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Pharmacological characterizationof synthetic cannabinoid MAM-2201：radioligand binding and abuse-related effects

中国药理学与毒理学杂志 2017年第10期31卷 1016-1017页

作者： William E FANTEGROSSI Aaron JANOWSKY Amy J ESHLEMAN Lauren N RUSSELL saki fukuda Jyoti GOGOI Cassandra PRIOLEAU Ambuja S BALE Srihari R TELLA Merle G PAULE Takato HIRANITA Department of Pharmacology and Toxicology College of Medicine University of Arkansas for Medical Sciences AR 72207 Division of Neurotoxicology National Center for Toxicological Research Food and Drug Administration AR 72079 Departments of Psychiatry and Behavioral Neuroscience Oregon Health & Science University Portland OR 97239-3098 VA Portland Health Care System Portland OR 97239 Drug and Chemical Evaluation Section Drug Enforcement Administration

OBJECTIVE Over 30% of all new psychoactive substances identified by the UN Office on Drugs and Crime in 2016 were synthetic *** recent emergence of MAM-2201 on the illicit market is troubling because this drug has no precedent in either the scientific or patent literature,and appears to be a novel compound developed specifically as a "graymarket" drug of abuse bystructurally combining the known synthetic cannabinoids JWH-122 and *** is currently no published information regarding the pharmacology of *** The present studies characterized cannabinoid-like effects of MAM-2201 in vitro(interactions with cannabinoid type 1 receptors[CB1 Rs]) and in vivo(in mice and rats).RESULTS In a radioligand binding assay using [3 H]CP55,940 in HEK cell membranes transfected with the CB1 R,MAM-2201(K i=5.4 nmol·L^(-1)),had higher binding affinity than WIN 55,212-2(K i=80 nmol·L^(-1)),and D9-THC(K i=8.3 nmol·L^(-1)).The E max values for MAM-2201 and WIN 55,212-2 in an assay of agonist inhibition of forskolin-stimulated c AMP were 85%(EC50=0.45 nmol·L^(-1)) and 95%,respectively,as compared with the D9-THC E max of 74%.In mice,MAM-2201(0.003-1.0 mg·kg^(-1),IP) produced dose-dependent cannabimimetic effects which were both more potent and more effective than those of ***-2201 and D9-THC dose-dependently produced hypothermia:ED50=0.287 and 25.4 mg·kg^(-1),analgesia:ED50=0.125 and 29.4 mg·kg^(-1),and catalepsy:ED50=0.301 and18.9 mg·kg^(-1) in adult male CD1 ***,MAM-2201 also elicited convulsant effects at a dose of 1.0 mg·kg^(-1) in 8/8 murine *** rats,MAM-2201 produced dose-dependent D9-THC-like interoceptive effects in subjects trained to discriminate 3.0 mg·kg^(-1)(IP) D9-THC from *** MAM-2201 binds CB1 Rs with high affinity and agonist efficacy,and functions as a potent cannabinoid agonist in vivo across several complementary measures of cannabinoid activity in two rodent species.

关键词： cannabinoid CB1 receptor behavior abuse liability

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