Lu AA33810

Lu AA33810 is an antagonist of neuropeptide Y (NPY) receptor Y5 (Ki = 1. nM for the human receptor). It is selective for Y5 over Y1, Y2, and Y4 (Kis = >10 µM for all in HEK293 membranes expressing rat receptors). Lu AA33810 also binds the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2B (Kis = 478 and 247 nM, respectively). It inhibits NPY-induced calcium mobilization and cAMP accumulation in COS-7 and HEK293 cells expressing the rat Y5 receptor, respectively, in a concentration-dependent manner. Lu AA33810 (10 mg/kg) increases social interaction time in a social exploration test, as well as decreases immobility time in the forced swim test, in rats, indicating anxiolytic- and antidepressant-like activities, respectively. Formal Name: N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide. CAS Number: 304008-29-5. Molecular Formula: C19H25N3O2S3. Formula Weight: 423.6. Purity: >98%. Formulation: A solid. Solubility: DMSO: 100 mM. lambdamax: 225, 244, 255, 363 nm. SMILES: CS(NC[C@@H](CC1)CC[C@H]1NC2=NC3=C(S2)CCSC4=CC=CC=C34)(=O)=O. InChi Code: InChI=1S/C19H25N3O2S3/c1-27(23,24)20-12-13-6-8-14(9-7-13)21-19-22-18-15-4-2-3-5-16(15)25-11-10-17(18)26-19/h2-5,13-14,20H,6-12H2,1H3,(H,21,22)/t13-,14-. InChi Key: UWSBTSAJZMIHBL-HDJSIYSDSA-N. Storage: -20°C. Stability: > 4 years.