The affinity, intrinsic activity and selectivity of a structurally novel EP₂ receptor agonist at human prostanoid receptors.

ABSTRACT:

Background and purpose

Prostanoid EP₂ receptor agonists exhibit several activities including ocular hypotension, tocolysis and anti-inflammatory activity. This report describes the affinity and selectivity of a structurally novel, non-prostanoid EP₂ receptor agonist, PGN-9856, and its therapeutic potential.

Experimental approach

The pharmacology of a series of non-prostanoid EP₂ receptor agonists was determined according to functional and radioligand binding studies, mostly using human recombinant prostanoid receptor transfectants. The selectivity of PGN-9856, as the preferred compound, was subsequently determined by using a diverse variety of non-prostanoid target proteins. The therapeutic potential of PGN-9856 was addressed by determining i

SUBMITTER: Coleman RA 

PROVIDER: S-EPMC6365485 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature