6-Iodopravadoline 是大麻素类CB2受体拮抗剂，其Ki=31.2 nM，选择性是 CB1 受体的 165 倍。它减弱了许多大麻素抑制小鼠离体输精管电诱发抽搐的能力。

6-Iodopravadoline is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.

6-Iodopravadoline is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). 6-Iodopravadoline (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner[3]. 6-Iodopravadoline (1 μM) blocks the CP-55,940 dose response with EC50 of 170 nM at human and EC50 of 110 nM at rat cannabinoid CB2 receptor[4]. The AM251 and 6-Iodopravadoline (AM630)-evoked Ca2+?influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC50 for AM251 and 6-Iodopravadoline are 7.37 μM and 15.6 μM, respectively. AM251 and 6-Iodopravadoline activate TRPA1 in TG sensory neurons. AM251 and 6-Iodopravadoline activation of TRPA1 is modulated by TRPV1[2]. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells.

6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used[1]. 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box, compared with vehicle group.

164178-33-0

C23H25IN2O3

504.36

AM630;[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮

DMSO:50 mg/mL (99.14 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years