Coupling between agonist and chloride ionophore sites of the GABA(A) receptor: Agonist/antagonist efficacy of 4-PIOL

European Journal of Pharmacology

Volumn 409, Issue 3, 2000, Pages 233-242

  Rabe, Holger ^a   Picard, Raymonde ^a   Uusi Oukari, Mikko ^b   Hevers, Wulf ^a   Lüddens, Hartmut ^a   Korpi, Esa R ^a,b  

^a JOHANNES GUTENBERG UNIVERSITY   (Germany)

^b UNIVERSITY OF TURKU   (Finland)

Author keywords

Alanine; 4 PIOL; 5 (4 piperidine)isoxa zol 3 ol; 35S TBPS binding; Agonist coupling; Brain regional heterogeneity; GABA(A) receptor subtype; Muscimol; Taurine

Indexed keywords

3 HYDROXY 5 (4 PIPERIDYL)ISOXAZOLE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 4 PIPERIDINESULFONIC ACID; BETA ALANINE; GABOXADOL; IONOPHORE; MUSCIMOL; RECEPTOR SUBTYPE; RECOMBINANT RECEPTOR; TAURINE; TERT BUTYLBICYCLOPHOSPHOROTHIOATE S 35; THIOMUSCIMOL;

ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BRAIN ELECTROPHYSIOLOGY; BRAIN REGION; CEREBELLUM; CONTROLLED STUDY; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; GABAERGIC TRANSMISSION; GRANULE CELL; HUMAN; HUMAN CELL; LIGAND BINDING; MALE; NONHUMAN; PATCH CLAMP; PRIORITY JOURNAL; RAT;

ANIMALS; BICYCLO COMPOUNDS, HETEROCYCLIC; BRAIN; CELL LINE; GABA AGONISTS; HUMANS; IONOPHORES; ISOXAZOLES; LIGANDS; MALE; PIPERIDINES; RATS; RATS, WISTAR; RECEPTORS, GABA-A;

EID: 0034672452     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(00)00838-4     Document Type: Article

References (39)

1. International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acid(A) receptors: Classification on the basis of subunit structure and receptor function
2. θ, a novel γ-aminobutyric acid type A receptor subunit
3. Partial agonists for brain GABA/benzodiazepine receptor complex
4. Taurine acts on a subclass of GABAA receptors in mammalian brain in vitro
5. GABA(A) receptor subtypes: Ligand binding heterogeneity demonstrated by photoaffinity labeling and autoradiography
6. Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different α, β, and γ receptor subunit combinations
7. Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human γ-aminobutyric acid type A receptors
8. 35S-t-butylbicyclophosphorothionate binding in rat brain: An autoradiographic study
9. GABA-mimetic activity and effects on diazepam binding of aminosulphonic acids structurally related to piperidine-4-sulphonic acid
10. Steroid modulation of the chloride ionophore in rat brain: Structure-activity requirements, regional dependence and mechanism of action
11. Improved patch-clamp technique for high resolution current recording from cells and cell-free membrane patches
12. Identification of amino acid residues of GABA(A) receptor subunits contributing to the formation and affinity of the tert-butylbicyclophosphorothionate binding site
13. A novel class of GABA(A) receptor subunit in tissues of the reproductive system
14. Taurine and β-alanine act on both GABA and glycine receptors in Xenopus oocyte injected with mouse brain messenger RNA
15. THIP and isoguvacine are partial agonists of GABA-stimulated benzodiazepine receptor binding
16. 35S]thionate binding depends on γ-aminobutyric acid(A) receptor α subunit
17. Furosemide interactions with brain GABA(A) receptors
18. 35S]TBPS in cerebellar granular cell layer
19. Subtype specificity of γ-aminobutyric acid type A receptor antagonism by clozapine
20. Selective antagonist for the cerebellar granule cell-specific γ-aminobutyric acid type A receptor
21. 35S]butylbicyclophosphorothionate binding by antagonists: Relationship to patterns of subunit expression
22. Electrophysiological studies of the GABA(A) receptor ligand, 4-PIOL, on cultured hippocampal neurones
23. GABA(A) receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects
24. Biological function of GABA(A)/benzodiazepine receptor heterogeneity
25. GABA antagonists differentiate between recombinant GABA(A)/benzodiazepine receptor subtypes
26. Cerebellar GABA(A) receptor selective for a behavioural alcohol antagonist
27. Cerebellar γ-aminobutyric acid type A receptors: Pharmacological subtypes revealed by mutant mouse lines
28. Thiomuscimol, a new photoaffinity label for the GABA(A) receptor
29. Importance of a novel GABA(A) receptor subunit for benzodiazepine pharmacology
30. 3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABA(A) receptors which contain the α5 subunit
31. 35S]TBPS binding to γ-aminobutyric acidA receptors in rat brain
32. The benzodiazepine binding site of GABA(A) receptors
33. GABA(A) receptor ε and θ subunits display unusual structural variation between species and are enriched in the rat locus ceruleus
34. 3H]RY 80: A high-affinity, selective ligand for γ-aminobutyric acid(A) receptors containing α5 subunits
35. 35S]t-Butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to γ-aminobutyric acid-A and ion recognition sites
36. 35S]-t-butylbicyclophosphorothionate binding sites in cortex and cerebellum
37. The distribution of 13 GABA(A) receptor subunit mRNAs in the rat brain: I. Telencephalon, diencephalon, mesencephalon
38. 3H]diazepam binding in rat cortical membranes by GABA(A) agonists