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Tandospirone

Product Name
Tandospirone
CAS No.
87760-53-0
Chemical Name
Tandospirone
Synonyms
(3aR,4S,7R,7aS)-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione;Sediel;TANDOSPIRONE;(3aR,4S,7R,7aS)-rel-;Tandospirone (SM3997);Tandospirone [inn:ban];TANDOSPIRONE USP/EP/BP;Tandospirone hydrochloride;3a,4,7,7a-Hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-4,7-methano-1H-isoindole-1,3(2H)-dione;(1R*,2S*,3R*,4S*)-N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-2,3-norbornanedicarboximide citrate salt
CBNumber
CB4796484
Molecular Formula
C21H29N5O2
Formula Weight
383.49
MOL File
87760-53-0.mol
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Tandospirone Property

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)
form 
Solid
color 
White to Off-White
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Safety

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
T6704
Product name
Tandospirone
Purity
≥98% (HPLC)
Packaging
5mg
Price
$150
Updated
2024/03/01
Sigma-Aldrich
Product number
T6704
Product name
Tandospirone
Purity
≥98% (HPLC)
Packaging
25mg
Price
$537
Updated
2024/03/01
Tocris
Product number
2854
Product name
Tandospironehydrochloride
Purity
≥98%(HPLC)
Packaging
10
Price
$165
Updated
2021/12/16
Usbiological
Product number
256809
Product name
Tandospirone hydrochloride
Packaging
10mg
Price
$403
Updated
2021/12/16
Usbiological
Product number
290605
Product name
Tandospirone hydrochloride
Packaging
5mg
Price
$545
Updated
2021/12/16
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Tandospirone Chemical Properties,Usage,Production

Description

Tandospirone is another 5-HT1A receptor agonist under development by Sumitomo Pharmaceutical Co., Ltd., in Japan and Pfizer in the United States. Results of phase II and phase III clinical trials show that tandospirone is effective for the treatment of anxiety neurosis. Significant improvement is also observed in patients with psychosomatic disease, phobia, and depersonalization (Murasaki 1995). The results have shown that initial treatment should be started at 30 mg daily, and the dose should be increased up to 60 mg daily according to symptoms (Murasaki 1995). A double-blind comparative study with diazepam revealed that tandospirone tends to be superior to diazepam in patients with depressive neurosis, whereas diazepam may be more effective than tandospirone in severely ill patients (Murasaki et al. 1992).

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.

Definition

ChEBI: Tandospirone is a dicarboximide that is (3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione which is substituted by a 4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl group at position 2. It is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM). It has a role as an antidepressant and an anxiolytic drug. It is a N-alkylpiperazine, a N-arylpiperazine, a member of pyrimidines, a bridged compound and a dicarboximide. It is a conjugate base of a tandospirone(1+).

Preparation

Tandospirone is attained from the exo diels-alder adduct of maleic anhydride and cyclopentadiene in a four step convergent approach.

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.

References

[1] shimizu h1, hirose a, tatsuno t, nakamura m, katsube j. pharmacological properties of sm-3997: a new anxioselective anxiolytic candidate. jpn j pharmacol. 1987 dec; 45(4):493-500.

Tandospirone Preparation Products And Raw materials

Raw materials

Preparation Products

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Tandospirone Suppliers

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View Lastest Price from Tandospirone manufacturers

Zibo Hangyu Biotechnology Development Co., Ltd
Product
Tandospirone 87760-53-0
Price
US $55.00-550.00/kg
Min. Order
10kg
Purity
0.99
Supply Ability
20tons
Release date
2023-11-07
Chengdu Aupone Pharmaceutical Co.Ltd.
Product
Tandospirone 87760-53-0
Price
US $0.00/gram
Min. Order
10gram
Purity
99.99
Supply Ability
10Tons
Release date
2024-03-18
Dideu Industries Group Limited
Product
TANDOSPIRONE 87760-53-0
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons min
Release date
2021-07-23

87760-53-0, TandospironeRelated Search:


  • 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
  • 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
  • Tandospirone hydrochloride
  • 3a,4,7,7a-Hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-4,7-methano-1H-isoindole-1,3(2H)-dione
  • (3aR,4S,7R,7aS)-rel-
  • 4,7-Methano-1H-isoindole-1,3(2H)-dione,hexahydro-2-[4-[4-(2-pyriMidinyl)-1-piperazinyl]butyl]-, (3aR,4S,7R,7aS)-rel-
  • (1R*,2S*,3R*,4S*)-N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-2,3-norbornanedicarboximide citrate salt
  • 4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aα,4β,7β,7aα)-
  • (3aR,4S,7R,7aS)-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
  • TANDOSPIRONE USP/EP/BP
  • rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
  • Tandospirone (SM3997)
  • 87760-53-0
  • C21H29N5O2HCl
  • C21H29N5O2
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Serotonin receptor