Finding order in chemical chaos - Continuing characterization of synthetic cannabinoid receptor agonists

作者: Julie A. Marusich , Jenny L. Wiley , Timothy W. Lefever , Purvi R. Patel , Brian F. Thomas

DOI: 10.1016/J.NEUROPHARM.2017.10.041

关键词:

摘要: Diversion of synthetic cannabinoids from the lab to drugs abuse has become increasingly prevalent in recent years. Moreover, as earlier were banned, manufacturers introduced a new supply novel compounds serve replacements. Hence, chemical diversity cannabinoid analogs also rapidly increased. The present study examined 8 cannabinoids: AM-1220, AM-2232, AM-2233, AM-679, EAM-2201, JWH-210, JHW-251, and MAM-2201. Each compound was assessed for binding affinity functional activation CB1 CB2 receptors, pharmacological equivalence with Δ9-tetrahydrocannabinol (THC) THC drug discrimination. All bound activated although efficacy at receptor reduced compared that receptor. Similarly, all stimulated [35S]GTPγS through receptor, except AM-1220 AM-2233 Furthermore, these compounds, along CP55,940, substituted Rank order potency discrimination correlated affinity. Together, results suggest test share THC-like subjective effects marijuana. Interestingly, most potent have been found recently U.S., MAM-2201, AM-1220. These indicate evolution market may be focused toward increased potency. This article is part Special Issue entitled 'Designer Drugs Legal Highs.'

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