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  • Title: 3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
    Author: Crawforth J, Goodacre S, Maxey R, Bourrain S, Patel S, Marwood R, O'Connor D, Herbert R, Hutson P, Rowley M.
    Journal: Bioorg Med Chem Lett; 2000 Dec 18; 10(24):2701-3. PubMed ID: 11133072.
    Abstract:
    A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indole is a high-affinity (1.2nM), selective (>800 fold over h5-HT2C and hD2 receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats.
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