Adiol-G (3a-androstanediol, metabolite of DHT) as neurosteroid in the brain - anticonvulsant

Interesting in that elevated estradiol is implicated in seizure susceptibility in men, whereas DHT (and Adiol-G) exert powerful anticonvulsant activity.

For those experiencing muscle twitches/fasciculations while on/after Fin, perhaps this is part of an explanation for why.


Mass spectrometric assay and physiological–pharmacological activity of androgenic neurosteroids

sciencedirect.com/science?_o … 08093295ba


Steroid hormones play a key role in the pathophysiology of several brain disorders. Testosterone modulates neuronal excitability, but the underlying mechanisms are obscure.

There is emerging evidence that testosterone-derived “androgenic neurosteroids”, 3α-androstanediol and 17β-estradiol, mediate the testosterone effects on neural excitability and seizure susceptibility.

Testosterone undergoes metabolism to neurosteroids via two distinct pathways. Aromatization of the A-ring converts testosterone into 17β-estradiol. Reduction of testosterone by 5α-reductase generates 5α-dihydrotestosterone, which is then converted to 3α-androstanediol, a powerful GABAA receptor-modulating neurosteroid with anticonvulsant properties.

Although the 3α-androstanediol is an emerging neurosteroid in the brain, there is no specific and sensitive assay for determination of 3α-androstanediol in biological samples.

This article describes the development and validation of mass spectrometric assay of 3α-androstanediol, and the molecular mechanisms underlying the testosterone modulation of seizure susceptibility. A liquid chromatography–tandem mass spectrometry assay to measure 3α-androstanediol is validated with excellent linearity, specificity, sensitivity, and reproducibility.

Testosterone modulation of seizure susceptibility is demonstrated to occur through its conversion to neurosteroids with “anticonvulsant” and “proconvulsant” actions and hence the net effect of testosterone on neural excitability and seizure activity depends on the levels of distinct testosterone metabolites.

The proconvulsant effect of testosterone is associated with increases in plasma 17β-estradiol concentrations. The 5α-reduced metabolites of testosterone, 5α-dihydrotestosterone and 3α-androstanediol, had powerful anticonvulsant activity.

Overall, the testosterone-derived neurosteroids 3α-androstanediol and 17β-estradiol could contribute to the net cellular actions of testosterone in the brain.

Because 3α-androstanediol is a potent positive allosteric modulator of GABAA receptors, it could serve as an endogenous neuromodulator of neuronal excitability in men.

The 3α-androstanediol assay is an important tool in this area because of the growing interest in the potential to use adjuvant aromatase inhibitor therapy to improve treatment of epilepsy.

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Furthermore…

Testosterone modulation of seizure susceptibility is mediated by neurosteroids 3α-androstanediol and 17β-estradiol

sciencedirect.com/science?_o … 61650468c3


Testosterone modulates seizure susceptibility in animals and humans, but the underlying mechanisms are obscure.

Here, testosterone modulation of seizure susceptibility is hypothesized to occur through its conversion to neurosteroids with “anticonvulsant” and “proconvulsant” actions, and hence the net effect of testosterone on neural excitability and seizure activity depends on the levels of distinct testosterone metabolites.

Testosterone undergoes metabolism to neurosteroids via two distinct pathways. Aromatization of the A-ring converts testosterone into 17β-estradiol. Reduction of testosterone by 5α-reductase generates 5α-dihydrotestosterone (DHT), which is then converted to 3α-androstanediol (3α-Diol), a powerful GABAA receptor-modulating neurosteroid with anticonvulsant properties.

Systemic doses of testosterone decreased seizure threshold in rats and increased the incidence and severity of pentylenetetrazol (PTZ)-induced seizures in mice. These proconvulsant effects of testosterone were associated with increases in plasma 17β-estradiol and 3α-Diol concentrations.

Pretreatment with letrozole, an aromatase inhibitor that blocks the conversion of testosterone to 17β-estradiol, significantly inhibited testosterone-induced exacerbation of seizures.

The 5α-reductase inhibitor finasteride significantly reduced 3α-Diol levels and also blocked letrozole’s ability to inhibit the proconvulsant effects of testosterone.

The 5α-reduced metabolites of testosterone, DHT and 3α-Diol, had powerful anticonvulsant activity in the PTZ test.

Letrozole or finasteride had no effect on seizure protection by DHT and 3α-Diol, but indomethacin partially reversed DHT actions. 3α-Diol but not 3β-androstanediol, a GABAA receptor-inactive stereoisomer, suppressed 4-aminopyridine-induced spontaneous epileptiform bursting in rat hippocampal slices.

Thus, testosterone-derived neurosteroids 3α-Diol and 17β-estradiol could contribute to the net cellular actions of testosterone on neural excitability and seizure susceptibility.

Very good study for anyone who hasn’t read it. It gives us some perspective regarding the effects of elevated estradiol and lowered DHT in the CFS; as the Italian study suggests is the case.

Here’s a study that mentions how estradiol may act on the nervous system:

Ongoing studies from this laboratory have demonstrated marked potentiating actions of the sex steroid 17β-estradiol (E2) on glutamate-induced excitation.

sciencedirect.com/science/ar … 9389916910

And a book:

Estrogen reduces the effectiveness of GABA-mediated neuronal inhibition by reducing chloride conductance through the GABA-a receptor complex. Excitatory neuro-transmission is modulated by estrogen through agonist binding sites on the NMDA receptor complex in the CA-1 region of the hippocampus (26).

books.google.ca/books?id=HAOY0q … ry&f=false

According to the above link, estrogen reduces chloride influx caused by GABA-a, activates the NMDA receptor, decreases GABA concentration, and reduces GABA-a receptor number.

Good finds. And are there any ways to overcome this issue? Like feeding the brain with those neurosteroids or increasing them, I don’t know, anything. Those muscle twitches are pissing me of man

JQD claims that his protocol gets rid of muscle twitches. These studies could explain why. It would involve increasing DHT and decreasing estrogen.

As for the other neurosteroids (allopregnanolone, THDOC), if they are indeed deficient, then we need to find out why. That would point toward 5ar to me.

By increasing DHT, you would probably also increase 3-adiol, which has similar effects as allopregnanolone and THDOC. But all of these neurosteroids might have paracrine and autocrine functions in neurons, which is the biggest problem with supplementing.

Does allo come back online after cessation? And other neurosteroids? Are there any papers, finds about this?

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