Home GPCR & G Protein Cannabinoid Receptor antagonist AM251 For research use only.

AM251

AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.

AM251 Chemical Structure

AM251 Chemical Structure

CAS: 183232-66-8

Selleck's AM251 has been cited by 11 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S281901 DMSO] 40 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.02%
99.02

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Biological Activity

Description AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Features A selective cannabinoid 1 blocker.
Targets
CB1 [2]
In vitro
In vitro AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. [1] AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. [2]
In Vivo
In vivo AM251 causes a sustained reduction of daily food intake in the rat. [3] AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. [4] AM251 disrupts memory consolidation of the inhibitory avoidance task. [5] AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. [6] AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. [7]
Animal Research Animal Models Moderately obese male Lewis rats
Dosages 1.25 mg/kg, 2.5 mg/kg and 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 555.24 Formula

C22H21Cl2IN4O
CAS No. 183232-66-8 SDF Download AM251 SDF
Smiles CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (72.04 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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