Molecular and Behavioral Pharmacological Characterization of Abused Synthetic Cannabinoids MMB- and MDMB-FUBINACA, MN-18, NNEI, CUMYL-PICA, and 5-Fluoro-CUMYL-PICA.

摘要: Synthetic cannabinoids are a class of novel psychoactive substances that exhibit high affinity at the cannabinoid type-1 (CB1) receptor and produce effects similar to those Δ-9-tetrahydrocannabinol (THC), primary constituent cannabis. Illicit drug manufacturers continually circumventing laws banning sale synthetic by synthesizing structures doing so with little regard for potential impact on pharmacological toxicological effects. wide range include cardiotoxicity, seizure activity, kidney damage, they can cause death. Six cannabinoids, recently detected in illicit preparations, MMB-FUBINACA, MDMB-FUBINACA, CUMYL-PICA, 5F-CUMYL-PICA, NNEI, MN-18 were assessed for: 1) binding human CB1 CB2 receptors, 2) function [35S]GTPγS cAMP signaling, 3) THC-like mouse discrimination assay. All six exhibited receptors type-2 produced greater maximal than THC signaling. Additionally, all substituted discrimination, suggesting probably possess subjective Notably, methylated analog had higher parent, showing minor structural modifications being introduced have large properties these drugs. This study demonstrates sold used illicitly as substitutes cannabis retaining receptor, exhibiting efficacy THC, producing models relevant humans.