Novel Highly Potent and Selective Sigma1 Receptor Antagonists Effectively Block the Binge Eating Episode in Female Rats.

ABSTRACT: In this paper, the benzo-cracking approach was applied to the potent sigma1 (σ₁) receptor antagonist 1 to afford the less conformationally constrained 1,3-dioxane derivatives 2 and 3. To evaluate the effect of the increase in the distance between the two hydrophobic structural elements that flank the basic function, the cis and trans diastereomers of 4 and 5 were also prepared and studied. Compounds 2 and 3 showed affinity values at the σ₁ receptor significantly higher than that of the lead compound 1. In particular, 3 displayed unprecedented selectivity over the σ₂ receptor, the phencyclidine site of the NMDA receptor, and opioid receptor subtypes, as well as over the dopamine tra

SUBMITTER: Cifani C 

PROVIDER: S-EPMC8011929 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature