Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.

@article{Hay2002NonpeptideTR,
  title={Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.},
  author={Douglas W. P. Hay and Giuseppe Giardina and Don E. Griswold and David C. Underwood and Charles J. Kotzer and Brian Bush and William Potts and Punam Sandhu and Dave Lundberg and James J. Foley and Dulcie B. Schmidt and Lenox D Martin and David Kilian and Jeffrey J. Legos and Frank Barone and Mark A. Luttmann and Mario Grugni and Luca Francesco Raveglia and Henry M. Sarau},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={300 1},
  pages={314-23}
}
In this report the in vitro and in vivo pharmacological and pharmacokinetic profile of (-)-(S)-N-(alpha-ethylbenzyl)-3-(carboxymethoxy)-2-phenylquinoline-4-carboxamide (SB 235375), a low central nervous system (CNS)-penetrant, human neurokinin-3 (NK-3) receptor (hNK-3R) antagonist, is described. SB 235375 inhibited (125)I-[MePhe(7)]-neurokinin B (NKB) binding to membranes of Chinese hamster ovary (CHO) cells expressing the hNK-3R (CHO-hNK-3R) with a K(i) = 2.2 nM and antagonized competitively… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 21 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 42 references

Functional characterization of the non-peptide neurokinin-3 (NK-3) receptor antagonist, SR 142801 on the human NK-3 receptor expressed in Chinese hamster ovary cells

F Oury-Donat, P Carayon, +4 authors G Le Fur
J Pharmacol Exp Ther 274:148–154 • 1995
View 5 Excerpts
Highly Influenced

Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor.

The Journal of pharmacology and experimental therapeutics • 1993
View 2 Excerpts
Highly Influenced

Similar Papers

Loading similar papers…