Use of the cutaneous anaphylactoid test to detect differences in mast cell mediator-releasing activity among LHRH peptides.
The cutaneous anaphylactoid test was evaluated as a screen for assessing mast cell mediator-releasing (MCMR) activity of luteinizing hormone-releasing hormone (LHRH) peptides. As expected, LHRH and D-Trp6-LHRH, an agonist of LHRH, were nonreactive at concentrations of antagonist which induced pronounced skin lesions. Differences between LHRH and antagonists were obvious, but it was difficult to detect differences among antagonists using arithmetic means. However, when the geometric means of the highest positive dilution were calculated, the MCMR activities of the antagonists differed and these differences appeared to be related to the hydrophobicities of their N-termini. Thus, it appears that the cutaneous anaphylactoid test is an appropriate screen to assess the MCMR activity of LHRH peptides and should assist in the development of clinically useful inhibitory analogs of LHRH.
D000707:Anaphylaxis / Q000139:chemically induced; D000818:Animals; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D008407:Mast Cells / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D017329:Triptorelin Pamoate
D017329:Triptorelin Pamoate; D007987:Gonadotropin-Releasing Hormone