Journal article

CSTI-300 (SMP-100); a Novel 5-HT3 Receptor Partial Agonist with Potential to Treat Patients with Irritable Bowel Syndrome or Carcinoid Syndrome.

Alexander Roberts, Gillian Grafton, Andrew D Powell, Kristian Brock, Chunlin Chen, Dejian Xie, Jinkun Huang, Shuang Liu, Alison J Cooper, Catherine A Brady, Omar Qureshi, Zania Stamataki, David D Manning, Nicholas A Moore, Bruce J Sargent, Peter R Guzzo, Nicholas M Barnes

J Pharmacol Exp Ther | Published : 2020


The 5-hydroxytryptamine (5-HT) (serotonin) 5-HT3 receptor represents a clinical target for antagonists to deliver symptomatic relief to patients with diarrhea-predominant irritable bowel syndrome (IBS-d) or carcinoid syndrome. Unfortunately, this pharmacological strategy can present side effects (e.g., severe constipation). The present study investigates the potential of a novel 5-HT3 receptor partial agonist, CSTI-300, to treat patients with IBS-d and other conditions associated with discomfort from colonic distension, with a predicted reduced side-effect profile. The in vitro and in vivo preclinical pharmacology of the drug CSTI-300 was investigated to explore the potential to treat patien..

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