Regulation of Central Adrenergic Receptors

  • David B. Bylund
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 116)


The mechanisms through which the catecholamines produce their effects in the central nervous system are not yet understood. Norepinephrine, which could be acting either as a neurotransmitter or neuromodulator, initially binds to its receptor site on the external surface of the cell membrane. This binding interaction eventually results in alterations of the electrical prop erties of the membrane and perhaps alterations in other cellular functions. Many of these effects appear to be mediated through the activation of the membrane bound enzyme, adenylate cyclase. It is well established that the responsiveness of the receptor systems which mediate the effects of norepinephrine is subject to regulation. Thus, under certain conditions, the response to a given concentration of norepinephrine may be either greater than or less than normal, i.e., supersensitive or subsensitive. There appear to be several biochemical events which are regulated, one or more of which might be important under a given set of conditions: the receptor binding site for norepinephrine; enzymes such as adenylate cyclase, phosphodiesterase, protein kinase, phosphoprotein phosphatase; the functional coupling between the receptor binding site and adenylate cyclase; and membrane properties such as fluidity, asymmetry, and lipid composition.


Receptor Binding Adenylate Cyclase Adrenergic Receptor Adenylate Cyclase Activity Receptor Binding Site 
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© Plenum Press, New York 1979

Authors and Affiliations

  • David B. Bylund
    • 1
  1. 1.Department of Pharmacology, School of MedicineUniversity of MissouriColumbiaUSA

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