Direct localisation of β-adrenoceptor sites in rat cerebellum by a new fluorescent analogue of propranolol

Abstract

NORADRENALINE (NA) is a putative neurotransmitter, possibly involved in mediation of information transfer across synapses in the mammalian central nervous system (CNS)¹, whose postsynaptic effect is exerted, in part, by stimulation of β-adrenoceptors coupled to adenylate cyclase². Although the rat cerebellum is known to contain NA³, and an afferent noradrenergic pathway has been found^4–7, little information is available concerning the noradrenergic synapses there. Indirect evidence such as increase in cyclic AMP content and inhibition of spontaneous electrical activity in rat Purkinje cells^8–10 (reduced by β-adrenoceptor blocking⁸), suggests, however, that such synapses are present and that the postsynaptic NA receptors are of the β type. β-adrenoceptors were identified in homogenates of whole rat cerebellum by a binding assay which used the β-adrenergic antagonist ³H-(–)-alprenolol¹¹. We have now developed a direct in vivo method, using 9-amino-acridin-propranolol (9-AAP), a potent fluorescent β-adrenergic blocker, as a fluorescent probe, in an attempt to detect β-adrenergic receptors in rat cerebellum.