Pharmacological Characteristics of Inhibitory Action of the Selective .ALPHA.1-Antagonist JTH-601 on the Positive Inotropic Effect Mediated by .ALPHA.1-Adrenoceptors in Isolated Rabbit Papillary Muscle.
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- Qiao Xiaoying
- Department of Pharmacology, Yamagata University School of Medicine, 2-2-2 lida-nishi, Yamagata 990-9585, Japan
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- Norota Ikuo
- Department of Pharmacology, Yamagata University School of Medicine, 2-2-2 lida-nishi, Yamagata 990-9585, Japan
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- Endoh Masao
- Department of Pharmacology, Yamagata University School of Medicine, 2-2-2 lida-nishi, Yamagata 990-9585, Japan
Bibliographic Information
- Other Title
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- Pharmacological Characteristics of Inhibitory Action of the Selective α1-Antagonist JTH-601 on the Positive Inotropic Effect Mediated by α1-Adrenoceptors in Isolated Rabbit Papillary Muscle
- Pharmacological Characteristics of Inhibitory Action of the Selective アルファ 1 Antagonist JTH 601 on the Positive Inotropic Effect Mediated by アルファ 1 Adrenoceptors in Isolated Rabbit Papillary Muscle
- Pharmacological Characteristics of Inhibitory Action of the Selective α1-Antagonist JTH-601 on the Positive Inotropic Effect Mediated by α1-drenoceptors in Isolated Rabbit Papillary Muscle
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Abstract
Influence of JTH-601 [N-(3-hydroxy-6-methoxy-2, 4, 5-trimethylbenzyl)-N-methyl-2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethylamine hemifumarate], a selective α1-adrenoceptor antagonist, on α1-mediated positive inotropic effect (PIE) was studied in isolated rabbit papillary muscle (1 Hz at 37°C). JTH-601 (0.1-10 μM) shifted the concentration-response curve (CRC) for PIE of phenylephrine mediated by α1-adrenoceptor (with timolol at 1 μM) to the right and downward. In the presence of 100 nM WB 4101, an α1A antagonist, the shift to the right disappeared and JTH-601 (1-3 μM) shifted CRC for phenylephrine downward. The antagonistic action of JTH-601 was unchanged by 100 nM (+)-niguldipine, another α1A antagonist. Following pretreatment with 10 μM chloroethylclonidine, an α1B antagonist, the shift of CRC for phenylephrine to the right disappeared and JTH-601 (3-10 μM) shifted CRC downward. Antagonistic action of JTH-601 (3 μM) was unaltered by 100 nM BMY 7378, an α1D antagonist. JTH-601 (10 μM) had no effect on β-mediated PIE of isoproterenol. These results indicate that JTH-601 exerts an inhibitory action on α1-mediated PIE through antagonism of α1A- and/or α1B-adrenoceptors in rabbit ventricular myocardium. As an α1 antagonist, JTH-601 is much less potent in rabbit ventricular muscle than in smooth muscle.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 84 (3), 301-309, 2000
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390001204287833472
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- NII Article ID
- 10008186202
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DC%2BD3cXosVKiu7c%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 5586895
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- PubMed
- 11138731
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- Web Site
- https://ndlsearch.ndl.go.jp/books/R000000004-I5586895
- https://api.elsevier.com/content/article/PII:S0021519819305104?httpAccept=text/xml
- https://api.elsevier.com/content/article/PII:S0021519819305104?httpAccept=text/plain
- https://www.jstage.jst.go.jp/article/jjp/84/3/84_3_301/_pdf
- https://search.jamas.or.jp/link/ui/2001072956
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed