Mechanism of tacrine block at adult human muscle nicotinic acetylcholine receptors

Journal of General Physiology

Volumn 120, Issue 3, 2002, Pages 369-393

  Prince, Richard J ^a   Pennington, Richard A ^b   Sine, Steven M ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b MAYO CLINIC   (United States)

Author keywords

Anticholinesterase; Kinetic analysis; Maximum likelihood; Open channel block; Single channel recording

Indexed keywords

ACETYLCHOLINE; CHOLINESTERASE INHIBITOR; NICOTINIC RECEPTOR; TACRINE;

ARTICLE; CHANNEL GATING; CONCENTRATION RESPONSE; DRUG MECHANISM; ELECTRIC POTENTIAL; HUMAN; HUMAN CELL; KINETICS; LIGAND BINDING; MAXIMUM LIKELIHOOD METHOD; MUSCLE; PATCH CLAMP; PROTEIN ANALYSIS; PROTEIN EXPRESSION;

ACETYLCHOLINE; ADULT; BINDING SITES; CELL LINE; CHOLINESTERASE INHIBITORS; HUMANS; LIGANDS; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES; RECEPTORS, NICOTINIC; TACRINE; TRANSFECTION;

EID: 0036715076     PISSN: 00221295     EISSN: None     Source Type: Journal    
DOI: 10.1085/jgp.20028583     Document Type: Article

References (61)

1. Voltage jump analysis of procaine action at frog end-plate
2. End-plate channel opening and the kinetics of quinacrine (mepacrine) block
3. A new look at the statistical model identification
4. Luminal and non-luminal non-competitive inhibitor binding sites on the nicotinic acetylcholine receptor
5. Desensitization of mouse nicotinic acetylcholine receptor channels. A two-gate mechanism
6. Voltage dependence of mouse acetylcholine receptor gating: Different charge movements in di-, mono- and unliganded receptors
7. Voltage dependencies of the effects of chlorpromazine on the nicotinic receptor channel from mouse muscle cell line So18
8. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors
9. Tacrine and physostigmine block nicotinic receptors in Xenopus oocytes injected with Torpedo electroplaque membranes
10. Functional architecture and dynamics of the nicotinic acetylcholine receptor, an allosteric ligand-gated ion channel
11. An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor
12. Substance P reduces acetylcholine-induced currens in isolated bovine chromaffin cells
13. Relationship between membrane excitability and single channel open-close kinetics
14. On the stochastic properties of single ion channels
15. The principles of the stochastic interpretation of ion-channel mechanisms
16. Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate
17. Mechanisms of barbiturate inhibition of acetylcholine receptor channels
18. Desensitization of acetylcholine receptors in BC3H-1 cells
19. Effect of tacrine on intracellular calcium in cholinergic SN56 neuronal cells
20. Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds
21. Activation and cooperative multi-ion block of single nicotinic-acetylcholine channel currents of Ascaris muscle by the tetrahydropyrimidine anthelmintic, morantel
22. Recovery from the rapid desensitization of nicotinic acetylcholine receptor channels on mouse muscle
23. Tetrahydroaminoacridine block of N-methyl-D-aspartate-activated cation channels in cultured hippocampal neurons
24. The cholinergic pharmacology of tetrahydroaminoacridine in vivo and in vitro
25. Deactivation and desensitization of mouse embryonic- and adult-type nicotinic receptor channel currents
26. A study of the desensitization produced by acetylcholine at the motor end-plate
27. Muscarinic subtype selectivity of tetrahydroaminoacridine: Possible relationship to its capricious efficacy
28. Effects of NIK-247 and tacrine on muscarinic receptor subtypes in rats
29. Block by acetylcholine of mouse muscle nicotinic receptors, stably expressed in fibroblasts
30. Genetic manipulation of ion channels: A new approach to structure and mechanism
31. Nicotinic acetylcholine receptor at 4.6 A resolution: Transverse tunnels in the channel wall
32. Trapping of an open-channel blocker at the frog neuromuscular acetylcholine channel
33. The charge carried by single-channel currents of rat cultured muscle cells in the presence of local anaesthetics
34. Local anaesthetics transiently block currents through single acetylcholine-receptor channels
35. Ion channel block by acetylcholine, carbachol and suberyldicholine at the frog neuromuscular junction
36. Congenital myasthenic syndrome caused by decreased agonist binding affinity due to a mutation in the acetylcholine receptor epsilon subunit
37. Mechanisms of noncompetitive inhibition of acetylcholine-induced single-channel currents
38. Delimiting the binding site for quaternary ammonium lidocaine derivatives in the acetylcholine receptor channel
39. Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitro
40. Molecular dissection of subunit interfaces in the acetylcholine receptor. Identification of residues that determine agonist selectivity
41. Epibatidine activates muscle acetylcholine receptors with unique site selectivity
42. Epibatidine binds with unique site and state selectivity to muscle nicotinic acetylcholine receptors
43. Estimating single-channel kinetic parameters from idealized patch-clamp data containing missed events
44. The anthelmintic pyrantel acts as a low efficacious agonist and an openchannel blocker of mammalian acetylcholine receptors
45. Single acetylcholine-activated channels show burst-kinetics in presence of desensitizing concentrations of agonist
46. Activation of Torpedo acetylcholine receptors expressed in mouse fibroblasts. Single channel current kinetics reveal distinct binding affinities
47. Agonists block currents through acetylcholine receptor channels
48. Activation of acetylcholine receptors on clonal BC3H-1 cells by high concentrations of agonist
49. Local anesthetics and histrionicotoxin are allosteric inhibitors of the acetylcholine receptor. Studies of clonal muscle cells
50. Lysine scanning mutagenesis delineates structural model of the nicotinic receptor ligand binding domain
51. The noncompetitive inhibitor quinacrine modifies the desensitization kinetics of muscle acetylcholine receptors
52. Tacrine interacts with different sites on nicotinic receptor subtypes in SH-SY5Y neuroblastoma and M10 cells
53. Tacrine interacts with an allosteric activator site on alpha 4 beta 2 nAChRs in M10 cells
54. Acetylcholine receptor channel imaged in the open state
55. Tetrahydroaminoacridine blocks and prolongs NMDA receptor-mediated responses in a voltage-dependent manner
56. The location of the gate in the acetylcholine receptor channel
57. Ionic blockage of sodium channels in nerve
58. Activation of recombinant mouse acetylcholine receptors by acetylcholine, carbamylcholine and tetramethylammonium
59. Competitive potentiation of acetylcholine effects on neuronal nicotinic receptors by acetylcholinesterase-inhibiting drugs