SR 141716A

Pricing Availability Delivery Time Qty
Cat.No. 0923 - SR 141716A | C22H21Cl3N4O.HCl | CAS No. 158681-13-1
Description: Selective CB1 receptor antagonist
Alternative Names: Rimonabant hydrochloride
Chemical Name: N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (9)
Literature

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
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 158681-13-1
PubChem ID 104849
InChI Key REOYOKXLUFHOBV-UHFFFAOYSA-N
Smiles O=C(NN4CCCCC4)C1=NN(C3=CC=C(Cl)C=C3Cl)C(C2=CC=C(Cl)C=C2)=C1C.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.02 100

Preparing Stock Solutions

The following data is based on the product molecular weight 500.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2 mL 10 mL 19.99 mL
5 mM 0.4 mL 2 mL 4 mL
10 mM 0.2 mL 1 mL 2 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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

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


If you know of a relevant reference for SR 141716A, please let us know.

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9 Citations for SR 141716A

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

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

Graham et al (2006) Induction of Krox-24 by endogenous cannabinoid type 1 receptors in Neuro2A cells is mediated by the MEK-ERK MAPK pathway and is suppressed by the phosphatidylinositol 3-kinase pathway. Br J Pharmacol 281 29085 PMID: 16864584

Martin et al (2000) Effects of cannabinoid receptor agonists on neuronally-evoked contractions of urinary bladder tissues isolated from rat, mouse, pig, dog, monkey and human. Front Mol Neurosci 129 1707 PMID: 10780977

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

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


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

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