Pharmacological characterization of vanilloid receptor located in the brain

Tamas Szabo, T. Bíró, Adamar F. Gonzalez, M. Palkóvits, Peter M. Blumberg

Research output: Contribution to journalArticle

78 Citations (Scopus)

Abstract

Specific [3H]resiniferatoxin (RTX) binding detects the vanilloid receptor type I (VR1). In the present study we demonstrate specific, high-affinity, saturable [3H]RTX binding in various areas of monkey brain not known to be innervated by primary afferent neurons as well as in spinal cord and dorsal root ganglion neurons of the same origin. Detailed pharmacological characterization and comparison revealed no major difference in binding affinities between the peripheral and the central sites as measured by Kd/Ki values. In general, lower receptor density was measured in selected brain areas than in the periphery. Areas with higher receptor density were detected in the locus ceruleus, preoptic area, and medial basal hypothalamus of the brain. Both capsaicin and the competitive antagonist capsazepine inhibited the specific binding of [3H]RTX to membrane preparations of the dorsal horn of the spinal cord and dorsal root ganglia with Ki values of 4.3±0.32 μM and 2.7±0.33 μM, respectively. Inhibition was observed in the central areas (hypothalamus) with Ki values of 0.95±0.1 μM for capsaicin and 0.86±0.11 μM for capsazepine. Previous biological and pharmacological evidence suggested that vanilloid receptors were present in the brain. Our results demonstrate that the pharmacological properties of both the peripheral and central receptor sites display appropriate pharmacological similarity to represent the same receptor class. The modest differences in ligand affinities for the vanilloid receptor expressed in the brain nuclei and the dorsal root ganglion neurons may correspond to differences in sequence, modification or associated proteins. Published by Elsevier Science B.V.

Original languageEnglish
Pages (from-to)51-57
Number of pages7
JournalMolecular Brain Research
Volume98
Issue number1-2
DOIs
Publication statusPublished - Jan 31 2002

Fingerprint

TRPV Cation Channels
Pharmacology
Spinal Ganglia
Brain
Spinal Nerve Roots
Capsaicin
Middle Hypothalamus
Neurons
Afferent Neurons
Preoptic Area
Locus Coeruleus
Hypothalamus
Haplorhini
Spinal Cord
Ligands
Membranes
resiniferatoxin
Proteins

Keywords

  • [H]Resiniferatoxin
  • Capsaicin
  • Vanilloid receptor

ASJC Scopus subject areas

  • Molecular Biology
  • Cellular and Molecular Neuroscience

Cite this

Pharmacological characterization of vanilloid receptor located in the brain. / Szabo, Tamas; Bíró, T.; Gonzalez, Adamar F.; Palkóvits, M.; Blumberg, Peter M.

In: Molecular Brain Research, Vol. 98, No. 1-2, 31.01.2002, p. 51-57.

Research output: Contribution to journalArticle

Szabo, Tamas ; Bíró, T. ; Gonzalez, Adamar F. ; Palkóvits, M. ; Blumberg, Peter M. / Pharmacological characterization of vanilloid receptor located in the brain. In: Molecular Brain Research. 2002 ; Vol. 98, No. 1-2. pp. 51-57.
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