Larazotide (acetate)

Larazotide is a peptide antagonist of alpha3beta4 subunit-containing nicotinic acetylcholine receptors (nAChRs). It selectively inhibits epibatidine-induced calcium mobilization in HEK293 cells expressing human alpha3beta4 subunit-containing nAChRs over HEK293 cells expressing alpha4beta2 subunit-containing nAChRs (IC50s = 91 and 276 nM, respectively). Larazotide (100 µM) decreases inflammatory cytokine-induced tight junction dysfunction in isolated rat intestinal epithelial cells. In vivo, larazotide (0. 3, and 30 µg/kg) inhibits nicotine self-administration and varenicline-induced reinstatement of nicotine-seeking behavior in rats. It also increases intestinal epithelial cell bridging and decreases intestinal damage without reducing liver damage in a rat model of thioacetamide-induced acute liver failure.. Solulibility: DMSO: Sparingly Soluble: 1-10 mg/ml: PBS pH 7.2: Sparingly Soluble: 1-10 mg/ml.