Pharmacological evaluation of new constituents of "Spice": synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds.

ABSTRACT:

Purpose

In the present study we characterized a series of synthetic cannabinoids containing various heterocyclic scaffolds that had been identified as constituents of "Spice", a preparation sold on the illicit drug market. All compounds were further investigated as potential ligands of the orphan receptors GPR18 and GPR55 that interact with some cannabinoids.

Methods

The compounds were studied in radioligand binding assays to determine their affinity for human cannabinoid CB₁ and CB₂ receptors expressed in CHO cells, and in cAMP accumulation assays to study their functionality.

Results

Structure-activity relationships were analyzed. The most potent CB₁ receptor agonist of the present series MDMB-FUBINACA (12) (K_i

SUBMITTER: Schoeder CT 

PROVIDER: S-EPMC6002460 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature