NK1 receptors mediate tachykinin-induced plasma extravasation in the rat knee joint

Agents Actions. 1993 Nov;40(3-4):171-5. doi: 10.1007/BF01984057.

Abstract

The tachykinin receptor type that mediates tachykinin-induced plasma extravasation in the rat knee joint was identified by using selective antagonists as well as natural or synthetic agonists. Substance P (SP) and neurokinin (NK) A induced plasma extravasation with almost the same potency and the maximum response was obtained at 5 nmol/knee. NKB was about ten times less potent than SP or NKA. The NK1 selective agonist, [Sar9, Met(O2)11]-SP, was about ten times more potent than SP, and the NK2 selective agonist, [Nle10]-NKA4-10, was about fifty times less potent than NK1 agonist. The NK3 agonist, Senktide, was totally ineffective at 0.5-50 nmol/knee. All responses induced by SP (5 nmol/knee), NKA (5 nmol/knee), NKB (50 nmol/knee), NK1 agonist (0.5 nmol/knee) or NK2 agonist (25 nmol/knee) were significantly and profoundly inhibited by the NK1 selective antagonist, RP67580, but not by the NK2 selective antagonist, SR48968. Taken together, we conclude that tachykinin-induced plasma extravasation in the rat knee joint is mediated via NK1 receptors.

MeSH terms

  • Animals
  • Benzamides / pharmacology
  • Capillary Permeability / physiology*
  • Evans Blue
  • Hindlimb / blood supply
  • Indoles / pharmacology
  • Isoindoles
  • Joints / blood supply*
  • Male
  • Neurokinin A / antagonists & inhibitors
  • Neurokinin-1 Receptor Antagonists
  • Piperidines / pharmacology
  • Rats
  • Rats, Wistar
  • Receptors, Neurokinin-1 / physiology*
  • Receptors, Neurokinin-2 / antagonists & inhibitors
  • Receptors, Neurokinin-2 / physiology
  • Substance P / antagonists & inhibitors
  • Synovial Fluid / metabolism
  • Tachykinins / pharmacology*

Substances

  • Benzamides
  • Indoles
  • Isoindoles
  • Neurokinin-1 Receptor Antagonists
  • Piperidines
  • Receptors, Neurokinin-1
  • Receptors, Neurokinin-2
  • Tachykinins
  • 7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one
  • Substance P
  • Evans Blue
  • SR 48968
  • Neurokinin A