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

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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

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Neurotensin
Cyclic GMP
Neuroblastoma
Clone Cells
Neurotensin Receptors
neurotensin (8-13)
Peptides
Culture Media
Tissue
Serum

ASJC Scopus subject areas

  • Pharmacology

Cite this

Neurotensin and its analogs-Correlation of specific binding with stimulation of cyclic GMP formation in neuroblastoma clone N1E-115. / Gilbert, Judith A.; Moses, C. Jill; Pfenning, Michael A.; Richelson, Elliott.

In: Biochemical Pharmacology, Vol. 35, No. 3, 01.02.1986, p. 391-397.

Research output: Contribution to journalArticle

Gilbert, Judith A. ; Moses, C. Jill ; Pfenning, Michael A. ; Richelson, Elliott. / Neurotensin and its analogs-Correlation of specific binding with stimulation of cyclic GMP formation in neuroblastoma clone N1E-115. In: Biochemical Pharmacology. 1986 ; Vol. 35, No. 3. pp. 391-397.
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