DPN increased GluR2 expression in the other lamina of the CA1.DPN acts as an agonist on both ER subtypes, but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha. DPN displayed subtype-selective agonism, being ca. 30-fold more potent through ERbeta.Both PPT and DPN can acutely relax isolated mesenteric arteries with the relative potency of PPT>17beta-oestrogen>DPN.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.
Waters EM, et al. Brain Res. 2009 Sep 22;1290:1-11. PMID: 19596275.
Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression.
Harrington WR, et al. Mol Cell Endocrinol. 2003 Aug 29;206(1-2):13-22. PMID: 12943986.
Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility.
Montgomery S, et al. Br J Pharmacol. 2003 Aug;139(7):1249-53. PMID: 12890703.
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Meyers MJ, et al. J Med Chem. 2001 Nov 22;44(24):4230-51. PMID: 11708925.
|Related Estrogen Receptor Products|
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ.
RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.
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