MCI-9042 : High Affinity for Serotonergic Receptors as Assessed by Radioligand Binding Assay
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概要
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This study assessed the specificity of displacement potencies of MCI-9042 ((±)-1-[o-[2-(m-methoxyphenyl)ethyl]phenoxy]-3-(dimethylamino)-2-propyl hydrogen succinate hydrochloride), a new antiplatelet agent, in [^3H]4-bromo-2,5-dimethoxyphenylisopropylamine ([^3H]DOB) and [^3H] ketanserin binding to 5HT_2-serotonergic receptors in the rat brain using the radioligand binding method. The assessment of the displacement potencies of MCI-9042 and its derivative, M-1 (((±)-1-[2-(3-methoxyphenyl) ethyl] phenoxy]-3-(dimethylamino)-2-propanol)hydrochloride), on α_1-, α_2-, β-adrenergic, 5HT_1-, 5HT_2- and muscarinic receptors were also studied. MCI-9042 and M-1 showed strong displacement effects to 5HT_2-receptors using [^3H] DOB binding and [^3H] ketanserin binding sites, and weak displacement effects for [^3H] serotonin, [^3H] prazosin, [^3H] p-aminoclonidine, [^3H] CGP12177 and [^3H] QNB binding to 5HT_1-, α_1-, α_2-, β-adrenergic receptors and muscarinic receptors. Thus, the present study suggests that MCI-9042 is specific for 5HT_2-receptor.
- 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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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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MARUYAMA Keiko
Department of Pharmacology, Niigata College of Pharmacy
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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Maruyama Keiko
Department Of Pharmacology Niigata College Of Pharmacy
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Maruyama Keiko
Department Of Neurology Suwa Red Cross Hospital
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SUGITA Yoko
Department of Pharmacology, Niigata College of Pharmacy
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TAKADA Yoko
Department of Pharmacology, Niigata College of Pharmacy
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SUGIYAMA Eri
Department of Pharmacology, Niigata College of Pharmacy
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Sugita Yoko
Department Of Pharmacology Niigata College Of Pharmacy
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Takada Yoko
Department Of Pharmacology Niigata College Of Pharmacy
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Takada Yoko
Department Of Applied Chemistry Faculty Of Science And Engineering Kinki University
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Sugiyama Eri
Department Of Pharmacology Niigata College Of Pharmacy
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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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Namikawa Tomoko
Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.
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Maruyama Keiko
Department Of Clinical Laboratory Science Kanazawa University Graduate School Kanazawa University
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