10] We had previously reported that rats exposed to IH and cigarette smoke exhibited an increase of hepatic inflammatory cytokines, a reduction of CYPs, and a decrease of the nuclear receptors pregnane X receptor (PXR), constitutive androstane
receptor (CAR), and glucocorticoid receptor (GR).
And the nuclear receptor CAR (Constitutive Androstane
Receptor) is mainly expressed in liver, where it is activated by structurally diverse ligands and then regulates cytochrome P450 and other genes whose products are involved in DMEs and transporters (Tien and Negishi, 2006; Osabe et al.
Miller, "Constitutive androstane
receptor-mediated up-regulation of ATP-driven xenobiotic efflux transporters at the blood-brain barrier," Molecular Pharmacology, vol.
The patents' claims cover transgenic mice having reduced constitutive androstane
receptor (CAR) activity, including CAR knockout mice, as well as "humanized" mice expressing a human CAR receptor.
There are two groups of families of neurosteroids: the inhibitory neurotransmitter receptor families of pregnane neurosteroids that include allopregnanolone and aIlotetrahydrodeoxycorticosterone, and the excitatory neurotransmitter receptor families of androstane
neurosteroids, such as androstanediol and etiocholanone.
Based on the accumulated evidence from data reported in the literature over the last 40 years, NGTxC may trigger hepatocarcinogenesis through different mechanisms, including the activation of Phase-1 enzymes via binding the Constitutive Androstane
Receptor (CAR) (e.
The Nrf2 activator oltipraz also activates the constitutive androstane
receptor," Drug Metabolism and Disposition, vol.
Silva is currently on a temporary suspension from the NSAC after testing positive for the steroids Drostanolone and Androstane
on January 9, and Drostanolone on January 31 following his UFC 183 bout against Diaz.
Klaassen, "Organ distribution of multidrug resistance proteins 1, 2, and 3 (Mrp1, 2, and 3) mRNA and hepatic induction of Mrp3 by constitutive androstane
receptor activators in rats," Journal of Pharmacology and Experimental Therapeutics, vol.
Induction of CYP3A4, CYP2C19, and CYP2C9 by the prenyloxycinnamic acids is most likely mediated via the pregnane x receptor (PXR), which regulates the expression of many CYPs and which is the major nuclear receptor in LS180 cells lacking the constitutive androstane
receptor (CAR) (Gupta et al.
A role for the androgen metabolite, 5alpha androstane
3beta, 17beta dlol (3[beta]-diol) in the regulation of the hypothalamo-pitultary-adrenal axis.
CYP1A1, CYP19A1, CYP3A4, and COMT are involved in the synthetic pathway of estrogen and testosterone; NR1I2 (PXR, pregnane X receptor) and NR1I3 (CAR, constitutive androstane
receptor) regulate the transcription of cytochrome P450s, such as CYP3A4, CYP2Cs, and CYP2B6 (Wang and LeCluyse 2003; Willson and Kliewer 2002).
Induction of drug-metabolizing enzymes by garlic and allyl sulfide compounds via activation of constitutive androstane
receptor and nuclear factor E2-related factor 2," Drug Metabolism and Disposition, vol.
NSAC Chairman Francisco Aguilar said in the ESPN report that Silva also tested for another kind of steroid called androstane
These androstene and androstane
hormones, designed to restore the biological activity of cellular signaling pathways disrupted by disease and aging, have been demonstrated in humans to possess several properties with potential therapeutic benefit -- they regulate innate and adaptive immunity, reduce nonproductive inflammation and stimulate cell proliferation.