Lung is one of the organs which possess most abundant β-adrenergic receptots. Direct radioligie binding methods for studying β-adrenergic receptors have been developed recently. These methods can provide new insights into the molecular characteristics and regulatory properties of β-adrenergic receptors in the lung.
In the present investigation we determined the number of β-adrenergic receptors in the lung membrane of Japanese Albino Rabbits, weighing 1.5-2.5kg, by direct binding methods using [
3H] (-)-dihydroalprenolol ([
3H]-DHA). Effects of isoproterenol, salbutamol and prednisolone on the β-adrnergic receptors in the lung were also investigased.
1) The mean values and standard deviations of the number of β-adrenergic receptors (the concentration of [
3H]-DHA binding sites) and of the dissociation constant (Kd) were 638.9±79.7f mol/mg protein and 1.25±0.17nM, respectively.
2) The treatment of rabbits with isoproterenol (0.05mg/kg, subcutaneously) 24 hours and 12 hours before their sacrifice induced a significant decrease in the number of β-adrenergic lung receptors, 542.5±62.0f mol/mg protein (n=6, p<0.05), while Kd did not show any significant change.
3) The treatment of rabbits with prednisolone (2mg/kg, intramuscularly) for 6 days induced a significant increase in the number of β-adrenergic lung receptors, 788.8±131.0f mol/mg protein (n=13, p<0.01), while Kd remained unchanged.
4) The treatment of rabbits with isoproterenal (0.01mg/kg, subcutaneously) and salbutamol (3mg/kg, orally) for 6 days induced no significant change in the number on β-adrenergic lung receptors.
5) Modified Scatchard analysis of the [
3H]-DHA binding inhibition curve of atenolol, a selective β
1, antagonist, revealed that rabbit lung possessed both β
1 and β
2 receptors, (β
1:β
2=63:37).
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