We previously reported that OT-7100 (5-n-butyl-7-(3,4,5-trimethoxybenzoylam
ino)pyrazolo[1,5-alpha-]pyrimidine) had antinociceptive potency in various
animal models. To further characterize this compound, the present study exa
mined the effects of OT-7100 on mechanical hyperalgesia and motor nerve con
duction velocity in streptozotocin-induced diabetic rats. OT-7100 significa
ntly increased the nociceptive threshold in the diabetic rat in a dose-depe
ndent manner. Gabapentin (anticonvulsant agent) and insulin strongly increa
sed the nociceptive threshold but gabapentin increased it above normal leve
ls. An aldose reductase inhibitor slightly increased the nociceptive thresh
old at a high dose. We also measured glucose levels and motor nerve conduct
ion velocity in OT-7100-treated rats. Insulin decreased glucose levels but
OT-7100 had no effect on glucose levels or on motor nerve conduction veloci
ty. These results suggest that OT-7100 alleviates hyperalgesia in a diabeti
c neuropathy model in a different manner from gabapentin or aldose reductas
e inhibitor and may be a new treatment for the pain associated with periphe
ral nerve injury. (C) 2001 Elsevier Science BN. All rights reserved.