Binding Affinity of a Newly Synthesized 5-HT_2 Antagonist, AT-1015(N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), in the Rabbit Platelet Membrane

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概要

• 論文の詳細を見る

• The object of this study was to investigate the binding affinity of a newly synthesized 5-HT_2 antagonist, (N-[2-[4-(5H-dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide monohydrochloride monohydrate)(AT-1015), in the rabbit platelet membrane using [^3H]-ketanserin by radioligand binding assay method and to compare the results with other selective 5-HT_2 antagonists. The results showed that AT-1015 displayed high affinity to 5-HT_2 receptors in rabbit platelet membranes. The pK_i value of AT-1015 was 7.40, which is slightly lower than that of ketanserin, but higher than that of cyproheptadine. On the other hand, the displacement potency of AT-1015 for 5-HT_2 receptors in rabbit platelets was similar to those of sarpogrelate and ritanserin. This is the first report of the high affinity of AT-1015 in rabbit platelets.

• 公益社団法人日本薬学会の論文
• 2001-10-01

著者

• Nakazawa Mikio

  Department of Medical Technology, School of Health Sciences, Faculty of Medicine, Niigata University

• 渡辺 光男

  Hamamatsu Photonics K. K.

• NAGATOMO Takafumi

  Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences

• 長友 孝文

  新潟薬科大学薬学部薬理学教室

• RASHID Mamunur

  Department of Pharmacology, Niigata College of Pharmacy

• Rashid M

  Department Of Cardiovascular Medicine Graduate School Of Medicine Tohoku University

• Rashid Mamunur

  Dep. Of Cardiovascular Medicine Graduate School Of Medicine Tohoku Univ. Jpn

• Nakazawa M

  Departement Of Medical Technology School Of Health Sciences Faculty Of Medicine Niigata University

• WATANABE Masatomo

  Department of Public Health, Niigata College of Medical Technology

• Watanabe M

  Faculty Of Pharmacy And Pharmaceutical Sciences Fukuyama University

• Nagatomo T

  Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie

• Rashid Mamunur

  Pharmaceutical Microbiology Research Laboratory Department Of Pharmacy University Of Rajshahi

• Watanabe M

  Department Of Public Health Niigata College Of Medical Technology

• Rashid Mamunur

  Department Of Cardiovascular Medicine Graduate School Of Medicine Tohoku University

• Nakazawa Mikio

  Departement Of Medical Technology School Of Health Sciences Faculty Of Medicine Niigata University

• Nagatomo Takafumi

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

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