Commercially available analogues of GnRH and LH secretion.
Six agonistic derivatives of GnRH, four of which have already been evaluated in clinical trials, were compared with GnRH itself in an in vitro test system (incubation of rat pituitary glands). It was investigated 1) how the release of LH was affected when the pituitary glands were incubated in the presence of these analogues or GnRH, and 2) how the release of LH continued after removal of the analogues or GnRH from the medium. It was also investigated how an in vivo pretreatment for 6 days with several doses of 5 of these analogues or GnRH affects 3) the plasma concentration of LH, 4) the pituitary content of LH, and, in vitro, 5) the autonomous and 6) agonist-stimulated secretion of LH. Each of the analogues showed for each of the six investigated parameters a 10- to 100-fold higher potency than GnRH itself. Between the six analogues there were only minor differences. It is discussed how the six investigated parameters may be the expression of one single property of all these analogues, namely a long retention in the pituitary gland with a strong binding to the GnRH receptor.
Koiter
T R
TR
Department of Obstetrics and Gynecology, Groningen University Hospital, The Netherlands.
Moes
H
H
Schuiling
G A
GA
D000818:Animals; D002064:Buserelin / Q000031:analogs & derivatives / Q000494:pharmacology; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives* / Q000494:pharmacology; D017273:Goserelin; D016729:Leuprolide; D007986:Luteinizing Hormone / Q000378:metabolism*; D010052:Ovariectomy; D010902:Pituitary Gland / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D017273:Goserelin; D007987:Gonadotropin-Releasing Hormone; C026031:LHRH, N-Et-AlaNH2(6)-; D007986:Luteinizing Hormone; D016729:Leuprolide; C030741:lutrelin acetate; D002064:Buserelin