Assessment of Affinities and Dissociation Potencies of Several 5-HT_2 Antagonists to and from M_2 Muscarinic Receptor in Rat Heart Membranes(Pharmacology)

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概要

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• The aim of the present study was to investigate the binding affinities and dissociation potencies of several 5-HT_2 antagonists in M_2 muscarinic receptor of rat heart membranes using [^3H]QNB as a radioligand. The 5-HT_2 antagonists used in this study were sarpogrelate, ketanserin and cyproheptadine. The results showed that sarpogrelate and ketanserin had very weak binding affinities to M_2 muscarinic receptor, whereas cyproheptadine had higher binding affinity to this receptor than the muscarinic receptor antagonist, atropine. All of these three 5-HT_2 antagonists as well as muscarinic receptor antagonists (atropine and pirenzepine) were readily dissociated from M_2 muscarinic receptor in rat heart membranes after washing. Therefore, the findings of the present investigation suggest that the dissociation potencies of neither 5-HT_2 antagonists nor muscarinic antagonists used correlate with their binding affinities to M_2 muscarinic receptors in rat heart.

• 社団法人日本薬学会の論文
• 2003-08-01

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

• Ozaki Masanobu

  Department Of Cardiology Fukuoka University School Of Medicine

• Ozaki Masanobu

  Department Of Toxicology Niigata College Of Pharmacy

• MUNTASIR Habib

  Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and A

• OZAKI Masanobu

  Experimental Animal Center, Niigata University of Pharmacy and Applied Life Sciences

• 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

• Muntasir Habib

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

• 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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