L-DOPA methyl ester antagonizes competitively L-DOPA-induced facilitation of noradrenaline release from rat hypothalamic slices.
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概要
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In rat hypothalamic slices, antagonism by L-DOPA methyl ester and (-)-propranolol against L-DOPA-induced facilitation of endogenous noradrenaline (NA) release was characterized under the inhibition of dopadecarboxylase. L-DOPA at 10 nM to 1 μM facilitated the evoked NA release in a concentration-dependent manner. L-DOPA methyl ester (3, 10 and 30 nM) progressively shifted the concentration-release curve for L-DOPA to the right: Schild plots gave a straight line with a slope of 1.00 and pA<SUB>2</SUB> was 8.9. This antagonistic action was not mimicked by L-phenylalanine, a substrate for L-DOPA transport system. In contrast, 10 and 100 nM propranolol concentration-dependently reduced the maximal effect of LDOPA without rightward shift of the concentration-release curve. L-DOPA methyl ester is a potent competitive antagonist for the action of L-DOPA, and the recognition site of L-DOPA differs from presynaptic β-adrenoceptors.
- 公益社団法人 日本薬理学会の論文
著者
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Goshima Yoshio
Department Of Molecular Neuropharmacology Yokohama City University Graduate School Of Medicine
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Nakamura Shinichi
Department Of Anesthesiology Saitama Medical School
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MISU Yoshimi
Department of Pharmacologv, faculty of Pharmaceutical Scieuces, Kyoto University
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