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Biotech / Medical : ACADIA Pharmaceuticals Inc (ACAD) -- Ignore unavailable to you. Want to Upgrade?

To: tuck who wrote (202)	11/24/2005 1:56:55 PM
From: tuck	Read Replies (1) \| Respond to of 588

[Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid beta2 Receptor Agonist] >>J Med Chem. 2005 Dec 1;48(24):7517-9. Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid beta2 Receptor Agonist. Lund BW, Piu F, Gauthier NK, Eeg A, Currier E, Sherbukhin V, Brann MR, Hacksell U, Olsson R. ACADIA Pharmaceuticals AB, Medeon Science Park, S-205 12 Malmo, Sweden, and ACADIA Pharmaceuticals Inc., 3911 Sorrento Valley Blvd., San Diego, California 92121. 4'-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARbeta2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorly soluble hit into a more potent and orally available compound (2, AC-261066) with retained beta2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARbeta2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.<< Cheers, Tuck