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  selective estrogen receptor modulators

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Author Topic:   selective estrogen receptor modulators
Pharm Animal

Elite Bodybuilder

Posts: 899
From:Honolulu, HI
Registered: Aug 2000

posted March 04, 2001 03:09 PM

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taken from another board....from my experiences, this sounds like useful info

vets, please make sure that this info is correct, as i try my best to provide correct information

thanks,
PA
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What is a SERM?

SERM stands for selective estrogen receptor modulator

A SERM is a molecule that binds with high affinity to the estrogen receptor
(ER) but has tissue-specific effects distinct from estradiol . (4,13)

There are a large number of compounds that display mixed agonist/antagonist
effects on the ER, including:

Benzothiophenes
raloxifene (Evista): prevent postmenopausal osteoporosis

Triphenylethylenes
clomiphene (Serophene)(Clomid): fertility drug
tamoxifen (Nolvadex): treat ER-positive breast CA

<<Sadly, neither clomid nor nolvadex will inhibit the production of estrogen.
If the doc measured your intra-cycle estrogen levels, they would be off the
scale - Thus warranting the usage of arimidex at 1mg a day. [Many bodybuilders
have reported significant anti-estrogen forming effects at doses as little as
1/6th of that daily dose..]>>

I agree that Clomid will not inhibit the production of estrogen; however,
Nolvadex, Proviron, and Arimidex will. Just for the record, Progesterone is an
estrogen-based hormone, it is also considered to be a steroid hormone. In some
cases Progesterone suppresses aromatase induction, in the following,
fibroblasts (anemia), (pre-menopause and menopause), some types of (breast
cancer, which is what we're talking about), (pregnancy and as a contraceptive
for birth control).

Progesterone acts as a weak anti-estrogen, reducing the mRNA synthesis.
(Protein Synthesis Process whereby DNA encodes for the production of amino
acids and proteins).

One last thing:

Androcur (Which is a steroid also), Arimidex, Nolvadex, and Proviron
demonstrates 2 distinct properties:

Antiandrogenic:

They block the binding of dihydrotestosterone - the active metabolite of
testosterone - to the specific receptors in the prostatic carcinoma cell.

Progestogenic/antigonadotrophic:

They exert a negative feedback on the hypothalamo-pituitary axis, by
inhibiting the secretion of LH leading to diminished production of testicular
testosterone. The absorption of these drugs, following oral administration is
complete. Peak plasma levels are reached 3 to 4 hours after administration.
These drugs are eliminated in the urine mainly in the form of unconjugated
metabolites and in the bile via feces in the form of glucuronidized
metabolites.


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Big Johnson

Pro Bodybuilder

Posts: 316
From:CALIFORNIA
Registered: Feb 2001

posted March 05, 2001 12:03 AM

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THIS SUCKS

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