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Technical Data
| Formula | C23H25IN2O3 |
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| Molecular Weight | 504.36 | CAS No. | 164178-33-0 | |
| Solubility (25°C)* | In vitro | DMSO | 50 mg/mL (99.13 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM. | ||
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| Targets |
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| 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] |
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| 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] |
Biological Activity
| Description | 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM. | ||
|---|---|---|---|
| Targets |
|
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| In vitro | AM630 is a CB2 cannabinoid receptor ligand with Ki of 31.2 nM and a CB2 /CB1 affinity ratio of 165. AM630 inhibits [35 S]-GTPγS binding to CB2 receptor membranes (EC50=76.6 nM), enhances forskolin-stimulated cyclic AMP production in CB2-transfected cells (5.2 fold by 1 μM ), and antagonizes the inhibition of forskolin-stimulated cyclic AMP production in this cell line induced by CP55940. AM630 (10 μM) inhibits forskolin-stimulated cyclic AMP production In CB1-transfected cells by 45.9%. [1] AM630 behaves as a competitive antagonist of △9-THC, CP 55,940, WIN 55212-2, anandamide and (R)-(+)-arachidonyl-l’-hydroxy-2’-propylamide (AM356) in mouse isolated vas deferens with Kd of 14.0, 17.3, 36.5, 278.8, and 85.9 nM, respectively. [2] AM630 ( 10 μM) activates a robust Ca2+ accumulation in a subset (35- 40%) of TG neurons, and with EC50 of 15.6 μM. AM630 are able to generate currents in TG sensory neurons with the activation threshold of 1 μM. AM630 responses are mediated by the TRPA1 channel in a majority of TG small-to-medium sensory neurons, which is modulated by TRPV1. Pre-treatment with AM630 (25 μM) is able to inhibits the Capsaicin (CAP) effects, mustard oil (MO) and WIN 55,212-2 (WIN) TRPA1 mediated responses. [3] AM630 (100 nM) effectively inhibits osteoclastogenesis in culture with RANKL in the presence and absence of Ti particles, as reducing the number of tartrate-resistant acid phosphatase-positive cells by more than 50%. AM630 (100 nM) inhibits mRNA expression of RANK and cathepsin K in RAW cells stimulated by Ti particles and RANKL. AM630 (100 nM) reduces protein expression of interleukin-1β and tumor necrosis factor-α in RAW cells cultured with Ti particles. AM630 has no toxic effect on RAW cells. [4] | ||
| In vivo | AM630 (30 μg) injection are not able to induce nociceptive behaviors or thermal hyperalgesia in hind paw of WT mice, but significantly attenuate CAP-induced thermal hyperalgesia. AM630 (30 μg) is able to reverse WIN inhibition CAP-induced thermal hyperalgesia. AM630 exerts its peripheral effects by not only inhibiting CB1 and CB2, but also activating TRPA1 channels and subsequently desensitizing TRPA1 as well as TRPV1 channels. [3] |
Protocol (from reference)
References
Selleck's 6-Iodopravadoline (AM630) has been cited by 2 publications
| CB2R activation ameliorates late adolescent chronic alcohol exposure-induced anxiety-like behaviors during withdrawal by preventing morphological changes and suppressing NLRP3 inflammasome activation in prefrontal cortex microglia in mice [ Brain Behav Immun, 2023, 110:60-79] | PubMed: 36754245 |
| Wwl70-induced ABHD6 inhibition attenuates memory deficits and pathological phenotypes in APPswe/PS1dE9 mice [ Pharmacol Res, 2023, 194:106864] | PubMed: 37480972 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.