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Synthesis and pharmacological characterization of
dibenzodiazepinone-type muscarinic M2-receptor
antagonists conjugated to fluorescent dyes or
small peptides.

URN to cite this document:
urn:nbn:de:bvb:355-epub-448399
Weinhart, Corinna G.
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Synthesis and pharmacological characterization of dibenzodiazepinone-type muscarinic M2-receptor antagonists conjugated to fluorescent dyes or small peptides.
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Date of publication of this fulltext: 18 Feb 2021 09:34


Abstract (English)

In humans, the family of muscarinic acetylcholine receptors (mAChR, MRs) comprises five subtypes (M1R-M5R), belonging to class A of the GPCR superfamily. MRs mediate the action of the neurotransmitter acetylcholine (ACh) in the central and peripheral nervous system. Whereas the M1R, M3R and M5R preferably couple to Gq-type G-proteins, the M2 and M4 receptor mainly activate Gi/o-type G-proteins. ...

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Translation of the abstract (German)

Beim Menschen umfasst die Familie der muskarinischen Acetylcholinrezeptoren (mAChR, MRs) fünf Subtypen (M1R-M5R), die zur Klasse A der GPCR-Superfamilie gehören. MRs vermitteln die die Wirkung des Neurotransmitters Acetylcholin (ACh) im zentralen und peripheren Nervensystem. Während der M1R, M3R und M5R bevorzugt an Gq-Typ G-Proteine koppeln, aktivieren der M2 und M4-Rezeptor hauptsächlich ...

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