1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE

Description

AM281 is a potent and selective central cannabinoid (CB₁) receptor antagonist/inverse agonist (K_is = 12 nM and 4,200 nM for CB₁ and CB₂, respectively). Structurally, it is an analog of the CB₁ inverse agonist rimonabant . It has no effect on the vanilloid TRPV1 receptor. AM281 has been used to evaluate the potential effects of compounds at CB₁. It has also been used to study the membrane localization and cycling of CB₁.

Uses

AM 281 acts as a potential CB1 selective receptor cannabinoid antagonist.

Definition

ChEBI: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(4-morpholinyl)-3-pyrazolecarboxamide is a member of pyrazoles and a ring assembly.

Biological Activity

Potent, selective CB 1 cannabinoid receptor antagonist/inverse agonist (K i values are 12 and 4200 nM for CB 1 and CB 2 receptors respectively). Increases locomotor activity following systemic administration in vivo . Analog of SR141716A (K i = 14 nM).

storage

+4°C (desiccate)

References

[1]. lan r, gatley j, lu q, et al. design and synthesis of the cb1 selective cannabinoid antagonist am281: a potential human spect ligand. aaps pharmsci, 1999, 1(2): e4.
[2]. gatley sj, lan r, volkow nd, et al. imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid cb1 receptors in vivo. j neurochem, 1998, 70(1): 417-423.
[3]. vaseghi g, rabbani m, hajhashemi v. the cb(1) receptor antagonist, am281, improves recognition loss induced by naloxone in morphine withdrawal mice. basic clin pharmacol toxicol, 2012, 111(3): 161-165.