EFFECTS OF PALYTOXIN ON ISOLATED INTESTINAL AND VASCULAR SMOOTH MUSCLES

• Published in: Japanese journal of pharmacology 1976, Vol.26(6), pp.683-692
• Main Authors: ITO, Katsuaki, KARAKI, Hideaki, ISHIDA, Yukisato, URAKAWA, Norimoto, DEGUCHI, Takehiko
• Format: Article
• Language: English
• Subjects: Acrylamides - pharmacology; Animals; Aorta, Thoracic - drug effects; Colon - drug effects; Coronary Vessels - drug effects; Dogs; Female; Guinea Pigs; Ileum - drug effects; In Vitro Techniques; Male; Marine Toxins - pharmacology; Membrane Potentials - drug effects; Mesenteric Arteries - drug effects; Muscle Contraction - drug effects; Muscle, Smooth - drug effects; Rabbits
• ISSN: 0021-5198; 1347-3506
• DOI: 10.1254/jjp.26.683

Palytoxin (PTX), the most potent marine toxin isolated from the Zoanthid, Palythoa tuberculosa, was studied to determine the effect on isolated smooth muscles. In guinea pig taenia coli PTX at above 3 × 10−10 g/ml caused a contraction which slowly subsided under isotonic recording. Under isometric recording PTX at above 1 × 10−10 g/ml caused a contraction which depended on the spontaneous activity. The PTX-induced contraction was not affected by atropine, tripelennamine or tetrodotoxin but was inhibited by 5 mM Mg, norepinephrine, isoprenaline or papaverine. PTX at above 1 x 10−9 g/ml induced an increase in spike frequency and a slight depolarization accompanied with a contraction when measured using a sucrose gap method. In some cases the spike generation was almost abolished after a long exposure to higher dose of PTX and the developed tension gradually decreased. Under isometric recording, PTX caused a sustained contraction in rabbit aorta, dog mesenteric and coronary arteries at above 1 × 10−10, 1 × 10−10 and 1 × 10−n g/ml, respectively, in a dose-dependent manner. The coronary artery was most sensitive among the preparations used. PTX-induced contraction in aorta was irreversible, was not influenced by phentolamine but diminished with 5 mM Mg and disappeared in a D-600 or Ca-free medium. PTX is thus an extremely potent and direct stimulant which acts on smooth muscles.