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Research ArticleArticle

Distribution in Rat Brain of Binding Sites of Kaliotoxin, a Blocker of Kv1.1 and Kv1.3 α-Subunits

Christiane Mourre, Marina N. Chernova, Marie-France Martin-Eauclaire, Richard Bessone, Guy Jacquet, Maurice Gola, Seth. L. Alper and Marcel Crest
Journal of Pharmacology and Experimental Therapeutics December 1999, 291 (3) 943-952;
Christiane Mourre
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Marina N. Chernova
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Marie-France Martin-Eauclaire
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Richard Bessone
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Guy Jacquet
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Maurice Gola
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Seth. L. Alper
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Marcel Crest
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Abstract

The distribution of the binding sites for kaliotoxin (KTX), a blocker of voltage-dependent K+ channels, was studied with quantitative autoradiography in adult rat brain and during postnatal brain maturation. Iodinated KTX bound specifically to tissue sections with a high affinity (Kd = 82 pM) and a maximal binding capacity of 13.4 fmol/mg protein. The distribution of KTX binding sites within the central nervous system was heterogeneous. The highest densities were found in the neocortex, hypothalamus, dentate gyrus, bed nucleus of the stria terminalis, and parabrachial nuclei. The lowest level was observed in the white matter. From postnatal day 5 onward, KTX binding sites were detectable only in the hindbrain. The density of KTX binding sites in whole brain drastically increased after postnatal day 15 to achieve adult levels at postnatal day 60 in the whole brain. Bath application of KTX to Xenopus laevis oocytes blocked recombinant Kv1.3 and Kv1.1 channels potently and Kv1.2 channels less potently, with respectiveKd values of 0.1, 1.5, and 25 nM. KTX affinities for each of these channels expressed in mammalian cells were about 10-fold lower. A comparison of the distribution of KTX binding sites with that of Kv1 channel polypeptides, together with the pharmacology of KTX block, suggests that the principal targets for KTX in rat brain are K+ channels containing Kv1.1 and Kv1.3 α-subunits.

Footnotes

  • Send reprint requests to: Dr. C. Mourre, Laboratoire de Neurobiologie Intégrative et Adaptative, UMR 6562, CNRS-Université de Provence, Escadrille Normandie-Niemen, Case 351, 13397, Marseille, Cedex 20, France. E-mail:mourre{at}newsup.univ-mrs.fr

  • ↵1 This work was supported by the Centre National de la Recherche Scientifique and by the Association Française contre les Myopathies (Grant 5030). M.N. and S.L.A. were supported by NIH Grants HL15157 (Boston Sickle Cell Center) and DK34854 (Harvard Digestive Diseases Center). S.L.A. is an Established Investigator of the American Heart Association.

  • Abbreviations:
    Kv
    voltage-gated potassium
    CTX
    charybdotoxin
    DTX
    dendrotoxin
    KTX
    kaliotoxin
    MCD
    mast cell-degranulating
    IKCa
    intermediate conductance Ca2+-activated K+
    MgTX
    margatoxin
    BK
    high conductance Ca2+-activated K+
    • Received April 20, 1999.
    • Accepted July 27, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 291 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 291, Issue 3
1 Dec 1999
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Research ArticleArticle

Distribution in Rat Brain of Binding Sites of Kaliotoxin, a Blocker of Kv1.1 and Kv1.3 α-Subunits

Christiane Mourre, Marina N. Chernova, Marie-France Martin-Eauclaire, Richard Bessone, Guy Jacquet, Maurice Gola, Seth. L. Alper and Marcel Crest
Journal of Pharmacology and Experimental Therapeutics December 1, 1999, 291 (3) 943-952;

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Research ArticleArticle

Distribution in Rat Brain of Binding Sites of Kaliotoxin, a Blocker of Kv1.1 and Kv1.3 α-Subunits

Christiane Mourre, Marina N. Chernova, Marie-France Martin-Eauclaire, Richard Bessone, Guy Jacquet, Maurice Gola, Seth. L. Alper and Marcel Crest
Journal of Pharmacology and Experimental Therapeutics December 1, 1999, 291 (3) 943-952;
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