Potent, selective CB1 receptor antagonist / inverse agonist
AM251 is a potent and selective prototypic cannabinoid 1 receptor (CB1) antagonist / inverse agonist (IC50 = 8 nM and Ki = 7.49 nM).
AM251 shows ~306-fold selectivity over CB2 receptors. Structural analog of SR141716A.
Also acts as a potent GPR55 orphan receptor agonist (EC50 = 39 nM) and shows activity at the µ-opioid receptor (MOR) (Ki = 251 nM). Additionally, directly potentiates GABAA receptors.
AM251 attenuates responses to established cannabinoid receptor agonists in vitro or in vivo.
Blocks heterosynaptic long term depression (LTD).
It (AM251) works - bang for your buck! Works as described! Great technical support. Verified customer, UC Denver
Another quality product from Hello Bio - AM251 works as expected in our experiments and at a good price as well. We always order with confidence from Hello Bio, and are often surprised at how quickly we receive our products. Verified customer, University of South Carolina
N-(Piperidin-1-yl)-5-(4-iodophenyl) -1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-car boxamide
Storing and Using Your Product
Soluble in DMSO (100 mM) and in ethanol (25 mM)
This compound is light sensitive; we therefore recommend protecting the solid material and solutions from exposure to light.
Ongoing solubility of AM251 in aqueous solutions can be unpredictable and the compound can precipitate out of solution.
We therefore recommend:
- If possible, make up solutions and use immediately. Do not store solutions.
- When creating your stock solutions, ensure the compound is fully dissolved in DMSO (use heat to achieve this if necessary).
- Heat DMSO stock solution prior to addition to ACSF
- Heat your ACSF solution to ~42°C before addition of AM251.
- Mix the compound with ACSF immediately before use
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References for AM251
AM-251 and SR141716 act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.Seely et al (2012) Neuropharmacology 63(5) : 905-15PubMedID: 22771770
Cannabinoid CB1 receptor antagonists attenuate cocaine's rewarding effects: experiments with self-administration and brain-stimulation reward in rats.Xi et al (2008) Neuropsychopharmacology 33(7) : 1735-45PubMedID: 17728698
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.Lan et al (1999) J Med Chem 42(4) : 769-76PubMedID: 10052983
The orphan receptor GPR55 is a novel cannabinoid receptor.Ryberg et al (2007) Br J Pharmacol 152(7) : 1092-101.PubMedID: 17876302
The cannabinoid CB1 receptor antagonists SR141716 and AM251 directly potentiate GABA(A) receptors.Baur et al (2012) Br J Pharmacol 165(8) : 2479-84PubMedID: 21470203
Reviews & Product Guides
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Another quality product from Hello Bio - AM251 works as expected in our experiments and at a good price as well. We always order with confidence from Hello Bio, and are often surprised at how quickly we receive our products.
It (AM 251) works - bang for your buck! Works as described! Great technical support.