Benextramine-neuropeptide Y (NPY) binding site interactions

Characterization of 3H-NPY binding site heterogeneity in rat brain

M. B. Doughty, K. Li, Longqin Hu, S. S. Chu, R. Tessel

Research output: Contribution to journalArticle

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Abstract

Pre-incubation of rat brain membranes with 200 μM benextramine followed by extensive dilution and washing to remove unbound ligand reduced Bmax for N-[propionyl-3H]-NPY (3H-NPY) specific binding by 61% relative to control membranes treated identically but in the absence of benextramine. When rat brain membranes were co-incubated with 3H-NPY and 57 μM benextramine, there was a significant shift to the right; the apparent Kd for 3H-NPY binding increased two-fold relative to control membranes. These data are consistent with the hypothesis that benextramine is a competitive and irreversible ligand for a population (60-65%) of rat brain NPY binding sites. 'Paired tube' assays were then used to determine the selectivity of these benextramine-sensitive and insensitive 3H-NPY binding site populations. PYY, NPY and NPY13-36 each displaced 100% of 3H-NPY from rat brain membrane binding sites both in the absence and presence of 1 mM benextramine. In contrast, [Leu31,Pro34]NPY displayed the same binding site selectivity as benextramine in displacing 65% of 3H-NPY from specific binding sites on untreated rat brain membranes, and it failed to displace 3H-NPY from membranes treated with 1 mM benextramine. Thus the selectivity of the benextramine-insensitive 3H-NPY binding site population-PYY >= NPY > NPY13-36 ≫[Leu31,Pro34]NPY-is characteristic of a Y2-like NPY binding site population, while the benextramine-sensitive 3H-NPY binding sites appear to be a Y1-like binding site population.

Original languageEnglish (US)
Pages (from-to)169-180
Number of pages12
JournalNeuropeptides
Volume23
Issue number3
DOIs
StatePublished - Jan 1 1992

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Neuropeptide Y
Binding Sites
Brain
Membranes
Population
benextramine
Ligands

All Science Journal Classification (ASJC) codes

  • Endocrinology
  • Neurology
  • Endocrine and Autonomic Systems
  • Cellular and Molecular Neuroscience

Cite this

@article{50371e945cea4e62b472bf60966eb3f7,
title = "Benextramine-neuropeptide Y (NPY) binding site interactions: Characterization of 3H-NPY binding site heterogeneity in rat brain",
abstract = "Pre-incubation of rat brain membranes with 200 μM benextramine followed by extensive dilution and washing to remove unbound ligand reduced Bmax for N-[propionyl-3H]-NPY (3H-NPY) specific binding by 61{\%} relative to control membranes treated identically but in the absence of benextramine. When rat brain membranes were co-incubated with 3H-NPY and 57 μM benextramine, there was a significant shift to the right; the apparent Kd for 3H-NPY binding increased two-fold relative to control membranes. These data are consistent with the hypothesis that benextramine is a competitive and irreversible ligand for a population (60-65{\%}) of rat brain NPY binding sites. 'Paired tube' assays were then used to determine the selectivity of these benextramine-sensitive and insensitive 3H-NPY binding site populations. PYY, NPY and NPY13-36 each displaced 100{\%} of 3H-NPY from rat brain membrane binding sites both in the absence and presence of 1 mM benextramine. In contrast, [Leu31,Pro34]NPY displayed the same binding site selectivity as benextramine in displacing 65{\%} of 3H-NPY from specific binding sites on untreated rat brain membranes, and it failed to displace 3H-NPY from membranes treated with 1 mM benextramine. Thus the selectivity of the benextramine-insensitive 3H-NPY binding site population-PYY >= NPY > NPY13-36 ≫[Leu31,Pro34]NPY-is characteristic of a Y2-like NPY binding site population, while the benextramine-sensitive 3H-NPY binding sites appear to be a Y1-like binding site population.",
author = "Doughty, {M. B.} and K. Li and Longqin Hu and Chu, {S. S.} and R. Tessel",
year = "1992",
month = "1",
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language = "English (US)",
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Benextramine-neuropeptide Y (NPY) binding site interactions : Characterization of 3H-NPY binding site heterogeneity in rat brain. / Doughty, M. B.; Li, K.; Hu, Longqin; Chu, S. S.; Tessel, R.

In: Neuropeptides, Vol. 23, No. 3, 01.01.1992, p. 169-180.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Benextramine-neuropeptide Y (NPY) binding site interactions

T2 - Characterization of 3H-NPY binding site heterogeneity in rat brain

AU - Doughty, M. B.

AU - Li, K.

AU - Hu, Longqin

AU - Chu, S. S.

AU - Tessel, R.

PY - 1992/1/1

Y1 - 1992/1/1

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