Improvement of Pulmonary Function by Oral Treatment with a VLA-4 Antagonist in a Mouse Asthmatic Model

We investigated in vivo efficacies of the newly synthesized VLA-4 antagonist Compound A {trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid} on Ascaris antigen-induced airway inflammation and hyperresponsiveness...

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主要な著者: Gensuke Takayama (著者), Keiko Matsumoto (著者), Tomoe Taira (著者), Misato Aonuma (著者), Mika Yokoyama (著者), Yutaka Iigo (著者), Tohru Takashi (著者)
フォーマット: 図書
出版事項: Elsevier, 2013-01-01T00:00:00Z.
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要約:We investigated in vivo efficacies of the newly synthesized VLA-4 antagonist Compound A {trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid} on Ascaris antigen-induced airway inflammation and hyperresponsiveness in a murine asthmatic model. Oral administration of Compound A significantly inhibited eosinophil infiltration into BALF and airway hyperresponsiveness 48 h after the antigen challenge. Histologic analysis of the lung sections confirmed the BALF result and revealed suppression of edema and mucus hyperplasia at 8 and 48 h after the challenge, respectively. These findings clearly show that orally active Compound A has therapeutic potential for treatment of asthma. Keywords:: VLA-4, eosinophil, airway hyperresponsiveness
記述事項:1347-8613
10.1254/jphs.12198SC