AM281

AM281 is a potent and selective cannabinoid receptor 1 (CB1) antagonist and inverse agonist (Ki = 12 nM). Structurally related to rimonabant (SR141716A), it exhibits high selectivity for CB1 over CB2 receptors (Ki = 4,200 nM). AM281 was originally synthesized at the University of Connecticut as a potential single-photon emission computed tomography (SPECT) imaging agent when radiolabeled with iodine-123 ([123I]AM281). While it has been evaluated in pilot human neuroimaging studies for conditions such as Tourette syndrome and schizophrenia, it is primarily utilized as a research-use-only laboratory tool to investigate the endocannabinoid system, memory, and metabolic processes.

Other names

1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholino-1H-pyrazole-3-carboxamideN-(morpholin-4-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide[123I]AM281[124I]AM281