Detail of "65807-02-5"

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Unresponsiveness of the reproductive organs of the male mouse to treatment with a potent luteinizing hormone-releasing hormone agonist (ICI-118,630)

Unresponsiveness of the reproductive organs of the male mouse to treatment with a potent luteinizing hormone-releasing hormone agonist (ICI-118,630). Van Steenbrugge, G. J.; Romijn, J. C.; De Jong, F. H.; Schroeder, F. H. (Dep. Urol., Erasmus Univ., Rotterdam, Neth.). Urol. Res., 12(3), 175-8 (English) 1984. CODEN: URLRA5. ISSN: 0300-5623. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The effects of administration of a LH-RH analog (ICI-118,630 [65807-02-5]) on plasma concns. of hormones and on wts. of reproductive organs were studied in male mice. A single injection of the analog (54 mg/kg) caused a transient elevation of the concn. of LH [9002-67-9] in the plasma, up to 7-fold the level in control mice at 2 h after injection. Daily administration of the analog for 3 wk caused only a small decrease in the wt. of the ventral prostate, and the wts. of the seminal vesicles did not differ from those in control animals. The concns. of testosterone [58-22-0] and LH in the plasma of these mice were not significantly different from those in control mice. Since the LH-RH analog has no castration-like effect on the accessory sex organs of the male mouse, this animal is not a suitable model for the study of such compds.

Potent agonist and antagonist analogs of luliberin containing an azaglycine residue in position 10

Potent agonist and antagonist analogs of luliberin containing an azaglycine residue in position 10. Dutta, A. S.; Furr, B. J. A.; Giles, M. B.; Valcaccia, B.; Walpole, A. L. (Pharm. Div., ICI Ltd., Macclesfield/Cheshire, Engl.). Biochem. Biophys. Res. Commun., 81(2), 382-90 (English) 1978. CODEN: BBRCA9. ISSN: 0006-291X. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Section cross-reference(s): 34 Potent agonist and antagonist analogs of luliberin [9034-40-6] contg. an azaglycine residue in position 10 were synthesized and tested for biol. activity in const. estrus rats. The agonist, [D-Ser(t-butyl)6,azaglycine10]-luliberin [65807-02-5], (6 ng/rat i. v.) or 10 mg/rat, orally) induced ovulation and was at least 5 times as potent as [D-Ser(t-butyl)6,des-Gly-NH210,Pro-ethylamide9]-luliberin [57982-77-1]. [D-Ser(t-butyl)6, azaglycine10]-luliberin (1 mg/rat) also prevented human chorionic gonadotropin [9002-61-3]-induced increases in ovarian and uterine wt. in immature rats and was a highly potent antitumor agent when given to rats bearing dimethylbenz[a]anthracene-induced mammary tumors. The antagonist, [D-Phe2,DPhe6,Azaglycine10]-luliberin [66612-00-8] (15 mg/rat) inhibited ovulation induced by luliberin (0.5 mg/rat), whereas [D-Phe2,D-Phe6]-luliberin [57292-41-8] had no activity at < 125 mg/rat.