Activity of B-Nor Analogues of Neurosteroids on the GABAA Receptor in Primary Neuronal Cultures

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F06%3A00041903" target="_blank" >RIV/61388963:_____/06:00041903 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

Activity of B-Nor Analogues of Neurosteroids on the GABAA Receptor in Primary Neuronal Cultures

Original language description

B-Norallopregnanolone was found comparable to allopregnanolone when measured with labelled TBPS. Analogous results were obtained from their effect on neurons in culture: this time, both 3alpha-hydroxy-7-nor-5alpha-and 3alpha-hydroxy-7-nor-5beta-pregnan-20-ones stimulated [3H]flunitrazepam binding and GABA-induced 36Cl- influx. A computational analysis of active and inactive neurosteroid analogues allowed the proposal of a 3D pharmacophoric hypothesis of their interaction with the GABAA receptor.

Czech name

Účinky B-noranalog neurosteroidů na GABAA receptor měřené na primární kultuře neuronů

Czech description

B-Norallopregnanolon vykazoval stejnou aktivitu jako allopregnanolone v TBPS testu. Analogické výsledky byly získány z jejich účinků na kultuře neuronů, tentokrát oba 3alpha-hydroxy-7-nor-5alpha- a 3alpha-hydroxy-7-nor-5beta-pregnan-20-ony stimulovaly vazbu [3H]flunitrazepamu a influx 36Cl- do neuronu. Molekulární modelování řady aktivních a neaktivních analog umožnilo formulovat hypotézu o 3D farmacoforu vazby neurosteriodů na GABAA receptor.

Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CC - Organic chemistry

OECD FORD branch

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Project

<a href="/en/project/GA203%2F06%2F1605" target="_blank" >GA203/06/1605: New steroid antiepileptics: synthesis and biological activity</a><br>

Continuities

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2006

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

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Volume of the periodical

49

Issue of the periodical within the volume

11

Country of publishing house

US - UNITED STATES

Number of pages

10

Pages from-to

3225-3224

UT code for WoS article

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EID of the result in the Scopus database

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