INHIBITORY EFFECTS OF FULLERENE C60 DERIVATIVES ON ENDOTHELIUM-DERIVED RELAXATION IN RABBIT THORACIC AORTA |
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| Authors: | Mitsutoshi Satoh Tadahiko Mashino Tetsuo Nagano Masaaki Hirobe Issei Takayanagi Katsuo Koike |
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| Affiliation: | a Department of Chemical Pharmacology, Toho University, School of Pharmaceutical Sciences, Funabashi, Chiba, Japanb Division of Organic Chemistry, Kyoritsu College of Pharmacy, Tokyo, Japanc Department of Bioorganic and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japand University of Shizuoka, Shizuoka, Japan |
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| Abstract: | Inhibitory effects of newly synthesized fullerene C60 derivatives 1 (C60-bis(N,N-dimethylpyrrolidinium iodide)), 2 (C60-proline-N-acetic acid) and 3 (C60-ethylenediamine-N, N'-diacetic acid) on acetylcholine-induced relaxation in endothelium-intact rabbit thoracic aorta precontracted by phenylephrine (10-6 M) were studied. Fullerene C60 derivative 1 (3 × 10-6 M), 2 (10-5 M) and 3 (10-5 M) reduced the maximum amplitude of the acetylcholine-induced relaxation without significantly changing the pD2 values obtained from the concentration - response curves. In the presence of fullerene C60 derivative 1 (10-5 M) the acetylcholine-induced relaxation was eliminated and an acetylcholine-induced contraction was observed. These results suggest that fullerene C60 derivative 1 strongly inhibits endothelium (nitric oxide)-dependent acetylcholine-induced relaxation in thoracic aorta of rabbit. |
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| Keywords: | Smooth muscle Endothelium Fullerene C60 derivative Nitric oxide (NO) Thoracic aorta of rabbit |
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