Neurotensin and its analogs-Correlation of specific binding with stimulation of cyclic GMP formation in neuroblastoma clone N1E-115

Judith A. Gilbert, C. Jill Moses, Michael A. Pfenning, Elliott Richelson

Research output: Contribution to journalArticle

53 Scopus citations

Abstract

The receptors which mediate neurotensin-stimulated intracellular cyclic GMP formation in murine neuroblastoma clone N1E-115 [J. A. Gilbert and E. Richelson, Eur. J. Pharmac. 99, 245 (1984)] were further characterized. The binding of [3H]neurotensin to intact N1E-115 cells at 0° displayed specificity, saturability, reversibility, and tissue linearity. A single class of neurotensin receptors was demonstrated with an apparent KD of 9-11 nM and a Bmax of 180-250 fmoles/106 cells, determined by the type of serum employed in the cellular culture medium. A number of neurotensin analogs and fragments were compared for their ability to inhibit [3H]neurotensin binding and stimulate intracellular cyclic GMP formation with intact N1E-115 cells. A direct correlation was found to exist between the KD and EC50 for each peptide. The carboxyl-terminal portion of neurotensin proved to be responsible for the binding and biochemical activities of this peptide with clone N1E-115. Neurotensin(8-13) was, in fact, fifty times more potent than native neurotensin in stimulating intracellular cyclic GMP formation and had an 18-fold higher affinity for the neurotensin receptor on this neuronal cell type.

Original languageEnglish (US)
Pages (from-to)391-397
Number of pages7
JournalBiochemical Pharmacology
Volume35
Issue number3
DOIs
StatePublished - Feb 1 1986

ASJC Scopus subject areas

  • Pharmacology

Fingerprint Dive into the research topics of 'Neurotensin and its analogs-Correlation of specific binding with stimulation of cyclic GMP formation in neuroblastoma clone N1E-115'. Together they form a unique fingerprint.

  • Cite this