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TANDOSPIRONE

$ 1.00 /1KG

Min. Order1KG
Purity99%
Cas No87760-53-0
Supply Ability100kg
Update time2019-12-26

career henan chemical co

5YR

China

Chemical Properties

Product Name	TANDOSPIRONE
CAS No	87760-53-0
EC-No
Min. Order	1KG
Purity	99%
Supply Ability	100kg
Release date	2019/12/26

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Product Name:

TANDOSPIRONE

Synonyms:

TANDOSPIRONE;4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aa,4b,7b,7aa)-;4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aR,4S,7R,7aS)-rel- (9CI);(3αα，4β，7β，7αα)-Hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4，7-methano-1H-isoindole-1，3(2H)-dione;Sediel;3a,4,7,7a-Hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-4,7-methano-1H-isoindole-1,3(2H)-dione;Tandospirone [inn:ban];(3aR,4S,7R,7aS)-rel-Hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-methano-1H-isoindole-1,3(2H)-dionehydrochloride

CAS:

87760-53-0

MF:

C21H29N5O2

MW:

383.49

EINECS:

Product Categories:

Serotonin receptor;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals

Mol File:

87760-53-0.mol

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TANDOSPIRONE Chemical Properties

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Melting point

112-113.5°

Boiling point

613.9±65.0 °C(Predicted)

density

1.239±0.06 g/cm3(Predicted)

storage temp.

Store at +4°C

solubility

DMSO: soluble38mg/mL

pka

7.71±0.10(Predicted)

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Safety Information

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Hazard Codes

Risk Statements

36/37/38

Safety Statements

WGK Germany

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MSDS Information

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TANDOSPIRONE Usage And Synthesis

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Description

Sediel was launched in Japan as an anxiolytic agent and is a member of the azapirone family. Ready access to the compound is attained from the ex0 Diels- Alder adduct of maleic anhydride and cyclopentadiene in a four step convergent approach. Biochemically, it is a partial agonist of the post-synaptic 5-HT_1a receptor. This metabotropic receptor is coupled to the G proteins and suppresses adenylate cyclase and phosphatidylinositol metabolism systems. It has low affinity for dopamine D₂, 5-HT₂ and α₁-adreneric receptors and no affinity for benzodiazepine, GABA or 5-HT_1b binding sites. The primary metabolic product is two orders of magnitude less active. Tandospirone is as effective as benzodiazepines in anxiolytic activity but does not have the side-effects (low abuse potential, weak sedative, no anticonvulsant activity).

Originator

Sumitomo (Japan)

Uses

Tandospirone is a 5HT1A receptor partial agonist. Studies indicate that tandospirone significantly reduces haloperidol-induced bradykinesia in a dose dependent manner. The potency of Tandospirone is equal to that of buspirone and approximate one-half that of diazepam. The potency of Tandospirone at dopamine antagonistic action is less than 1/4 that of buspirone.

Brand name

Sediel

Biological Activity

5-HT 1A receptor partial agonist (K i = 27 nM) that displays selectivity over 5-HT 2 , 5-HT 1C , α 1 , α 2 , D 1 and D 2 receptors (K i values ranging from 1300-41000 nM). Inactive at 5-HT uptake sites, 5-HT 1B , β -adrenergic, muscarinic and benzodiazepine receptors. Displays anxiolytic activity.

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