Function and Mechanism of the Interaction of GTP-Binding Proteins with α2-Adrenoceptors in the Brain

  • Yasuyuki Nomura
  • Yoshihisa Kitamura
  • Keiko Kawata
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 236)


Multiple subtypes of adrenoceptors including αl-, α2-, β1- and β2-adrenoceptors have been found in the central nervous system (CNS) (1, 2). Stimulation of α2-adrenoceprtors causes inhibition of adenylate cyclase activity (3), and inhibition of noradrenaline (NA) release from central and peripheral noradrenergic nerve terminals (4). Clonidine exerts hypotensive and sedative effects by its acting on α2-adrenoceptors in the brain (5). Pertussis toxin, isletactivating protein (IAP), suppresses the inhibition of adenylate cyclase activity mediated by inhibitory receptors such as α2-adrenoceptor, D2-dopamine receptor, muscarinic acetylcholine receptor and opiate receptor, and modulates the agonist-binding affinities of these receptors as result of ADP-ribosylation of α-subunit of inhibitory GTP-binding protein, Gi (6). To gain insight into the functional roles, the molecular mechanism and aging in coupling of α2-adrenoceptor with Gi in the CNS, we investigated influences of clonidine and IAP on locomotor activity in rats, NA release from brain slices and adenylate cyclase activity in brain membranes.


Adenylate Cyclase Cholera Toxin Pertussis Toxin Adenylate Cyclase Activity Noradrenaline Release 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© Springer Science+Business Media New York 1988

Authors and Affiliations

  • Yasuyuki Nomura
    • 1
    • 2
  • Yoshihisa Kitamura
    • 1
    • 2
  • Keiko Kawata
    • 1
  1. 1.Department of Pharmacology Research Institute for WAKAN-YAKU (Oriental Medicine)Toyama Medical and Pharmaceutical UniversityToyamaJapan
  2. 2.Department of Pharmacology Faculty of Pharmaceutical SciencesHokkaido UniversitySapporo 060Japan

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