A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists

5-HT4 receptor agonists such as tegaserod have demonstrated efficacy in the treatment of constipation predominant irritable bowel syndrome (IBS-C), a highly prevalent disorder characterized by chronic constipation and impairment of intestinal propulsion, abdominal bloating, and pain. The 5-HT4 recep...

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Veröffentlicht in:	Journal of medicinal chemistry 2009-09, Vol.52 (17), p.5330-5343
Hauptverfasser:	McKinnell, R. Murray, Armstrong, Scott R, Beattie, David T, Choi, Seok-Ki, Fatheree, Paul R, Gendron, Roland A. L, Goldblum, Adam, Humphrey, Patrick P, Long, Daniel D, Marquess, Daniel G, Shaw, J. P, Smith, Jacqueline A. M, Turner, S. Derek, Vickery, Ross G
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Binding Sites Biological and medical sciences Biological Availability Cell Line Digestive system Dogs Drug Design Gastrointestinal Diseases - drug therapy Humans Male Medical sciences Movement - drug effects Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - administration & dosage Piperazines - chemical synthesis Piperazines - pharmacokinetics Piperazines - pharmacology Rats Rats, Sprague-Dawley Receptors, Serotonin, 5-HT4 - metabolism Serotonin 5-HT4 Receptor Agonists Serotoninergic system Substrate Specificity
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