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ATD~1,4,6 Androstatriene-dione

heavyiron

Chemistry Experiment
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1,4,6 Androstatriene-dione (ATD)

Characteristics

ATD is a steroidal aromatase inhibitor, known as a suicidal inhibitor because it permanently binds to the aromatase enzyme.

ATD is used for its aromatase inhibiting and testosterone boosting effect. Its effectiveness at lowering estrogen appears to be stronger than 6-oxo. It converts to 1,4,6-testosterone, which would also be expected to cause falsely high readings for a testosterone analysis.

The 1,4,6-testosterone metabolite of ATD can also bind to the androgen receptor (AR) and induce androgenic (or possibly anti-androgenic) effects similar to what is seen from 6-oxo. This would be expected since 1,4,6-testosterone has about one third the binding affinity for the AR, therefore it may interefere with the anabolic or androgenic action of hormones which bind the androgen receptor.

ATD would also be expected to interfere with production of natural testosterone by acting upon the hypothalamus pituitary testicular axis (HPTA), therefore this compound should not be used during post cycle therapy (PCT), however it could successfully be used during a cycle to help keep estrogen in control. Anecdotal reports and animal studies have also shown ATD inhibits libido and general sexual potency.

References

Effect of an inhibitor of aromatization, 1,4,6 androstatriene-3,17-dione (ATD) on LH release and steroid binding in hypothalamus of adult female rats.

Exp Brain Res. 1986;64(3):407-10.
Slama A, Gogan F, Sarrieau A, Vial M, Rostene W, Kordon C.

Effects of ATD on male sexual behavior and androgen receptor binding: a reexamination of the aromatization hypothesis.
ME Kaplan and MY McGinnis
Horm Behav, Mar 1989; 23(1): 10-26.

Anabolic Pharmacology
Seth Roberts (2009)

By Jason Rowland

1_4_6_androstatriene_dione.gif

Chemical Name(s):

Androsta-1,4,6-triene-3,17-dione
1,4,6-androstatriene-3,17-dione

Chemical Formula: C19H22O2
Molecular Weight: 282
CAS: NA
Q Qatio: NA
Anabolic #: NA
Androgenic #: NA
Oral Bioavailability: Estimated at 4%
AR Binding Affinity: NA
SHBG Binding Affinity: NA
Half Life: 2 days
Legal Status (US): Not listed as a controlled substance
Average Dose: 25-100mg/day
Average Cycle Length: 4-8 weeks

http://www.ironmaglabs.com/e-control-anti-estrogen.php
 
J Clin Endocrinol Metab. 1984 Dec;59(6):1088-96.

Inhibition of aromatization stimulates luteinizing hormone and testosterone secretion in adult male rhesus monkeys.

Ellinwood WE, Hess DL, Roselli CE, Spies HG, Resko JA.

Abstract

Experiments were conducted to examine the role of aromatization in the control of LH and testosterone secretion in adult male rhesus monkeys. Treatment of male monkeys (n = 7) with sc Silastic packets containing the aromatase inhibitor 1,4,6-androstatriene-3,17-dione (ATD) resulted in 1.5- to 3-fold elevations in serum LH and testosterone concentrations in six of seven animals. Concurrent treatment of ATD-treated monkeys with small quantities of estradiol-17 beta (n = 4) abolished the stimulatory effect of ATD. During ATD treatment, peripheral estradiol levels were reduced by 30% and hypothalamic aromatase activity, as determined in vitro, was reduced 80-90%. The lack of androgenic or antiandrogenic activity of ATD was demonstrated by its inactivity in either a mouse seminal vesicle bioassay or a highly sensitive penile spine bioassay. Furthermore, ATD did not react with rat prostatic or hypothalamic cytosol androgen receptors. 1,4,6-Androstatriene-17-ol-3-one, a possible metabolite of ATD in vivo, did react with prostatic and hypothalamic androgen receptors, but possessed no antiandrogenic activity in either bioassay. Thus, treatment of adult males with an aromatase inhibitor that inhibits both peripheral and central aromatization, and which has no apparent antiandrogenic activity, results in stimulation of LH and testosterone secretion. These data demonstrate that aromatization of androgens to estrogens plays an important role in negative feedback regulation of LH secretion and maintenance of normal testosterone levels in adult male primates.


PMID: 6541658 [PubMed - indexed for MEDLINE]
 
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