Enhanced Affinity for 3-Amino-Chromane-Derived σ1 Receptor Ligands.
ACS Omega
; 5(50): 32724-32737, 2020 Dec 22.
Article
in English
| MEDLINE | ID: covidwho-1120896
ABSTRACT
The σ1 receptor is implicated in regulating a diverse range of physiology and is a target for developing therapies for cancer, pain management, neural degradation, and COVID-19. This report describes 36 phenethylamine-containing 3-amino-chromane ligands, which bind to σ1 with low nM affinities. The family consists of 18 distinct compounds and each enantiomer was independently assayed. Three compounds with the greatest affinity bind in the 2 nM K i range (â¼8.7 pK i). Furthermore, ligands with the (3R,4R) absolute stereochemistry on the 3-amino-chromane core have a higher affinity and greater σ1 versus TMEM97 selectivity. The most promising ligands were assayed in 661W cells, which did not show significant protective effects.
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Collection:
International databases
Database:
MEDLINE
Language:
English
Journal:
ACS Omega
Year:
2020
Document Type:
Article
Affiliation country:
Acsomega.0c05117
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