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Luteolytic potency of 16-phenoxy-derivatives of prostaglandin F2α

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Summary

The binding of 16-phenoxy derivatives of prostaglandin (PG) F2α 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 PGF2α receptor as well as, or even better than the parent compound PGF2α. 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>COOH>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 PGF2α may augment the binding to the receptor as well as the biological responses induced by the post receptor effect.

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Authors and Affiliations

  1. College of Health Sciences, Department of Pharmacology, University of Port Harcourt, P.M.B. 5323, Port Harcourt, Nigeria

    N. Brambaifa

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  1. N. Brambaifa
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Brambaifa, N. Luteolytic potency of 16-phenoxy-derivatives of prostaglandin F2α. Experientia 44, 45–47 (1988). https://doi.org/10.1007/BF01960240

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