E-6837

E-6837 is a selective and orally active 5-HT₆ receptor ligand. E-6837 demonstrates partial agonism at a presumably silent rat 5-HT₆ receptor and full agonism at a constitutively active human 5-HT₆ receptor by monitoring the cAMP signaling pathway. E-6837 induces hypophagia, reduces fat mass and body weight, and improves glycemic control. E-6837 can be used for the research of obesity^[1]. In Vitro:E-6837 binds selectively and with high affinity (pK_i = 9.13 ± 0.17) to the recombinant human 5-HT₆ receptor in HEK-293 membrane preparations^[1].
E-6837 acts as a potent partial agonist (E_max = 67 ± 4%, pEC₅₀ = 9.19 ± 0.11) and partial antagonist (I_max = 41 ± 3%, pIC₅₀ = 8.37 ± 0.09) at the presumably silent rat 5-HT₆ receptor stably expressed in HEK-293F cells^[1].
E-6837 acts as a potent, nearly full agonist (E_max = 96 ± 4%, pEC₅₀ = 9.53 ± 0.09) at the constitutively active human 5-HT₆ receptor stably expressed in HEK-293F cells^[1]. In Vivo:E-6837 (5-30 mg/kg; p.o.; single dose) induces transient, 6-hour suppression of food intake in male Sprague-Dawley rats at 30 mg/kg, while 5 mg/kg has no effect on feeding^[1].
E-6837 (60 mg/kg; p.o.; single dose) does not induce conditioned taste aversion or kaolin consumption in male Sprague-Dawley rats, indicating no emetic or aversive effects at these doses^[1].
E-6837 (30 mg/kg; p.o.; twice daily; 28 days) induces a maximal 15.7% body weight loss in diet-induced obese female Wistar rats^[1].