Muscarinic allosteric modulation: M2/M3 subtype selectivity of gallamine is independent of G-protein coupling specificity

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 364, Issue 2, 2001, Pages 172-178

  Trankle C ^a   Kostenis, Evi ^b   Mohr, K ^a  

^a UNIVERSITY OF BONN   (Germany)

^b NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

Author keywords

Allosteric modulation; G protein coupling; Gallamine; Muscarinic M2 receptor; Muscarinic M3 receptor

Indexed keywords

CHOLINERGIC RECEPTOR; GALLAMINE; GUANINE NUCLEOTIDE BINDING PROTEIN; MUSCARINIC M2 RECEPTOR; MUSCARINIC M3 RECEPTOR; RECEPTOR SUBTYPE;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHIMERA; CONTROLLED STUDY; DISSOCIATION; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; MOUSE; NONHUMAN; RAT; RECEPTOR SENSITIVITY;

ALLOSTERIC REGULATION; ANIMALS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; GALLAMINE TRIETHIODIDE; GTP-BINDING PROTEINS; HUMANS; N-METHYLSCOPOLAMINE; NEUROMUSCULAR NONDEPOLARIZING AGENTS; PARASYMPATHOLYTICS; RATS; RECEPTOR, MUSCARINIC M2; RECEPTOR, MUSCARINIC M3; RECEPTORS, MUSCARINIC;

EID: 0034906290     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002100100441     Document Type: Article

References (43)

1. Identification of a family of muscarinic acetylcholine receptor genes
2. Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells
3. XVII. Classification of muscarinic acetylcholine receptors
4. High-efficiency transformation of mammalian cells by plasmid DNA
5. Allosteric interactions at muscarinic cholinoceptors
6. Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3′-phthalimido-propyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors
7. Propylbenzilylcholine mustard labels an acidic residue in transmembrane helix 3 of the muscarinic receptor
8. Calculating receptor number from binding experiments using same compound as radioligand and competitor
9. Estimation of the affinities of allosteric ligands using radioligand binding and pharmacologic null methods
10. Gallamine allosterically antagonizes muscarinic receptor-mediated inhibition of adenylate cyclase activity in the rat myocardium
11. Allosteric binding sites on muscarinic receptors
12. Two allosteric modulators interact at a common site on cardiac muscarinic receptors
13. Interactions of alcuronium, TMB-8, and other allosteric ligands with muscarinic acetylcholine receptors: Studies with chimeric receptors
14. 5 muscarinic receptor subtypes
15. Use of chimeric muscarinic receptors to investigate epitopes involved in allosteric interactions
16. Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors
17. Site-directed mutagenesis of the putative human muscarinic M2 receptor binding site
18. Allosteric modulators of ligand binding to muscarinic acetylcholine receptors
19. Positive interactions on cardiac muscarinic receptors: Effect of chemical modifications of disulphide and carboxyl groups
20. 5 muscarinic acetylcholine receptors
21. Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
22. Influence of ligand choice on the apparent binding profile of gallamine to cardiac muscarinic receptors. Identification of three main types of gallamine-muscarinic receptor interactions
23. Allosteric antagonists of the muscarinic acetylcholine receptor
24. Allosteric interactions at the m1, m2 and m3 muscarinic receptor subtypes
25. Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor
26. Protein measurement with the folin phenol reagent
27. On the interaction of gallamine with muscarinic receptor subtypes
28. Allosteric effect of gallamine on muscarinic cholinergic receptor binding: Influence of guanine nucleotides and conformational state
29. A cDNA cloning vector that permits expression of cDNA inserts in mammalian cells
30. Modulation of the structure-binding relationships of antagonists for muscarinic acetylcholine receptor subtypes
31. 2 receptors as deduced from buffer dependent potency shifts
32. Modification of the binding properties of muscarinic receptors by gallamine
33. Divergent modes of action among cationic allosteric modulators of muscarinic M2 receptors
34. Search for lead structures to develop new allosteric modulators of muscarinic receptors
35. 2 receptor binding of the selective antagonist AF-DX 384: Possible involvement of the common allosteric site
36. 2 receptors
37. Allosteric modulation of muscarinic acetylcholine receptors
38. Molecular biology of muscarinic acetylcholine receptors
39. Molecular basis of receptor/G-protein-coupling selectivity
40. Identification of a small intracellular region of the muscarinic m3 receptor as a determinant of selective coupling to PI turnover
41. Delineation of muscarinic receptor domains conferring selectivity of coupling to guanine nucleotide-binding proteins and second messengers
42. Peptide mapping studies on muscarinic receptors: Receptor structure and location of the ligand binding site
43. The third extracellular loop of the 2-adrenergic receptor can modulate receptor/G protein affinity