This study investigates the anti-inflammatory effects of 1-(2-chlorophenyl)-N-methyl-N(1-methylpropyl)-3-isoquinoline carboxamide and 7-chloro-5-(4-chlorophenyl)-1, 3-dihydro-1-methyl-2-H-1,4-benzodiazepin-2-one in paw oedema induced by carrageenan in mice. Pretreatment (24 h) with both ligands inhibited oedema formation in at different doses (0.00001-10 mg/kg, i.p.) with range of inhibition of 25% to 70%, in animals with or without adrenal glands. These results demonstrate, for the first time, an in vivo anti-inflammatory property of peripheral benzodiazepine receptor ligands.