cDNA sequence and heterologous expression of the human neurokinin-3 receptor

Biochem Biophys Res Commun. 1992 Apr 30;184(2):966-72. doi: 10.1016/0006-291x(92)90685-e.

Abstract

Functional cDNA clones encoding the human neurokinin-3 receptor were isolated from human brain mRNA. The cloned human neurokinin-3 receptor was expressed in COS cells and Xenopus oocytes, where peptide binding affinity and intracellular effector activation were determined. Neurokinin B is the most potent agonist, followed by eledoisin, substance K and substance P. The binding affinities of these peptides at the human neurokinin-3 receptor differ quantitatively from the rat receptor, implying a functional consequence of the sequence divergence between the two species. Heterologous expression in oocytes revealed that, unlike the neurokinin-1 receptor, the efficacy of ion channel activation mediated by the neurokinin-3 receptor does not approximate the binding affinity. The heterologous expression of the human neurokinin-3 receptor will facilitate further investigation into its biochemical functions.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding, Competitive
  • Brain / physiology*
  • Cell Line
  • Chloride Channels
  • Chlorides / metabolism
  • Cloning, Molecular
  • DNA / genetics*
  • Gene Expression
  • Humans
  • Kinetics
  • Membrane Proteins / drug effects
  • Membrane Proteins / physiology
  • Molecular Sequence Data
  • Neurokinin A / metabolism
  • Neurokinin A / pharmacology*
  • Oocytes / physiology
  • RNA, Messenger / genetics*
  • Rats
  • Receptors, Neurokinin-2
  • Receptors, Neurotransmitter / genetics*
  • Receptors, Neurotransmitter / metabolism
  • Receptors, Neurotransmitter / physiology
  • Recombinant Proteins / metabolism
  • Sequence Homology, Nucleic Acid
  • Substance P / pharmacology
  • Transfection
  • Xenopus

Substances

  • Chloride Channels
  • Chlorides
  • Membrane Proteins
  • RNA, Messenger
  • Receptors, Neurokinin-2
  • Receptors, Neurotransmitter
  • Recombinant Proteins
  • Substance P
  • Neurokinin A
  • DNA

Associated data

  • GENBANK/D10556
  • GENBANK/M89473
  • GENBANK/M97582
  • GENBANK/M97583
  • GENBANK/M97584
  • GENBANK/M97585
  • GENBANK/M97586
  • GENBANK/M97587
  • GENBANK/M97588
  • GENBANK/M97589