FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity.

@article{Morimoto1992FK2A,
  title={FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity.},
  author={Hiroshi Morimoto and Masatoshi Murai and Yasue Maeda and Michiyo Yamaoka and Mitsunori Nishikawa and S Kiyotoh and Toshihide Fujii},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1992},
  volume={262 1},
  pages={398-402}
}
We have discovered a novel cyclopeptide substance P (SP) antagonist, FK 224 (N-[N2-[N-[N-[N-[2,3-didehydro-N-methyl-N-[N-[3-(2-pentylphenyl )- propionyl]-L-threonyl]tyrosyl-L-leucynyl]-D-phenylalanyl]-L-allo- threonyl]-L-asparaginyl]-L-serine-nu-lactone), which inhibited [3H]SP binding to guinea pig lung membranes in a dose-dependent manner. According to Rosenthal analysis, the inhibitory effect of FK 224 on [3H]SP binding appears to be competitive. In order to clarify the receptor subtype… CONTINUE READING
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