Benzodiazepines induce a conformational change in the region of the γ-aminobutyric acid type a receptor α1-subunit M3 membrane-spanning segment

Molecular Pharmacology

Volumn 58, Issue 5, 2000, Pages 1129-1136

  Williams, Daniel B ^a   Akabas, Myles H ^b  

^a New York Presbyterian Columbia University Medical Center   (United States)

^b ALBERT EINSTEIN COLLEGE OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; BENZODIAZEPINE DERIVATIVE; CYSTEINE; DIAZEPAM; FLUMAZENIL; GLUTAMIC ACID; PHENYLALANINE; RECEPTOR SUBUNIT;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CHEMICAL REACTION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG MECHANISM; DRUG RECEPTOR BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN DOMAIN; RAT; REACTION TIME;

EID: 0033789013     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.58.5.1129     Document Type: Article

References (46)

1. Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the alpha subunit
2. Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allostoric modulation of gamma-aminobutyric acid A receptors
3. GABA(A) receptor needs two homologous domains of the beta-subunit for activation by GABA but not by pentobarbital
4. The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid
5. Identification of transduction elements for benzodiazepine modulation of the GABA(A) receptor: Three residues are required for allosteric coupling
6. Mapping the agonist binding site of the GABAA receptor: Evidence for a beta-strand
7. Molecular dissection of benzodiazepine binding and allosteric coupling using chimeric gamma-aminobutyric acid A receptor subunits
8. A single residue in the M2-M3 loop is a major determinant of coupling between binding and gating in neuronal nicotinic receptors
9. Modulation of neurotransmitter action: Control of the gamma-aminobutyric acid response through the benzodiazepine receptor
10. Stoichiometry of a recombinant GABA(A) receptor
11. Conformational changes in benzediazepine receptors induced by the antagonist Ro 15-1788
12. Cysteine and disulfide scanning reveals a regulatory alpha-helix in the cytoplasmic domain of the aspartate receptor
13. The major site of photoaffinity labeling of the gamma-aminobutyric acid type A receptor by [3H]flunitrazepam is histidine 102 of the alpha subunit
14. Mutagenesis of the rat alpha1 subunit of the gamma-aminobutyric acid(A) receptor reveals the importance of residue 101 in determining the allosteric effects of benzodiazepine site ligands
15. Hippocampal GABA(A) channel conductance increased by diazepam
16. Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer
17. Benzodiazepines do not modulate desensitization of recombinant alpha1beta2gamma2 GABA(A) receptors
18. Benzodiazepine-insensitive mice generated by targeted disruption of the gamma 2 subunit gene of gamma-aminobutyric acid type A receptors
19. Kinetics of the reaction of p-chloromercuribenzoate with the sulfhydryl groups of glutathione, 2-mercapto-ethanol, and phosphorylase b
20. The diversity of GABA(A) receptors: Pharmacological and electrophysiological properties of GABA(A) channel subtypes
21. Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins
22. Identification of intracellular and extracellular domains mediating signal transduction in the inhibitory glycine receptor chloride channel
23. GABA(A) receptor channels
24. Which GABA(A)-receptor subtypes really occur in the brain?
25. Benzodiazepine and beta-carboline interactions with GABA(A) receptor-gated chloride channels in mammalian cultured spinal cord neurons
26. Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors
27. Quaternary structure of the native GABA(A) receptor determined by electron microscopic image analysis
28. + antiporter of Escherichia coli is exposed and faces the cell exterior
29. Importance of a novel GABA(A) receptor subunit for benzediasepine pharmacology
30. From ion currents to genomic analysis: Recent advances in GABA(A) receptor research
31. Benzodiazepine and betacarboline regulation of single GABA(A) receptor channels of mouse spinal neurones in culture
32. Sequence and functional expression of the GABA(A) receptor shows a ligand-gated receptor super-family
33. Structure and pharmacology of gamma-aminobutyric acid A receptor subtypes
34. Allosteric modulation by benzodiazepine receptor ligands of the GABA(A) receptor channel expressed in Xenopus oocytes
35. The benzodiazepine binding site of GABA(A) receptors
36. Role of the conserved lysine residue in the middle of the predicted extracellular loop between M2 and M3 in the GABA(A) receptor
37. Functional domains of GABA(A) receptors
38. The gamma 2 subunit is an integral component of the gamma-aminobutyric acid A receptor but the alpha 1 polypeptide is the principal site of the agonist benzodiazepine photoaffinity labeling reaction
39. Beta-Carboline gamma-aminobutyric acid(A) receptor inverse agonists modulate gamma-aminobutyric acid via the loreclezole binding site as well as the benzodiazepine site
40. Diasepam and (-)-pentobarbital: Fluctuation analysis reveals different mechanisms for potentiation of gamma-aminobutyric acid responses in cultured central neurons
41. Stoichiometry and assembly of a recombinant GABA(A) receptor subtype
42. Localization of erythrocyte membrane sulfhydryl groups essential for glucose transport
43. Gamma-Aminobutyric acid increases the water accessibility of M3 membrane-spanning segment residues in gamma-aminobutyric acid type A receptors
44. Amino acids lining the channel of the gamma-aminobutyric acid type A receptor identified by cysteine substitution
45. Identification of channel-lining residues in the M2 membrane-spanning segment of the GABA(A) receptor alpha1 subunit
46. Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones