Benzomalvin B was first isolated as a weakly active inhibitor of substance P from mammalian neurokinin NK1 receptors by researchers at Sterling Winthrop Pharmaceuticals (now Sanofi Aventis) in 1994. The core benzodiazepine structure of benzomalvin B is formed biosynthetically by the condensation of two molecules of anthranilic acid and phenylalanine. Benzomalvin B is related to the asperlicins, potent and selective antagonists of peripheral cholecystokinin receptors. Lack of availability has hampered further exploration of the pharmacology of benzomalvin B.