6-Iodopravadoline (AM630)

For research use only.

Catalog No.S8033

6-Iodopravadoline (AM630) Chemical Structure

CAS No. 164178-33-0

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

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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

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]

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]

Protocol

Cell Research:

[2]

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  • 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).


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: male Swiss ICR mice, DBA/2 Ola Hs mice
  • Dosages: 1 mg/kg, 2 mg/kg, 3 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (99.13 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 504.36
Formula

C23H25IN2O3

CAS No. 164178-33-0
Storage 2 years -80 in solvent
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID