| Bioactivity | 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist (Ki=31.2 nM) that displays 165-fold selectivity over CB1 receptors. 6-Iodopravadoline attenuates the ability of a number of cannabinoids to inhibit electrically-evoked twitches of the mouse isolated vas deferens[1][2]. | ||||||||||||
| Target | Ki: 31.2 nM (CB2) | ||||||||||||
| In Vivo | 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.; Swiss ICR mice) significantly reduces the time spent in the light box compared with vehicle group. 6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day; Swiss ICR mice) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used[3]. | ||||||||||||
| Name | 6-Iodopravadoline | ||||||||||||
| CAS | 164178-33-0 | ||||||||||||
| Formula | C23H25IN2O3 | ||||||||||||
| Molar Mass | 504.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Garcia-Gutierrez, Maria S., et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABAA receptors. British Journal of Pharmacology (2012), 165(4), 951-964. [2]. Pertwee R, et al. AM630, a competitive cannabinoid receptor antagonist. Life Sci. 1995;56(23-24):1949-1955. [3]. Ross RA, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630. Br J Pharmacol. 1999;126(3):665-672. |