A possible involvement of cyclic AMP in the expression of desensitization of the nicotinic acetylcholine receptor

FEBS Letters

Deshpande, S.S.²  Daly, J.W.¹  Alkondon, M.²  Aracava, Y.²  Albuquerque, E.X.² 

[1] Laboratory of Chemistry, National Institute of Arthritis, Diabetes,and Digestive and Kidney Diseases, Bethesda, MD 20892, USA;Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, 655 W. Baltimore Street, Baltimore, MD 21201, USA

关键词: Forskolin;    Nicotinic receptor;    cyclic AMP;    Desensitization;    Adenylate cyclase;    Acetylcholine sensitivity;   

DOI  :  10.1016/0014-5793(86)81235-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Forskolin, an activator of adenylate cyclase, and its analogs were studied on the nicotinic acetylcholine receptor-ion channel complex (AChR) of rat and frog skeletal muscles. At nanomolar concentrations, forskolin caused desensitization of the AChR located at the junctional region of innervated and the extrajunctional region of chronically denervated rat soleus muscles. The desensitization of the AChR occurred without alteration of the conducting state (channel lifetime, conductance or bursting) as shown by single channel currents. Accordingly, forskolin decreased the peak amplitude of the repetitive evoked endplate currents in frog sartorius muscles. These findings taken together with the good correlation found between the effects of forskolin and its analogs on the desensitization of the nicotinic AChR and their ability to activate adenylate cyclase suggested a possible involvement of phosphorylation of AChR via cyclic AMP on the desensitization process.

【 授权许可】

Unknown