Epiallopregnanolone (Synonyms: 5α-Pregnan-20-one,3β,21-dihydroxy-5α-Pregnan-20-one,3β,5α-Tetrahydrodeoxycorticosterone,3β,5α-Tetrahydroprogesterone) |
Catalog No.GC11054 |
inactive as a GABAA receptor modulator and used as a control substance to examine GABA neurotransmission.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 567-01-1
Sample solution is provided at 25 µL, 10mM.
Epiallopregnanolone, a endogenous 3 β-isomer of allopregnanolone, is a metabolite of progesterone. Epiallopregnanolone is a competitive antagonist at the neurosteroid site on the GABAA receptor [1]. GABAA receptors are GABA -gated chloride channels involved in mediating neuronal inhibition in the brain [2].
In vitro: Epiallopregnanolone showed no effects on the GABA-mediated chloride flux through several types of recombinant GABA receptors. Epiallopregnanolone inhibited the allopregnanolone-stimulated GABA-mediated chloride flux through GABAA receptors. Epiallopregnanolone antagonized the inhibitory effects of allopregnanolone and ethanol on the population spike in the CA1 region of the hippocampal brain slices [1]. Epiallopregnanolone selectively blocked the allopregnanolone inhibition of the population spike in the rat hippocampal CA1[3].
In vivo: In rats trained to discriminate either 0.8g/kg or 1.2 g/kg ethanol, 100 mg/kg epiallopregnanolone treatment decreased the maximum effect by 40% and 54% ethanol lever, respectively. Epiallopregnanolone significantly decreased response rates when compared with control condition [1].
References:
[1] Ginsburg B C, Lamb R J. Alphaxalone and epiallopregnanolone in rats trained to discriminate ethanol[J]. Alcoholism: Clinical and Experimental Research, 2005, 29(9): 1621-1629.
[2] Macdonald R L, Olsen R W. GABAA receptor channels[J]. Annual review of neuroscience, 1994, 17(1): 569-602.
[3] Wang M, Bckstrm T, Landgren S. Epiallopregnanolone selectively blocks the allopregnanolone inhibition of the population spike in the rat hippocampal CA1[J]. Acta physiologica Scandinavica, 1999, 167(2): A5-A5.
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