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Benproperine is an antitussive agent and actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor.1,2 It increases the latency to first cough and decreases the number of coughs during and after a citric acid aerosol challenge in a guinea pig model of cough when administered at a dose of 27 mg/kg.1 It binds to ARPC2 and delays the initiation of actin polymerization in the presence of actin, the Arp2/3 complex, and the Wiskott-Aldrich syndrome protein (WASP) VCA domain, but not actin alone, when used at a concentration of 10 µM.2 Benproperine (1-10 µM) inhibits the migration and invasion of DLD-1 and AsPC-1 cancer cells and reduces lung metastasis in an AsPC-1 mouse model of metastasis when administered at a dose of 50 m/kg. Formulations containing benproperine have been used as cough suppressants.
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1. Identification of some benproperine metabolites in humans and investigation of their antitussive effect. Acta Pharmacol. Sin. 26(12), 1519-1526 (2005).
2. Benproperine, an ARPC2 inhibitor, suppresses cancer cell migration and tumor metastasis. Biochem. Pharmacol. 163, 46-59 (2019).