Tandospirone

Tandospirone is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It selectively binds to 5-HT1A receptors (Ki = 0.027 µM) over 5-HT2, 5-HT1B, 5-HT1C, and 5-HT1D receptors (Kis = 1.3, >100, 2.6, and >100 µM, respectively), as well as alpha1-adrenergic receptors (alpha1-ARs), alpha2-ARs, beta-ARs, and dopamine D1 and D2 receptors (Kis = 1.6, 1.9, >100, 1.7, and 41 µM, respectively). Tandospirone (0.1-100 µM) reduces forskolin-induced adenylate cyclase activity in rat hippocampal homogenates. In vivo, tandospirone (10 and 20 mg/kg) reduces immobility time in the forced swim test in mice. Tandospirone (10 mg/kg) increases food intake and overall survival, as well as decreases body weight loss in a Yoshida hepatoma rat model of cancer cachexia. Formulations containing tandospirone have been used in the treatment of depression.Formal Name: (3aR,4S,7R,7aS)-rel-hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-methano-1H-isoindole-1,3(2H)-dione. CAS Number: 87760-53-0. Synonyms: SM-3997. Molecular Formula: C21H29N5O2. Formula Weight: 383.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Ethanol: Sparingly soluble: 1-10 mg/ml. SMILES: O=C1[C@]2([H])[C@@](C(N1CCCCN3CCN(C4=NC=CC=N4)CC3)=O)([H])[C@]5([H])C[C@@]2([H])CC5. InChi Code: InChI=1S/C21H29N5O2/c27-19-17-15-4-5-16(14-15)18(17)20(28)26(19)9-2-1-8-24-10-12-25(13-11-24)21-22-6-3-7-23-21/h3,6-7,15-18H,1-2,4-5,8-14H2/t15-,16+,17+,18-. InChi Key: CEIJFEGBUDEYSX-FZDBZEDMSA-N.