(-)-Enantiomer EMD 57439 Antagonizes the Ca2+ Sensitizing Effect of (+)-Enantiomer EMD 57033 0n Diastolic Function but Not on Systolic Function in Rabbit Ventricular Cardiomyocytes

• Sugawara Hiromi

  Department of Pharmacology, Yamagata University School of Medicine

• Endoh Masao

  Department of Pharmacology, Yamagata University School of Medicine

書誌事項

タイトル別名

• (-)-Enantiomer EMD 57439 Antagonizes the Ca2+ Sensitizing Effect of (+)-Enantiomer EMD 57033 on Diastolic Function but Not on Systolic Function in Rabbit Ventricular Cardomyocytes.
• Enantiomer EMD 57439 Antagonizes the Ca2 Sensitizing Effect of Enantiomer EMD 57033
• (−)-Enantiomer EMD 57439 Antagonizes the Ca2+ Sensitizing Effect of (+)-Enantiomer EMD 57033 on Diastolic Function but Not on Systolic Function in Rabbit Ventricular Cardiomyocytes

抄録

EMD 53998 (5-[1-(3, 4-dimethoxybenzoyl)-1, 2, 3, 4-tetrahydro-6-quinolyl]-6-methyl-3, 6-dihydro-2H-1, 3, 4-thiadiazin-2-one), the racemic mixture of (+)-enantiomer EMD 57033 and (-)-enantiomer EMD 57439, is a prototype of Ca²⁺ sensitizers that act via a central and/or down-stream mechanism in cardiac E-C coupling. In rabbit ventricular cardiomyocytes loaded with indo-1/AM, EMD 53998 and EMD 57033 shifted the relationship between Ca²⁺ transients and cell shortening (systolic function) to the left to the same extent as compared with that of elevation of [Ca²⁺]_o. EMD 57439 did not elicit a positive inotropic effect (PIE). The PIE of EMD 57033 was associated with a more pronounced decrease in the diastolic cell length than that of EMD 53998, whereas the systolic effects of these compounds were equivalent. These results indicate that weak phosphodiesterase (PDE) III inhibition may exert a differential action on diastolic and systolic function. Thus, EMD 57439 antagonizes the Ca²⁺-sensitizing effect of EMD 57033 on diastolic function with no effect on systolic function, which may lead to a decease in diastolic cell length of a lesser extent with the racemate EMD 53998 compared with (+)-enantiomer EMD 57033.

収録刊行物

• Jpn.J.Pharmacol.

  Jpn.J.Pharmacol. 80 (1), 55-65, 1999

  公益社団法人 日本薬理学会

キーワード

• EMD 53998
• EMD 57033
• Ca<SUP>2+</SUP> transient
• Ca<SUP>2+</SUP> sensitizer
• Rabbit ventricular cardiomyocyte

詳細情報

• CRID: 1390282679261752320
• NII論文ID: 10008194606
• NII書誌ID: AA00691188
• DOI: 10.1254/jjp.80.55
• COI: 1:CAS:528:DyaK1MXjtlGis7w%3D
• ISSN: 13473506
• ISSN: 00215198
• NDL書誌ID: 4733125
• PubMed: 10446757
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I4733125
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819308893?httpAccept=text/xml
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819308893?httpAccept=text/plain
• Web Site: https://www.jstage.jst.go.jp/article/jjp/80/1/80_1_55/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1999225802
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
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