British Journal of Pharmacology · 1992 · 57 citations · 10 references
MedicineMedicinal ChemistryPharmacologyInflammationPain MedicinePain ScienceAnalgesiaAnalgesic PharmacologyAnti-inflammatory PharmacologyInflammatory PainInflammatory ProcessesNociceptive PainAnalgesic Anti-inflammatory PharmacologyAnalgesic Drug MechanismsAnimal Disease ModelsAnti-inflammatory ResponseInflammatory Pain ModulationPain Inflammation PharmacologyPain PharmacologyReceptor-mediated Analgesia
The non-peptide NK1 receptor antagonist, CP-96,345, and its 2R,3R enantiomer CP-96,344, which is not an NK1 receptor antagonist (IC50 > 10 microM), were evaluated for antinociceptive and anti-inflammatory activities in several classical models of pain and inflammation in the rat. Both CP-96,345 and CP-96,344 reduced carrageenin-induced paw oedema and hyperalgesia, and attenuated the second phase of formalin-induced paw licking with equal potency. These results indicate that NK1 antagonism is not responsible for the activity of (+/-)-CP-96,345 in the above animal models.
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A Potent Nonpeptide Antagonist of the Substance P (NK <sub>1</sub> ) Receptor
R. Michael Snider, Jay W. Constantine, John Lowe et al. · Science · 1991 · 864 citations