Structure-activity relationships of valine, tert-leucine, and phenylalanine amino acid-derived synthetic cannabinoid receptor agonists related to ADB-BUTINACA, APP-BUTINACA, and ADB-P7AICA.

ABSTRACT: Synthetic cannabinoid receptor agonists (SCRAs) remain one the most prevalent classes of new psychoactive substances (NPS) worldwide, and examples are generally poorly characterised at the time of first detection. We have synthesised a systematic library of amino acid-derived indole-, indazole-, and 7-azaindole-3-carboxamides related to recently detected drugs ADB-BUTINACA, APP-BUTINACA and ADB-P7AICA, and characterised these ligands for in vitro binding and agonist activity at cannabinoid receptor subtypes 1 and 2 (CB₁ and CB₂), and in vivo cannabimimetic activity. All compounds showed high affinity for CB₁ (K _i 0.299-538 nM) and most at CB₂ (K _i = 0.912-2190 nM), and most functioned as high effi

SUBMITTER: Sparkes E 

PROVIDER: S-EPMC8864554 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature