SR 141716A

Cat. No. 0923

SR 141716A C22H21Cl3N4O.HCl [158681-13-1]

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Alternative Name: Rimonabant hydrochloride

Chemical Name: N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride

Biological Activity

Potent and selective cannabinoid CB1 receptor antagonist (Ki = 1.98 nM). Also acts as an inverse agonist reversing adenylyl cyclase inhibition by WIN 55,212-2 (Cat.No. 1038) (IC50 = 48 nM). Displays no activity at CB2 receptors. Reduces food intake and body weight in orally dosed non-obese Wistar rats.

Technical Data

M.Wt:
500.25
Formula:
C22H21Cl3N4O.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
158681-13-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Janiak et al (2007) Blockade of cannabinoid CB1 receptors improves renal function, metabolic profile, and increased survival of obese Zucker rats. Kidney Int. 72 1345. PMID: 17882151.

Colombo et al (1998) Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci. 63 113. PMID: 9718088.

Rinaldi-Carmona et al (1995) Biochemical and pharmacological characterisation of SR 141716A, the first potent and selective brain cannabinoid receptor antagonist. Life Sci. 56 1941. PMID: 7776817.

Rinaldi-Carmona et al (1994) SR 141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 350 240. PMID: 8070571.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SR 141716A include:

Klingerman et al (2016) Acute Metabolic Effects of Olanzapine Depend on Dose and Injection Site. Dose Response 13 1559325815618910. PMID: 26740814.

Mahmoud et al (2015) (4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs. Mol Pharmacol 87 197. PMID: 25411367.

Tang and Alger (2015) Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome. J Neurosci 35 3938. PMID: 25740522.

Marcu et al (2013) Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2. J Pharmacol Exp Ther 345 189. PMID: 23426954.

Sumislawski et al (2011) Reversible gating of endocannabinoid plasticity in the amygdala by chronic stress: a potential role for monoacylglycerol lipase inhibition in the prevention of stress-induced behavioral adaptation. Neuropsychopharmacology 36 2750. PMID: 21849983.

Kapur et al (2008) Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction. J Pharmacol Exp Ther 325 341. PMID: 18174385.

MacLennan et al (1998) Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors. Br J Pharmacol 124 619. PMID: 9690851.

Do you know of a great paper that uses SR 141716A from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: SR 141716A, supplier, SR141716A, rimonabant, cannabinoid, cb1, selective, potent, orally, available, inverse, agonists, antagonists, RIMO, Tocris Bioscience, CB1 Receptor Antagonist products

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