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Vol. 71, No. 1, 2004
Issue release date: May 2004
Section title: Original Paper
Pharmacology 2004;71:38–45
(DOI:10.1159/000076260)

DY-9760e, a Novel Calmodulin Antagonist, Reduces Infarction after Permanent Focal Cerebral Ischemia in Rats

Sato T. · Takamori H. · Shirasaki Y.
New Product Research Laboratories II, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 7/16/2003
Accepted: 9/25/2003
Published online: 4/8/2004
Issue release date: May 2004

Number of Print Pages: 8
Number of Figures: 5
Number of Tables: 0

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA

Abstract

DY-9760e (3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate), a novel calmodulin antagonist, provides effective protection against Ca2+ ionophore-induced cytotoxicity and brain injury induced by transient focal ischemia. In this study, we evaluated the effect of DY-9760e on ischemic infarct volume in rats subjected to permanent focal ischemia. DY-9760e (0.5 mg/kg/h for 6 h) significantly reduced the infarct volume when administered immediately after middle cerebral artery occlusion. Furthermore, this neuroprotection was also exerted by treatment with a 3-hour delay, implying that the therapeutic time window for this compound is at least 3 h. In addition, although treatment with 0.1 mg/kg/h for 24 h was ineffective, the combination of a loading dose of 0.3 mg/kg/h for 2 h followed by 0.1 mg/kg/h for 22 h yielded a significant reduction in infarct volume. Thus, prolonged infusion preceded by a loading dose is an efficacious dosing regimen for DY-9760e, especially at a low infusion rate. These data demonstrate the substantial neuroprotective effect of DY-9760e in a permanent focal ischemia model and indicate that this neuroprotectant may be of therapeutic value for the treatment of acute stroke.

© 2004 S. Karger AG, Basel


  

Author Contacts

Yasufumi Shirasaki, PhD
New Product Research Laboratories II, Daiichi Pharmaceutical Co., Ltd.
1-16-13, Kitakasai, Edogawa-Ku
Tokyo 134-8630 (Japan)
Tel. +81 3 3680 0151, Fax +81 3 5696 8718, E-Mail shiram8s@daiichipharm.co.jp

  

Article Information

Received: July 16, 2003
Accepted: September 25, 2003
Number of Print Pages : 8
Number of Figures : 5, Number of Tables : 0, Number of References : 48

  

Publication Details

Pharmacology (International Journal of Experimental and Clinical Pharmacology)
Founded 1959 as ‘Medicina Experimentalis’, continued 1965–1967 as ‘Medicina et Pharmacologia Experimentalis’; Founder: R. Domenjoz (1959–1977); Successors: B.B. Brodie (1968–1977); K. Lederis (1973–1985); K.-F. Sewing (1978–1998); E.S. Vesell (1970–2000)

Vol. 71, No. 1, Year 2004 (Cover Date: May 2004)

Journal Editor: J. Donnerer, Graz; M.L. Billingsley, Hershey, Pa.; T. Iijima, Akita
ISSN: 0031–7012 (print), 1423–0313 (Online)

For additional information: http://www.karger.com/pha


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 7/16/2003
Accepted: 9/25/2003
Published online: 4/8/2004
Issue release date: May 2004

Number of Print Pages: 8
Number of Figures: 5
Number of Tables: 0

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA


Copyright / Drug Dosage

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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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