Effects of Sarpogrelate, a Novel 5-HT_2 Antagonist, on 5-HT-Induced Endothelium-Dependent Relaxations in Porcine Coronary Artery

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概要

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• The aim of the present study was to examine the effects of sarpogrelate, a 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxation in isolated porcine coronary artery preincubated with ketanserin (3 × 10−6 M) and precontracted by U 46619 (5 × 10−9 M) and compare its effects with other 5-HT2 antagonists such as ritanserin and cyproheptadine. The investigation showed that sarpogrelate (10−7 – 10−5 M) had a weak antagonistic effect on 5-HT-induced relaxation and its effect was weaker than that of ritanserin (10−9 – 10−7 M) and cyproheptadine (10−8 – 10−6 M). The rank order of the antagonistic effects was: ritanserin > cyproheptadine > sarpogrelate. The study also showed that both sarpogrelate and ritanserin had no inhibitory effect on bradykinin-induced relaxation. In our previous study, we investigated the binding affinity of sarpogrelate, ritanserin and cyproheptadine to the 5-HT2A-receptor in rabbit cerebral cortex membranes and the pKi values found were 7.22, 8.98 and 7.54, respectively (M. Rashid et al., Jpn J Pharmacol 87, 189 – 194, 2001). Rank order of the calculated ratio of concentration of pA2 or pD′2 vs Ki was: sarpogrelate > ritanserin > cyproheptadine. Thus, these findings suggest that sarpogrelate has the lowest antagonistic effect on 5-HT-induced endothelium-dependent relaxation and the highest selectivity towards 5-HT2A receptor and might also be the safest drug with respect to its clinical implications in comparison with ritanserin and cyproheptadine.

• 社団法人 日本薬理学会の論文
• 2002-08-01

著者

• Nakazawa Mikio

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

• 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

• 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

• 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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