RO-1138452, soluble in DMSO and ethanol and insoluble in water, inhibits the signaling pathway between G-protein-coupled receptors (GPCRs) and G proteins. It targets guinea-pig 5-HT4 receptor, human α2A adrenoceptor, human α2A adrenoceptor, human 5-HT1A receptor, human 5-HT1A receptor, human muscarinic M1 receptor, human muscarinic M1 receptor, human muscarinic M2 receptor, human muscarinic M2 receptor, and human muscarinic M4 receptor.
Molecular Weight
309.41
Molecular Formula
C19H23N3O
Targets
Guinea-pig 5-HT4 receptor: 8910 nM; Guinea-pig 5-HT4 receptor: 5.35 (pKi); Human α2A adrenoceptor: 724 nM; Human α2A adrenoceptor: 6.49 (pKi); Human 5-HT1A receptor: 8580 nM; Human 5-HT1A receptor: 5.37 (pKi); Human muscarinic M1 receptor: 2570 nM; Human muscarinic M1 receptor: 5.66 (pKi); Human muscarinic M2 receptor: 2220 nM; Human muscarinic M2 receptor: 5.88 (pKi); Human Muscarinic M4 receptor: 1450 nM
RO-1138452 can be used to research and develop therapeutic strategies for certain diseases that involve excessive activation of GPCR-G protein signaling pathways.
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