Zuclomiphene-d5 citrate

Names

[ CAS No. ]:
1795132-80-7

[ Name ]:
Zuclomiphene-d5 citrate

Biological Activity

[Description]:

Zuclomiphene-d5 (citrate) is the deuterium labeled Zuclomiphene citrate[1]. Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[2][3][4][5].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  

[2]. Fontenot GK, et al. Differential effects of isomers of clomiphene citrate on reproductive tissues in male mice. BJU Int. 2016 Feb;117(2):344-50.  

[3]. Mikkelson TJ, et al. Single-dose pharmacokinetics of clomiphene citrate in normal volunteers. Fertil Steril. 1986 Sep;46(3):392-6.  

[4]. Sutherland RL. Estrogen antagonists in chick oviduct: antagonist activity of eight synthetic triphenylethylene derivatives and their interactions with cytoplasmic and nuclear estrogen receptors. Endocrinology. 1981 Dec;109(6):2061-8.  

[5]. Ramsey RB, et al. The biochemical and morphological response of hydrolytic enzymes in the developing brain to hypocholesterolemic agents. Acta Neuropathol. 1980;49(2):89-94.  

Chemical & Physical Properties

[ Molecular Formula ]:
C32H31D5ClNO8

[ Molecular Weight ]:
603.11

Related Compounds