Benzomalvin A was isolated as an active inhibitor of substance P binding to mammalian neurokinin NK1 receptors by researchers at Sterling Winthrop Pharmaceuticals (now Sanofi Aventis). The core benzodiazepine structure of benzomalvin A is formed biosynthetically by the condensation of two molecules of anthranilic acid and a phenylalanine. Benzomalvin A 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 A.