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用于治疗兴奋剂滥用的药物:基于激动剂的策略及混合作用D2部分激动剂阿立哌唑(安律凡)的临床前评估

Medications for stimulant abuse: agonist-based strategies and preclinical evaluation of the mixed-action D-sub-2 partial agonist aripiprazole (Abilify).

作者信息

Bergman Jack

机构信息

Harvard Medical School-McLean Hospital, 115 Mill Street, Belmont, MA 02478-9106, USA.

出版信息

Exp Clin Psychopharmacol. 2008 Dec;16(6):475-83. doi: 10.1037/a0014398.

Abstract

The utility of full and partial agonists for the management of opioid addiction and smoking behavior has encouraged the development of dopamine partial agonist-based medications for treating monoaminergic stimulant abuse and addiction. Aripiprazole, a recently introduced atypical antipsychotic with D-sub-2 partial agonist actions, has been studied in mice, rats, and man, but its ability to attenuate abuse- and addiction-related effects of cocaine or methamphetamine remains controversial. The present studies in monkeys were conducted to further evaluate aripiprazole as a candidate medication. The effects of aripiprazole on overt behavior were first compared with those of other dopamine-related drugs. In contrast to D-sub-2 full agonists, aripiprazole did not induce self-scratching. Like D-sub-2 receptor blockers, however, aripiprazole occasioned dose-related increases in catalepsy-associated behavior that, at the highest doses, were characterized most prominently by periods of stillness and immobility. In methamphetamine-discrimination experiments, aripiprazole did not engender responding on the methamphetamine-associated lever; rather, aripiprazole antagonized the discriminative-stimulus effects of methamphetamine by shifting its dose-effect function rightward. In self-administration "choice" experiments, acute or chronic treatment with aripiprazole did not attenuate the reinforcing strength of intravenous cocaine relative to food delivery. However, like D-sub-2 full agonists, priming injections of aripiprazole prior to sessions of intravenous saline availability engendered comparable levels of responding on levers leading to food delivery and intravenous injections. The present findings indicate that agonist and antagonist effects of aripiprazole are evident under different experimental conditions and that, like D-sub-2 full agonists, aripiprazole may have limited value for treating monoaminergic stimulant abuse and addiction.

摘要

完全激动剂和部分激动剂在阿片类药物成瘾及吸烟行为管理中的效用,促使了基于多巴胺部分激动剂的药物研发,用于治疗单胺能兴奋剂滥用和成瘾。阿立哌唑是一种最近引入的具有D2部分激动剂作用的非典型抗精神病药物,已在小鼠、大鼠和人类身上进行了研究,但其减弱可卡因或甲基苯丙胺滥用及成瘾相关效应的能力仍存在争议。本研究在猴子身上进行,以进一步评估阿立哌唑作为候选药物的情况。首先将阿立哌唑对明显行为的影响与其他多巴胺相关药物的影响进行了比较。与D2完全激动剂不同,阿立哌唑不会诱发自我抓挠。然而,与D2受体阻滞剂一样,阿立哌唑会引起与僵住相关行为的剂量相关增加,在最高剂量时,其最显著的特征是静止不动期。在甲基苯丙胺辨别实验中,阿立哌唑不会在与甲基苯丙胺相关的杠杆上引发反应;相反,阿立哌唑通过将其剂量效应函数向右移动,拮抗了甲基苯丙胺的辨别刺激效应。在自我给药“选择”实验中,阿立哌唑的急性或慢性治疗并没有减弱静脉注射可卡因相对于食物递送的强化强度。然而,与D2完全激动剂一样,在静脉注射生理盐水可获得之前,注射阿立哌唑引发了在导致食物递送和静脉注射的杠杆上相当水平的反应。目前的研究结果表明,阿立哌唑的激动剂和拮抗剂作用在不同实验条件下是明显的,并且与D2完全激动剂一样,阿立哌唑在治疗单胺能兴奋剂滥用和成瘾方面可能价值有限。

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