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SR141716

Chemical Structure : SR141716

CAS No.: 168273-06-1

SR141716 (Rimonabant, SR141617, SR141716A)

Catalog No.: PC-22188Not For Human Use, Lab Use Only.

Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with Ki of 1.8 nM, no affinity for peripheral cannabinoid receptor.

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Biological Activity

Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with Ki of 1.8 nM, no affinity for peripheral cannabinoid receptor.
Rimonabant (SR141716) antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and dopamine-stimulated adenylyl cyclase activities in rat brain membranes.
After oral administration Rimonabant (SR141716) totally inhibited the ex vivo [3H]-CP55,940 binding to cerebral membranes with a ED50 value of 3.5 mg/kg.
Rimonabant (SR141716) antagonizes the classical pharmacological responses elicited by cannabinoid receptor agonists.
Rimonabant (SR141716) reverses the inhibitory effect of WIN55212-2 on isoniazid-induced elevation of cGMP in rat cerebellum.

Physicochemical Properties

M.Wt 463.79
Formula C22H21Cl3N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

References

1. Yaksh TL, et al. J Pharmacol Exp Ther. 2006 Jan;316(1):466-75.

2. Rinaldi-Carmona M, et al. FEBS Lett. 1994 Aug 22;350(2-3):240-4.

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