6,7-Dihydro-2-benzothiophen-4(5H)-ones: A novel class of GABA-A α5 receptor inverse agonists

Journal of Medicinal Chemistry

Volumn 45, Issue 6, 2002, Pages 1176-1179

  Chambers, Mark S ^a   Atack, John R ^a   Bromidge, Frances A ^a   Broughton, Howard B ^a   Cook, Susan ^a   Dawson, Gerard R ^a   Hobbs, Sarah C ^a   Maubach, Karen A ^a   Reeve, Austin J ^a   Seabrook, Guy R ^a   Wafford, Keith ^a   Ma, Angus M ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 6,6 DIMETHYL 3 (2 HYDROXYETHYL)THIO 1 (THIAZOL 2 YL) 6,7 DIHYDRO 2 BENZOTHIOPHEN 4(5H)ONE; CHLORIDE CHANNEL; LIGAND; NOOTROPIC AGENT; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING SITE; COGNITION; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ANIMALS; CELLS, CULTURED; COGNITION; HUMANS; KETONES; MICE; RECEPTORS, GABA-A; THIAZOLES; THIOPHENES; XENOPUS LAEVIS;

EID: 0037075810     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010471b     Document Type: Article

References (41)

1. A receptors: Classification on the basis of subunit structure and receptor function
2. Effects of benzodiazepines on acquisition and performance: A critical assessment
3. Benzodiazepines and human memory: A review
4. Benzodiazepine receptor antagonists flumazenil and CGS 8216 and inverse agonist β-CCM enhance spatial learning in the rat: Dissociation from anxiogenic actions
5. Severe anxiety induced by FG 7142, a β-carboline ligand for benzodiazepine receptors
6. DMCM: A potent convulsive benzodiazepine receptor ligand
7. Acute and chronic effects of the benzodiazepine receptor ligand FG 7142: Proconvulsant properties and kindling
8. Psychotogenic properties of benzodiazepine receptor inverse agonists
9. A receptors have α5β3γ2 pharmacological characteristics
10. A receptor subtypes
11. β-carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of β-carboline-3-carboxylic acid
12. Synthesis of 3,6-disubstituted β-carbolines which possess either benzodiazepine antagonist or agonist activity
13. Synthesis of novel 3-substituted β-carbolines as benzodiazepine receptor ligands: Probing the benzodiazepine receptor pharmacophore
14. Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b′]diindoles. A novel class of rigid, planar benzodiazepine receptor ligands
15. Synthesis of substituted 7,12-dihydropyrido [3,2-b:5,4-b′] diindoles. Rigid planar benzodiazepine receptor ligands with inverse agonist/antagonist properties
16. 2-Arylpyrazolo[4,3-c]-quinolin-3-ones: Novel agonist, partial agonist, and antagonist of benzodiazepines
17. Structure-activity relationship studies at the benzodiazepine receptor (BZR): A comparison of the substituent effects of pyrazoloquinolinone analogs
18. Thienylpyrazoloquinolines: Potent agonists and inverse agonists to benzodiazepine receptors
19. A/benzodiazepine receptors
20. 6-(Alkylamino)-3-aryl-l,2,4-triazolo[3,4-a]-phthalazines. A new class of benzodiazepine receptor ligands
21. Synthesis and binding affinity of 2-phenylimidazo[1,2-a]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type
22. Novel 2-phenylimidazo[1,2-a] pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: Synthesis, binding affinity, and in vivo studies
23. Pharmacological profile of the imidazopyridine zolpidem at benzodiazepine receptors and electrocorticogram in rats
24. A/BzR subtypes: Effect of C(3) substituents on receptor subsite selectivity
25. A/benzodiazepine receptor subtype
26. A receptors
27. Synthetic and computer-assisted analysis of the structural requirements for selective, high affinity ligand binding to diazepam-insensitive benzodiazepine receptors
28. A receptor
29. A/BzR subtypes (α1/β3γ2, α5/β3γ2, and α6β3γ2) via a comprehensive ligand-mapping approach
30. ABzR sites
31. Chemical similarity using physiochemical property descriptors
32. A receptors
33. Cloning of cDNAs encoding the human γ-aminobutyric acid type A receptor α6 subunit and characterization of the pharmacology of α6-containing receptors
34. A receptor subtypes
35. A receptors containing γ3 subunits
36. A receptors containing bovine α1,β1, γ21 subunits stably transfected into mouse fibroblast L-cells