ChemSpider ID: 52084419
PubChem CID: 102107923
Molar mass: 245.366 g·mol−1
α-Pyrrolidinohexiophenone (APHP) is a synthetic stimulant drug of the cathinone class developed in the 1960s which has been reported as a novel designer drug.
α-Pyrrolidinopentiophenone (α-PVP, “flakka”) control led to use of analogs.
α-PPP and α-PHP are less well characterized in scientific literature.
Effects in rats confirm similar psychomotor stimulant effects of all three drugs.
In vitro pharmacology and structure-activity inferences fail to predict in vivo effects.
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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