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Investigation of the Role of Chirality in the Interaction with σ Receptors and Effect on Binge Eating Episode of a Potent σ1 Antagonist Analogue of Spipethiane.

Abstract：

:The enantiomers of the potent σ1 receptor antagonist (±)-1 were synthesized and evaluated for their affinity at σ1, σ2 receptors and dopamine transporter (DAT). Analogously to (±)-1, both of the enantiomers showed very high affinity for the σ1 receptor and unprecedented selectivity over both the σ2 receptor and DAT. The lack of enantioselectivity between (+)-1 and (-)-1 indicated that the center of chirality in the 2-position of the benzothiochromane nucleus does not play a crucial role in the interaction with any of the studied targets. Docking studies confirmed that the configuration of the enantiomers has only marginal effects on the molecular interactions with the σ1 receptor. In in vivo studies in a female rat model of binge eating, (±)-1 dose-dependently decreased the binge eating episode elicited by a history of intermittent food restriction and stress, confirming and strengthening the important role played by the σ1 receptor in bingeing-related eating disorders.

journal_name

ACS Chem Neurosci

journal_title

ACS chemical neuroscience

authors

Del Bello F,Micioni Di Bonaventura MV,Bonifazi A,Wünsch B,Schepmann D,Giancola JB,Micioni Di Bonaventura E,Vistoli G,Giorgioni G,Quaglia W,Piergentili A,Cifani C

doi

10.1021/acschemneuro.9b00261

subject

Has Abstract

pub_date

2019-08-21 00:00:00

pages

3391-3397

issue

8

issn

1948-7193

journal_volume

10

pub_type

杂志文章

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