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E-6837

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Title: E-6837  
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Subject: 5-HT6 receptor, RS-56812, MPPF, BRL-54443, 6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide
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E-6837

E-6837
Properties
Molecular formula C22H22ClN3O2S
Molar mass 427.95 g/mol
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)

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

References

  1. ^ a b Fisas, Angels (August 2006). "Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats".  
  2. ^ Kirkpatrick, Peter (1 August 2006). "Anti-obesity drugs: Fighting fat". Nature Reviews Drug Discovery 5 (8): 634–634.  
  3. ^ Garfield, A. S.; Heisler, L. K. (24 November 2008). "Pharmacological targeting of the serotonergic system for the treatment of obesity". The Journal of Physiology 587 (1): 49–60.  


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