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Tandospirone

CAS No. : 87760-53-0

MCE 站：Tandospirone

产品活性：Tandospirone (SM-3997) 是一种高效、选择性的 5-HT_1A 受体部分激动剂，其 K_i 值为 27 nM。Tandospirone 具有抗焦虑和抗抑郁作用。Tandospirone 可用于中枢神经系统疾病及其潜在机制的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Tandospirone is approximately two to three orders of magnitude less potent at 5-HT₂, 5-HT_1C, α1-adrenergic, α2-adrenergic and dopamine D1 and D2 receptors (K_i values ranging from 1300 to 41000 nM) than 5-HT_1A.
Tandospirone is essentially inactive at 5-HT_1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors.
Tandospirone activats postsynaptic 5-HT_1A receptor coupled with G-protein (G_i/o), resulting in inhibition of protein kinase A (PKA)-mediated protein phosphorylation and neuronal activity.

In Vivo: Tandospirone (10-80 mg/kg; i.p.) inhibits freezing behavior in the conditioned fear stress-induced freezing behavior rat model.
Tandospirone exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours.

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