Compounds > inositol-1-4-5-trisphosphate

inositol-1-4-5-trisphosphate and Weight-Gain

inositol-1-4-5-trisphosphate has been researched along with Weight-Gain* in 1 studies

Other Studies

1 other study(ies) available for inositol-1-4-5-trisphosphate and Weight-Gain

Article	Year
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. Journal of medicinal chemistry, 2008, Jan-24, Volume: 51, Issue:2 The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosphoinositol turnover: 5-HT2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). Lorcaserin was further characterized in a single-dose pharmacokinetic study in rat (t1/2 = 3.7 h; F = 86%) and a 28-day model of weight gain in growing Sprague-Dawley rat (8.5% decrease in weight gain observed at 36 mg/kg b.i.d.). Lorcaserin was selected for further evaluation in clinical trials for the treatment of obesity. Topics: Animals; Anti-Obesity Agents; Benzazepines; Cell Line; Eating; Humans; Inositol 1,4,5-Trisphosphate; Male; Obesity; Rats; Rats, Sprague-Dawley; Serotonin 5-HT2 Receptor Agonists; Stereoisomerism; Structure-Activity Relationship; Weight Gain	2008

Article

Year

Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.

Journal of medicinal chemistry, 2008, Jan-24, Volume: 51, Issue:2

The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosphoinositol turnover: 5-HT2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). Lorcaserin was further characterized in a single-dose pharmacokinetic study in rat (t1/2 = 3.7 h; F = 86%) and a 28-day model of weight gain in growing Sprague-Dawley rat (8.5% decrease in weight gain observed at 36 mg/kg b.i.d.). Lorcaserin was selected for further evaluation in clinical trials for the treatment of obesity.

Topics: Animals; Anti-Obesity Agents; Benzazepines; Cell Line; Eating; Humans; Inositol 1,4,5-Trisphosphate; Male; Obesity; Rats; Rats, Sprague-Dawley; Serotonin 5-HT2 Receptor Agonists; Stereoisomerism; Structure-Activity Relationship; Weight Gain

2008