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)
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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:
17 Citations: Showing 1 - 10
Glucose metabolism links astroglial mitochondria to cannabinoid effects.
Authors: Jimenez-Blasco Et al.
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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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.