The noncompetitive inhibitor quinacrine modifies the desensitization kinetics of muscle acetylcholine receptors

Molecular Pharmacology

Volumn 60, Issue 2, 2001, Pages 235-243

  Spitzmaul, Guillermo ^a   Dilger, James P ^b   Bouzat, Cecilia ^a  

^a UNIVERSIDAD NACIONAL DEL SUR   (Argentina)

^b STONY BROOK UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; MEPACRINE; NICOTINIC RECEPTOR;

AGONIST; ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; DRUG EFFECT; DRUG INHIBITION; DRUG MECHANISM; MEMBRANE CURRENT; MEMBRANE PERMEABILITY; PRIORITY JOURNAL; RECEPTOR DOWN REGULATION;

EID: 0034925442     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.60.2.235     Document Type: Article

References (32)

1. Quinacrine (mepacrine) action at frog end-plate
2. Identification of acetylcholine receptor channel-lining residues in the M1 segment of the α-subunit
3. The high-affinity quinacrine binding site is located at a non-annular lipid domain of the nicotinic acetylcholine receptor
4. Binding sites for exogenous and endogenous non-competitive inhibitors of the nicotinic acetylcholine receptor
5. Quinacrine and ethidium bind to different loci on the Torpedo acetylcholine receptor
6. Desensitization of mouse Nicotinic Acetylcholine Receptor channels. A two-gate mechanism
7. Structural basis of the different gating kinetics of fetal and adult nicotinic acetylcholine receptors
8. Mutations at lipid-exposed residues of the acetylcholine receptor affect its gating kinetics
9. Identifying the lipid-protein interface of the Torpedo nicotinic acetylcholine receptor: Secondary structure implications
10. Time-resolved photolabeling by quinacrine azide of a noncompetitive inhibitor site of the nicotinic acetylcholine receptor in a transient, agonist-induced state
11. Mechanisms of barbiturate inhibition of acetylcholine receptor channels
12. Desensitization of acetylcholine receptors in BC3H-1 cells
13. 3H]quinacrine azide in the active state of the nicotinic acetylcholine receptor
14. A hydrophobic photolabel inhibits Nicotinic Acetylcholine Receptors via open-channel block following a slow step
15. A molecular scheme for the reaction between acetylcholine and nicotinic channels
16. Asymmetric contribution of the conserved disulfide loop to subunit oligomerization and assembly of the nicotinic acetylcholine receptor
17. Studies on the electrogenic action of acetylcholine with Torpedo marmorata electric organ
18. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches
19. Quinacrine noncompetitive inhibitor binding site localized on the Torpedo acetylcholine receptor in the open state
20. Opening rate of acetylcholine receptor channels
21. Epibatidine binds with unique site and state selectivity to muscle nicotinic acetylcholine receptors
22. Acetylcholine and epibatidine binding to muscle acetylcholine receptors distinguish between concerted and uncoupled models
23. A conformational intermediate between the resting and desensitized states of the nicotinic acetylcholine receptor
24. Single acetylcholine-activated channels show burst-kinetics in the presence of desensitizing concentrations of agonist
25. γ- and δ-subunits regulate the affinity and the cooperativity of ligand-binding to the acetylcholine receptor
26. Molecular dissection of subunit interfaces in the acetylcholine receptor: Identification of determinants of alpha-conotoxin M1 selectivity
27. Conserved tyrosines in the alpha subunit of the nicotinic acetylcholine receptor stabilize quaternary ammonium groups of agonists and curariform antagonists
28. Functional consequences of agonist-mediated state transitions in the cholinergic receptor
29. Local anesthetics and histrionicotoxin are allosteric inhibitors of the acetylcholine receptor
30. Amphetamine acts as a channel blocker of the acetylcholine receptor
31. Mutations in the M1 region of the icotinic acetylcholine receptor alter the sensitivity to inhibition by quinacrine
32. Quinacrine binds to the lipid-protein interface of the Torpedo acetylcholine receptor: A fluorescence study