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Abstract：
Lorcaserin is a modestly selective agonist for 2C serotonin receptors (5-HT2CR) approved for weight-loss therapy. This class can attenuate cue-induced responding and drug taking in preclinical studies, but effects in humans have not been reported.
We evaluated effects of single 10 mg doses of lorcaserin on the subjective and reinforcing effects of cocaine, using a randomized, double-blind, within-subject, cross-over design. Male, non-treatment-seeking, regular cocaine users received either single doses of oral placebo (n = 9) or lorcaserin (n = 9), followed by low- or high- doses of intravenous cocaine (0.23 or 0.46 mg/kg-injection). They were then allowed to self-administer the lower dose of cocaine.
Cocaine was well tolerated after lorcaserin pretreatment. Oral lorcaserin did not modify the number of cocaine injections self-administered. However, it prolonged the time over which participants made intravenous choices relative to the duration of monetary (cash) decisions. Lorcaserin increased ratings of \'high\' and \'stimulated\' after low-dose cocaine or vehicle, but decreased craving for cocaine after intravenous vehicle. It also caused small but significant increases in heart rate following noncontingent injections of intravenous placebo or cocaine. When active cocaine was self-administered, lorcaserin decreased heart rate after selection of a monetary choice, but increased it following an intravenous choice.
Combined treatment with cocaine and lorcaserin was safe in a limited number of subjects, but did not diminish cocaine-motivated behavior or drug-induced \'high\'. Some positive subjective effects of cocaine were enhanced by lorcaserin, and it delayed intravenous choices and decreased craving under some conditions. Effects on heart rate depended on the type of reinforcer being self-administered.
clinicaltrials.gov Identifier, NCT02680288.
We evaluated effects of single 10 mg doses of lorcaserin on the subjective and reinforcing effects of cocaine, using a randomized, double-blind, within-subject, cross-over design. Male, non-treatment-seeking, regular cocaine users received either single doses of oral placebo (n = 9) or lorcaserin (n = 9), followed by low- or high- doses of intravenous cocaine (0.23 or 0.46 mg/kg-injection). They were then allowed to self-administer the lower dose of cocaine.
Cocaine was well tolerated after lorcaserin pretreatment. Oral lorcaserin did not modify the number of cocaine injections self-administered. However, it prolonged the time over which participants made intravenous choices relative to the duration of monetary (cash) decisions. Lorcaserin increased ratings of \'high\' and \'stimulated\' after low-dose cocaine or vehicle, but decreased craving for cocaine after intravenous vehicle. It also caused small but significant increases in heart rate following noncontingent injections of intravenous placebo or cocaine. When active cocaine was self-administered, lorcaserin decreased heart rate after selection of a monetary choice, but increased it following an intravenous choice.
Combined treatment with cocaine and lorcaserin was safe in a limited number of subjects, but did not diminish cocaine-motivated behavior or drug-induced \'high\'. Some positive subjective effects of cocaine were enhanced by lorcaserin, and it delayed intravenous choices and decreased craving under some conditions. Effects on heart rate depended on the type of reinforcer being self-administered.
clinicaltrials.gov Identifier, NCT02680288.
摘要：
Lorcaserin是2C5-羟色胺受体（5-HT2CR）的适度选择性激动剂，已被批准用于减肥治疗。这类可以减弱临床前研究中提示诱导的反应和药物服用，但是对人类的影响还没有报道。
Weevaluedeffectsofsingle10mgdosesoflorcaserinonthesubjectiveandenhancingeffectsofcocaine,使用随机的，双盲,在主题内，交叉设计。男性,不寻求治疗，常规可卡因使用者接受单剂量口服安慰剂（n=9）或lorcaserin（n=9），其次是低或高剂量的静脉注射可卡因（0.23或0.46mg/kg注射）。然后允许他们自己服用较低剂量的可卡因。
氯卡色林预处理后，可卡因的耐受性良好。口服lorcaserin并没有改变自己服用的可卡因注射剂的数量。然而,相对于货币（现金）决定的持续时间，它延长了参与者进行静脉选择的时间。Lorcaserin在低剂量可卡因或车辆后增加了“高”和“刺激”的评级，但静脉注射后对可卡因的渴望减少了。在非偶然注射安慰剂或可卡因后，它还引起心率的小幅但显着增加。当活性可卡因自行服用时，lorcaserin在选择货币选择后降低了心率，但在静脉注射后增加了它。
在有限数量的受试者中，可卡因和氯卡色林的联合治疗是安全的，但并没有减少可卡因动机的行为或药物诱导的“高”。氯卡色林增强了可卡因的一些积极主观影响，在某些情况下，它延迟了静脉注射的选择并减少了渴望。对心率的影响取决于自我管理的增强剂的类型。
clinicaltrials.gov标识符，NCT02680288。
Weevaluedeffectsofsingle10mgdosesoflorcaserinonthesubjectiveandenhancingeffectsofcocaine,使用随机的，双盲,在主题内，交叉设计。男性,不寻求治疗，常规可卡因使用者接受单剂量口服安慰剂（n=9）或lorcaserin（n=9），其次是低或高剂量的静脉注射可卡因（0.23或0.46mg/kg注射）。然后允许他们自己服用较低剂量的可卡因。
氯卡色林预处理后，可卡因的耐受性良好。口服lorcaserin并没有改变自己服用的可卡因注射剂的数量。然而,相对于货币（现金）决定的持续时间，它延长了参与者进行静脉选择的时间。Lorcaserin在低剂量可卡因或车辆后增加了“高”和“刺激”的评级，但静脉注射后对可卡因的渴望减少了。在非偶然注射安慰剂或可卡因后，它还引起心率的小幅但显着增加。当活性可卡因自行服用时，lorcaserin在选择货币选择后降低了心率，但在静脉注射后增加了它。
在有限数量的受试者中，可卡因和氯卡色林的联合治疗是安全的，但并没有减少可卡因动机的行为或药物诱导的“高”。氯卡色林增强了可卡因的一些积极主观影响，在某些情况下，它延迟了静脉注射的选择并减少了渴望。对心率的影响取决于自我管理的增强剂的类型。
clinicaltrials.gov标识符，NCT02680288。
