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编 号:F545261
分子式:C21H30ClN5O2
分子量:419.95
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生物活性:
Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms.

体内研究:
Tandospirone (SM-3997) hydrochloride (10-80 mg/kg; i.p.) inhibits freezing behavior in the conditioned fear stress-induced freezing behavior rat model.Tandospirone hydrochloride exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours.Animal Model:Seven-week-old male Sprague-Dawley rats (260-300 g), conditioned fear stress-induced freezing behavior rat model
Dosage:10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg
Administration:Intraperitoneal injection
Result:Inhibited freezing behavior in a dose-dependent manner.

体外研究:
Tandospirone (SM-3997) hydrochloride 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.Tandospirone hydrochloride is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors.Tandospirone hydrochloride 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.
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