Chemical Name: N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride
Biological ActivityPotent 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)
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.
Appetite suppression and weight loss after the cannabinoid antagonist SR 141716.
Colombo et al.
Life Sci., 1998;63:113
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
SR 141716A, a potent and selective antagonist of the brain cannabinoid receptor.
Rinaldi-Carmona et al.
FEBS Lett., 1994;350:240
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
AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.
Seely et al.
Citations for SR 141716A
The citations listed below are publications that use Tocris products. Selected citations for SR 141716A include:
16 Citations: Showing 1 - 10
Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation.
Authors: Cecconi Et al.
Int J Mol Sci 2019;20
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
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
Acute Metabolic Effects of olanz. Depend on Dose and Injection Site.
Authors: Klingerman Et al.
Dose Response 2016;13:1559325815618910
Putative Epigenetic Involvement of the Endocannabinoid System in Anxiety- and Depression-Related Behaviors Caused by Nicotine as a Stressor.
PLoS One 2016;11:e0158950
Behavioral Characterization of the Effects of Cannabis Smoke and Anandamide in Rats.
Authors: Bruijnzeel Et al.
PLoS One 2016;11:e0153327
(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
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
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
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.
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
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
Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network.
Authors: Kettunen Et al.
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
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
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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