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  • Title: SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
    Author: Forbes IT, Douglas S, Gribble AD, Ife RJ, Lightfoot AP, Garner AE, Riley GJ, Jeffrey P, Stevens AJ, Stean TO, Thomas DR.
    Journal: Bioorg Med Chem Lett; 2002 Nov 18; 12(22):3341-4. PubMed ID: 12392747.
    Abstract:
    A focused SAR study around the previously reported selective 5-HT(7) receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improved pharmacokinetic profile. Replacement of the phenolic group in SB-269970-A with an indole moiety, and replacement of the piperidinyl 4-methyl group with a heterocyclic ring system proved to be the key changes leading to the identification of SB-656104-A.
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