Binding Characteristics of [^3H] Ketanserin for Serotonin-2 Receptor in the Rabbit Platelet
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概要
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The present study was designed to examine 1) the properties of [^3H] ketanserin binding to serotonin-2 (5HT_2)-serotonergic receptors in the rabbit platelet membranes, 2) displacement affinities of various chemicals and 3) difference of the affinities between their chemicals and new agents, MCI-9042 and M-1. The plots of specific binding obtained from the Scatchard analysis using [^3H] ketanserin for the platelet membranes were monophasic when the non-specific binding was determined by the use of 0.1 mM serotonin (5HT), and the K_d and B_<max> values were 3.93±0.41 nM and 1.19±0.20 pmol/mg protein, respectively. The displacement potencies of chemicals which were serotonin receptor-, dopamine receptor-, histamine receptor-, and α-adrenoceptor-related agents were characterized by [^3H] ketanserin binding to 5HT_2-serotonergic receptor. The pK_i values of a new antiplatelet agent, MCI-9042,and its metabolite, M-1,were 7.19 and 7.59,respectively and these values were lower than those of ketanserin and pirenperone but higher than those of methysergide, cinanserin and cyproheptadine. The affinities of ketanserin for 5HT_2-receptors in the rabbit platelet were similar to those for 5HT_2-receptors previously identified in the rat frontal lobe and in canine aorta, but cinancerin was selective to 5HT_2-receptors in the rat frontal lobe and in canine aorta, prazosin was selective to 5HT_2-receptor in the rabbit platelet, and MCI-9042 and M-1 had the same affinities to the receptors in the rat frontal lobe and in the rabbit platelet. It is suggested that 1) the binding of [^3H] ketanserin to 5HT_2-receptors in the rabbit platelet is dissociated by the new antiplatelet agents, MCI-9042 and M-1,2) the affinities of some chemicals for 5HT_2-receptors in the rabbit platelet are not identical with those in the rat frontal lobe or in the canine aorta, and 3) [^3H] ketanserin binding sites in platelets, neurons and/or blood vessels may consist of various subtypes.
- 公益社団法人日本薬学会の論文
著者
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NAGATOMO Takafumi
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
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KIMURA Masako
Department of Molecular Physiology, The Jikei University School of Medicine
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Kimura Masako
Department Of Molecular Physiology Jikei University School Of Medicine
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Kimura Masako
Department Of Pharmacology Niigata College Of Pharmacy
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Nagatomo T
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie
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TSUCHIHASHI HIROSHI
Department of Surgery, Department of Medicine, Shiga University of Medical Science
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Shimada Kenji
Division Of Cardiovascular Research Laboratories Tsubame Rosai Hospital:department Of Internal Medic
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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YAGI Naoyuki
Department of Pharmacology, Niigata College of Pharmacy
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SHIROTA Kenichiro
Department of Pharmacology, Niigata College of Pharmacy
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Yagi N
Univ. Shizuoka Shizuoka Jpn
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Tsuchihashi Hiroshi
新潟薬科大学 薬理
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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Yagi Naoyuki
Department Of Pharmacology Niigata College Of Pharmacy
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Namikawa Tomoko
Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.
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KIMURA Masako
Department of Integrative Physiology, Kagawa Nutrition University
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