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Literature DB >> 1320747

5 beta-pregnan-3 beta-ol-20-one, a specific antagonist at the neurosteroid site of the GABAA receptor-complex.

Abstract

Studies were made on the potentiation of [3H]flunitrazepam binding to rat brain membranes by gamma-aminobutyric acid (GABA), pentobarbitone and pregnanolone (5 beta-pregnan-3 alpha-ol-20-one). Epipregnanolone, the 3 beta isomer of pregnanolone, inhibited competitively the potentiation by pregnanolone with a Ki of 10.5 microM without affecting that of GABA. The potentiation by pentobarbitone was slightly enhanced. Epipregnanolone alone showed only slight potentiation of benzodiazepine binding. These findings demonstrate that epipregnanolone is a specific antagonist of the neurosteroid site of the GABAA receptor and raise the possibility of a physiological role for 3 beta-hydroxysteroids in modulating this receptor.

Entities: Chemical Species

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Year: 1992 PMID： 1320747 DOI： 10.1016/0304-3940(92)90454-f

Source DB: PubMed Journal: Neurosci Lett ISSN： 0304-3940 Impact factor: 3.046

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Cited

10 in total

1. Neurosteroid modulators of GABA(A) receptors differentially modulate Ethanol intake patterns in male C57BL/6J mice.

Authors: Matthew M Ford; Jeffrey D Nickel; Tamara J Phillips; Deborah A Finn
Journal: Alcohol Clin Exp Res Date: 2005-09 Impact factor: 3.455

2. Cyp7b, a novel brain cytochrome P450, catalyzes the synthesis of neurosteroids 7alpha-hydroxy dehydroepiandrosterone and 7alpha-hydroxy pregnenolone.

Authors: K A Rose; G Stapleton; K Dott; M P Kieny; R Best; M Schwarz; D W Russell; I Björkhem; J Seckl; R Lathe
Journal: Proc Natl Acad Sci U S A Date: 1997-05-13 Impact factor: 11.205

Review 3. Neurosteroid interactions with synaptic and extrasynaptic GABA(A) receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability.

Authors: Chase Matthew Carver; Doodipala Samba Reddy
Journal: Psychopharmacology (Berl) Date: 2013-09-27 Impact factor: 4.530

4. Neurosteroid Structure-Activity Relationships for Functional Activation of Extrasynaptic δGABA(A) Receptors.

Authors: Chase Matthew Carver; Doodipala Samba Reddy
Journal: J Pharmacol Exp Ther Date: 2016-02-08 Impact factor: 4.030

Review 5. The relevance of neuroactive steroids in schizophrenia, depression, and anxiety disorders.

Authors: Erin M MacKenzie; John Odontiadis; Jean-Michel Le Mellédo; Trevor I Prior; Glen B I Baker
Journal: Cell Mol Neurobiol Date: 2007-08 Impact factor: 5.046

6. 3beta -hydroxypregnane steroids are pregnenolone sulfate-like GABA(A) receptor antagonists.

Authors: Mingde Wang; Yejun He; Lawrence N Eisenman; Christopher Fields; Chun-Min Zeng; Jose Mathews; Ann Benz; Tao Fu; Erik Zorumski; Joe Henry Steinbach; Douglas F Covey; Charles F Zorumski; Steven Mennerick
Journal: J Neurosci Date: 2002-05-01 Impact factor: 6.167

Review 10. Brexanolone, a neurosteroid antidepressant, vindicates the GABAergic deficit hypothesis of depression and may foster resilience.

Authors: Bernhard Lüscher; Hanns Möhler
Journal: F1000Res Date: 2019-05-29

10 in total

5 beta-pregnan-3 beta-ol-20-one, a specific antagonist at the neurosteroid site of the GABAA receptor-complex.

1. Neurosteroid modulators of GABA(A) receptors differentially modulate Ethanol intake patterns in male C57BL/6J mice.

2. Cyp7b, a novel brain cytochrome P450, catalyzes the synthesis of neurosteroids 7alpha-hydroxy dehydroepiandrosterone and 7alpha-hydroxy pregnenolone.

Review 3. Neurosteroid interactions with synaptic and extrasynaptic GABA(A) receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability.

4. Neurosteroid Structure-Activity Relationships for Functional Activation of Extrasynaptic δGABA(A) Receptors.

Review 5. The relevance of neuroactive steroids in schizophrenia, depression, and anxiety disorders.

6. 3beta -hydroxypregnane steroids are pregnenolone sulfate-like GABA(A) receptor antagonists.

7. Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor.

Review 8. Mechanisms of neurosteroid interactions with GABA(A) receptors.

9. Photoaffinity labeling identifies an intersubunit steroid-binding site in heteromeric GABA type A (GABA_A) receptors.

Review 10. Brexanolone, a neurosteroid antidepressant, vindicates the GABAergic deficit hypothesis of depression and may foster resilience.

5 beta-pregnan-3 beta-ol-20-one, a specific antagonist at the neurosteroid site of the GABAA receptor-complex.

1. Neurosteroid modulators of GABA(A) receptors differentially modulate Ethanol intake patterns in male C57BL/6J mice.

2. Cyp7b, a novel brain cytochrome P450, catalyzes the synthesis of neurosteroids 7alpha-hydroxy dehydroepiandrosterone and 7alpha-hydroxy pregnenolone.

Review 3. Neurosteroid interactions with synaptic and extrasynaptic GABA(A) receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability.

4. Neurosteroid Structure-Activity Relationships for Functional Activation of Extrasynaptic δGABA(A) Receptors.

Review 5. The relevance of neuroactive steroids in schizophrenia, depression, and anxiety disorders.

6. 3beta -hydroxypregnane steroids are pregnenolone sulfate-like GABA(A) receptor antagonists.

7. Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor.

Review 8. Mechanisms of neurosteroid interactions with GABA(A) receptors.

9. Photoaffinity labeling identifies an intersubunit steroid-binding site in heteromeric GABA type A (GABAA) receptors.

Review 10. Brexanolone, a neurosteroid antidepressant, vindicates the GABAergic deficit hypothesis of depression and may foster resilience.

9. Photoaffinity labeling identifies an intersubunit steroid-binding site in heteromeric GABA type A (GABA_A) receptors.