177976-12-4

Sarizotan dihydrochloride (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].

5-HT_1A Receptor: 0.1 nM (IC₅₀); Human D₃ Receptor: 6.8 nM (IC₅₀); 5-HT_2A Receptor: 587 nM (IC₅₀); 5-HT_2B Receptor: 108 nM (IC₅₀); 5-HT_5A Receptor: 313 nM (IC₅₀); Human 5-HT₆ Receptor: 3300 nM (IC₅₀); Human 5-HT₇ Receptor: 10 nM (IC₅₀)

[1] G D Bartoszyk, et al. Sarizotan, a Serotonin 5-HT1A Receptor Agonist and Dopamine Receptor Ligand. J Neural Transm (Vienna). 2004 Feb;111(2):113-26. DOI:10.1007/s00702-003-0094-7
[2] C Marin, et al. Local Administration of Sarizotan Into the Subthalamic Nucleus Attenuates Levodopa-Induced Dyskinesias in 6-OHDA-lesioned Rats. Psychopharmacology (Berl). 2009 Jun;204(2):241-50. DOI:10.1007/s00213-008-1452-9