351862-32-3
- Name: Sarizotan
- Chemical Name: 1-[(2R)-3,4,4a,8a-tetrahydro-2H-chromen-2-yl]-N-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]methanamine
- CAS Number: 351862-32-3
- Molecular Formula: C22H21FN2O
- Molecular Weight: 350.42900
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2017-03-11 07:12:54
- Modify Date: 2024-01-08 22:19:34
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Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively[1].
| Name | 1-[(2R)-3,4,4a,8a-tetrahydro-2H-chromen-2-yl]-N-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]methanamine |
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| Synonyms |
1-(5-(4-Fluorophenyl)pyridin-3-yl)-N-((2R)-3,4,4a,8a-tetrahydro-2H-chromen-2-ylmethyl)methanamine
3-Pyridinemethanamine,5-(4-fluorophenyl)-N-(((2R)-3,4,4a,8a-tetrahydro-2H-1-benzopyran-2-yl)methyl) |
| Description | Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively[1]. |
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| Related Catalog | |
| Target |
5-HT1A Receptor:6.5 nM (IC50, rat) 5-HT1A Receptor:0.1 nM (IC50, human) D2 Receptor:15.1 nM (IC50, rat) D2 Receptor:17 nM (IC50, human) D3 Receptor:6.8 nM (IC50, human) D4.2:2.4 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) |
| In Vitro | Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) [1]. |
| 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). |
| References |
| Molecular Formula | C22H21FN2O |
|---|---|
| Molecular Weight | 350.42900 |
| Exact Mass | 350.17900 |
| PSA | 34.15000 |
| LogP | 4.65800 |