. Author manuscript; available in PMC: 2014 Dec 15.

Published in final edited form as: Biochem Pharmacol. 2013 Oct 4;86(12):10.1016/j.bcp.2013.09.024. doi: 10.1016/j.bcp.2013.09.024

Table 2.

Vascular estrogen receptor distribution, function, signaling, agonists and antagonists

	ERα	ERβ	GPR30

Molecular Weight	66–70 kDa	53–59 kDa	38 kDa

Vascularz Distribution
Endothelium	++	++	+
VSM	++	++	+

Cellular Distribution
Plasma Membrane	++	++	++
Nucleus	++	++	+ (Envelope)
Cytosol	++	++	+
Endop Reticulum	+	+	++
Golgi	+	+
Mitochondria	+	+

Function	Transcription regulation, vascular relaxation, inhibition of VSM contraction, growth & proliferation	Transcription regulation, vascular relaxation, inhibition of VSM contraction, growth & proliferation	Vascular relaxation
Signaling Pathway Activate	cSrc/PI₃K/Akt, Src/MAPK, NO-cGMP, PGI₂-cAMP	cSrc/PI₃K/Akt, Src/MAPK, NO-cGMP, PGI₂-cAMP	AC-cAMP, PI3K EGFR/Erk1/2

Inhibit	Ca²⁺ influx, MLC kinase, PKC Rho-kinase, MAPK	Ca²⁺ influx, MLC kinase, PKC Rho-kinase, MAPK

Agonists Natural	Estradiol, Estrone, Estriol Conjugated equine estrogen	Estradiol, Estrone, Estriol Conjugated equine estrogen	Estradiol

Synthetic	Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate, S-S tetrahydrochrysene Estradiol cypionate, valerate	Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate, S-S tetrahydrochrysene Estradiol cypionate, valerate	-Kepone, ICI 182,780 Bisphenol A, Nonylphenol

Phytoestrogens Isoflavones	Daidzein	Genistein, Daidzein, Biochanin A	Genistein

Flavonols			Quercetin

Flavanones	Naringenin, Taxifolin	Naringenin, Taxifolin

Coumestans	Coumestrol, 4′ methoxycoumestrol	Coumestrol, 4′ methoxycoumestrol

Lignans	Enterodiol, Enterolactone, Secoisolariciresinol, Matairesinol	Enterodiol, Enterolactone, Secoisolariciresinol, Matairesinol

Stilbenes	Resveratrol	Resveratrol
SERMS (partial agonists)	Raloxifene,Tamoxifen, Idoxifene, Toremifene, Bazedoxifene	Raloxifene,Tamoxifen, Idoxifene, Toremifene, Bazedoxifene	Raloxifene, Tamoxifen

Specific Agonists	PPT, 16 α-LE2, ERA-45	DPN, 8β-VE2, Androstene 3,5 diene, DCW234, ERB-041, Monoaryl-Substituted Salicylaldoximes, WAY-202196, WAY-214156	G1

Antagonists	ICI 182,780, Clomifene, Glyceollin	ICI 182,780, Clomifene	Pertussis Toxin

Specific Antagonists	MPP	RR-tetrahydrochrysene	G15