6-Iodopravadoline (AM630)

Catalog No.S8033

For research use only.

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

6-Iodopravadoline (AM630) Chemical Structure

CAS No. 164178-33-0

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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 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)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 504.36
Formula

C23H25IN2O3

CAS No. 164178-33-0
Storage 2 years -80 in solvent

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