SR 141716A

Pricing Availability   Qty
Description: Selective CB1 inverse agonist
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)
Citations (18)
Reviews (2)
Literature (2)

Biological Activity for SR 141716A

SR 141716A is a 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. Also μ-opioid receptor antagonist (Ki = 652 nm)

Technical Data for SR 141716A

M. Wt 500.25
Formula C22H21Cl3N4O.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 158681-13-1
PubChem ID 104849
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SR 141716A

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

Preparing Stock Solutions for SR 141716A

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

Select a batch to recalculate based on the batch molecular weight:
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 for SR 141716A

Certificate of Analysis / Product Datasheet
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References for SR 141716A

References are publications that support the biological activity of the product.

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

Seely et al (2012) AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies. Neuropharmacology 63 905 PMID: 22771770

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

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Keywords: SR 141716A, SR 141716A supplier, SR141716A, rimonabant, cannabinoid, cb1, selective, potent, orally, available, inverse, agonists, antagonists, RIMO, Rimonabant, hydrochloride, CB1, Receptors, 0923, Tocris Bioscience

18 Citations for SR 141716A

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

Jimenez-Blasco et al (2020) Glucose metabolism links astroglial mitochondria to cannabinoid effects. Nature 583 603 PMID: 32641832

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

Pedersen et al (2021) A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors J Biol Chem 296 100503 PMID: 33684444

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

Cecconi et al (2019) Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation. Int J Mol Sci 20 PMID: 31212770

Jiang et al (2017) Antidepressant-like effects of fenofi. in mice via the hippocampal brain-derived neurotrophic factor signalling pathway. Br J Pharmacol 174 177 PMID: 27861729

Khan et al (2018) Involvement of the CB2 cannabinoid receptor in cell growth inhibition and G0/G1 cell cycle arrest via the cannabinoid agonist WIN 55,212-2 in renal cell carcinoma. BMC Cancer 18 583 PMID: 29792186

Hayase (2016) Putative Epigenetic Involvement of the Endocannabinoid System in Anxiety- and Depression-Related Behaviors Caused by Nicotine as a Stressor. PLoS One 11 e0158950 PMID: 27404492

Bruijnzeel et al (2016) Behavioral Characterization of the Effects of Cannabis Smoke and Anandamide in Rats. PLoS One 11 e0153327 PMID: 27065006

Klingerman et al (2016) Acute Metabolic Effects of olanz. 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

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

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

Stanford et al (2001) Identification of two distinct vasodilator pathways activated by ATP in the mesenteric bed of the rat. Br J Pharmacol 133 825 PMID: 11454655

Kettunen et al (2005) Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network. Neuron 45 95 PMID: 15629705

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

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

Reviews for SR 141716A

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Rimonabant treatment in mice.
By Sebastiaan Dalle on 05/24/2023
Assay Type: In Vivo
Species: Mouse

10mg/kg body weight, dissolved in solution with 6.7% dmso, 1.7% tween80 and 91.6% saline; intraperitoneally injected.

Rimonabant stock was prepared in dmso and tween80, and consequently freshly diluted with saline.

review image

Highly recommend..
By Anonymous on 06/01/2020
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Bed nucleus of the stria terminalis

SR 141716A was solubilized in DMSO and bath applied at a 5 micromolar concentration. It effectively blocked CB1-receptor-dependent long term depression of evoked excitatory postsynaptic current in the bed nucleus of the stria terminalis.

PMID: 27956747
review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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