High affinity NK1 antagonist
High affinity NK1 antagonist (pIC50 = 9.8). Suppresses recruitment of immunocytes in respiratory syncytial virus (RSV)-infected rats after capsaicin stimulation. Also blocks substance P-induced excitation of locus ceruleus cells in guinea pig brain slices (IC50 = 7 nM). Exhibits anxiolytic and antidepressant-like effects. Active in vivo.
McLean et al (1996) Characterization of CP-122,721; a nonpeptide antagonist of the neurokinin NK1 receptor. J.Pharmacol.Exp.Ther. 277 900 PMID:8627572 |Gonsalves et al (1996) Broad spectrum antiemetic effects of CP-122,721, a tachykinin NK1 receptor antagonist, in ferrets. Eur.J.Pharmacol. 305 181 PMID:8813551 |Auais et al (2003) Immunomodulatory effects of sensory nerves during respiratory syncytial virus infection in rats. Am.J.Physiol. Lung Cell Mol.Physiol. 285 L105 PMID:12639840
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