Gonadotropin inhibitor

Nafarelin aoetate Antiendometriotic agent gonadotropin inhibitor... 

Much further research in the area of gonadotropin inhibitors is obviously necessary. Such work must seek to establish whether such inhibitors occur naturally in human urine, whether they are also present in blood, and whether they subserve any physiological function in man and in other species. 

F9. Futterweit, W., Margoulis, S. A., Soffer, L. J., and Dorfman, R. I., Effect of urinary gonadotropin inhibitor on the mouse uterine response to various gonadotropins. Endocrinology 72, 903-907 (1963). 

Other new but conventional radioimmunoassays have involved oestra-l,3,5(10)-triene-3,15a,16a,17/S-tetrol ( oestetrol ), as its 6-(0-carboxy-methyloximino)-derivative, the 16-carboxymethyloximino-derivative of androst-5-ene-3/S,17 8-diol, the 15-hemisuccinate of 15a-hydroxy-testosterone, some oestriol monoglucoside derivatives, the 6-carboxy-methyloximino- and 3-hemisuccinate derivatives of the synthetic oestrogen 17a-ethynyloestradiol, the 3-carboxymethyloximes of the contraceptive steroids norethindrone and norgestrel , and the pituitary gonadotropin inhibitor, the isoxazole derivative Danazol (25), which was effectively bound by an antiserum for the corresponding 17-carboxymethyloxime (26)7°... 

In vivo studies proved the excellent performance of drug nanoparticles. For example, in humans the oral administration of the analgesic naproxene as drug nanoparticles led to an AUC (0-2 h) of 97.5 mg h 1 compared with just 44.7 mg h 1 for a commercial suspension and of 32.7 mg hP for the same drug as a tablet product. The corresponding tmax values were 1.96 h for the nanoparticles, 3.33 h and 3.20 h for the two commercial products. In a canine study, oral administration of the gonadotropin inhibitor danazol as a suspension of nanoparticles led to an absolute bioavailability of 82.3%, whereas with the conventional dispersion only 5.2% was achieved. 

Reichert, L. E., Jr., Gavin, J. R., Ill, and Neill, J. D., 1971, Studies on a neuraminidase containing gonadotropin inhibitor substance in bovine putuitary extracts. Endocrinology 88 1497-1502. 

Leucine residues 2, 5, 7, 12, 20, and 24 of the motif are invariant in both type A and type B repeats of the ribonuclease inhibitor. An examination of more than 500 tandem repeats from 68 different proteins has shown that residues 20 and 24 can be other hydrophobic residues, whereas the remaining four leucine residues are present in all repeats. On the basis of the crystal structure of the ribonuclease inhibitor and the important structural role of these leucine residues, it has been possible to construct plausible structural models of several other proteins with leucine-rich motifs, such as the extracellular domains of the thyrotropin and gonadotropin receptors. 

In premenopausal women the ovary is the richest source of aromatase and hence estrogen. Aromatase is confined to the granulosa cells and is produced under the influence of gonadotropins (FSH and LH). Despite being a rich source of aromatase, three separate studies have shown that aromatase inhibitors are unable to sufficiently suppress ovarian estrogen production to postmenopausal levels. One explanation for this phenomenon may be a compensatory rise in gonadotrophins which maintains adequate estrogen production, despite the presence of the inhibitor. As such aromatase inhibitors cannot be used in premenopausal breast cancer patients. After menopause, ovarian... 

Mechanism of Action A testosterone derivative that suppresses the pituitary-ovarian axis by inhibiting the output of pituitary gonadotropins. Causes atrophy of both normal and ectopic endometrial tissue in endometriosis. Follicle-stimulating hormone (FSH) and luteinizing hormone (LH) are depressed in fibrocystic breast disease. Inhibits steroid synthesis and binding of steroids to their receptors in breast tissues. Increases serum levels of esterase inhibitor. Therapeutic Effect Produces anovulation and amenorrhea, reduces the production of est rogen, corrects biochemical deficiency as seen in hereditary angioedema. 

Fruzzetti F, de Lorenzo D, Parrini D, Ricci C. Effects of finasteride, a 5 alpha-reductase inhibitor, on circulating androgens and gonadotropin secretion in hirsute women. J Clin Endocrinol Metab 1994 79(3) 831-5. 

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