Article
Neurosteroid analogues. 14. Alternative ring system scaffolds: GABA modulatory and anesthetic actions of cyclopenta[b]phenanthrenes and cyclopenta[b]anthracenes.
Journal of medicinal chemistry - 13 Mar 2008
Scaglione Jamie B, Jastrzebska Izabella, Krishnan Kathiresan, Li Ping, Akk Gustav, Manion Brad D, Benz Ann, Taylor Amanda, Rath Nigam P, Evers Alex S, Zorumski Charles F, Mennerick Steven, Covey Douglas F
Abstract excerpt
Although the structural features of binding sites for neuroactive steroids on gamma-aminobutryic acid type A (GABA A) receptors are still largely unknown, structure-activity studies have established a pharmacophore for potent enhancement of GABA A receptor function by neuroactive steroids. This pharmacophore emphasizes the importance of the position and stereochemistry of hydrogen-bonding groups on the steroid....
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