Antinociceptive activity of CP‐101,606, an NMDA receptor NR2B subunit antagonist

1 The analgesic activity of CP‐101,606, an NR2B subunit‐selective N‐methyl‐D‐aspartate (NMDA) receptor antagonist, was examined in carrageenan‐induced hyperalgesia, capsaicin‐ and 4β‐phorbol‐12‐myristate‐13‐acetate (PMA)‐induced nociceptive tests in the rat. 2 CP‐101,606 30 mg kg−1, s.c., at 0.5 and...

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Bibliographic Details
Published in:British journal of pharmacology 1997-11, Vol.122 (5), p.809-812
Main Authors: Taniguchi, Kana, Shinjo, Katsuhiro, Mizutani, Mayumi, Shimada, Kaoru, Ishikawa, Toshihisa, Menniti, Frank S., Nagahisa, Atsushi
Format: Article
Language:English
Subjects:
Analgesics
Analgesics, Non-Narcotic - administration & dosage
Analgesics, Non-Narcotic - pharmacology
Animals
Biological and medical sciences
Brain - metabolism
Capsaicin
Carrageenan
CP‐101,606
Excitatory Amino Acid Antagonists - blood
Excitatory Amino Acid Antagonists - cerebrospinal fluid
Excitatory Amino Acid Antagonists - metabolism
Excitatory Amino Acid Antagonists - pharmacology
hyperalgesia
Hyperalgesia - chemically induced
Hyperalgesia - drug therapy
Injections, Subcutaneous
Male
Medical sciences
Motor Activity - drug effects
Neuropharmacology
NMDA receptor antagonist
nociception
Pain Measurement
Pharmacology. Drug treatments
Piperidines - blood
Piperidines - cerebrospinal fluid
Piperidines - metabolism
Piperidines - pharmacology
Rats
Rats, Sprague-Dawley
Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors
Spinal Cord - metabolism
Tetradecanoylphorbol Acetate
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Summary:1 The analgesic activity of CP‐101,606, an NR2B subunit‐selective N‐methyl‐D‐aspartate (NMDA) receptor antagonist, was examined in carrageenan‐induced hyperalgesia, capsaicin‐ and 4β‐phorbol‐12‐myristate‐13‐acetate (PMA)‐induced nociceptive tests in the rat. 2 CP‐101,606 30 mg kg−1, s.c., at 0.5 and 2.5 h after carrageenan challenge suppressed mechanical hyperalgesia without any apparant alternations in motor coordination or behaviour in the rat. 3 CP‐101,606 also inhibited capsaicin‐ and PMA‐induced nociceptive responses (licking behaviour) with ED50 values of 7.5 and 5.7 mg kg−1, s.c., respectively. 4 These results suggest that inhibition of the NR2B subunit of the NMDA receptor is effective in vivo at modulating nociception and hyperalgesia responses without causing the behavioural side effects often observed with currently available NMDA receptor antagonists. British Journal of Pharmacology (1997) 122, 809–812; doi:10.1038/sj.bjp.0701445
ISSN:0007-1188
1476-5381
DOI:10.1038/sj.bjp.0701445