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Chemical Compound Review

SureCN678696     (2R,3S)-1-[[2-methoxy-5...

Synonyms: AG-D-89772, KB-62486, CTK4C4679, DNC000470, LS-113868, ...
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Disease relevance of Cp 122721

  • RESULTS: In the initial dose-ranging study, only 10% of the patients experienced emesis within the first 8 h after surgery with CP-122,721 200 mg compared with 50% in the placebo group [1].
  • In addition, the median times for 75% of patients to remain free from postoperative nausea and vomiting were 82, 75, and 362 min in the ondansetron, CP-122,721, and combination groups, respectively [1].
  • In addition, consistent with insurmountable blockade observed in vitro, CP-122,721 (0.01, 0.03 0.3 mg/kg, p.o.) produced a rightward shift in the dose response curve for SP-induced hypotension in the awake dog that was accompanied by a decrease in the maximal response [2].

Psychiatry related information on Cp 122721


High impact information on Cp 122721


Biological context of Cp 122721


Anatomical context of Cp 122721

  • Results show that treatment with CP-122,721 significantly increased SP-encoding mRNA and NK-1R mRNA levels in the striatum, but not in the hindbrain [4].

Gene context of Cp 122721


Analytical, diagnostic and therapeutic context of Cp 122721


  1. Substance P (Neurokinin-1) antagonist prevents postoperative vomiting after abdominal hysterectomy procedures. Gesztesi, Z., Scuderi, P.E., White, P.F., Wright, W., Wender, R.H., D'Angelo, R., Black, L.S., Dalby, P.L., MacLean, D. Anesthesiology (2000) [Pubmed]
  2. Characterization of CP-122,721; a nonpeptide antagonist of the neurokinin NK1 receptor. McLean, S., Ganong, A., Seymour, P.A., Bryce, D.K., Crawford, R.T., Morrone, J., Reynolds, L.S., Schmidt, A.W., Zorn, S., Watson, J., Fossa, A., DePasquale, M., Rosen, T., Nagahisa, A., Tsuchiya, M., Heym, J. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  3. The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Varty, G.B., Cohen-Williams, M.E., Morgan, C.A., Pylak, U., Duffy, R.A., Lachowicz, J.E., Carey, G.J., Coffin, V.L. Neuropsychopharmacology (2002) [Pubmed]
  4. Chronic non-peptide neurokinin receptor antagonist treatment alters striatal tachykinin peptide and receptor gene expression in the rat. McCarson, K.E., Krause, J.E., McLean, S. Neurosci. Lett. (1998) [Pubmed]
  5. Metabolism, pharmacokinetics and excretion of a potent tachykinin NK1 receptor antagonist (CP-122,721) in rat: characterization of a novel oxidative pathway. Kamel, A., Davis, J., Potchoiba, M.J., Prakash, C. Xenobiotica (2006) [Pubmed]
  6. Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist. Rosen, T.J., Coffman, K.J., McLean, S., Crawford, R.T., Bryce, D.K., Gohda, Y., Tsuchiya, M., Nagahisa, A., Nakane, M., Lowe, J.A. Bioorg. Med. Chem. Lett. (1998) [Pubmed]
  7. Broad spectrum antiemetic effects of CP-122,721, a tachykinin NK1 receptor antagonist, in ferrets. Gonsalves, S., Watson, J., Ashton, C. Eur. J. Pharmacol. (1996) [Pubmed]
  8. Diphenidol has no actual broad antiemetic activity in dogs and ferrets. Nakayama, H., Yamakuni, H., Nakayama, A., Maeda, Y., Imazumi, K., Matsuo, M., Mutoh, S. J. Pharmacol. Sci. (2004) [Pubmed]
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