"Calcium entry blockers" as cerebral protecting agents: Comparative activity in tests of hypoxia and hyperexcitability.
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- WAUQUIER Albert
- Department of Neuropharmacology, Janssen Pharmaceutica
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- ASHTON David
- Department of Neuropharmacology, Janssen Pharmaceutica
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- CLINCKE Gilbert
- Department of Neuropharmacology, Janssen Pharmaceutica
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- FRANSEN Johannes
- Department of Neuropharmacology, Janssen Pharmaceutica
書誌事項
- 公開日
- 1985
- 資源種別
- journal article
- DOI
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- 10.1254/jjp.38.1
- 公開者
- 公益社団法人 日本薬理学会
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説明
The group of drugs described as “Ca2+-entry blockers” is chemically and pharmacologically heterogenous. It is believed now that these drugs are useful in the treatment of ischemic disease. In an effort to define which drugs could offer the best therapeutic alternative, a comparative pharmacological study was made. Nine drugs (D-600 diltiazem, flunarizine, nicardipine, nifedipine, nimodipine, nitrendipine, verapamil, tiapamil) were tested in experimental screening models of brain hypoxia, ischemia, cellular intoxication and against bicucullineinduced seizures. Three types of activity were found. Verapamil, D-600, tiapamil and diltiazem were almost inactive, possibly due to their poor brain penetration. The dihydropyridines had a broad spectrum of activity, but considerable differences between these compounds exist. They all were active against hypoxia and less active against ischemia. Out of this subgroup, only nicardipine protected against metabolic intoxication and nifedipine and nicardipine could block seizure components at very high doses. Flunarizine was the only compound with a doserelated effect in all the tests. These results suggested that this combination of screening tests could be used to find compounds with an interesting activity in the field of cerebral protection.
収録刊行物
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- Jpn.J.Pharmacol.
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Jpn.J.Pharmacol. 38 (1), 1-7, 1985
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390001204287783040
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- NII論文ID
- 130000834907
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- NII書誌ID
- AA00691188
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- DOI
- 10.1254/jjp.38.1
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- COI
- 1:CAS:528:DyaL2MXhvFOkurk%3D
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- ISSN
- 13473506
- 00215198
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- PubMed
- 4021225
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- 本文言語コード
- en
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- 資料種別
- journal article
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
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