Identification of evodiamine and rutecarpine as novel TMEM16A inhibitors and their inhibitory effects on peristalsis in isolated Guinea-pig ileum

2021 ◽  
pp. 174340
Author(s):  
Zhijun Zhao ◽  
Yurun Xue ◽  
Gaohua Zhang ◽  
Jie Jia ◽  
Ruilian Xiu ◽  
...  
1996 ◽  
Vol 10 (1) ◽  
pp. 66-69 ◽  
Author(s):  
J. Gálvez ◽  
J. Duarte ◽  
F. Sánchez de Medina ◽  
J. Jiménez ◽  
A. Zarzuelo

1997 ◽  
Vol 73 ◽  
pp. 105
Author(s):  
Joji Tomioka ◽  
Shinichiro Suzaki ◽  
Akira Kurokawa ◽  
Yasuhiro Yamamoto ◽  
Toshibumi Oluka ◽  
...  

1986 ◽  
Vol 64 (3) ◽  
pp. 303-306 ◽  
Author(s):  
Christopher H. S. McIntosh ◽  
Victoria Bakich ◽  
Yin Nam Kwok ◽  
John C. Brown

A number of studies have suggested that somatostatin-14 (SS-14) and somatostatin-28 (SS-28) exhibit a similar spectrum of biological activities but have different potencies. In the present study the effects of SS-14, SS-28, and somatostatin-25 on electrically induced contractions of the guinea pig ileum have been compared. All three peptides exhibited equipotent inhibitory effects. Inhibition was obtained at a threshold concentration less than 10−10 M, with maximal inhibition at 10−7 M and IC50 values of 6.0–6.5 × 10−10 M. The N-terminal 14 amino acid fragment of SS-28 had no effect either on motility, when added alone, or on the actions of SS-28, suggesting that this region of the molecule is not critical for biological activity.


Pharmacology ◽  
2018 ◽  
Vol 101 (5-6) ◽  
pp. 330-336 ◽  
Author(s):  
Josef Donnerer ◽  
Ingrid Liebmann

This study aimed at investigating whether the synthetic cannabinoid receptor agonist (+)-WIN 55212-2 has neurogenic and myogenic relaxant effects on the longitudinal muscle-myenteric plexus (LMMP) strip of the guinea-pig ileum. (+)-WIN 55212-2, 1–1,000 nmol/L, concentration-dependently inhibited both the electrical stimulation-induced cholinergic twitch responses as well as the myogenic smooth muscle contractions in the LMMP preparation. SR-141716A (rimonabant) 1–1,000 nmol/L, the cannabinoid CB1 receptor antagonist, being without effect on its own, antagonized the (+)-WIN 55212-2-induced effects. The allyl isothiocyanate (mustard oil, 100 µmol/L) induced a relaxant effect in the guinea-pig ileum, which can be regarded as neurogenic and myogenic, was augmented by (+)-WIN 55212-2, and inhibited by SR-141716A. (+)-WIN 55212-2 only moderately modified the 60 mmol/L KCl-evoked contractions. These results provide functional evidence that the CB1 agonist (+)-WIN 55212-2-induced inhibitory effects in the guinea-pig ileum are exerted both at the neuronal as well as at the intestinal smooth muscle cell level.


1987 ◽  
Vol 336 (4) ◽  
pp. 419-424 ◽  
Author(s):  
S. M. Johnson ◽  
M. Costa ◽  
C. M. S. Humphreys ◽  
R. Shearman

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