Effect of YM-44781, YM-44778 and YM-49598, Novel Tachykinin Antagonists, in a Drug-Induced Bladder Contraction Model

@article{Choppin2002EffectOY,
  title={Effect of YM-44781, YM-44778 and YM-49598, Novel Tachykinin Antagonists, in a Drug-Induced Bladder Contraction Model},
  author={Agnes Choppin and Gretchen Groke and Analyn Bringas and George J Stepan and Michael Patrick Dillon},
  journal={Pharmacology},
  year={2002},
  volume={65},
  pages={96 - 102}
}
The radioligand binding profiles and in vivo pharmacological characteristics of YM-44781, YM-44778 and YM-49598, novel non-peptide tachykinin receptor antagonists, were examined and compared to those of FK-888 and GR-159897. Since no functional NK<sub>3</sub> receptors were found in the rat bladder, the emphasis will be on the other two subtypes. YM-44781 and YM-49598 exhibited high binding affinities at NK<sub>2</sub> (pK<sub>i</sub> = 9.94 ± 0.03) and NK<sub>1</sub> (pK<sub>i</sub> = 9.09 ± 0… 

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