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Tandospirone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tandospirone图片
CAS NO:87760-53-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
Tandospirone (SM-3997) 是一种有效的选择性 5-HT1A 受体部分激动剂,Ki 为 27 nM。
Cas No.87760-53-0
别名坦度螺酮; SM-3997
化学名(3aR,4S,7R,7aS)-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Canonical SMILESO=C([C@@]1([H])[C@@](C([H])([H])C2([H])[H])([H])C([H])([H])[C@@]2([H])[C@]13[H])N(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N4C([H])([H])C([H])([H])N(C5=NC([H])=C([H])C([H])=N5)C([H])([H])C4([H])[H])C3=O
分子式C21H29N5O2
分子量383.49
溶解度≥ 38.3mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

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.