PHIL 2015 Chapter Notes - Chapter 9.6: Ethinyl Estradiol, Endometrial Hyperplasia, Conjugated Estrogen
23 May 2020
School
Department
Course
Professor
Receptor
Endogenous ligand
Homo or
heterodimer?
Physiologic pathway/function
Agonists
Antagonists
SEX STEROID RECEPTORS
Estrogen
receptor(ER)
2 isoforms: and
(different
genes)
17- estradiol
Homodimer
Maintenance of reproductive
(uterine and breast tissue),
cardiovascular, musculoskeletal
(bone density) systems
Ethinyl estradiol,
diethylstilbestrol,
conjugated estrogens,
mestranol
Tamoxifen,
clomiphene,
fulvestrant
Androgen
receptor (AR)
Dihydrotestosterone
(DHT) &
testosterone
Homodimer
Development and maintenance
of male reproductive tract
Protein anabolism in skeletal
muscle (“anabolic steroids”)
Methyltestosterone,
fluoxymesterone,
stanozolol
Cyptroterone
flutamide,
bicalutamide,
spironolactone
Progesterone
receptor (PR)
2 isoforms: A and
B (same gene,
different
promoter use)
Progesterone
Homodimer
PR-A: Uterine development and
reproductive function
(inhibition of endometrial cell
proliferation)
PR-B: mammary gland
development
Used mainly in hormonal
contraception and prevention
of endometrial hyperplasia in
HRT
Norethindrone,
levonorgestrel,
medroxyprogesterone
Mifepristone
(RU486)
STRESS STEROID RECEPTORS
