304008-29-5

Usage

Uses

Used in Pharmaceutical Industry:
N-[[trans-4-[(4,5-Dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]methanesulfonamide is used as a neuropeptide Y Y5 receptor antagonist for its potential anxiolyticand antidepressant-like effects in mammalian models. This application is based on its ability to modulate the neuropeptide Y system, which is involved in the regulation of mood and anxiety.
Used in Research and Development:
In addition to its potential therapeutic applications, N-[[trans-4-[(4,5-Dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]methanesulfonamide may also be used in research and development for the study of neuropeptide Y receptors and their role in mood disorders. This can contribute to the development of new drugs and therapies for the treatment of anxiety and depression.

Upstream product

• 108-98-5 thiophenol 
• 21609-70-1 3,4-dihydro-2H-benzo[b]thiepin-5-one 
• 17742-51-7 4-phenylsulfanyl-butyric acid 
• 124-63-0 methanesulfonyl chloride 
• 866548-92-7 tert-butyl ((trans-1,4)-4-aminocyclohexyl)methylcarbamate 
• 21609-66-5 4-bromo-2,3-dihydro-1-benzothiepin-5(4H)-one 

Relevant academic research and scientific papers

Discovery of Lu AA33810: A highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder

The structure-activity relationship of a series of tricyclic-sulfonamide compounds 11-32 culminating in the discovery of N-[trans-4-(4,5-dihydro-3,6- dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmethyl]-methanesulfonamide (15, Lu AA33810) is reported. Compound 15 was identified as a selective and high affinity NPY5 antagonist with good oral bioavailability in mice (42%) and rats (92%). Dose dependent inhibition of feeding was observed after i.c.v. injection of the selective NPY5 agonist ([cPP1-7,NPY19-23,Ala 31,Aib32,Gln34]-hPP). In addition, ip administration of Lu AA33810 (10 mg/kg) produced antidepressant-like effects in a rat model of chronic mild stress.

Selective NPY (Y5) antagonists (tricyclics)

This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.