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Image Search Results
Journal: Frontiers in Pharmacology
Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
doi: 10.3389/fphar.2017.00418
Figure Lengend Snippet: Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) Linaclotide, a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.
Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of
Techniques: Derivative Assay, Activation Assay, Activity Assay
Journal: Frontiers in Pharmacology
Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
doi: 10.3389/fphar.2017.00418
Figure Lengend Snippet: Luminally acting agents for constipation treatment.
Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of
Techniques: Inhibition, Injection
Journal: Frontiers in Pharmacology
Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
doi: 10.3389/fphar.2017.00418
Figure Lengend Snippet: Proposed mechanisms of luminally acting agents for constipation treatment. The prosecretory agents linaclotide and plecanatide activate CFTR chloride channel in the enterocytes by elevating intracellular cGMP level through GC-C receptor and thereby enhancing salt and water secretion. Lubiprostone stimulates CFTR-dependent chloride secretion directly and/or via EP4 receptor pathway. Elobixibat accelerates colonic transit through enhancing delivery of bile acids to the colon, thus increasing stool frequency in CIC patients. The ORL-1 receptor antagonists naloxegol and methylnaltrexone reduce OIC through antagonizing the μ-receptor in the GI tract without reducing its central analgesic effect. Velusetrag, naronapride, prucalopride and tegaserod are selective agonists of 5-HT4 receptor and increase transepithelial secretion of Cl − and HCO 3 - .
Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of
Techniques: