PF-04995274 (PF-4995274, TBPT) is a potent, selective, orally active and partial serotonin 4 receptor (5-HT4R) agonist with Ki of 0.15-0.46 nM.
PF-04995274 exhibits an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E and 0.59-0.65 nM for rat 5-HT4S/4L/4E.
PF-04995274 (3-10 mg/kg, i.v.) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior in mice.
PF-04995274 is brain penetrant for investigation of cognitive disorders associated with Alzheimer's disease.
