Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists
Katsuhiko Itoh
1
,
Koji Kanzaki
2
,
Tsuguo IKEBE
2
,
Takanobu KUROITA
2
,
Hideo TOMOZANE
2
,
Shuji Sonda
2
,
Noriko Sato
2
,
Keiichiro HAGA
2
,
Takeshi KAWAKITA
2
1
Research Laboratories, Yoshitomi Pharmaceutical Industries Ltd., 955 Koiwai, Yoshitomi-cho, Chikujo-gun, 871-8550, Fukuoka, Japan
|
2
Research Laboratories, Yoshitomi Pharmaceutical Industries Ltd., 955 Koiwai, Yoshitomi-cho, Chikujo-gun, Fukuoka 871-8550, Japan
|
Publication type: Journal Article
Publication date: 1999-11-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
10889321
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
A number of new carboxamide derivatives were synthesized. The affinity of these compounds for the serotoninergic 5-HT 4 receptor was evaluated by use of radioligand-binding techniques. The agonistic activity was evaluated as the contractile effect of the ascending colon isolated from guinea-pigs. Among these compounds, 4-amino-5-chloro-2-methoxy- N -[1-[2-[(methylsulfonyl)amino]ethly]-4-piperidinylmethyl]benzamide ( 24 ) showed a high affinity for the 5-HT 4 receptor ( Ki = 9.6 nM). Compound 24 displayed a higher affinity for 5-HT 4 receptors than the other receptors, including, 5-HT 3 and dopamine D 2 receptors. In addition, compound 24 was confirmed to be a potent 5-HT 4 receptor agonist (ED 50 = 7.0 nM). An interaction model between compound 24 and 5-HT 4 receptor was proposed.
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Itoh K. et al. Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists // European Journal of Medicinal Chemistry. 1999. Vol. 34. No. 11. pp. 977-989.
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Itoh K., Kanzaki K., IKEBE T., KUROITA T., TOMOZANE H., Sonda S., Sato N., HAGA K., KAWAKITA T. Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists // European Journal of Medicinal Chemistry. 1999. Vol. 34. No. 11. pp. 977-989.
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RIS
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TY - JOUR
DO - 10.1016/S0223-5234(99)00158-0
UR - https://doi.org/10.1016/S0223-5234(99)00158-0
TI - Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists
T2 - European Journal of Medicinal Chemistry
AU - Itoh, Katsuhiko
AU - Kanzaki, Koji
AU - IKEBE, Tsuguo
AU - KUROITA, Takanobu
AU - TOMOZANE, Hideo
AU - Sonda, Shuji
AU - Sato, Noriko
AU - HAGA, Keiichiro
AU - KAWAKITA, Takeshi
PY - 1999
DA - 1999/11/01
PB - Elsevier
SP - 977-989
IS - 11
VL - 34
PMID - 10889321
SN - 0223-5234
SN - 1768-3254
ER -
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BibTex (up to 50 authors)
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@article{1999_Itoh,
author = {Katsuhiko Itoh and Koji Kanzaki and Tsuguo IKEBE and Takanobu KUROITA and Hideo TOMOZANE and Shuji Sonda and Noriko Sato and Keiichiro HAGA and Takeshi KAWAKITA},
title = {Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists},
journal = {European Journal of Medicinal Chemistry},
year = {1999},
volume = {34},
publisher = {Elsevier},
month = {nov},
url = {https://doi.org/10.1016/S0223-5234(99)00158-0},
number = {11},
pages = {977--989},
doi = {10.1016/S0223-5234(99)00158-0}
}
Cite this
MLA
Copy
Itoh, Katsuhiko, et al. “Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists.” European Journal of Medicinal Chemistry, vol. 34, no. 11, Nov. 1999, pp. 977-989. https://doi.org/10.1016/S0223-5234(99)00158-0.