Estrogen receptor beta: nootropics and compounds | sci-wiki

Ecdysterone

Ecdysterone, also known as 20-hydroxyecdysone, is a naturally occurring steroid of the ecdysteroid class that serves as a molting hormone in insects and is also produced by many plants. Sold as a dietary supplement to athletes, it has drawn attention as a possible non-conventional anabolic agent. A controlled human study reported gains in muscle mass and strength, prompting researchers to recommend its addition to sports doping-control lists.

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Nootropic

3α-Androstanediol

3α-Androstanediol (5α-androstane-3α,17β-diol) is an endogenous neurosteroid formed as the terminal 3α-reduced metabolite of dihydrotestosterone (DHT, the most potent natural androgen). Despite its androgenic origin it binds the androgen receptor only weakly; its defining pharmacology is potent positive allosteric modulation of the GABA-A receptor (the brain's principal inhibitory chloride ion channel), which produces anxiolytic (anxiety-reducing) and anticonvulsant (seizure-suppressing) effects in animal models. It is widely regarded as the androgenic counterpart of allopregnanolone (the analogous progesterone-derived neurosteroid), and is proposed to mediate much of the influence that testosterone exerts on seizure threshold, anxiety, and mood in males. It additionally acts as a ligand of estrogen receptor beta (ERβ), which may underlie some of its cognitive and neuroprotective actions.

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Neurosteroid

Androstenediol

Androstenediol (androst-5-ene-3β,17β-diol, commonly abbreviated 5-androstenediol or 5-AED) is an endogenous Δ5 androstane steroid formed as a direct metabolite of dehydroepiandrosterone (DHEA, the most abundant circulating adrenal steroid). It sits at a branch point in steroidogenesis, functioning both as a weak, ERβ-preferring estrogen (a steroid that activates the estrogen receptor) and as a prohormone that can be converted onward to testosterone. Its most distinctive documented activity is immunomodulatory and hematopoietic; under the development code Neumune it was investigated as a radiation countermeasure that accelerates recovery of white blood cells and platelets after whole-body irradiation. Its inclusion in the neurosteroid grouping is one of exhaustiveness, since unlike allopregnanolone it has only a marginal classic neurosteroid profile at the GABA-A and NMDA receptors, and its central effects are attributed mainly to estrogen receptor beta signaling.

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Estrogen

WAY-200070

WAY-200070 is a synthetic nonsteroidal agonist of estrogen receptor beta, made at Wyeth as one of a series designed to tell the two estrogen receptors apart [5]. It binds ERbeta in the low nanomolar range and ERalpha roughly two orders of magnitude more weakly, which is exactly what makes it useful: an effect that appears with WAY-200070 and vanishes in an ERbeta knockout mouse belongs to that receptor rather than to estrogen in general, and that control was actually run [6]. Its reputation in neuroscience comes from hippocampal work, where ERbeta activation raised synaptic proteins and improved memory in rodents [1]. Outside the brain the same compound has been used to study asthma, kidney fibrosis, insulin secretion and cancer cell growth. It is a laboratory probe throughout; there is no approved human use, no human trial, and no human safety data of any kind.

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