Allosteric site in M2 acetylcholine receptors: Evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 372, Issue 4, 2006, Pages 267-276

  Großmüller, Maren ^a   Antony, Johannes ^a   Tränkle, Christian ^a   Holzgrabe, Ulrike ^b   Mohr, Klaus ^a  

^a UNIVERSITY OF BONN   (Germany)

^b UNIVERSITY OF WÜRZBURG   (Germany)

Author keywords

3H oxotremorine M; Allosteric modulation; Gallamine; Muscarinic M2 receptor; Receptor conformation; W84; WDuo3

Indexed keywords

1,3 BIS[4 (PHTHALIMIDOMETHOXYIMINOMETHYL)PYRIDINIUM 1 YL]PROPANE DIBROMIDE; 1,6 HEXAMETHYLENEBIS[DIMETHYL(3 PHTHALIMIDOPROPYL)AMMONIUM BROMIDE]; GALLAMINE; METHYLSCOPOLAMINE; MUSCARINIC M2 RECEPTOR; MUSCARINIC M2 RECEPTOR AGONIST; MUSCARINIC M2 RECEPTOR ANTAGONIST; OBIDOXIME; OXOTREMORINE; PHTHALIMIDE DERIVATIVE; PYRIDINIUM DERIVATIVE; RADIOLIGAND; TRITIUM; UNCLASSIFIED DRUG; 1,3 BIS(4 (PHTHALIMIDOMETHOXYIMINOMETHYL)PYRIDINIUM 1 YL)PROPANE; 1,3-BIS(4-(PHTHALIMIDOMETHOXYIMINOMETHYL)PYRIDINIUM-1-YL)PROPANE; DRUG DERIVATIVE; GALLAMINE TRIETHIODIDE; HEXAMETHYLENEBIS(DIMETHYL (3 PHTHALIMIDOPROPYL)AMMONIUM BROMIDE); HEXAMETHYLENEBIS(DIMETHYL-(3-PHTHALIMIDOPROPYL)AMMONIUM BROMIDE); MUSCARINIC AGENT; MUSCARINIC RECEPTOR BLOCKING AGENT; OXOTREMORINE M;

ALLOSTERISM; ANIMAL TISSUE; ARTICLE; BINDING ASSAY; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; HEART; NONHUMAN; RECEPTOR AFFINITY; SWINE; TISSUE HOMOGENATE; ANIMAL; BINDING COMPETITION; BINDING SITE; CHEMISTRY; DRUG EFFECT; HEART MUSCLE; IN VITRO STUDY; METABOLISM; PROTEIN CONFORMATION;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; ANIMALS; BINDING, COMPETITIVE; GALLAMINE TRIETHIODIDE; MUSCARINIC AGONISTS; MUSCARINIC ANTAGONISTS; MYOCARDIUM; N-METHYLSCOPOLAMINE; OBIDOXIME CHLORIDE; OXOTREMORINE; PHTHALIMIDES; PROTEIN CONFORMATION; PYRIDINIUM COMPOUNDS; RECEPTOR, MUSCARINIC M2; SWINE;

EID: 31144458160     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-005-0023-4     Document Type: Article

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