PF-04995274

Research use only, not for human use.

PF-04995274 (TBPT) is a novel potent, sellective, partial agonist of 5-HT4 receptor under investigation for neurological disorders.

PF-04995274 (TBPT) is a novel potent, sellective, partial agonist of 5-HT4 receptor under investigation for neurological disorders.Alzheimer Disease Phase 1 Discontinued(In Vitro):PF-04995274 has EC50 values of 0.47 nM, 0.36 nM, 0.37 nM, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively. PF-04995274 has Ki values of 0.36 nM, 0.46 nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively.(In Vivo):PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior.

PF-04995274 has EC50 values of 0.47 nM, 0.36 nM, 0.37 nM, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively. PF-04995274 has Ki values of 0.36 nM, 0.46 nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively.

PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior. Animal Model:Male 129S6/SvEv mice (7-8 weeks) treated with contextual fear conditioning (CFC) and forced swim test (FST) Dosage:3 mg/kg, 10 mg/kg Administration:Intravenous injection; for 17 days Result:Attenuated learned fear and decreased stress-induced depressive-like behavior.

PF-4995274 | TBPT

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Neurological Disease

Alzheimer Disease

1331782-27-4

432.5214

C23H32N2O6

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (231.21 mM)

C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O

(R)-4-((4-(((4-(Tetrahydrofuran-3-yloxy)-1,2-benzisoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol

(-20℃)

With Ice Pack

≥ 2 years