Abstract
The possibility of direct regulation of an ion channel by a G-protein, i.e., as shown in cell-free systems not involving soluble second messengers, and hence of G-protein-gated ion channels, emerged from studies on the mechanism by which muscarinic acetylcholine receptors (mAChR) activate the atrial muscarinic K+ channel that mediates vagal regulation of chronotropy. Ion channels have since then been found that are affected either by Gi (Gi-gated channels), Go (Go-gated channels), or Gs (Gs-gated channels). G-protein-gated K+ channels are physiologically very relevant as modulators of cellular function. Activation of these K+ channels causes cells to hyperpolarize and become less excitable. As a consequence secretion is attenuated in endocrine and nerve cells such as found in sympathetic ganglia (Eccles and Libet 1961; Hartzel et al. 1977), parasympathetic ganglia (Griffith et al. 1981; Hill-Smith and Purves 1978), and the central nervous system (Nakajima et al. 1986; Trautwein and Dudel 1958). In heart they cause a decrease in chronotropy (Trautwein and Dudel 1958; Giles and Noble 1976; reviewed by Hartzell 1981).
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Birnbaumer, L. (1993). Modulation of K+ Channels by G-Proteins. In: Dickey, B.F., Birnbaumer, L. (eds) GTPases in Biology II. Handbook of Experimental Pharmacology, vol 108 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-78345-6_33
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DOI: https://doi.org/10.1007/978-3-642-78345-6_33
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