PF-04781340 TFA is a potent and selective 5-HT 2 C receptor agonist, with an EC 50 of 9 nM and a K i of 3 nM, respectively. PF-04781340 TFA exhibits weak partial agonist activity at the 5-HT 2 B receptor, with an EC 50 of 1484 nM. PF-04781340 TFA can be used in the research of obesity and psychiatric disorders [1].
In Vitro, PF-04781340 TFA exhibits metabolic stability in human liver microsomes, with a CLint of 19 mL/min/mg[1]. PF-04781340 TFA exhibits moderate passive permeability in RRCK cells, with a Papp value of 8 × 10-6 cm/s[1]. PF-04781340 TFA exhibits a low P-gp efflux ratio of only 2.8 in MDCK-MDR1 cells, indicating a reduced risk of efflux from the central nervous system[1].
References:
[1]. Rouquet G, et al. Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. ACS medicinal chemistry letters. 2015 Mar 12;6(3):329-33.
In Vitro, PF-04781340 TFA exhibits metabolic stability in human liver microsomes, with a CLint of 19 mL/min/mg[1]. PF-04781340 TFA exhibits moderate passive permeability in RRCK cells, with a Papp value of 8 × 10-6 cm/s[1]. PF-04781340 TFA exhibits a low P-gp efflux ratio of only 2.8 in MDCK-MDR1 cells, indicating a reduced risk of efflux from the central nervous system[1].
References:
[1]. Rouquet G, et al. Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. ACS medicinal chemistry letters. 2015 Mar 12;6(3):329-33.