Home GPCR & G Protein Cannabinoid Receptor antagonist 6-Iodopravadoline (AM630)

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6-Iodopravadoline (AM630) Cannabinoid Receptor antagonist

Cat.No.S8033

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

Chemical Structure

Molecular Weight: 504.36

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

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (99.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 504.36 Formula

C23H25IN2O3

 Storage (From the date of receipt) 3 years-21°C powder
CAS No. 164178-33-0 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC=C(C=C1)C(=O)C2=C(C)[N](CCN3CCOCC3)C4=C2C=CC(=C4)I

Mechanism of Action

Targets/IC50/Ki
CB2 receptor
(Cell-free assay)
31.2 nM(Ki)
In vitro
AM630 (6-Iodopravadoline) is a CB2 cannabinoid receptor ligand with Ki of 31.2 nM and a CB2 /CB1 affinity ratio of 165. It 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. This compound (10 μM) inhibits forskolin-stimulated cyclic AMP production In CB1-transfected cells by 45.9%. It 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. At 10 μM, it activates a robust Ca2+ accumulation in a subset (35- 40%) of TG neurons, and with EC50 of 15.6 μM. This compound is able to generate currents in TG sensory neurons with the activation threshold of 1 μM. Its 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. At 100 nM, it 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%. This compound (100 nM) inhibits mRNA expression of RANK and cathepsin K in RAW cells stimulated by Ti particles and RANKL. It (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.
In vivo
6-Iodopravadoline (AM630) (30 μg) injection is not able to induce nociceptive behaviors or thermal hyperalgesia in hind paw of WT mice, but significantly attenuates CAP-induced thermal hyperalgesia. This compound (30 μg) is able to reverse WIN inhibition of CAP-induced thermal hyperalgesia. It 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/20623669/

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