Presence of NK1 receptors on a mucosal-like mast cell line, RBL-2H3 cells

Can J Physiol Pharmacol. 1998 Feb;76(2):188-93.

Abstract

Reverse transcription--polymerase chain reaction of mRNA from rat RBL-2H3 cells yielded a 316 base pair band consistent with that predicted for the neurokinin-1 (NK1) receptor. Saturation and competition binding with 125I-labeled Bolton-Hunter substance P, substance P fragments, and a series of selective tachykinin receptor agonists and antagonists demonstrated that RBL-2H3 cells express high affinity binding sites for substance P on their surfaces with the kinetic and pharmacological properties of NK1 receptors. The pharmacology of these 125I-labeled substance P binding sites was (from most to least potent) [Sar9,Met(O2)11]substance P > substance P 4-11 >> GR82334 << MEN 10,376. However, substance P 1-4, substance P 8-11, substance P 9-11, and [Trp7, beta-Ala8]neurokinin A 4-10 failed to compete for binding. The metabolically stable NK1 receptor agonist, [Sar9,Met(O2)11] substance P, caused a 49% increase in 5-hydroxytryptamine release above basal levels. The results demonstrate the presence of functional NK1 receptors on RBL-2H3 cells, a mucosal-like mast cell line.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cells, Cultured / drug effects
  • Mast Cells / metabolism*
  • Neurokinin A / analogs & derivatives
  • Neurokinin A / pharmacology
  • Peptide Fragments / pharmacology
  • Polymerase Chain Reaction
  • Rats
  • Receptors, Neurokinin-1 / drug effects
  • Receptors, Neurokinin-1 / genetics
  • Receptors, Neurokinin-1 / metabolism*
  • Substance P / metabolism*
  • Substance P / pharmacology

Substances

  • Peptide Fragments
  • Receptors, Neurokinin-1
  • neurokinin A(4-10), Tyr(5)-Trp(6,8,9)-Lys(10)-
  • Substance P
  • Neurokinin A