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Quaternised renzapride as a potent and selective 5-HT4 receptor agonist

โœ Scribed by G.S. Baxter; P. Boyland; L.M. Gaster; F.D. King


Book ID
108477147
Publisher
Elsevier Science
Year
1993
Tongue
English
Weight
128 KB
Volume
3
Category
Article
ISSN
0960-894X

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Azabicyclic indole esters as potent 5-HT
โœ Paul A. Wyman; Laramie M. Gaster; Frank D. King; Jonathon M. Sutton; Elizabeth S ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 641 KB

The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon l