Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.

ABSTRACT: Pharmacological targeting of the dopamine D₄ receptor (D₄R)─expressed in brain regions that control cognition, attention, and decision-making─could be useful for several neuropsychiatric disorders including substance use disorders (SUDs). This study focused on the synthesis and evaluation of a novel series of benzothiazole analogues designed to target D₄R. We identified several compounds with high D₄R binding affinity (K_i ≤ 6.9 nM) and >91-fold selectivity over other D₂-like receptors (D₂R, D₃R) with diverse partial agonist and antagonist profiles. Novel analogue 16f is a potent low-efficacy D₄R partial agonist, metabolically stable in rat and human liver microsomes, and has exc

SUBMITTER: Boateng CA 

PROVIDER: S-EPMC10510399 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature