Luteolytic potency of 16-phenoxy-derivatives of prostaglandin F2 alpha.
The binding of 16-phenoxy derivatives of prostaglandin (PG) F2 alpha to rat luteal membranes, and also their abortifacient potency in pregnant rats, have been studied. Competitive binding studies with various PG-analogues were performed in ovaries of juvenile rats pretreated with PMSG and HCG, and in parallel studies the abortifacient potency of these substances was tested in pregnant rats. It was observed that this class of derivatives bound to the PGF2 alpha receptor as well as, or even better than the parent compound PGF2 alpha. Modifications in the carboxyl group at C-1 yielded derivatives with a higher affinity for the receptor, in decreasing order of effectiveness as follows: -COOR greater than COOH greater than OH. The data obtained from the binding studies also compared well with data on the abortifacient potency in pregnant rats. It is concluded that the addition of a phenoxy group to either the lower or upper side chain of PGF2 alpha may augment the binding to the receptor as well as the biological responses induced by the post receptor effect.
Brambaifa
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College of Health Sciences, Department of Pharmacology, University of Port Harcourt, Nigeria.
D000019:Abortifacient Agents; D000818:Animals; D001667:Binding, Competitive; D003338:Corpus Luteum / Q000378:metabolism*; D015237:Dinoprost; D005260:Female; D008186:Luteolytic Agents; D011247:Pregnancy; D011460:Prostaglandins F / Q000378:metabolism*; D011461:Prostaglandins F, Synthetic / Q000378:metabolism*; D051381:Rats; D011982:Receptors, Prostaglandin / Q000378:metabolism; D013329:Structure-Activity Relationship
D000019:Abortifacient Agents; D008186:Luteolytic Agents; D011460:Prostaglandins F; D011461:Prostaglandins F, Synthetic; D011982:Receptors, Prostaglandin; C034671:prostaglandin F2alpha receptor; D015237:Dinoprost