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Binding of β1-adrenoreceptor antagonist [3H]CGP 26505 in rat cerebral cortex and sinus atrial nodeantagonist [3H]CGP 26505 in rat cerebral cortex and sinus atrial node

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Abstract

Specific β1-adrenoreceptors antagonist [3H]CGP 26505 binding was characterized in rat cerebral cortex and heart sinus atrial node. In both tissues [3H]CGP 26505 binding was maximal at 25°C, it was specific, saturable and protein concentration dependent. Scatchard analysis of saturation isotherms of specific [3H]CGP 26505 binding in cerebral cortex showed that [3H]CGP 26505 binds a single class of high affinity sites with a dissociation constant (KD) of 1±0.3 nM and a maximal number of binding sites (Bmax) of 40±2 fmol/mg of protein. In sinus atrial node, [3H]-CGP 26505 binds a single class of high affinity sites (KD=1.9±0.4 nM, Bmax=28±2 fmol/mg of protein).

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Authors and Affiliations

  1. Istituto Policattedra di Discipline Biologiche dell'Università di Pisa, via Bonanno 6, 56126, Pisa, Italy

    G. Chiellini, G. Giannaccini, C. Martini & A. Lucacchini

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  1. G. Chiellini
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  2. G. Giannaccini
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  3. C. Martini
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  4. A. Lucacchini
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Correspondence to A. Lucacchini.

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Chiellini, G., Giannaccini, G., Martini, C. et al. Binding of β1-adrenoreceptor antagonist [3H]CGP 26505 in rat cerebral cortex and sinus atrial nodeantagonist [3H]CGP 26505 in rat cerebral cortex and sinus atrial node. Neurochem Res 21, 1149–1153 (1996). https://doi.org/10.1007/BF02532388

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