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. 1982;13(Suppl 2):181S–186S. doi: 10.1111/j.1365-2125.1982.tb01908.x

β-adrenoceptor blocking agents and lipolysis

H H Harms, J De Vente, J Zaagsma
PMCID: PMC1402182  PMID: 6125168

Abstract

1 The pharmacological characteristics of β-adrenoceptor subtypes on adipocytes of various mammalian species, including man, are reviewed.

2 Rat adipocytes possess a homogeneous population of β-adrenoceptors with properties that clearly distinguish them from `classic' β1- and β2-adrenoceptors, although they share certain features with both. Thus, rat adipocyte β-adrenoceptors should be considered as non-β1-non-β2 receptors, like the atypical β-adrenoceptors found on erythrocytes of turkey, chicken and frog.

3 Preliminary data suggest that adipocyte β-adrenoceptors of guinea pig and swine are different from `classic' β1- and β2-adrenoceptors as well, whereas in the dog and possibly in the cat, a mixture of β1- and β2-receptors mediates catecholamine induced lipolysis.

4 Human adipocyte β-adrenoceptors probably also consist of at least two subtypes. Insufficient data are available to decide if these β-adrenoceptors are identical with `classic' β1- and β2-receptors, or share some hybrid characteristics with rat adipocyte β-adrenoceptors.

5 In vivo studies in animals as well as in man, tend to corroborate in vitro results. Cardioselective β-adrenoceptor blocking agents, like atenolol, metoprolol and practolol are not as effective in blocking catecholamine induced lipolysis as non-cardioselective agents like propranolol and pindolol. The relatively low potency of cardioselective β-adrenoceptor blocking agents is found using either isoprenaline, adrenaline or exercise as the agonist, suggesting that β2-adrenoceptors are involved. On the other hand, cardioselective agents, though less effective than non-cardioselective compounds, have a significant inhibitory effect on catecholamine induced lipolysis at doses that have only minimal effect on other β2-adrenoceptor mediated responses, which argues for participation of β1-adrenoceptors.

6 Thus, human in vitro and in vivo data are consistent with, but not proof of the hypothesis that a mixture of β1- and β2-adrenoceptors mediates lipolysis induced by sympathetic activation.

7 Species differences in β-adrenoceptor subtype characteristics may complicate the interpretation of the relevance of animal data for the understanding of β-adrenoceptor mediated effects in human adipocytes.

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Selected References

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