Home / Cannabinoid R1 / CB1 Inverse Agonists / SR 141716A

SR 141716A

Catalog #: 0923
18 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
0923/10
SR 141716A | CAS No. 158681-13-1 | Cannabinoid R1 / CB1 Inverse Agonists
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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%

Product Details
Citations (18)
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Biological Activity

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

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

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Citations for SR 141716A

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

18 Citations: Showing 1 - 10

  1. A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors
    Authors: Pedersen Et al.
    J Biol Chem  2021;296:100503
  2. Glucose metabolism links astroglial mitochondria to cannabinoid effects.
    Authors: Jimenez-Blasco Et al.
    Nature  2020;583:603
  3. Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation.
    Authors: Cecconi Et al.
    Int J Mol Sci  2019;20
  4. 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.
    Authors: Khan Et al.
    BMC Cancer  2018;18:583
  5. Antidepressant-like effects of fenofi. in mice via the hippocampal brain-derived neurotrophic factor signalling pathway.
    Authors: Jiang Et al.
    Br J Pharmacol  2017;174:177
  6. Acute Metabolic Effects of olanz. Depend on Dose and Injection Site.
    Authors: Klingerman Et al.
    Dose Response  2016;13:1559325815618910
  7. Putative Epigenetic Involvement of the Endocannabinoid System in Anxiety- and Depression-Related Behaviors Caused by Nicotine as a Stressor.
    Authors: Hayase
    PLoS One  2016;11:e0158950
  8. Behavioral Characterization of the Effects of Cannabis Smoke and Anandamide in Rats.
    Authors: Bruijnzeel Et al.
    PLoS One  2016;11:e0153327
  9. (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  2015;87:197
  10. 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  2015;35:3938
  11. 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  2013;345:189
  12. 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.
    Neuropsychopharmacology  2011;36:2750
  13. Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction.
    Authors: Kapur Et al.
    J Pharmacol Exp Ther  2008;325:341
  14. 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  2006;281:29085
  15. Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network.
    Authors: Kettunen Et al.
    Neuron  2005;45:95
  16. Identification of two distinct vasodilator pathways activated by ATP in the mesenteric bed of the rat.
    Authors: Stanford Et al.
    Br J Pharmacol  2001;133:825
  17. 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  2000;129:1707
  18. Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors.
    Authors: MacLennan Et al.
    Br J Pharmacol  1998;124:619

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