| Company Name: |
Bide Pharmatech Ltd.
|
| Tel: |
400-1647117 13681763483 |
| Email: |
product02@bidepharm.com |
| Products Intro: |
Product Name:(R)-1-(Chroman-2-yl)-N-((5-(4-fluorophenyl)pyridin-3-yl)methyl)methanamine
CAS:351862-32-3
Purity:98% Package:25mg;50mg;100mg;250mg Remarks:BD01407742
|
| Company Name: |
Suzhou Zhixin Biotechnology Co., Ltd.
|
| Tel: |
0512-65118909 18100677375 |
| Email: |
sales@szzxbio.com |
| Products Intro: |
Product Name:Sarizotan
CAS:351862-32-3
Purity:98%+ Package:1g;10g;100g
|
| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
|
| Tel: |
021-65675885 18964387627 |
| Email: |
customer_service@efebio.com |
| Products Intro: |
Product Name:Sarizotan
CAS:351862-32-3
Purity:95.00% Package:2mg;5mg;25mg
|
| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:Sarizotan
CAS:351862-32-3
Package:2mg/RMB 1220;5mg/RMB 2270;25mg/RMB 7690
|
|
| | Sarizotan Basic information |
| Product Name: | Sarizotan | | Synonyms: | Sarizotan free base;3-Pyridinemethanamine, N-[[(2R)-3,4-dihydro-2H-1-benzopyran-2-yl]methyl]-5-(4-fluorophenyl)-;(R)-1-(Chroman-2-yl)-N-((5-(4-fluorophenyl)pyridin-3-yl)methyl)methanamine;Rotigotine Impurity 26-d3 | | CAS: | 351862-32-3 | | MF: | C22H21FN2O | | MW: | 348.41 | | EINECS: | | | Product Categories: | | | Mol File: | 351862-32-3.mol |  |
| | Sarizotan Chemical Properties |
| Boiling point | 507.7±45.0 °C(Predicted) | | density | 1.172±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (287.02 mM; Need ultrasonic) | | form | Viscous Liquid | | pka | 7.01±0.20(Predicted) | | color | Colorless to light yellow |
| | Sarizotan Usage And Synthesis |
| Uses | Treatment—associated dyskinesia in Parkinson’s disease. | | in vivo | Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex[1].
Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease[1].
Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2].
| Animal Model: | Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2]. | | Dosage: | 1 ng, 10 ng and 1 μg in 0.3 μL solution. | | Administration: | Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days. | | Result: | On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively). |
| | IC 50 | 5-HT1A Receptor: 6.5 nM (IC50, rat); 5-HT1A Receptor: 0.1 nM (IC50, human); rD2 Receptor: 15.1 nM (IC50, rat); D3 Receptor: 6.8 nM (IC50, human); 5-HT1B Receptor: 600 nM (IC50, rat); 5-HT1D Receptor: 500 nM (IC50, calf); 5-HT2A Receptor: 960 nM (IC50, rat, agonist site); 5-HT2A Receptor: 587 nM (IC50, human, antagonist site); 5-HT2B Receptor: 108 nM (IC50, human); 5-HT2C Receptor: 800 nM (IC50, pig); 5-HT3 Receptor: 3500 nM (IC50, NG 108 cells); 5-HT5A Receptor: 313 nM (IC50, human); 5-HT6 Receptor: 3300 nM (IC50, human); 5-HT7 Receptor: 10 nM (IC50, human); hD4.2 Receptor: 2.4 nM (IC50); hD2 Receptor: 17 nM (IC50) |
| | Sarizotan Preparation Products And Raw materials |
|