TY - JOUR
T1 - Analysis of fk1052, a. new potent 5-ht3 and 5-ht4 receptor dual antagonist, on ion transport of guinea-pig distal colon
AU - Kuwahara, Atsukazu
AU - Kuwahara, YUKo
AU - Kadowaki, Makot0
PY - 1994
Y1 - 1994
N2 - The effect of the newly developed 5-HT, and 5-HT4 receptor dual antagonist, FK1052 on short-circuit current was investigated using submucosa-mucosa sheets of guinea-pig distal colon. 5-Hydroxytryptamine (5-HT) evoked an increase in short-circuit current in a concentration- dependent manner. FK1052 concentration-dependently decreased the 5-HT-evoked increase in short-circuit current with pIC50 value of 8.84 i 0.1. Specific 5-HT3 antagonists, ondansetron, granisetron and ICS205-930 significantly decreased the 5-HT-evoked increases in short-circuit current with pIC50 values of 7.92 i 0.05, 7.65 i 0.08 and 6.62 i 0.14, respectively. Both 5-HT3 agonist, 2-methyl-5-HT- and 5-HT4 agonist 5-methoxytryptamine (5- MeOT) evoked increases in short-circuit current similar to that of 5-HT. FK1052 decreased both the 2-methyl-5-HT- and 5-MeOT-evoked increases in short-circuit current in a concentration- dependent manner with pIC50 values of 7.7 i 0.5 and 7.5 i 0.2, respectively. The results suggest that FK1052 is a 5-HT, and 5-HT4 receptor dual antagonist on ion transport of guinea-pig distal colon.
AB - The effect of the newly developed 5-HT, and 5-HT4 receptor dual antagonist, FK1052 on short-circuit current was investigated using submucosa-mucosa sheets of guinea-pig distal colon. 5-Hydroxytryptamine (5-HT) evoked an increase in short-circuit current in a concentration- dependent manner. FK1052 concentration-dependently decreased the 5-HT-evoked increase in short-circuit current with pIC50 value of 8.84 i 0.1. Specific 5-HT3 antagonists, ondansetron, granisetron and ICS205-930 significantly decreased the 5-HT-evoked increases in short-circuit current with pIC50 values of 7.92 i 0.05, 7.65 i 0.08 and 6.62 i 0.14, respectively. Both 5-HT3 agonist, 2-methyl-5-HT- and 5-HT4 agonist 5-methoxytryptamine (5- MeOT) evoked increases in short-circuit current similar to that of 5-HT. FK1052 decreased both the 2-methyl-5-HT- and 5-MeOT-evoked increases in short-circuit current in a concentration- dependent manner with pIC50 values of 7.7 i 0.5 and 7.5 i 0.2, respectively. The results suggest that FK1052 is a 5-HT, and 5-HT4 receptor dual antagonist on ion transport of guinea-pig distal colon.
UR - http://www.scopus.com/inward/record.url?scp=0028362659&partnerID=8YFLogxK
U2 - 10.2220/biomedres.15.205
DO - 10.2220/biomedres.15.205
M3 - 学術論文
AN - SCOPUS:0028362659
SN - 0388-6107
VL - 15
SP - 205
EP - 210
JO - Biomedical Research (Japan)
JF - Biomedical Research (Japan)
IS - 3
ER -