Evidence of functional α2-adrenergic receptors in adult-rat adipocytes by using the agonist UK 14304

Abstract
The aim of this study was to re-assess whether .alpha.2-adrenergic receptors were present in rat adipocytes, by using UK 14304, a new and very selective .alpha.2-agonist. The following observations demonstrate the presence of functional .alpha.2-adrenoceptors in rat adipocytes. (1) Adipocyte lipolysis was dose-dependently inhibited by UK 14304 (maximal effect 80% at 1 .mu.m-UK 14304, 45% at 10 .mu.m-UK 14304, under basal or theophylline-stimulated conditions respectively). (2) UK 14304 bound specifically to purified plasma membranes, with Bmax. = 744 fmol/mg of protein and KD = 9 nM. (3) The effect of UK 14304 was suppressed by .alpha.2-antagonists. (4) Adrenaline inhibited lipolysis upon .beta.-adrenergic blockade (propranolol). (5) The anti-lipolytic effect of UK 14304 was modulated by the age of the rats.

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