The effect of intrathecal administration of RP67580, a potent neurokinin 1 antagonist on nociceptive transmission in the rat spinal cord.
The effect of intrathecal application of the selective neurokinin 1 (NK1) receptor antagonist RP67580 and its enantiomer RP68651 was studied on the responses of dorsal horn nociceptive neurones to formalin in the rat. The first and second phases of the formalin response were inhibited by RP67580 in a dose-related manner (1-10 micrograms), whereas RP68651 (5 micrograms) facilitated the second phase of the response. The same doses of RP67580 had minimal effects on the acute C-fibre responses. The NK1 receptor appears to play a role in prolonged nociceptive transmission in the spinal cord.
Chapman
V
V
Department of Pharmacology, University College London, UK.
Dickenson
A H
AH
D000818:Animals; D004305:Dose-Response Relationship, Drug; D005557:Formaldehyde / Q000633:toxicity; D007211:Indoles / Q000494:pharmacology*; D007278:Injections, Spinal; D054833:Isoindoles; D008297:Male; D009412:Nerve Fibers / Q000187:drug effects*; D064729:Neurokinin-1 Receptor Antagonists; D010146:Pain / Q000139:chemically induced / Q000503:physiopathology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013116:Spinal Cord / Q000187:drug effects* / Q000503:physiopathology; D009435:Synaptic Transmission / Q000187:drug effects
D007211:Indoles; D054833:Isoindoles; D064729:Neurokinin-1 Receptor Antagonists; C071693:7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one; D005557:Formaldehyde