929221-88-5

929221-88-5 structure

Name: Rimonabant-d10
Chemical Name: 1H-Pyrazole-3-carboxamide, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1-piperidinyl-2,2,3,3,4,4,5,5,6,6-d10)
CAS Number: 929221-88-5
Molecular Formula: C₂₂H₁₁D₁₀Cl₃N₄O
Molecular Weight: 473.85
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2017-03-17 15:44:29
Modify Date: 2024-01-10 07:45:15
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

Name	1H-Pyrazole-3-carboxamide, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1-piperidinyl-2,2,3,3,4,4,5,5,6,6-d10)
Synonyms	rimonabant-d10

Description	Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Related Catalog	Research Areas >> Cancer Research Areas >> Infection Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor Signaling Pathways >> Anti-infection >> Bacterial
In Vitro	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Leite, C.E., et al. Rimonabant: An antagonist drug of the endocannabinoid system for the treatment of obesity. Pharmacol Rep 61 217-224 (2009). [3]. Seely KA, Brents LK, Franks LN, Rajasekaran M, Zimmerman SM, Fantegrossi WE, Prather PL.AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies.Neuropharmacology. 2012 Oct;63(5):905-15. [4]. Zhang B, et al. Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. Cell. 2019 Jan 24;176(3):636-648.e13. [5]. Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: Evidence from postmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268.

Molecular Formula	C₂₂H₁₁D₁₀Cl₃N₄O
Molecular Weight	473.85
Exact Mass	462.07800
PSA	50.16000
LogP	6.26740

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