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Research ArticleBEHAVIORAL PHARMACOLOGY

Characterization of Epibatidine Binding to Medial Habenula: Potential Role in Analgesia

Per Plenge, Erling T. Mellerup and Gitta Wörtwein
Journal of Pharmacology and Experimental Therapeutics August 2002, 302 (2) 759-765; DOI: https://doi.org/10.1124/jpet.102.033498
Per Plenge
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Erling T. Mellerup
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Gitta Wörtwein
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Abstract

The objective of the present study was to characterize a recently described binding site in the habenula, which has high affinity for [3H]epibatidine and low affinity for nicotine and acetylcholine. We report that the extension of this binding area in coronal and horizontal sections corresponds to the anatomical extension of the medial habenula. The affinity (KD) of the medial habenula receptors for [3H]epibatidine was estimated to be 0.5 nM using an autoradiographic saturation assay, whereas the affinity of the binding site for nicotine and acetylcholine was estimated to be 5 and 8 μM, respectively. The receptor density (Bmax) in the medial habenula was estimated to be about 1100 fmol/mg wet weight using [3H]epibatidine. The subunit composition of the “epibatidine receptor” was investigated by the ability of different compounds with affinity to various subtypes of nicotinic receptors to displace [3H]epibatidine bound to the receptor. The results suggest that the receptor contains α3 subunits but that it is unlikely to be an α3β4 nicotinic receptor. Systemic administration of epibatidine has analgesic effects in rats. Here we report that 2 × 1 μl of 10 nM epibatidine, resulting in a 2 × 10-fmol dose, administered directly to the medial habenula by bilateral stereotactic injection had an analgesic effect measured in the hot-plate test. This dose of epibatidine increased hot-plate latency significantly, whereas 2 × 2 fmol of epibatidine or 2 × 10 fmol of nicotine were without effect. This leads us to suggest that the medial habenular epibatidine binding site might be a valuable target for the development of non-opiate analgesics.

Footnotes

  • G.W. was the recipient of a postdoctoral stipend from the NeuroScience PharmaBiotec Center (the Danish Medical Research Council).

  • DOI: 10.1124/jpet.102.033498

  • Abbreviations:
    nAChR
    neuronal acetylcholine receptor
    mHb
    medial habenula
    CNS
    central nervous system
    ABT-594
    (R)-5-(2-azetidinylmethoxy)-2-cloropyridine
    • Received February 5, 2002.
    • Accepted April 15, 2002.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 302 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 302, Issue 2
1 Aug 2002
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Research ArticleBEHAVIORAL PHARMACOLOGY

Characterization of Epibatidine Binding to Medial Habenula: Potential Role in Analgesia

Per Plenge, Erling T. Mellerup and Gitta Wörtwein
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 759-765; DOI: https://doi.org/10.1124/jpet.102.033498

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Research ArticleBEHAVIORAL PHARMACOLOGY

Characterization of Epibatidine Binding to Medial Habenula: Potential Role in Analgesia

Per Plenge, Erling T. Mellerup and Gitta Wörtwein
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 759-765; DOI: https://doi.org/10.1124/jpet.102.033498
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