Home GPCR & G Protein Cannabinoid Receptor antagonist 6-Iodopravadoline (AM630) For research use only.

6-Iodopravadoline (AM630)

6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.

6-Iodopravadoline (AM630) Chemical Structure

6-Iodopravadoline (AM630) Chemical Structure

CAS No. 164178-33-0

Purity & Quality Control

Batch: S803301 DMSO]50 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.87%
99.87

6-Iodopravadoline (AM630) Related Products

Signaling Pathway

Cannabinoid Receptor Signaling Pathways

Cannabinoid Receptor Signaling Pathway

Biological Activity

Description 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Targets
CB2 receptor [1]
(Cell-free assay)
31.2 nM(Ki)
In vitro
In vitro

AM630 behaves as a low-potency neutral competitive antagonist in AM630-pre-incubated cells, a low-potency agonist in SR144528-pre-incubated cells, and a much higher-potency inverse agonist/antagonist in vehicle-pre-incubated cells. AM630 is a protean ligand that can target a constitutively active form of the hCB2 receptor with low affinity to produce agonism or neutral antagonism and a constitutively inactive form of this receptor with much higher affinity to produce inverse agonism.[2]
Cell Research Cell lines CHO cells
Concentrations 10 μM
Incubation Time 24 h
Method

Binding assays with [3H]-CP55940 or [35S]-GTPγS are performed with hCB2 CHO cell membranes. The hCB2 CHO cells are pre-incubated in complete medium with 10 μM AM630 or vehicle (dimethyl sulphoxide) for up to 24 h and then subjected to intense washing. For membrane preparation, cells are removed from flasks by scraping, centrifuged at 489× g and then frozen as a pellet at −20°C until required. Before use in a radioligand binding assay, cells are defrosted and diluted in Tris binding buffer (radioligand displacement assay) or GTPγS binding buffer ([35S]-GTPγS binding assay).
In Vivo
In vivo

Chronic AM630 treatment is anxiolytic in light-dark box (LDB) and elevated plus maze (EPM) tests. Chronic AM630 treatment increases gene and reduces protein expression of CB2 receptors, GABAAα2 and GABAAγ2 in cortex and amygdala. In addition, chronic AM630 administration decreases the anxiety of DBA/2 mice in the LDB test. The efficacy of AM630 in reducing the anxiety of the spontaneously anxious DBA/2 strain of mice strengthens the potential of the CB2 receptor as a new target in the treatment of anxiety-related disorders.[1]
Animal Research Animal Models male Swiss ICR mice, DBA/2 Ola Hs mice
Dosages 1 mg/kg, 2 mg/kg, 3 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 504.36 Formula

C23H25IN2O3
CAS No. 164178-33-0 SDF --
Smiles COC1=CC=C(C=C1)C(=O)C2=C(C)[N](CCN3CCOCC3)C4=C2C=CC(=C4)I
Storage (From the date of receipt) 3 years-21°C powder

In vitro
Batch:

DMSO : 50 mg/mL ( (99.13 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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