New class of benzothiophene morpholine analogues with high selectivity and affinity were designed and evaluated for anti-drug addiction.

Abstract

To probe the mechanism of dopamine receptors in drug addiction and look for potential new methods for treating this disease, we have designed and synthesized benzothiophene morpholine analogues that were considered as dopamine D3 receptor-selective ligands. Radioligand binding assay was used to determine the binding affinity of target compounds. Members of this class have great selectivity and binding affinity in D3 receptor. In addition, the ability of these compounds to mitigate the symptoms of addiction from opioids was investigated in animal behavior patterns, and we have found that two compounds (18a and 18d) have good affinity in the D3R and exhibit the efficacy of anti-drug addiction in morphine-dependent mice induced by naloxone.

• Authors: Jin Cai, Yuhong Wang, Xixi Chen, Min Ji
• Journal: Chemical biology & drug design (Chem Biol Drug Des) Vol. 99 Issue 4 Pg. 634-649 (04 2022) ISSN: 1747-0285 [Electronic] England
• PMID: 35148466 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2022 John Wiley & Sons Ltd.

Chemical References

• Ligands
• Morpholines
• Receptors, Dopamine D3
• Thiophenes
• benzothiophene

Topics

• Animals
• Ligands
• Mice
• Morpholines (pharmacology)
• Radioligand Assay
• Receptors, Dopamine D3 (chemistry)
• Structure-Activity Relationship
• Substance-Related Disorders
• Thiophenes