E-6837

E-6837

Names
IUPAC name 5-chloro-N-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)naphthalene-2-sulfonamide
Identifiers
Properties
Chemical formula	C22H22ClN3O2S
Molar mass	427.95 g/mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

E-6837 is an orally active, 5-HT₆ agonist developed in an attempt to create an anti-obesity medication. In cell lines expressing rat 5-HT₆ receptors, it acted as a partial agonist (on presumed silent receptors), while it acted as a full agonist on human 5-HT₆ receptors (which are constitutively active). Oral administration of E-6837 reduced food intake, but only transiently. In rats, twice daily administration of E-6837 over the course of 4 weeks resulted in a 15.7% reduction in body weight, compared to 11% reduction for sibutramine. This weight loss remained significant for E-6837 after a 43-day withdrawal period, whereas the weight difference was non-significant for sibutramine (i.e., sibutramine had a rebound effect while E-6837 did not), and this weight loss was found to be due to a loss of fat mass. The reduction in fat mass in E-6837 treated animals was associated with a 50% decrease in plasma leptin levels, and also reduced glucose and insulin levels in plasma after a glucose tolerance test. This indicates that weight loss from E-6837 is associated with improved insulin sensitivity, and thus, better glycemic control.^{[1] [2] [3]}

One proposed mechanism of action is that E-6837 acts on neurons in the hypothalamus, which has shown significant levels of 5-HT₆ receptor mRNA. The hypothalamus is one key structure involved in regulating food intake.^[1]

See also

• E-6801

References