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3α,21-Dihydroxy-5α-pregnan-20-one

Cat. No. M30302
3α,21-Dihydroxy-5α-pregnan-20-one Structure
Synonym:

THDOC

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Quality Control & Documentation
Biological Activity

3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

Chemical Information
Molecular Weight 334.49
Formula C21H34O3
CAS Number 567-02-2
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Paul C M Piette. Best Pract Res Clin Obstet Gynaecol. The pharmacodynamics and safety of progesterone

[2] Latha Ramakrishnan, et al. Biochemistry. Mechanism of potentiation of a dysfunctional epilepsy-linked mutated GABA(A) receptor by a neurosteroid (3alpha, 21-dihydroxy-5alpha-pregnan-20-one): transient kinetic investigations

[3] M L Barbaccia, et al. Int Rev Neurobiol. Stress and neuroactive steroids

[4] B G Xue, et al. J Pharmacol Exp Ther. Partial agonism by 3alpha,21-dihydroxy-5beta-pregnan-20-one at the gamma-aminobutyric acidA receptor neurosteroid site

[5] A C Grobin, et al. Brain Res. Regulation of the prefrontal cortical dopamine system by the neuroactive steroid 3a,21-dihydroxy-5a-pregnane-20-one

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Keywords: 3α,21-Dihydroxy-5α-pregnan-20-one, THDOC supplier, GABA Receptor, inhibitors, activators


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