TMU4142 is a potent, GoA pathway-selective 5-HT1A receptor (5-HT1AR) agonist with pEC50 of 8.80 (EC50=1.59 nM), Emax=92.78%.
TMU4142 displays nearly full agonist activity at the 5-HT1AR GoA pathway, whereas its Gi3 activity is significantly lower than that of 5-HT.
TMU4142 strongly activates the GoA protein over other tested Gi/o family proteins.
TMU4142 shows no discernible activity at 5-HT1AR β-arrestin-2 pathway, and weak or no activity at other serotonin and dopamine receptors.
TMU4142 (1.5 mg/kg) elicits rapid antidepressant-like activity without triggering significant DRN autoreceptor activation in mouse model of depression.
