Preti A
Genneruxi Medical Center, via Costantinopoli 42, I-09129, Cagliari, Italy.
Curr Opin Investig Drugs. 2000 Sep;1(1):110-5.
BP-897 is a dopamine D3 receptor agonist which is under development by Bioprojet for the potential treatment of drug craving and vulnerability to relapse that are elicited by drug-associated environmental stimuli; it is undergoing phase I trials [318397,334036,340721]. Preclinical investigations were carried out by Cambridge University and INSERM [295680]. BP-897 functions as a partial agonist in vitro and as either an agonist or an antagonist in vivo. It inhibits cocaine-seeking behavior that depends upon the presentation of drug-associated cues, without having any intrinsic, primary rewarding effects [334036]. In preclinical studies, BP-897 administration before testing reduced cocaine-seeking behavior in rats in a dose-dependent manner [304557,307758,334036]. In D3 receptor knockout mice, BP-897 has no effect [345710]. It does not reduce self-administration of cocaine in monkeys [318397].
BP - 897是一种多巴胺D3受体激动剂，由Bioprojet公司研发，用于潜在治疗由药物相关环境刺激引发的药物渴望和复发易感性；它正在进行I期试验[318397,334036,340721]。临床前研究由剑桥大学和法国国家健康与医学研究院进行[295680]。BP - 897在体外起部分激动剂作用，在体内起激动剂或拮抗剂作用。它抑制依赖药物相关线索呈现的觅药行为，而没有任何内在的、主要的奖赏效应[334036]。在临床前研究中，测试前给予BP - 897以剂量依赖方式降低了大鼠的觅药行为[304557,307758,334036]。在D3受体基因敲除小鼠中，BP - 897没有效果[345710]。它不会减少猴子对可卡因的自我给药[318397]。
