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Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit.
Busby RW, Bryant AP, Bartolini WP, Cordero EA, Hannig G, Kessler MM, Mahajan-Miklos S, Pierce CM, Solinga RM, Sun LJ, Tobin JV, Kurtz CB, Currie MG. Busby RW, et al. Among authors: solinga rm. Eur J Pharmacol. 2010 Dec 15;649(1-3):328-35. doi: 10.1016/j.ejphar.2010.09.019. Epub 2010 Sep 20. Eur J Pharmacol. 2010. PMID: 20863829
Pharmacologic properties, metabolism, and disposition of linaclotide, a novel therapeutic peptide approved for the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation.
Busby RW, Kessler MM, Bartolini WP, Bryant AP, Hannig G, Higgins CS, Solinga RM, Tobin JV, Wakefield JD, Kurtz CB, Currie MG. Busby RW, et al. Among authors: solinga rm. J Pharmacol Exp Ther. 2013 Jan;344(1):196-206. doi: 10.1124/jpet.112.199430. Epub 2012 Oct 22. J Pharmacol Exp Ther. 2013. PMID: 23090647
MRP4 Modulation of the Guanylate Cyclase-C/cGMP Pathway: Effects on Linaclotide-Induced Electrolyte Secretion and cGMP Efflux.
Tchernychev B, Ge P, Kessler MM, Solinga RM, Wachtel D, Tobin JV, Thomas SR, Lunte CE, Fretzen A, Hannig G, Bryant AP, Kurtz CB, Currie MG, Silos-Santiago I. Tchernychev B, et al. Among authors: solinga rm. J Pharmacol Exp Ther. 2015 Oct;355(1):48-56. doi: 10.1124/jpet.115.224329. Epub 2015 Jul 27. J Pharmacol Exp Ther. 2015. PMID: 26216942