Name | tandospirone citrate |
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Synonyms |
(1R,2S,6R,7S)-4-{4-[4-(Pyrimidin-2-yl)piperazin-1-yl]butyl}-4-azatricyclo[5.2.1.0]decane-3,5-dione 2-hydroxypropane-1,2,3-tricarboxylate (1:1)
[14C]-Tandospirone citrate Sediel (TN) tandospirone dihydrogen citrate Tandospirone citrate [USAN] SM-3997 4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aR,4S,7R,7aS)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt) UNII-0R8E9BWM4J (1R,2S,6R,7S)-4-{4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl}-4-azatricyclo[5.2.1.0]decane-3,5-dione 2-hydroxy-1,2,3-propanetricarboxylate (1:1) 4,7-Methano-1H-isoindole-1,3(2H)-dione,hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-,(3aalpha,4beta,7beta,7aalpha)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1) metanopirone citrate (3aR,4S,7R,7aS)-2-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (1:1) Sediel Tandospirone (citrate) |
Description | Tandospirone citrate 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. |
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Related Catalog | |
References |
Boiling Point | 613.9ºC at 760 mmHg |
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Molecular Formula | C27H37N5O9 |
Molecular Weight | 575.611 |
Flash Point | 325.1ºC |
Exact Mass | 575.259155 |
PSA | 201.77000 |
LogP | 0.10220 |
Vapour Pressure | 5.23E-15mmHg at 25°C |
Storage condition | 2-8℃ |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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HS Code | 2933990090 |
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HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |