Catalog Number: 0923
Alternate Names: 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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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.
Background References
  1. Appetite suppression and weight loss after the cannabinoid antagonist SR 141716.
    Colombo et al.
    Life Sci., 1998;63:113
  2. Blockade of cannabinoid CB1 receptors improves renal function, metabolic profile, and increased survival of obese Zucker rats.
    Janiak et al.
    Kidney Int., 2007;72:1345
  3. SR 141716A, a potent and selective antagonist of the brain cannabinoid receptor.
    Rinaldi-Carmona et al.
    FEBS Lett., 1994;350:240
  4. Biochemical and pharmacological characterisation of SR 141716A, the first potent and selective brain cannabinoid receptor antagonist.
    Rinaldi-Carmona et al.
    Life Sci., 1995;56:1941

The citations listed below are publications that use Tocris products. Selected citations for SR 141716A include:

Showing Results 1 - 9 of 9

  1. Acute Metabolic Effects of Olanzapine Depend on Dose and Injection Site.
    Authors: Klingerman Et al.
    Dose Response
  2. (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.
    Authors: Mahmoud Et al.
    Mol Pharmacol
  3. Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome.
    Authors: Tang and Alger
    J Neurosci
  4. Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2.
    Authors: Marcu Et al.
    J Pharmacol Exp Ther
  5. 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.
    Authors: Sumislawski Et al.
  6. Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction.
    Authors: Kapur Et al.
    J Pharmacol Exp Ther
  7. 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.
    Authors: Graham Et al.
    Br J Pharmacol
  8. Effects of cannabinoid receptor agonists on neuronally-evoked contractions of urinary bladder tissues isolated from rat, mouse, pig, dog, monkey and human.
    Authors: Martin Et al.
    Front Mol Neurosci
  9. Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors.
    Authors: MacLennan Et al.
    Br J Pharmacol
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