1434515-70-4

UCSF924 is a selective, high-affinity dopamine D4 receptor (DRD4) partial agonist (Ki = 3 nM for human D4) with a 7.4-fold bias toward arrestin recruitment over Gαi (Gαi/0; Gi/G0) signaling activation with respect to quinpirole. UCSF924 exhibits no detectable affinity for D2, D3 or the F261V/L328F D4 mutant and no agonist activity toward a panel of 320 nonolfactory GPCRs even at a high concentration of 1 μM. The UCSF924 structure analog UCSF924NC is the recommended negative control compound with a 1/2500-fold reduced D4 affinity.

UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has no off-target effects on more than 320 non-olfactory GPCRs. UCSF924 can be used for research in the field of neuropsychiatric diseases[1][2].

D₄ Receptor

[1] Wang S, et al. D4 dopamine receptor high-resolution structures enable the discovery of selective agonists. Science. 2017 Oct 20;358(6361):381-386. DOI:10.1126/science.aan5468
[2] Thomas G E. Characterizing antipsychotic behavioral and corticostriatal neurophysiological effects to psychotomimetic challenge. Duke University, 2022.