cas 20592-20-5, 13,14-DIHYDRO PROSTAGLANDIN F1ALPHA

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Design and synthesis of 13,14-dihydro prostaglandin F(1α) analogues as potent and selective ligands for the human FP receptor
The in vitro evaluation of a new class of potential bone anabolic agents for the treatment of osteoporosis is described. These compounds are potent and selective ligands for the human prostaglandin F receptor (hFP receptor). The compounds lack the olefin unsaturation required for potency in the natural ligand PGF(2α) yet retain binding affinity for the hFP receptor in the nanomolar to micromolar range. Removal of the alkenes also results in a better selectivity ratio for the hFP receptor over the other prostaglandin receptors tested. A rationale for the selectivity differences of various analogues, based on ligand docking experiments to a putative hFP receptor model, is also described.
Wang, Yili,Wos, John A.,Dirr, Michelle J.,Soper, David L.,DeLong, Mitchell A.,Mieling, Glen E.,De, Biswanath,Amburgey, Jack S.,Suchanek, Eric G.,Taylor, Cynthia J.
p. 945 - 952
(2007/10/03)

Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues
The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chin aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF(2α). (C) 2000 Published by Elsevier Science Ltd.
DeLong, Mitchell A.,Amburgey, Jack,Taylor, Cynthia,Wos, John A.,Soper, David L.,Wang, Yili,Hicks, Renee
p. 1519 - 1522
(2007/10/03)