Chemical and Pharmaceutical Bulletin p. 1116 - 1124 (1998)
Update date:2022-07-30
Topics:
Suzuki, Takeshi
Imanishi, Naoki
Itahana, Hirotsune
Watanuki, Susumu
Miyata, Keiji
Ohta, Mitsuaki
Nakahara, Hideaki
Yamagiwa, Yoko
Mase, Toshiyasu
A novel series of 4-amino-N-[2-(1-aminocycloalkan-1-yl)ethyl]-5-chloro- 2-methoxybenzamide derivatives (1), which had amines conformationally restricted due to the effect of repulsion by neighboring substituents, were prepared and evaluated for 5-hydroxytryptamine 4 (5-HT4) agonistic activities by using the contraction of longitudinal muscle myenteric plexus (LMMP) of guinea pig ileum. One of the most potent compounds in this series was 4-amino-5-chloro-N-[2-(1-dimethylamino-1-cyclohexyl)ethyl]-2- methoxybenzamide (1c, YM-47813) with an EC50 value of 1.0 μM on LMMP. This compound effectively enhanced gastric motility and gastric emptying in conscious dogs by oral administration (1-3 mg/kg).
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(1984)Doi:10.1016/S0040-4039(98)01192-7
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(1998)