LU AA33810 is a potent NPY5-R antagonist. Displays ≥ 3300-fold affinity for NPY5-R over NPY1-R, NPY2-R and NPY4-R. LU AA33810 also binds human 5-HT2B and 5-HT1A receptors (Ki values are 247 and 478 nM respectively). Exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity. Neuropeptide Y (NPY) receptors belong to the Gi/o-protein-coupled receptor family in four subtypes, NPY1-R, NPY2-R, NPY4-R, NPY5-R, which are found in high concentrations in the brain and in the colon.
Walker et al (2009) The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydrobenzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress anxiety. J.Pharmacol.Exp.Ther. 328 900.
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