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GPCR/G Protein 5-HT Receptor Tandospirone

Tandospirone

Catalog No. TQ0315   CAS 87760-53-0
Synonyms: SM-3997

Tandospirone (SM-3997) is a selective partial agonist of 5-HT1A receptor (Ki: 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Kis: 1300-41000 nM).

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Tandospirone, CAS 87760-53-0
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50 mg Inquiry 361.00
100 mg Inquiry 527.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tandospirone (SM-3997) is a selective partial agonist of 5-HT1A receptor (Ki: 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Kis: 1300-41000 nM).
In vitro 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].
Synonyms SM-3997
Purity
Molecular Weight 383.49
Formula C21H29N5O2
CAS No. 87760-53-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 6 months

Solubility Information

DMSO: 30mg/mL

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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