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Pharmacology of Neurotransmitter Release pp 261–288Cite as

Presynaptic Metabotropic Receptors for Acetylcholine and Adrenaline/Noradrenaline

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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 184))

Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline were first described more than three decades ago. Molecular cloning has resulted in the identification of five G protein-coupled muscarinic receptors (M1 – M5) which mediate the biological effects of acetylcholine. Nine adrenoceptors (α1ABD,α2ABC,β123) transmit adrenaline/noradrenaline signals between cells. The lack of sufficiently subtype-selective ligands has prevented identification of the physiological role and therapeutic potential of these receptor subtypes for a long time. Recently, mouse lines with targeted deletions for all muscarinic and adrenoceptor genes have been generated. This review summarizes the results from these gene-targeting studies with particular emphasis on presynaptic auto- and heteroreceptor functions of muscarinic and adrenergic receptors. Specific knowledge about the function of receptor subtypes will enhance our understanding of the physiological role of the cholinergic and adrenergic nervous system and open new avenues for subtype-selective therapeutic strategies.

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  1. Institute of Experimental and Clinical Pharmacology and Toxicology, University of Freiburg, Albertstrasse 25, 79104, Freiburg, Germany

    Ralf Gilsbach & Lutz Hein

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  1. Ralf Gilsbach
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  1. Howard Hughes Medical Institute and Center for Basic Neuroscience, UT Southwestern Medical Center, 6000 Harry Hines Blvd. NA4.118, Dallas, TX 75390, USA

    Thomas C. Südhof

  2. Institut für Experimentelle und Klinische Pharmakologie und Toxikologie, Albert-Ludwigs-Universität Freiburg, Albertstrasse 25, D-79104 Freiburg i.Br., Germany

    K. Starke  & Klaus Starke  & 

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Gilsbach, R., Hein, L. (2008). Presynaptic Metabotropic Receptors for Acetylcholine and Adrenaline/Noradrenaline. In: Südhof, T.C., Starke, K. (eds) Pharmacology of Neurotransmitter Release. Handbook of Experimental Pharmacology, vol 184. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-74805-2_9

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