Non-specific activity of (+/-)-CP-96,345 in models of pain and inflammation.
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.
Nagahisa
A
A
Department of Medicinal Biology, Pfizer Inc., Aichi, Japan.
Asai
R
R
Kanai
Y
Y
Murase
A
A
Tsuchiya-Nakagaki
M
M
Nakagaki
T
T
Shieh
T C
TC
Taniguchi
K
K
D000704:Analysis of Variance; D000818:Animals; D001665:Binding Sites; D001713:Biphenyl Compounds / Q000494:pharmacology*; D004195:Disease Models, Animal; D004487:Edema / Q000139:chemically induced; D007249:Inflammation / Q000188:drug therapy*; D008297:Male; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D051381:Rats; D017207:Rats, Sprague-Dawley; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism
D001713:Biphenyl Compounds; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; C066892:CP 96345