Sarizotan 2HCl salt

  • Chemical Properties
CAS No. 177976-12-4 Cat. No. BCP18870
Name Sarizotan 2HCl salt
Synonyms Sarizotan dihydrochloride;
Formula C22H23Cl2FN2O M. Wt 421.34
  • Biological Activity
Description Sarizotan, also known as EMD-128130, 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).
Pathways Neuro Signaling Pathway GPCR/G Protein 
Targets 5 HT Receptor/Serotonin Receptor Dopamine Receptor 

Structure

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