Baumann M H, Ayestas M A, Rothman R B
Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA.
J Neurosci. 1998 Nov 1;18(21):9069-77. doi: 10.1523/JNEUROSCI.18-21-09069.1998.
Repeated administration of D,L-fenfluramine (FEN) is known to cause prolonged depletion of forebrain serotonin (5-HT) in animals. Ironically, few studies have evaluated functional consequences of such FEN-induced 5-HT loss. In the present work, we examined neuroendocrine and behavioral responses evoked by acute FEN injection in rats that had previously received a 4 d FEN-dosing regimen known to deplete forebrain 5-HT (D,L-FEN, 20 mg/kg, s.c., b. i.d.). Rats were fitted with indwelling jugular catheters before the study to allow for repeated intravenous challenge injections and stress-free blood sampling. At 1 and 2 weeks after the 4 d dosing regimen, acute FEN (1.5 or 3.0 mg/kg, i.v.) produced dose-related elevations in plasma corticosterone and prolactin; these hormonal responses were markedly attenuated in FEN-pretreated rats. Behavioral effects of acute FEN, namely flat body posture and forepaw treading, were also blunted in FEN-pretreated rats. Interestingly, rats exposed to repeated FEN did not display overt abnormalities in hormonal or behavioral parameters under basal (i.e., unprovoked) conditions, despite dramatic decreases in postmortem tissue levels of 5-HT in numerous brain areas. Our results suggest that FEN-induced 5-HT depletion is accompanied by multiple impairments in 5-HT function. Although the clinical relevance of our data are debatable, the findings clearly show the utility of the FEN challenge test for uncovering in vivo functional deficits that might otherwise go undetected. FEN should remain an important pharmacological tool for determining the role of 5-HT neurons in mediating diverse physiological and behavioral processes.
已知重复给予D,L-芬氟拉明(FEN)会导致动物前脑血清素(5-HT)长期耗竭。具有讽刺意味的是,很少有研究评估这种FEN诱导的5-HT缺失的功能后果。在本研究中,我们检测了急性注射FEN在先前接受了已知会耗尽前脑5-HT的4天FEN给药方案(D,L-FEN,20mg/kg,皮下注射,每日两次)的大鼠中引发的神经内分泌和行为反应。在研究前给大鼠植入颈静脉导管,以便进行重复静脉内激发注射和无应激采血。在4天给药方案后的1周和2周,急性注射FEN(1.5或3.0mg/kg,静脉注射)使血浆皮质酮和催乳素呈剂量相关升高;这些激素反应在FEN预处理的大鼠中明显减弱。急性FEN的行为效应,即扁平体位和前爪踩踏,在FEN预处理的大鼠中也减弱。有趣的是,尽管在多个脑区中5-HT的死后组织水平显著降低,但暴露于重复FEN的大鼠在基础(即未激发)条件下的激素或行为参数未显示明显异常。我们的结果表明,FEN诱导的5-HT耗竭伴随着5-HT功能的多种损害。尽管我们数据的临床相关性存在争议,但这些发现清楚地表明了FEN激发试验在揭示体内可能未被发现的功能缺陷方面的效用。FEN应仍然是确定5-HT神经元在介导各种生理和行为过程中的作用的重要药理学工具。