Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent

2016 ◽  
Vol 109 ◽  
pp. 75-88 ◽  
Author(s):  
Jung Sang Park ◽  
Weonbin Im ◽  
Sunghak Choi ◽  
Sook Jin Park ◽  
Jun Min Jung ◽  
...  
Keyword(s):  
Prokinetic Agent

Experimental pancreatitis disturbs gastrointestinal and colonic motility in mice: effect of the prokinetic agent tegaserod

2007 ◽  
Vol 19 (10) ◽  
pp. 856-864 ◽  
Author(s):  
t. c. seerden ◽  
j. g. de man ◽  
p. holzer ◽  
r. m. van den bossche ◽  
a. g. herman ◽  
...  
Keyword(s):  
Colonic Motility ◽  
Experimental Pancreatitis ◽  
Prokinetic Agent

scholarly journals Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride

1997 ◽  
Vol 273 (5) ◽  
pp. H2534-H2538 ◽  
Author(s):  
Saeed Mohammad ◽  
Zhengfeng Zhou ◽  
Qiuming Gong ◽  
Craig T. January
Keyword(s):  
Ventricular Arrhythmias ◽  
Current Amplitude ◽  
Hek293 Cells ◽  
K Channel ◽  
Delayed Rectifier ◽  
Patch Clamp Recording ◽  
Channel Activation ◽  
Prokinetic Agent ◽  
Tail Current ◽  
Herg Channels

Cisapride, a gastrointestinal prokinetic agent, is known to cause long Q-T syndrome and ventricular arrhythmias. The cellular mechanism is not known. The human ether-á-go-go-related gene ( HERG), which encodes the rapidly activating delayed rectifier K+current and is important in cardiac repolarization, may serve as a target for the action of cisapride. We tested the hypothesis that cisapride blocks HERG. The whole cell patch-clamp recording technique was used to study HERG channels stably expressed heterologously in HEK293 cells. Under voltage-clamp conditions, cisapride block of HERG is dose dependent with a half-maximal inhibitory concentration of 6.5 nM at 22°C ( n = 25 cells). Currents rapidly recovered with drug washout. The onset of block by cisapride required channel activation indicative of open or inactivated state blockage. Block of HERG with cisapride after channel activation was voltage dependent. At −20 mV, 10 nM cisapride reduced HERG tail-current amplitude by 5%, whereas, at +20 mV, the tail-current amplitude was reduced by 45% ( n = 4 cells). At −20 and +20 mV, 100 nM cisapride reduced tail-current amplitude by 66 and 90%, respectively. We conclude that cisapride is a potent blocker of HERG channels expressed in HEK293 cells. This effect may account for the clinical occurrence of Q-T prolongation and ventricular arrhythmias observed with cisapride.

Pre Endoscopy Use of Prokinetic Agent, Metoclopramide, to Influence Outcome in Upper GI Bleeding. Is There Evidence to Support Its Use?

2010 ◽  
Vol 105 ◽  
pp. S538-S539
Author(s):  
Ghulam Mujtaba ◽  
Vijaypal Arya ◽  
Siddharth Mathur ◽  
Ajay Gupta ◽  
Mahesh Krishnaiah ◽  
...  
Keyword(s):  
Gi Bleeding ◽  
Prokinetic Agent ◽  
Upper Gi Bleeding ◽  
Upper Gi

Intestinal Absorption and Presystemic Elimination of the Prokinetic Agent, EM574, in the Rabbit

2002 ◽  
Vol 91 (1) ◽  
pp. 217-228 ◽  
Author(s):  
Guanfa Gan ◽  
Linda L. Cartier ◽  
Yue Huang ◽  
Zheng Yang ◽  
Ronald J. Sawchuk
Keyword(s):  
Intestinal Absorption ◽  
Prokinetic Agent ◽  
Presystemic Elimination

scholarly journals Effects of SK-951, a Benzofuran Derivative, as a Prokinetic Agent in Rats and Dogs.

1999 ◽  
Vol 81 (3) ◽  
pp. 292-297 ◽  
Author(s):  
Motohiro Takeda ◽  
Katsura Tsukamoto ◽  
Masaya Yamano ◽  
Hiroshi Uesaka
Keyword(s):  
Benzofuran Derivative ◽  
Prokinetic Agent

Development of a novel botanical drug (DA-9701), as a new prokinetic agent

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
J Ryu ◽  
Y Kwon ◽  
Y Cho ◽  
S Choi ◽  
T Lee ◽  
...  
Keyword(s):  
Prokinetic Agent ◽  
Botanical Drug
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