Product overview
Name | AM251 |
Description | Potent, selective CB1 receptor antagonist / inverse agonist |
Purity | >98% |
Customer comments | 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 |
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Biological Data
Biological description | AM251 is a potent and selective prototypic cannabinoid 1 receptor (CB1) antagonist / inverse agonist (IC50 = 8 nM and Ki = 7.49 nM).
AM251 attenuates responses to established cannabinoid receptor agonists in vitro or in vivo.
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Solubility & Handling
Storage instructions | Room temperature |
Solubility overview | Soluble in DMSO (100 mM) and in ethanol (25 mM) |
Handling | This compound is light sensitive; we therefore recommend protecting the solid material and solutions from exposure to light.
We therefore recommend:
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Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
Chemical name | N-(Piperidin-1-yl)-5-(4-iodophenyl) -1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-car boxamide |
Molecular Weight | 555.24 |
Chemical structure | |
Molecular Formula | C22H21Cl2IN4O |
CAS Number | 183232-66-8 |
PubChem identifier | 2125 |
SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I |
Source | Synthetic |
InChi | InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
InChiKey | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
MDL number | MFCD01861181 |
Appearance | White solid |
References for AM251
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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) : 905-15 -
The cannabinoid CB1 receptor antagonists SR141716 and AM251 directly potentiate GABA(A) receptors.
Baur et al (2012) Br J Pharmacol 165(8) : 2479-84 -
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) : 1735-45 -
The orphan receptor GPR55 is a novel cannabinoid receptor.
Ryberg et al (2007) Br J Pharmacol 152(7) : 1092-101. -
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
Lan et al (1999) J Med Chem 42(4) : 769-76
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Activity-Dependent Modulation of Tonic GABA Currents by Endocannabinoids in Hirudo verbana
Paulsen RT et al (2022) Front Synaptic Neurosci 14 : 760330PubMedID: 35368247 -
Differential regulation of prelimbic and thalamic transmission to the basolateral amygdala by acetylcholine receptors
Mott et al (2021) bioRxiv https://doi.org/10.1101/2021.12.28.474396 : doi -
Differential regulation of prelimbic and thalamic transmission to the basolateral amygdala by acetylcholine receptors
Tryon et al (2019) University of Columbia : Thesis