Effect of a novel tachykinin NK-2-receptor antagonist, TAC-363, on bronchoconstriction and airway hyperresponsiveness in guinea pigs.
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- HIGASHIDE Yasushi
- Pharmaceuticals Research Laboratories, Fujirebio, Inc.
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- YATABE Yoriko
- Pharmaceuticals Research Laboratories, Fujirebio, Inc.
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- ARAI Yoko
- Pharmaceuticals Research Laboratories, Fujirebio, Inc.
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- SHIBATA Masahiro
- Pharmaceuticals Research Laboratories, Fujirebio, Inc.
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- YAMAURA Tetsuaki
- Pharmaceuticals Research Laboratories, Fujirebio, Inc.
Bibliographic Information
- Other Title
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- 新規タキキニンNK‐2受容体きっ抗薬,TAC‐363のモルモット気道収縮反応および気道過敏性に対する作用
- シンキ タキキニン NK-2 ジュヨウタイ キッコウヤク TAC-363 ノ
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Abstract
We examined the effect of a novel tachykinin NK-2-receptor antagonist, Nα-(tert-Butylcarbamoyl)-L-glutaminyl-L-tryptophyl-α-aza-phenylalanine 2-benzyloxyethylamide (TAC-363), on hyperventilation- and citric acid-induced bronchoconstriction and neurokinin A (NKA)-, capsaicin- and antigen-induced airway hyperresponsiveness in guinea pigs. The i.v. administration of TAC-363 at doses of 0.01-1 mg/kg inhibited hyperventilation- and citric acid-induced bronchoconstriction in a dose-dependent manner, while FK-888, a tachykinin NK-1-receptor antagonist, did not inhibit hyperventilation-induced bronchoconstriction. NKA-induced airway hyperresponsiveness to acetylcholine was attenuated by i.v. injection of TAC-363, but not by the thromboxane A2 synthetase inhibitor ozagrel and the mast cell stabilizer DSCG. Furthermore, TAC-363 prevented the occurrence of capsaicin- and antigen-induced airway hyperresponsiveness to acetylcholine, while FK-888 did not prevent occurrence of capsaicin-induced airway hyperresponsiveness. In summary, TAC-363 inhibits bronchoconstriction and airway hyperresponsiveness induced by various stimuli. These results suggest that NKA mediates bronchoconstriction and airway hyperresponsiveness. Thus, TAC-363 is expected to be useful in the treatment of airway diseases such as asthma.
Journal
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- Folia Pharmacologica Japonica
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Folia Pharmacologica Japonica 109 (1), 19-29, 1997
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390001204271968896
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- NII Article ID
- 10004946816
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- NII Book ID
- AN00198335
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- COI
- 1:CAS:528:DyaK2sXjtlGiug%3D%3D
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- ISSN
- 13478397
- 00155691
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- NDL BIB ID
- 4108026
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- PubMed
- 9067996
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- Text Lang
- ja
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed