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Your search keyword '"Jeong, Eun-Jeong"' showing total 13 results
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13 results on '"Jeong, Eun-Jeong"'

8. P-16: Integration of the 4.5ʺ Active Matrix Organic Light-emitting Display with Organic Transistors

Author

Lee, Sangyun, primary, Koo, Bon-Won, additional, Jeong, Eun-Jeong, additional, Lee, Eunkyung, additional, Kim, Sangyeol, additional, Kim, Jungwoo, additional, Lee, Honyeon, additional, Ko, Ickhwan, additional, Lee, Younggu, additional, Chun, Youngtea, additional, Oh, Taesik, additional, Kang, Sungkee, additional, Pu, Lyoungson, additional, and Kim, Jongmin, additional

Published
2006
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13. The novel, potent and highly selective 5-HT 4 receptor agonist YH12852 significantly improves both upper and lower gastrointestinal motility.

Author

Jeong EJ, Chung SY, Hong HN, Oh SW, and Sim JY

Subjects
Animals, CHO Cells, Colon physiology, Cricetinae, Cricetulus, Dogs, Dose-Response Relationship, Drug, Gastrointestinal Motility physiology, Humans, Intestine, Small physiology, Macaca fascicularis, Male, Pyrimidines, Rats, Rats, Sprague-Dawley, Colon drug effects, Gastrointestinal Motility drug effects, Intestine, Small drug effects, Receptors, Serotonin, 5-HT4 metabolism, Serotonin 5-HT4 Receptor Agonists metabolism, Serotonin 5-HT4 Receptor Agonists pharmacology
Abstract

Background and Purpose: 5-HT 4 receptor agonists have been shown to be effective at treating various gastrointestinal tract disorders. However, a lack of selectivity against off-targets has been a limiting factor for their clinical use., Experimental Approach: The binding affinity and selectivity of YH12852 for human 5-HT 4(a) receptor in CHO-K1 cells were evaluated using radioligand binding assays, and agonistic activity was assessed using a β-lactamase reporter system. Contractile activity and propulsive motility were measured in the guinea pig isolated distal colon. Its prokinetic effect on the gastrointestinal tract was evaluated in guinea pigs, dogs and monkeys. Its tissue distribution was evaluated in rats., Key Results: YH12852 exhibited high affinity and potency for human recombinant 5-HT 4(a) receptor with high selectivity over other 5-HT and non-5-HT receptors, ion channels, enzymes and transporters. YH12852 induced contractions and increased propulsive motility in guinea pig isolated colon. These effects were abolished by the 5-HT 4 receptor antagonist GR113808. YH12852 increased defecation more effectively than prucalopride in guinea pigs and dogs and improved gastric emptying more effectively than mosapride in guinea pigs, dogs and monkeys. YH12852 was highly distributed to the gastrointestinal tract as the target organ., Conclusion and Implications: The high in vitro potency and selectivity of YH12852 for 5-HT 4 receptor translated into potent in vivo efficacy with good tolerability. YH12852 significantly improved both upper and lower bowel motility in the animal models tested and has the potential to address considerable unmet needs in patients with functional constipation, gastroparesis or both., (© 2017 The British Pharmacological Society.)

Published
2018
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