Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents

Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents
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DOI:
10.1016/s0960-894x(02)00060-4
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发表时间:
2002-03-25
影响因子:
2.7
通讯作者:
Kato, S
Kato, S
中科院分区:
医学4区
文献类型:
--
作者:
Harada, H;Yamazaki, H;Kato, S

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A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT4 receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[l-(4aminobutyl)-4-piperidinylmethyi]-4-piperidinyl]-5-chloro-2-methoxybenzamide (15) was found to have a potent binding affinity for 5-HT4 receptors (IC50: 6.47 nM) and showed excellent colonic prokinetic activity. (C) 2002 Published by Elsevier Science Ltd.