616201-89-9

Usage

Uses

Used in Pharmaceutical Industry:
1H-3-Benzazepine, 7-chloro-2,3,4,5-tetrahydro-1-methylis used as an impurity in Lorcaserin (L469890, HCl), a novel selective 5-HT2C-receptor agonist. The application reason for 1H-3-Benzazepine, 7-chloro-2,3,4,5-tetrahydro-1-methyl- is its role in the development and production of Lorcaserin, which is a medication designed for the treatment of obesity. By targeting the 5-HT2C receptor, Lorcaserin helps to regulate appetite and promote weight loss, making it a valuable tool in the fight against obesity.

Upstream product

• 34164-13-1 N-(3-chlorophenethyl)-2-chloropropanamide 
• 13078-79-0 2-(3-chlorophenyl)ethylamine 
• 849663-05-4 7-chloro-1-methyl-1,3,4,5-tetrahydro-benzo[d]azepin-2-one 

Relevant academic research and scientific papers

5ht2c receptor modulator compositions and methods of use

The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.

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

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 [3H]phosphoinositol turnover: 5-HT 2C = 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.

Discovery and SAR of new benzazepines as potent and selective 5-HT 2C receptor agonists for the treatment of obesity

We report on the synthesis, biological evaluation and structure-activity relationships for a series of 3-benzazepine derivatives as 5-HT2C receptor agonists. The compounds were evaluated in functional assays measuring [3H] phosphoinositol turnover in HEK-293 cells transiently transfected with h5-HT2C, h5-HT2A or h5-HT2B receptors. Several compounds are shown to be potent and selective 5-HT 2C receptor agonists, which decrease food intake in a rat feeding model.

5HT2c receptor modulators

The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.