"目录号: HY-14558
GPCR/G ProteinNeuronal Signaling-
Tandospirone(SM-3997)是5-HT1A受体部分激动剂，Ki为27 nM，对SR-2，SR-1C，_alpha_1，_alpha_2，D1和D2受体的Ki为1300到41000 nM。
5-HT Receptor
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生物活性
Description
Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1]Target: 5-HT1Ain vitro: Tandospirone is most potent at the 5-HT1A receptor, displaying a Ki value of 27 +/- 5 nM. The agent is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, alpha 1-adrenergic, alpha 2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM). Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors [1]. 3H-SM-3997 bound rapidly, reversibly and in a saturable manner with high affinity to rat brain hippocampal membranes (Kd = 9.4 nM, Bmax = 213 fmol/mg protein) [2]. in vivo: Chronic treatment with tandospirone, at 0.2 and 1.0mg/kg/day, but not 2.0mg/kg/day, attenuated footshock stress-induced eLAC elevation in the mPFC [3]. Rats were acutely administered tandospirone (0, 0.1, and 1 mg/kg, i.p.). Tandospirone decreased the number of premature responses, an index of impulsive action, in a dose-dependent manner [4].Toxicity: It is not believed to be addictive but it is known to produce mild withdrawal effects (e.g. anorexia) after abrupt discontinuation.
Clinical Trial
NCT01614041
Sumitomo Pharmaceutical (Suzhou) Co., Ltd.
Generalized Anxiety Disorder
November 2011
Phase 4
NCT02040883
Qingyun Yin-Guangzhou Psychiatric Hospital
Schizophrenia
February 2014
Phase 4
NCT03151382
Zhejiang Provincial People’s Hospital
Alzheimer Disease-Cognitive Function
May 20, 2017
Phase 4
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References
[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].Shimizu H, et al. Characterization of the putative anxiolytic SM-3997 recognition sites in rat brain. Life Sci. 1988;42(24):2419-27.
[3].Uehara T, et al. Chronic treatment with tandospirone, a 5-HT1A receptor partial agonist, suppresses footshock stress-induced lactate production in the prefrontal cortex of rats. Pharmacol Biochem Behav. 2013 Nov 15;113:1-6.
[4].Ohmura Y, et al. Tandospirone suppresses impulsive action by possible blockade of the 5-HT1A receptor. J Pharmacol Sci. 2013;122(2):84-92.