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CAS No. | 351862-32-3 | Cat. No. | BCP24751 |
Name | Sarizotan | ||
Synonyms | EMD-128130; EMD128130; EMD 128130; EMD-77697; EMD-77697; EMD-77697; | ||
SMILES | C1CC2=CC=CC=C2OC1CNCC3=CC(=CN=C3)C4=CC=C(C=C4)F | ||
Chemical Name | |||
Formula | C22H21FN2O | M. Wt | 348.41 |
Purity | 98% | Storage | Store at 4-8°C |
Description | Sarizotan is a Dopamine D2 receptor partial agonist and Serotonin 1A receptor agonist. Sarizotan exhibits affinity at serotonin and dopamine receptors. Sarizotan effectively suppresses levodopa-induced dyskinesia in primate and rodent models of Parkinson's disease, and tardive dyskinesia in a rodent model. Sarizotan is a full agonist at D3 and D4.4 receptors (EC50=5.6 and 5.4 nM, respectively) but a partial agonist at D2S, D2L and D4.2 receptors (EC50=29, 23 and 4.5 nM, respectively). Sarizotan is an antagonist at D2S and D2L receptors (IC50=52 and 121 nM, respectively). Sarizotan is a full agonist at D2L, D3, D4.2 and D4.4 receptors (EC50=0.51, 0.47, 0.48 and 0.23 nM, respectively) but a partial agonist at D2S receptors (EC50=0.6 nM). |
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