Agonist (ovulation induction) and post-coital contraceptive properties of [D-Ala6] and [D-Trp6]-LHRH series.
Seven derivatives of LH-RH, representing the [D-Ala6] or [D-Trp6] series, with or without a Fujino modification, were evaluated for ovulation-inducing (agonist and post-coital contraceptive activity in rats. Six of these analogues had a high degree of agonist and pregnancy-terminating potency. In general, several modifications can result in a particular series of composite molecules that possess a biologic potency greater than each of its predecessors; this correlation of structure with activity was more consistent in the [D-Ala6]-series than in the [D-Trp6]-series. The relationship between structural modifications, resistance to enzyme degradation (based on literature reports) and increased biologic potency is discussed.
D000818:Animals; D003281:Contraceptives, Postcoital / Q000494:pharmacology*; D003282:Contraceptives, Postcoital, Hormonal / Q000494:pharmacology*; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D010062:Ovulation Induction; D011247:Pregnancy; D051381:Rats; D013329:Structure-Activity Relationship
D003281:Contraceptives, Postcoital; D003282:Contraceptives, Postcoital, Hormonal; D007987:Gonadotropin-Releasing Hormone