Differential modulation by GTPγS of agonist and inverse agonist binding to h5-HT1A receptors revealed by [3H]-WAY100,635

British Journal of Pharmacology

Volumn 132, Issue 2, 2001, Pages 518-524

  Newman Tancredi, A ^a   Verriele L ^a   Millan, M J ^a  

^a INSTITUT DE RECHERCHES SERVIER   (France)

Author keywords

Affinity ratios; GTP S; Inverse agonist; S14506; S14671; WAY100,635

Indexed keywords

1 (7 METHOXY 1 NAPHTHYL) 4 [2 (2 THENOYLAMINO)ETHYL]PIPERAZINE; 1 [2 (4 FLUOROBENZAMIDO)ETHYL] 4 (7 METHOXY 1 NAPHTHYL)PIPERAZINE; 2 DIPROPYLAMINO 8 HYDROXYTETRALIN; BUSPIRONE; GUANOSINE TRIPHOSPHATE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; SEROTONIN; SEROTONIN 1 RECEPTOR; SEROTONIN ANTAGONIST; 4 (BENZODIOXAN 5 YL) 1 (INDAN 2 YL)PIPERAZINE; 4-(BENZODIOXAN-5-YL)-1-(INDAN-2-YL)PIPERAZINE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); LIGAND; PIPERAZINE DERIVATIVE; PYRIDINE DERIVATIVE; SEROTONIN AGONIST; SEROTONIN RECEPTOR;

ARTICLE; BINDING AFFINITY; CHO CELL; DISSOCIATION CONSTANT; LIGAND BINDING; MOLECULAR DYNAMICS; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN INTERACTION; RECEPTOR BINDING; ANIMAL; DRUG EFFECT; HAMSTER; HUMAN; KINETICS; METABOLISM;

8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN; ANIMALS; CHO CELLS; CRICETINAE; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; KINETICS; LIGANDS; PIPERAZINES; PYRIDINES; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 0034746150     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703832     Document Type: Article

References (37)

1. 1A receptor antagonist (S)UH301 blocks (R)-8-OH-DPAT-induced inhibition of serotonergic dorsal raphe cell firing in the rat
2. 1A receptors and intrinsic activity
3. Signal transduction by G-proteins: 1994 edition
4. Molecular biology of 5-HT receptors
5. 1A agonist and potential anxiolytic agent
6. Intrinsic activity of enantiomers of 8-hydroxy-2-(di-n-propylamino)tetralin and its analogs at 5-hydroxytryptamine 1A receptors that are negatively coupled to adenylate cyclase
7. 1A receptors
8. Inverse agonism at heptahelical receptors: Concept, experimental approach and therapeutic potential
9. 1A receptor agonists: Recent developments and controversial issues
10. 2C receptors
11. 1A receptor antagonist
12. Relative affinities of drugs acting at cholinoceptors in displacing agonist and antagonist radioligands: The NMS/Oxo-M ratio as an index of efficacy at cortical muscarinic receptors
13. 3H]-PAT
14. 1A receptors in rat brain membranes
15. A three binding site hypothesis for the interaction of ligands with monoamine G-protein-coupled receptors: Implications for combinatorial drug design
16. 3H]-WAY100,635
17. 3H]-p-MPPF
18. 2 G-protein-coupled receptor: Utilization of receptor binding affinities
19. 1A receptors
20. 1A receptors
21. 1A receptors: II. Modulation of hippocampal serotonin release in relation to potential anxiolytic properties
22. 2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in models of potential antidepressant activity
23. S 14671: A naphtylpiperazine 5-hydroxytryptamine1A agonist of exceptional potency and high efficacy possessing antagonist activity at 5-hydroxytryptamine1C/2 receptors
24. 1A receptors
25. 1A receptors
26. 1A) receptors
27. 1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY100,635
28. 35S]-GTPγS binding study
29. 3H]-S 15535: Definition of its binding profile using agonists, antagonists and inverse agonists
30. 1A receptor antagonists
31. 1A receptor antagonists
32. 35S]GTPγS binding
33. 3H]spiperone discriminates between the G-protein-coupled and uncoupled forms
34. 3H]-lisuride labels free receptor and receptor coupled to G-protein
35. 1A receptor agonist - Antagonist binding difference as a measure of intrinsic activity in recombinant and native systems