A possible mechanism of a new antispasmodic drug,2-(1,2-benzisoxazol-3-yl)-3-(2-(2-piperidinoethoxy) phenyl)acrylonitrile (SX-284).
- 1 January 1982
- journal article
- research article
- Published by Elsevier in The Japanese Journal of Pharmacology
- Vol. 32 (6) , 973-979
- https://doi.org/10.1254/jjp.32.973
Abstract
A newly synthesized drug, SX-284, depressed the twitch response of the ileum from guinea pig to electrical stimulation at 0.1 Hz. SX-284 was almost as active as atropine on electrically stimulated ileum. The responses of guinea pig ileum to nicotine and serotonin were also inhibited by SX-284. SX-284 did not influence the release of transmitters from the motor, sympathetic, nonadrenergic inhibitory and noncholinergic excitatory nerves, and responses of various smooth muscles mediated through drug receptors, and at these doses, SX-284 inhibited the release of acetylcholine from the vagus nerve. Apparently, SX-284 specifically inhibits the acetylcholine release from the vagus nerve. Spontaneous movement of the guinea pig ileum was dose-dependently depressed by SX-284. The potency ratio for SX-284 relative to atropine was 1.7.This publication has 6 references indexed in Scilit:
- Effects of Nonspecific Smooth Muscle Relaxants and Ca–Blocker on Ca–Release and Ca–Binding in Microsomal Fractions from Rabbit Taenia ColiThe Japanese Journal of Pharmacology, 1980
- EFFECT OF THEOPHYLLINE ON THE RESPONSES OF THE GUINEA-PIG URINARY-BLADDER TO NERVE-STIMULATION, ADENOSINE 5' TRIPHOSPHATE AND HISTAMINE1978
- EFFECTS OF 5-HYDROXYTRYPTAMINE AND MORPHINE ON THE STOMACH MOTILITY IN SITUThe Japanese Journal of Pharmacology, 1975
- The inhibitory innervation of the taenia of the guinea‐pig caecumThe Journal of Physiology, 1966
- THE SITE OF THE 5‐HYDROXYTRYPTAMINE RECEPTOR ON THE INTRAMURAL NERVOUS PLEXUS OF THE GUINEA‐PIG ISOLATED ILEUMBritish Journal of Pharmacology and Chemotherapy, 1963
- A SENSITIVE METHOD FOR THE ASSAY OF 5‐HYDROXYTRYPTAMINEBritish Journal of Pharmacology and Chemotherapy, 1957