Nestoron

Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor. IC50 value:Tareget: progesterone receptorNestorone acts primarily as a high-affinity agonist of the progesterone receptor. It lacks significant affinity for the androgen receptor, and accordingly, does not produce any androgenic or anabolic effects. It does not bind to the estrogen receptor either. Nestorone does however have some affinity for the glucocorticoid receptor, where it appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. Nestorone does not bind to sex hormone-binding globulin, and is instead bound to serum albumin.

Signaling Pathways >> Others >> Progesterone Receptor

Research Areas >> Endocrinology

Natural Products >> Steroids

[1]. Ilani N, et al. A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception.J Clin Endocrinol Metab. 2012 Jul 12.

[2]. Rad M, et al. Discriminant analysis of the metabolic effects of a new combined contraceptive vaginal ring containing Nestorone/EE vs. a second-generation oral contraceptive containing levonorgestrel/EE.Contraception. 2012 Sep;86(3):231-7. Epub 2012 Mar 23

[3]. Hussain R, et al. Progesterone and Nestorone facilitate axon remyelination: a role for progesterone receptors.Endocrinology. 2011 Oct;152(10):3820-31. Epub 2011 Aug 9.

[4]. Prasad PV, et al. Single-dose pharmacokinetics of Nestorone, a potential female-contraceptive.Steroids. 2010 Mar;75(3):252-64. Epub 2010 Jan 11.

[5]. Elsimar M Coutinho et al. Use of a single implant of elcometrine (ST-1435), a nonorally active progestin, as a long acting contraceptive for postpartum nursing women Contraception Volume 59, Issue 2, February 1999, Pages 115-122

Mifepristone | Progesterone | Tanaproget | Megestrol acetate | Dydrogesterone | Drospirenone | Dienogest | Ethynodiol diacetate | 19-Norethindrone acetate | Altrenogest | Chlormadinone Acetate | Gestodene | Gestonorone Capronate

MOLECULAR FORMULA :

C23-H30-O4

MOLECULAR WEIGHT :

370.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Administration onto the skin

DOSE :

240 ug/kg

SEX/DURATION :

female 24 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :

FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 58,680,1992

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Implant

DOSE :

800 ug/kg

SEX/DURATION :

female 56 week(s) pre-mating

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

REFERENCE :

CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 25,299,1982

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Implant

DOSE :

2200 ug/kg

SEX/DURATION :

female 43 week(s) pre-mating

TOXIC EFFECTS :

Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :

CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 18,411,1978

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Implant

DOSE :

700 ug/kg

SEX/DURATION :

female 26 week(s) pre-mating

TOXIC EFFECTS :

Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :

FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 36,737,1981