1443990-85-9

Basic information

• Product Name: 2-(2-(4-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamido)piperidin-1-yl)-2-oxoethoxy)acetic acid
• Synonyms: 2-(2-(4-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamido)piperidin-1-yl)-2-oxoethoxy)acetic acid
• CAS NO: 1443990-85-9
• Molecular Weight: 579.867
• Mol File: 1443990-85-9.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 2-(2-(4-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamido)piperidin-1-yl)-2-oxoethoxy)acetic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(2-(4-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamido)piperidin-1-yl)-2-oxoethoxy)acetic acid(1443990-85-9)
• EPA Substance Registry System: 2-(2-(4-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamido)piperidin-1-yl)-2-oxoethoxy)acetic acid(1443990-85-9)

Safety Data

• Hazardous Substances Data: 1443990-85-9(Hazardous Substances Data)

Upstream product

• 1365037-83-7 tert-butyl 4-[5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-amido]piperidine-1-carboxylate 
• 168273-05-0 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carbonyl chloride 
• 4480-83-5 1,4-dioxane-2,6-dione 
• 1365037-86-0 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide 
• 162758-35-2 rimonabant acid 

Downstream Products

• 1443990-82-6 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1-(3,7,14-trioxo-5,16-dioxa-2,8,13-triazaoctadecan-18-oyl)piperidin-4-yl)-1H-pyrazole-3-carboxamide 
• 1443990-79-1 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(1-(14-(((4αS,7S,7αR,12βS)-4α,9-dihydroxy-3-methyl-2,3,4,4α,5,6,7,7α-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)amino)-5,10,14-trioxo-3,12-dioxa-6,9-diazatetradecan-1-oyl)piperidin-4-yl)-4-methyl-1H-pyrazole-3-carboxamide 
• 1443990-80-4 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(1-(18-(((4αS,7-S,7αR,12βS)-4α,9-dihydroxy-3-methyl-2,3,4,4α,5,6,7,7α-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)amino)-5,14,18-trioxo-3,16-dioxa-6,13-diazaoctadecan-1-oyl)piperidin-4-yl)-4-methyl-1H-pyrazole-3-carboxamide 
• 1443990-81-5 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(1-(19-(((4αS,7S,7αR,12βS)-4α,9-dihydroxy-3-methyl-2,3,4,4α,5,6,7,7α-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)amino)-5,15,19-trioxo-3,17-dioxa-6,14-diazanonadecan-1-oyl)piperidin-4-yl)-4-methyl-1H-pyrazole-3-carboxamide 
• 1443990-78-0 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(1-(2-(2-(((4αS,7S,7αR,12βS)-4α,9-dihydroxy-3-methyl-2,3,4,4α,5,6,7,7α-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)amino)-2-oxoethoxy)acetyl)piperidin-4-yl)-4-methyl-1H-pyrazole-3-carboxamide 

Relevant articles and documents

Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB 1) receptors are potent analgesics devoid of tolerance

Given that μ opioid (MOP) and canabinoid (CB1) receptors are colocalized in various regions of the central nervous system and have been reported to associate as heteromer (MOP-CB1) in cultured cells, the possibility of functional, endogenous MOP-CB1 in nociception and other pharmacologic effects has been raised. As a first step in investigating this possibility, we have synthesized a series of bivalent ligands 1-5 that contain both μ agonist and CB1 antagonist pharmacophores for use as tools to study the functional interaction between MOP and CB1 receptors in vivo. Immunofluorescent studies on HEK293 cells coexpressing both receptors suggested 5 (20-atom spacer) to be the only member of the series that bridges the protomers of the heteromer. Antinociceptive testing in mice revealed 5 to be the most potent member of the series. As neither a mixture of monovalent ligands 9 + 10 nor bivalents 2-5 produced tolerance in mice, MOR-CB1 apparently is not an important target for reducing tolerance.