啶)对抗由mCPP引起的食欲减退。另一种据报道对5-HT1C位点具有高亲和力的药物1-萘基哌嗪(1-NP),在减弱mCPP诱导的运动减少的剂量下,也阻断了对mCPP的食欲减退反应。上述药物中只有一种(美替拉酮)对其他5-HT位点也具有高亲和力,它对抗由RU 24969引起的食欲减退。三种5-HT1B受体拮抗剂中的两种[(+/-)氰吲哚洛尔、(-)普萘洛尔,但不是(-)吲哚洛尔],它们对抗由RU 24969引起的食欲减退(肯尼特等人,1987年),也对抗由mCPP引起的食欲减退。5-HT2拮抗剂酮色林和利坦色林、5-HT3拮抗剂ICS 205-930和α2肾上腺素能受体拮抗剂伊达唑烷均不对抗mCPP的食欲减退作用。与mCPP的结果一致,由TFMPP引起的食欲减退被米安色林和(+/-)氰吲哚洛尔两者所对抗。单独给予时,米安色林、1-NP和赛庚啶,但不是ICS 205-930,增加了正常喂养大鼠的食物消耗量。结果表明,RU 24969诱导的食欲减退取决于5-HT1B受体而不是5-HT1C受体,而mCPP(和TFMPP)诱导的食欲减退可能取决于这两种受体。(摘要截断于250字)