898532-85-9

D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile[1].

D₃ Receptor: 4.5 nM (Ki); 5-HT_1A Receptor: 11.9 nM (Ki); 5-HT_2A Receptor: 15.3 nM (Ki); 5-HT_2C Receptor: 206 nM (Ki); D₂ Receptor: 263 nM (Ki); D₁ Receptor: 3290 nM (Ki); hERG Channels: 930 nM (Ki)

[1] Butini S, et al. Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. J Med Chem. 2009 Jan 8;52(1):151-69. DOI:10.1021/jm800689g