Английская Википедия:3α-Androstanediol
3α-Androstanediol also known as 5α-androstane-3α,17β-diol and sometimes shortened in the literature to 3α-diol, is an endogenous steroid hormone and neurosteroid and a metabolite of androgens like dihydrotestosterone (DHT).[1][2][3]
Biological activity
3α-Androstanediol is an inhibitory androstane neurosteroid and weak androgen and estrogen.[1][2][3]
As a neurosteroid, it acts as a potent positive allosteric modulator of the GABAA receptor,[4] and has been found to have rewarding,[5][6] anxiolytic,[7] pro-sexual,[8] and anticonvulsant effects.[9][10] As androgens such as testosterone and DHT are known to have many of the same effects as 3α-diol and are converted into it in vivo, it is thought that this compound may in part be responsible for said effects.[5][6][7][10]
Relative to its isomer 3β-androstanediol, which is a potent estrogen, 3α-androstanediol has substantially lower, though still significant affinity for the estrogen receptors, with a several-fold preference for ERβ over ERα.[11][12] It has approximately 0.07% and 0.3% of the affinity of estradiol at the ERα and ERβ, respectively.[13]
Biochemistry
Шаблон:Testosterone metabolism mini
3α-Androstanediol shows high affinity for sex hormone-binding globulin (SHBG), similar to that of testosterone.[14]
Chemistry
3α-Androstanediol, also known as 5α-androstane-3α,17β-diol, is a naturally occurring androstane steroid and a structural analogue of DHT (5α-androstan-17β-ol-3-one). A notable positional isomer of 3α-androstanediol is 3β-androstanediol.
An orally active synthetic analogue of 3α-androstanediol, 17α-ethynyl-3α-androstanediol (HE-3235, Apoptone), was formerly under investigation for the treatment of prostate cancer and breast cancer.[15]
References
Шаблон:Endogenous steroids
Шаблон:Androgen receptor modulators
Шаблон:Estrogen receptor modulators
Шаблон:GABAA receptor positive modulators
- ↑ 1,0 1,1 Шаблон:Cite book
- ↑ 2,0 2,1 Шаблон:Cite journal
- ↑ 3,0 3,1 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 5,0 5,1 Шаблон:Cite journal
- ↑ 6,0 6,1 Шаблон:Cite journal
- ↑ 7,0 7,1 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 10,0 10,1 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- Английская Википедия
- 5α-Reduced steroid metabolites
- Anabolic–androgenic steroids
- Androstanes
- Estrogens
- Human metabolites
- Neurosteroids
- GABAA receptor positive allosteric modulators
- Selective ERβ agonists
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