The D3R partial agonist, BP 897, attenuates the discriminative stimulus effects of cocaine and D-amphetamine and is not self-administered
The D3R partial agonist, BP 897, attenuates the discriminative stimulus effects of cocaine and D-amphetamine and is not self-administered
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DOI：
10.1097/00008877-200102000-00001
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发表时间：
2001-02-01
影响因子：
1.6
通讯作者：
Schwartz, JC
中科院分区：
文献类型：
--
作者：
Beardsley, PM;Sokoloff, P;Schwartz, JC
多巴胺D3受体（D3 R）在精神兴奋剂调节作用中的潜在参与已引起越来越多的关注。BP 897（N-[4-[4-（2-甲氧基苯基）-1-哌嗪基]丁基]-2-萘基甲酰胺;又名BP 4.897和DO 897）是迄今为止报道的D3 R受体最具选择性的部分激动剂之一。测试了BP 897在恒河猴中支持自我给药的能力（0.3-30 μ g/kg），以及在小鼠中产生可卡因和D-苯丙胺样辨别刺激效应的能力（0.01-17 mg/kg i. p.）。BP 897在测试的四只猴子中的任何一只中都没有超过溶剂和生理盐水水平的自我给药，并且从可卡因或D-安非他明刺激中产生的泛化率低于30%。当BP 897在可卡因或D-苯丙胺给药前给药时，药物杠杆选择百分比降低，这些结果表明BP 897具有适合考虑作为可卡因依赖性障碍的潜在治疗的活性特征。(C)2001年利平科特威廉姆斯&威尔金斯。
Growing attention has been directed towards the potential involvement of the dopamine D3 receptor (D3R) in modulating effects of psychomotor stimulants. BP 897 (N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-naphthylrarboxamide; aka BP 4.897 and DO897) is amongst the most selective partial agonists for the D3R receptor thus far reported. BP 897 was tested for its ability to support self-administration in rhesus monkeys (0.3-30 mug/kg) and for its ability to produce cocaine- and D-amphetamine-like discriminative stimulus effects in mice (0.01-17 mg/kg i.p.). BP 897 was not self-administered above vehicle and saline levels in any of the four monkeys tested, and produced less than 30% generalization from either the cocaine or D-amphetamine stimulus. When BP 897 was administered before administrations of cocaine or D-amphetamine, percent drug-lever selections were reduced, These results suggest that BP 897 has a profile of activity suitable for consideration as a potential treatment for cocaine dependency disorders. (C) 2001 Lippincott Williams & Wilkins.