Lipophilic beta-adrenoceptor antagonists and local anesthetics are effective direct activators of G-proteins

URN to cite this document:: urn:nbn:de:bvb:355-epub-232997
DOI to cite this document:: 10.5283/epub.23299

Hagelüken, A. ; Grünbaum, L. ; Nürnberg, B. ; Harhammer, R. ; Schunack, W. ; Seifert, Roland

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Date of publication of this fulltext: 26 Jan 2012 08:21

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Abstract

We studied the effects of various beta-adrenoceptor (beta AR) antagonists and local anesthetics (LAs), i.e. substances possessing one basic and one lipophilic domain each, on activation of regulatory heterotrimeric guanine nucleotide-binding proteins (G-proteins). In membranes of differentiated HL-60 cells, propranolol activated high-affinity GTP hydrolysis with a half-maximal effect at 0.19 mM ...