a d lh-rh

[D-Phe2,D-Ala6]-LH-RH is a potent LH-RH antagonist. [D-Phe2,D-Ala6]-LH-RH shows anti-LH/FSH-RH and antiovulatory activities[1].

Research Areas >> Endocrinology

Signaling Pathways >> Others >> Others

[D-Phe2,D-Ala6]-LH-RH inhibits the LH and FSH release induced by LH-RH in immature male rats[1]. [D-Phe2,D-Ala6]-LH-RH (1 mg/rat, SC) shows marked antiovulatory and contraceptive activity[2].[D-Phe2,D-Ala6]-LH-RH (0.625, 1.25, 2.5 mg/kg; s.c.; single dose; sacrificed 30 minutes) results a dose-dependent increase in stalk-median eminence (SME)-LHRH activity and decreases plasma LHRH activity as well in rats with hypophysectomized (hypox) at 25 days old[3]. [D-Phe2,D-Ala6]-LH-RH (25 mg/kg; s.c.; single dsoe) is effective in blocking the ovulation normally induced by LRH alone[4]. Animal Model: Adult female Sprague-Dawley rats (200-250 g)[2] Dosage: 1 mg/rat Administration: SC injections, from 12:00 to 14:30 hr on the day of proestrus Result: Showed marked antiovulatory and contraceptive activity, with 96% inhibition of ovulation.

[1]. Vilchez-Martinez JA, et al. Comparison of the anti-LH/FSH-RH and anti-ovulatory activities of (D-Phe2, D-Leu6)-LH-RH and (D-Phe2, D-Ala6)-LH-RH. Endocr Res Commun. 1976;3(3-4):231-41.

[2]. Beattie CW, et al. Luteinizing hormone-releasing hormone. Antiovulatory activity of analogs substituted in positions 2 and 6. J Med Chem. 1975 Dec;18(12):1247-50.

[3]. Corbin A, et al. Effect of luteinizing hormone releasing hormone (LHRH) and an LHRH antagonist of hypothalamic and plasma LHRH of hypophysectomized rats. Endocrinology. 1976 Jan;98(1):247-50.

[4]. Corbin A, et al. Ihibition of the pre-ovulatory proestrous gonadotropin surge, ovulation and pregnancy with a peptide analogue of luteinizing hormone releasing hormone. Endocr Res Commun. 1975;2(1):1-23.

MOLECULAR FORMULA :

C59-H79-N15-O13

MOLECULAR WEIGHT :

1206.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

3750 ug/kg

SEX/DURATION :

female 1 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

REFERENCE :

JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 18,1247,1975

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

2500 ug/kg

SEX/DURATION :

female 1 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :

IJGOAL International Journal of Gynaecology & Obstetrics. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.7- 1969- Volume(issue)/page/year: 16,359,1979

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intramuscular

DOSE :

30 mg/kg

SEX/DURATION :

female 1 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

REFERENCE :

EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

12500 ug/kg

SEX/DURATION :

female 1 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

REFERENCE :

EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975