RELAXANT ACTIONS OF PGE<SUB>2</SUB> AND ITS DERIVATIVE (YPG-209) ON CANINE TRACHEAL SMOOTH MUSCLE AND THEIR ENHANCEMENT OF Ca<SUP>++</SUP> UPTAKE BY THE MICROSOMAL FRACTION
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概要
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The spasmogenic action of tetraethylammonium on canine tracheal smooth muscle was dependent on the extracellular Ca<SUP>++</SUP> concentration. Acetylcholine, on the contrary, produced partial contraction for a certain period of time after removal of extracellular Ca<SUP>++</SUP>, suggesting the release of Ca<SUP>++</SUP> from intracellular Ca<SUP>++</SUP> stores into the cytosol. PGE<SUB>2</SUB>, 16(S)-methyl-20-methoxy-PGE<SUB>2</SUB> (YPG-209), verapamil, and dibutyryl cyclic AMP relaxed the acetylcholine-induced contraction of the trachea. Pretreatment with prostaglandins or dibutyryl cyclic AMP more efficiently suppressed acetylcholine-induced contraction, whereas verapamil blocked the spasmogenic action of tetraethylammonium in a relatively selective manner. The prostaglandins and dibutyryl cyclic AMP also inhibited the spasmogenic action of acetylcholine in a Ca<SUP>++</SUP>-free medium. Influx of <SUP>45</SUP>Ca into tracheal smooth muscle which was produced by 83 mM KCl plus 20 mM tetraethylammonium was not significantly affected by prostaglandins as measured by the lanthanum method. In addition, PGE<SUB>2</SUB> increased ATP-dependent Ca<SUP>++</SUP> uptake by the microsomes from tracheal smooth muscle. These results suggest that prostaglandins induce relaxation of the airway smooth muscle mainly through affecting the intracellular Ca<SUP>++</SUP> movement such as by enhancement of sequestration of Ca<SUP>++</SUP> to the microsomes.
- 社団法人 日本薬理学会の論文
著者
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Tomioka Kenichi
Department Of Physics Konan University
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TERAI Michio
Department of Pharmacology and Biochemistry, Central Research Laboratories, Yamanouchi Pharmaceutica
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MAENO Hiroo
Department of Pharmacology and Biochemistry, Central Research Laboratories, Yamanouchi Pharmaceutica
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Maeno Hiroo
Department Of Biochemistry Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.
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TERAI Michio
Department of Pharmacology and Biochemistry, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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TOMIOKA Kenichi
Department of Pharmacology and Biochemistry, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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