(+/-)-CP-96,345, an NK1 receptor antagonist, has local anaesthetic-like effects in a mammalian sciatic nerve preparation.
The effect of the non-peptide NK1 receptor antagonist (+/-)-CP-96,345 was investigated on the compound action potential (cAP) recorded in the isolated guinea-pig nerve, and compared to the effects of the local anaesthetic lidocaine and the L-type Ca2+ channel antagonist diltiazem. (+/-)-CP-96,345, as well as lidocaine and diltiazem, produced a concentration dependent reduction of the cAP amplitude. All three drugs showed frequency dependent block. The block of the cAP by lidocaine was fully reversible at all concentrations tested, while the block by (+/-)-CP-96,345 and diltiazem were only partly reversible at higher concentrations. The present findings indicate that (+/-)-CP-96,345 exerts a local anaesthetic-like effect on nerve conduction.
Karlsson
U
U
Näsström
J
J
Berge
O G
OG
D000200:Action Potentials / Q000187:drug effects; D000704:Analysis of Variance; D000818:Animals; D001713:Biphenyl Compounds / Q000494:pharmacology*; D004110:Diltiazem / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006993:Hypnotics and Sedatives / Q000494:pharmacology*; D066298:In Vitro Techniques; D008012:Lidocaine / Q000494:pharmacology; D008297:Male; D009407:Nerve Block; D009431:Neural Conduction / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists; D012584:Sciatic Nerve / Q000187:drug effects*
D001713:Biphenyl Compounds; D006993:Hypnotics and Sedatives; D064729:Neurokinin-1 Receptor Antagonists; D008012:Lidocaine; D004110:Diltiazem; C066892:CP 96345