Ca2+-Channel Blockade in Rat Thoracic Aorta by Protopine Isolated from Corydalis Tubers.

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概要

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• The pharmacological properties and mechanism of the action of protopine on isolated rat thoracic aorta were examined. It inhibited norepinephrine (NE, 3μM)-induced tonic contraction in rat thoracic aorta in a concentration-dependent manner (25-100 μg/ml). The phasic contraction caused by NE was inhibited only by a high concentration of protopine (100 μg/ml). At the plateau of NE-induced tonic contraction, the addition of protopine also caused relaxation. This relaxing effect of protopine was not antagonized by indomethacin (20 μM) or methylene blue (50 μM), and it still existed in denuded rat aorta or in the presence of nifedipine (2-100 μM). Protopine also inhibited high potassium (60 mM)-induced, calcium-dependent (0.03-3 mM) contraction of rat aorta in a concentration-dependent manner. Neither cAMP nor cGMP level was changed by protopine. Both the formation of inositol monophosphate caused by NE and the phasic contraction induced by caffeine were also not affected by protopine. <SUP>45</SUP>Ca<SUP>2+</SUP> influx caused by either NE or K<SUP>+</SUP> was inhibited by protopine concentration-dependently. It is concluded that protopine relaxed the rat thoracic aorta mainly by suppressing the Ca<SUP>2+</SUP> influx through both voltage- and receptor-operated calcium channels.

• 公益社団法人 日本薬理学会の論文

著者

• Wu Tian-shung

  Department Of Applied Chemistry Providence College Of Arts And Science

• Teng Che-ming

  Pharmacological Institute College Of Medicine National Taiwan University

• Lu Sheng-teh

  School Of Pharmacy Kaohsiung Medical College

• WU Yang-Chang

  School of Chinese Medicine, College of Chinese Medicine, China Medical University

• Teng Che-Ming

  Pharmacological Institute, College of Medicine, National Taiwan University

• Ko Feng-Nien

  Pharmacological Institute, College of Medicine, National Taiwan University

• Huang Tur-Fu

  Pharmacological Institute, College of Medicine, National Taiwan University

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