Endocrine-2 Flashcards
no med chem of male reproductive
Naturally occurring estrogens
17β-estradiol > estrone > estriol
Estrogen is synthesized from what two things
androstenedione or testosterone
Anterior Pituitary Gonadotropins
- Luteinizing Hormone (LH)
- Follicle Stimulating Hormone (FSH)
Trophoblast gonadotrophin
Human chorionic gonadotropin (hCG)
Gonadotropin Receptors
FSHR: FSH
LHR: LH, hCG
Growth/maturation _________ follicle of ovary
Graafian
Corpus Luteum hormones
Progesterone, Estrogen
Endometrium:
endothelial lining, stroma
myometrium
smooth muscle
Perimetrium
outer serous coat
Follicular phase
estrogen builds endometrium
* Cell proliferation, increased thickness
* Induction of progesterone receptor
Luteal phase
progesterone prepares for implantation
* Ends estrogen effects on growth
* Stimulates endothelial secretions
* Blood vessel growth
Post-implantation
Stimulates LHR in corpus luteum to maintain
estrogen, progesterone synthesis
What does the ERalpha and ERbeta estrogen receptors do
ERα: female reproductive tract, mammillary gland, hypothalamus, endothelial cells, vascular smooth muscle
ERβ: Prostate, ovaries, lung, brain, bone, vasculature
Osteoblasts
↑ synthesis, type I collagen, osteocalcin, osteopontin
Estrogens plasma bound: _______________________ (SHBG) albumin
sex-hormone binging globulin
Single PR gene; two main isoforms: PR-A and PR-B which is inhibitory and which is excitatory
PR-A - inhibitory
PR-B - excitatory
Ligand-binding: dimerization, binding to what
progesterone response element (PRE)
What are Anti-progestins and Progestin Modulators used for
Early pregnancy termination
Ulipristal acetate (ELLA)
progesterone receptor modulator/partial PR agonist
inhibits ovulation
emergency contraception
Anti-Estrogens: “Pure” Estrogen Antagonists
Clomiphene and Fulvestrant
Estrogen Modulators/Anti-estrogens
Tamoxifen, Raloxifene, Clomiphene, Fluvestrant
Aromatase Inhibitors: steridal and non-steridal
Steroidal: formestane, exemestane (AROMASIN)
* irreversible
Non-steroidal: anastrozole (ARIMIDEX), letrozole (FEMERA), vorozole
* Reversible
Effects of estrogen
-Maturation of the female reproductive organs
-Maintains skin & blood vessels / & thickness of the vaginal lining
-↓ the resorption (breakdown) of the bone by osteoclasts
-↑ the coagulability of the blood
-Normal development of the endometrial (uterine) lining
-Can increase various hormone binding globulin