Name | Metanopirone |
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Synonyms |
tandospirone hydrochloride
unii-rwr6slb9p6 |
Description | 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[1][2][3]. |
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Related Catalog | |
Target |
5-HT1A Receptor:27 nM (Ki) |
In Vitro | 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[1]. Tandospirone hydrochloride is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors[1]. 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[1]. |
In Vivo | Tandospirone (SM-3997) hydrochloride (10-80 mg/kg; i.p.) inhibits freezing behavior in the conditioned fear stress-induced freezing behavior rat model[3]. Tandospirone hydrochloride exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours[3]. Animal Model: Seven-week-old male Sprague-Dawley rats (260-300 g), conditioned fear stress-induced freezing behavior rat model[3] 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. |
References |
Molecular Formula | C21H30ClN5O2 |
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Molecular Weight | 419.94800 |
Exact Mass | 419.20900 |
PSA | 69.64000 |
LogP | 2.15270 |