Inhibitory Effects of a Newly Synthesized 5-HT_2 Receptor Antagonist, AT-1015 (N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)piperidino]-ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), on Contraction and Relaxation of Pig Coronary

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概要

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• Inhibitory effects of a newly synthesized 5-HT_2 receptor antagonist, AT-1015 (N-[2-[4-(5H-dibenzo[a, d]cyclohepten-5-ylidene)piperidino]ethyl]-1-formyl-4-piperidinecarboxamide monohydrochloride monohydrate) on contraction and relaxation of coronary arteries of pig hearts mediated by 5-HT_2 subtypes were evaluated and these results were compared with those of ketanserin. Contraction and relaxation were determined by adding 5-HT or α-methylserotonin (α-Me-5-HT) as agonists. Although ketanserin induced rightward shifts of contraction, AT-1015 inhibited the maximal response. In addition, ketanserin inhibited relaxation induced by high concentration of agonists, but there were no inhibitory effects of AT-1015 on relaxation. Thus, these results suggest that AT-1015 is a strong non-competitive 5-HT_2 antagonist in porcine coronary arteries and that this drug clearly exhibited different effects on the contraction and relaxation of coronary arteries of pig hearts from those of ketanserin.

• 公益社団法人日本薬学会の論文
• 2000-09-01

著者

• Nakamura Takashi

  Department of Cardiology, Saiseikai Shigaken Hospital

• 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

• Hattori K

  Niigata Coll. Pharmacy Niigata Jpn

• Hattori Kaoru

  Department Of Cardiology Miki City Hospital

• Hattori Kaoru

  新潟薬科大学 薬理

• 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

• YOSHIMOTO Ryota

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.

• 長友 孝文

  新潟薬科大学・薬・薬理

• 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

• Hattori K

  Tohoku Univ. Sendai Jpn

• 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

• GONG Haibin

  Department of Pharmacology, Niigata College of Pharmacy

• KIHARA Hideaki

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.,

• Gong Haibin

  Department Of Pharmacology Niigata College Of Pharmacy

• Kihara Hideaki

  Pharmaceutical Research Laboratories Ajinomoto Co. Inc.

• Nagatomo Takafumi

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

• Yoshimoto Ryota

  Pharmaceutical Research Laboratories Ajinomoto Co. Inc.

• Nakamura Takashi

  Department Of Cardiology Saiseikai Shiga Hospital

• Hattori Kaoru

  Department of Pharmacology, Niigata College of Pharmacy

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