Synthesis and Pharmacological Characterization of a Novel Cannabinoid Receptor 1 Antagonist.

ABSTRACT: The endocannabinoid (eCB) system regulates several brain functions and is implicated in numerous conditions affecting the brain. Thus, the pharmacological blockade of cannabinoid receptors has a therapeutic potential but produces severe psychiatric side effects. Hence, new cannabinoid compounds with different pharmacological profiles are needed to potentially minimize this toxicity. The objective of this study, featuring original chemical insights, pharmacological analysis, and robust computational methods, was to synthesize and characterize a series of novel antagonists/inverse agonists of cannabinoid receptors. To do so, we first synthesized and then screened 11 novel compounds for affinity for cannabinoid receptors. After that, we characterized in depth the pharmacological profile of th

SUBMITTER: Bengoetxea de Tena I 

PROVIDER: S-EPMC12163822 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature