Effects of Novel Pyridothiazepines and Pyridothiazines on Contractility of Isolated Guinea-Pig Heart Muscle and Vascular Smooth Muscle Preparations.
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説明
The effects of newly synthesized pyridothiazepines MM 4 (1-[N-[2-(3, 4-dimethoxy-phenyl)ethyl]-N-methyl-aminoacetyl]-1, 2, 3, 4-tetrahydro-pyrido[2, 3-b][1, 4]thiazepine fumarate), MM 6 (1-[N-[2-(3, 4-dimethoxyphenyl)-ethyl]-N-methylaminopropionyl]-1, 2, 3, 4-tetrahydro-pyrido[2, 3-b][1, 4] thiazepine fumarate) and the novel pyridothiazines MM 10 (2, 3-dihydro-1-[N-[2-(3, 4-dimethoxypheny)ethyl]-N-methylaminoacetyl]-1H-pyrido[2, 3-b]-[1, 4]thiazine fumarate) and MM 11 (2, 3-dihydro-1-[N-[2-(3, 4-dimethoxy-phenyl)ethyl-N-methylaminopropionyl]-1H-pyrido[2, 3-b][1, 4]thiazine fumarate) on the contracility of isolated papillary muscles and aortic preparations of guinea pigs were studied using isometric contraction force measurements. The EC50values for the negative inotropic effect were 27 μmol/l MM 4), 19 μmol/l (MM 6), 32 μmol/l (MM 10) and 24 μmol/l (MM 11). In K+-precontracted aortic rings ([K+]0 60 mmol/l), the compounds induced relaxation with EC50 values of 27μmol/l (MM 4), 24 μmol/l (MM 6), 84 μmol/l MM 10) and 68 μmol/l (MM 11). Pyridothiazepines as well as pyridothiazines (100 μmoll/l) were able to depress norepinephrine bitartrate (NE 10 μmol/l)-induced contraction of aortic rings in a calcium-free solution. It was concluded that the investigated compounds exert calcium antagonistic properties in both cardiac and smooth muscle. This antagonistic effect be due to the inhibition of transmembrane calcium influx and/or intracellular calcium release.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 22 (7), 683-686, 1999
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204625194368
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- NII論文ID
- 110003639736
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- NII書誌ID
- AA10885497
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- COI
- 1:CAS:528:DyaK1MXks1Ohtr0%3D
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- ISSN
- 13475215
- 09186158
- http://id.crossref.org/issn/09186158
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- NDL書誌ID
- 4801946
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- PubMed
- 10443462
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可