PF-04995274

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay). It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.Formal Name: tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-2H-pyran-4-ol. CAS Number: 1331782-27-4. Molecular Formula: C23H32N2O6. Formula Weight: 432.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 30 mg/ml, DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.25 mg/ml. SMILES: OC1(CCOCC1)CN(CC2)CCC2COC3=NOC4=CC=CC(O[C@H]5COCC5)=C43. InChi Code: InChI=1S/C23H32N2O6/c26-23(7-12-27-13-8-23)16-25-9-4-17(5-10-25)14-29-22-21-19(30-18-6-11-28-15-18)2-1-3-20(21)31-24-22/h1-3,17-18,26H,4-16H2/t18-/m1/s1. InChi Key: WLLOFQROROXOMO-GOSISDBHSA-N.