Author/Authors :
Takahide Nishi، نويسنده , , Tetsuya Fukazawa، نويسنده , , Koki Ishibashi، نويسنده , , Katsuyoshi Nakajima، نويسنده , , Yuki Sugioka، نويسنده , , Yukiko Iio، نويسنده , , Hitoshi Kurata، نويسنده , , Kazuhiro Itoh، نويسنده , , Osamu Mukaiyama، نويسنده , , Yumiko Satoh، نويسنده , , Takeshi Yamaguchi، نويسنده ,
Abstract :
We report herein the synthesis and structure-activity relationships of a series of novel oxazolidine analogues with regards to NK1 and NK2 tachykinin receptor binding affinity. Among this series of oxazolidine analogues, some compounds exhibited excellent high binding affinities for both NK1 and NK2 receptors. In addition, we describe the inhibitory effect in vivo on SP-induced airway vascular hyperpermeability and NKA-induced bronchoconstriction in guinea pigs.