Multiple conformations of native and recombinant human 5-hydroxytryptamine2A receptors are labeled by agonists and discriminated by antagonists

Molecular Pharmacology

Volumn 60, Issue 4, 2001, Pages 690-699

  López Giménez, Juan F ^a   Villazón, María ^b   Brea, José ^b   Loza, M Isabel ^b   Palacios, José M ^c   Mengod, Guadalupe ^a   Vilaró, M Teresa ^a  

^a INST D INVESTIGACIONS B   (Spain)

^b UNIVERSITY OF SANTIAGO DE COMPOSTELA   (Spain)

^c Almirall Prodesfarma SA ^*  (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

4 IODO 2,5 DIMETHOXYAMPHETAMINE; 6 CHLORO 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL]INDOLINE; ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; BROLAMFETAMINE; GUANOSINE TRIPHOSPHATE; KETANSERIN; MESULERGINE; RECEPTOR SUBTYPE; SEROTONIN 2A AGONIST; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR;

ANIMAL CELL; ARTICLE; AUTORADIOGRAPHY; BRAIN REGION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG COMPETITION; DRUG LABELING; DRUG RECEPTOR BINDING; FRONTAL CORTEX; HUMAN; HUMAN TISSUE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY;

ANIMALS; AUTORADIOGRAPHY; BINDING SITES; BRAIN; CHO CELLS; CRICETINAE; FLUOROBENZENES; HUMANS; INOSITOL PHOSPHATES; PIPERIDINES; PROTEIN CONFORMATION; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; TRANSFECTION; TRITIUM;

EID: 0034807596     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. 1c receptors in rat brain
2. A review of central 5-HT receptors and their function
3. 2 receptor subtypes: A family re-united?
4. Signal transduction differences between 5-hydroxytryptamine type 2A and type 2C receptor systems
5. Lithium amplifies agonist-dependent phosphatidylinositol responses in brain and salivary glands
6. 3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor
7. 1D/1B receptor antagonist
8. (2C) receptors
9. Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: Inverse agonist activity of antipsychotic drugs
10. 2C receptors: Evidence favoring the ternary complex and two-state models of agonist action
11. 1B receptor on CHO cells: Functional responses in the absence of radioligand binding
12. 2 serotonin receptors
13. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin)
14. 2 recognition sites
15. 2A antagonist with a favorable CNS safety profile
16. Agonist-receptor efficacy. I: Mechanisms of efficacy and receptor promiscuity
17. The classification of seven transmembrane receptors in recombinant expression systems
18. Agonist-specific receptor conformations
19. Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry
20. On the importance of the "antagonist assumption" to how receptors express themselves
21. 2C receptor antagonist
22. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
23. 2 receptors
24. 3H]ketanserin
25. 2A serotonin receptors selectively in primate brain
26. 2 and affinity constants for pharmacological competitive antagonists be estimated?
27. 125I-DOI, a new psychotomimetic radioligand, in the rat brain
28. 125I]DOI, a new psychotomimetic radioligand
29. 3H-ketanserin
30. 2C receptors
31. 3H]spiroperidol
32. Evidence for distinct 5-hydroxytryptamine2 binding site subtypes in cortical membrane preparations
33. 1D receptors
34. High-affinity agonist binding is not sufficient for agonist efficacy at 5-hydroxytryptamine2A receptors: Evidence in favor of a modified ternary complex model
35. 1D receptor antagonist
36. 2A receptor with an agonist, a partial agonist and an antagonist: Effects on apparent agonist affinities
37. Three-state and two-state models
38. G-Protein coupled receptors: Conformations and states
39. 2 receptor subtypes
40. 2 agonist radioligand
41. Binding sites for 5-hydroxytryptamine-2 receptor agonists are predominantly located in striosomes in the human basal ganglia