7-Benzyl-6-methyl-6,7-dihydroquinazolino[3,2-a][1,4]benzodiazepine-5,13-dione

DescriptionBenzomalvin A is a fungal metabolite produced by Penicillium. It inhibits yeast α-glucosidase in vitro (IC50 = 383.2 μM). In vivo, benzomalvin A (3.1-31.6 mg/kg) decreases plasma glucose levels in mice following administration of sucrose. It also decreases the plasma glucose postprandial peak in nicotinamide-streptozotocin-induced hyperglycemic mice when administered at a dose of 10 mg/kg. Benzomalvin A also acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P to guinea pig, rat, and human NK1 (Kis = 12, 42, and 43 μM, respectively).

UsesBenzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively[1].