Effects of α-pyrrolidino-phenone cathinone stimulants on locomotor behavior in female rats.
Effects of α-pyrrolidino-phenone cathinone stimulants on locomotor behavior in female rats.
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DOI：
10.1016/j.drugalcdep.2021.108910
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发表时间：
2021-10-01
影响因子：
4.2
通讯作者：
Dickerson, Tobin J.
中科院分区：
文献类型：
--
作者：
Taffe, Michael A.;Nguyen, Jacques D.;Vandewater, Sophia A.;Grant, Yanabel;Dickerson, Tobin J.
α-吡咯烷基-苯乙酮类兴奋剂首次引起广泛关注，是因为大众媒体报道了α-吡咯烷基-戊二酮(α-PVP，“flakka”)的使用引起了奇怪的行为。与其他设计药物一样，卡西诺酮的多样化受到理想的主观效果的推动，但也受到试图保持对特定分子的法律控制的领先地位的推动。α-吡咯烷基己酮(α-php)和α-吡咯烷基丙酮(α-pPP)化合物相对于α-pvp的研究相对较少，这为研究结构-活性关系，即α碳链的延长如何影响效力或功效提供了一个关键机会。用雌性大鼠比较α-php和α-ppp与α-pvp对车轮活动的影响，以及对自发活动、体温和颅内自我刺激奖赏的影响。α-ppp、α-php和α-pvp化合物(5、10 mg/kg，i.p.)已抑制轮子活动。吸入α-php或α-pvp也抑制车轮活动，但与注射路线相比持续时间较短。所有三种化合物都以剂量依赖的方式增加了自发活动，降低了大脑奖励阈值；仅观察到体温略有下降。这些数据表明，这三个α-吡咯烷基-苯酮卡西酮类化合物在雌性大鼠体内都表现出明显的刺激性活性。差异很小，因此，所有三种α-吡咯烷基苯酚的滥用责任可能是相同的。
The α-pyrrolidino-phenone cathinone stimulants first came to widespread attention because of bizarre behavior consequent to the use of α-pyrrolidinopentiophenone (α-PVP, “flakka”) reported in popular press. As with other designer drugs, diversification of cathinones has been driven by desirable subjective effects, but also by attempts to stay ahead of legal controls of specific molecules. The α-pyrrolidinohexiophenone (α-PHP) and α-pyrrolidinopropiophenone (α-PPP) compounds have been relatively under-investigated relative to α-PVP and provide a key opportunity to also investigate structure-activity relationships, i.e., how the extension of the alpha carbon chain may affect potency or efficacy. Female rats were used to contrast the effects of α-PHP and α-PPP with those of α-PVP in altering wheel activity and effects on spontaneous locomotion, temperature and intracranial self-stimulation reward. The α-PPP, α-PHP and α-PVP compounds (5, 10 mg/kg, i.p.) suppressed wheel activity. Inhalation of α-PHP or α-PVP also suppressed wheel activity, but for an abbreviated duration compared with the injection route. Spontaneous activity was increased, and brain reward thresholds decreased, in a dose-dependent manner by all three compounds; only small decrements in body temperature were observed. These data show that all three of the α-pyrrolidino-phenone cathinones exhibit significant stimulant-like activity in female rats. Differences were minor and abuse liability is therefore likely to be equivalent for all three α-pyrrolidino-phenones.
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影响因子：
7.6
作者：
Gannon, Brenda M.;Baumann, Michael H.;Collins, Gregory T.
通讯作者：
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