For research use only. Not for therapeutic Use.
Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms[1][2][3].
Tandospirone is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, α1-adrenergic, α2-adrenergic and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM) than 5-HT1A[1].
Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors[1].
Tandospirone activates postsynaptic 5-HT1A receptor coupled with G-protein (Gi/o), resulting in inhibition of protein kinase A (PKA)-mediated protein phosphorylation and neuronal activity[1].
Tandospirone (10-80 mg/kg; i.p.) inhibits freezing behavior in the conditioned fear stress-induced freezing behavior rat model[3].
Tandospirone exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours[3].
| Catalog Number | I005281 |
| CAS Number | 87760-53-0 |
| Synonyms | (1R,2S,6R,7S)-4-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dione |
| Molecular Formula | C21H29N5O2 |
| Purity | ≥95% |
| InChI | 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- |
| InChIKey | CEIJFEGBUDEYSX-FZDBZEDMSA-N |
| SMILES | C1CC2CC1C3C2C(=O)N(C3=O)CCCCN4CCN(CC4)C5=NC=CC=N5 |
| Reference | [1]. Hamik A, et al. Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites. Biol Psychiatry. 1990 Jul 15;28(2):99-109. [2]. Xuefei Huang, et al. Role of tandospirone, a 5-HT1A receptor partial agonist, in the treatment of central nervous system disorders and the underlying mechanisms. Oncotarget. 2017 Nov 24; 8(60): 102705–102720. [3]. Kyoko Nishitsuji, et al. The pharmacokinetics and pharmacodynamics of tandospirone in rats exposed to conditioned fear stress. Eur Neuropsychopharmacol. 2006 Jul;16(5):376-82. |
