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ChemInform Abstract: Synthesis and in vitro Activity of 3β-Substituted-3α- hydroxypregnan-20-ones: Allosteric Modulators of the GABAA Receptor.

✍ Scribed by D. J. HOGENKAMP; S. H. TAHIR; J. E. HAWKINSON; R. B. UPASANI; M. ALAUDDIN; C. L. KIMBROUGH; M. ACOSTA-BURRUEL; E. R. WHITTEMORE; R. M. WOODWARD; N. C. LAN; K. W. GEE; M. B. BOLGER

Publisher: John Wiley and Sons
Year: 2010
Weight: 36 KB
Volume: 28
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199717196

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✦ Synopsis

Synthesis and in vitro Activity of 3β-Substituted-3α-hydroxypregnan-20-ones: Allosteric Modulators of the GABAA Receptor.

-A series of 3β-substituted 3α-hydroxy-5α-(24 examples) and -5β-pregnan-20-ones (7 examples) is evaluated as potent allosteric modulators for the γ-aminobutyric acidA (GABAA) receptor. The most active compounds are (IV) and (V). The former (CCD 1042) is an orally active anticonvulsant in animals.

-(HOGENKAMP, D.

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