Diverse signalling by 5-hydroxytryptamine (5-HT) receptors

Biochemical Pharmacology

Volumn 60, Issue 12, 2000, Pages 1743-1750

  Pauwels, Petrus J ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

5 HT receptor; Differential signalling; Receptor isoform; Signal transduction pathway

Indexed keywords

1 NAPHTHYLPIPERAZINE; 2,3,6,7 TETRAHYDRO 1' METHYL 5 [[2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL) 4 BIPHENYLYL]CARBONYL]SPIRO[FURO[2,3 F]INDOLE 3,4' PIPERIDINE]; 3 (3 DIMETHYLAMINOPROPYL) 4 HYDROXY N [4 (4 PYRIDINYL)PHENYL]BENZAMIDE; 3,N DIMETHYL N [1 METHYL 3 (4 METHYL 1 PIPERIDINYL)PROPYL]BENZENESULFONAMIDE; 4 AMINO 5 CHLORO 2 METHOXYBENZOIC ACID 2 (3,5 DIMETHYLPIPERIDINO)ETHYL ESTER; CHLORPROMAZINE; CLOZAPINE; CYPROHEPTADINE; GUANINE NUCLEOTIDE BINDING PROTEIN; HALOPERIDOL; KETANSERIN; LOXAPINE; MESULERGINE; METITEPINE; MIANSERIN; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL)[1,1' BIPHENYL] 4 CARBOXAMIDE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 3 METHYL 4 (4 PYRIDYL)BENZAMIDE; OLANZAPINE; RECEPTOR SUBTYPE; RISPERIDONE; SEROTONIN; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR; SPIPERONE; UNCLASSIFIED DRUG;

ALTERNATIVE RNA SPLICING; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; PROTEIN VARIANT; RECEPTOR AFFINITY; REVIEW; RNA EDITING; SIGNAL TRANSDUCTION;

EID: 0034672622     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(00)00476-7     Document Type: Article

References (73)

1. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin)
2. The classification of seven transmembrane receptors in recombinant expression systems
3. The structure and signalling properties of 5-HT receptors: An endless diversity?
4. Agonist-receptor efficacy II: Agonist trafficking of receptor signals
5. 7TM receptors: The splicing on the cake
6. Genetic variation in human 5-HT receptors: Potential pathogenetic and pharmacological role
7. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor
8. 2-adrenergic receptor: Extending the ternary complex model
9. Inverse agonist activity of β-adrenergic antagonists
10. G protein-coupled receptors. II: Mechanisms of agonist activation
11. Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors
12. 35S]GTPγS binding by 5-HT(1A) receptor agonists in recombinant cell lines: Modulation of apparent efficacy by G-protein activation state
13. Interaction of 5-HT(1B/D) ligands with recombinant h 5-HT(1A) receptors: Intrinsic activity and modulation by G-protein activation state
14. μ-Opioid receptor-stimulated guanosine-5'-O-(γ-thio)-triphosphate binding in rat thalamus and culture cell lines: Signal transduction mechanisms underlying agonist efficacy
15. S 14506: A novel, potent, high-efficacy 5-HT(1A) agonist and potential anxiolytic agent
16. 5-HT(1B/D) receptor antagonists
17. How receptors talk to trimeric G proteins
18. 2 adrenergic receptor. Evidence for ligand-specific conformational changes
19. Cellular signalling by an agonist-activated receptor/G(sα) fusion protein
20. GPCR-G(α) fusion proteins: Molecular analysis of receptor-G-protein coupling
21. Insights into ligand pharmacology using receptor-G-protein fusion proteins
22. 3
23. 351 in the rat G(αo) protein
24. Modulation of 5-HT(1A) receptor activation by its interaction with wild-type and mutant G(αi3) proteins
25. Regulation of G protein activation and effector modulation by fusion proteins between the human 5-hydroxytryptamine(1A) receptor and the α subunit of G(i1)α. Differences in receptor constitutive activity imparted by single amino acid substitutions in G(i1)α
26. Agonist occupation of an α(2A)-adrenoreceptor-G(i1)α fusion protein results in activation of both receptor-linked and endogenous G(i) proteins. Comparisons of their contributions to GTPase activity and signal transduction and analysis of receptor-G protein activation stoichiometry
27. 370Lys α(2B)-adrenoceptor: G(α15) fusion proteins
28. G(α15) and G(α16) couple a wide variety of receptors to phospholipase C
29. 373Lys) and G(αo) protein co-expression: Evidence for inverse agonism
30. A conserved threonine residue in the second intracellular loop of the 5-hydroxytryptamine 1A receptor directs signalling specificity
31. Selective coupling of prostaglandin E receptor EP3D to G(i) and G(s) through interaction of α-carboxylic acid of agonist and arginine residue of seventh transmembrane domain
32. 2-adrenergic receptor inhibition of stimulus-secretion coupling
33. Constitutive activation of a single effector pathway: Evidence for multiple activation states of a G protein-coupled receptor
34. 2-adrenergic receptor
35. 2-adrenoceptor by sustained treatment with inverse agonists but not antagonists
36. 2-adrenoceptor in transfected neuroblastoma X glioma hybrid cells
37. Novel actions of inverse agonists on 5-HT(2C) receptor systems
38. Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus
39. 2 receptor: A mechanistic hypothesis from molecular dynamics stimulations of the three-dimensional model of the receptor complexed to ligands
40. 2-adrenergic receptor-G(s) complex: Evidence for agonist-specific receptor states
41. A three-state model of agonist action
42. Selective activation of inhibitory G-protein α-subunits by partial agonists of the human 5-HT(1A) receptor
43. Influence of G protein type on agonist efficacy
44. 351 of the G protein G(i1)α determines the extent of activation by the α(2A)-adrenoceptor
45. 4 receptor splice variants show marked constitutive activity: Role of the C-terminal intracellular domain
46. 7) receptor isoforms in human and rat produced by alternative splicing: Species differences due to altered intron-exon organization
47. Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor
48. G-protein-coupled receptor regulation: Role of G-protein-coupled receptor kinases and arrestins
49. Desensitization of G protein-coupled receptors
50. Regulation of serotonin-2C receptor G-protein coupling by RNA editing
51. RNA editing
52. RNA editing of the human serotonin 5-hydroxytryptamine 2C receptor silences constitutive activity
53. Agonist-directed signalling of serotonin 5-HT(2A) receptors: Differences between serotonin and lysergic acid diethylamide (LSD)
54. Serotonin 5-HT(2C) receptor RNA editing alters receptor basal activity: Implications for serotonergic signal transduction
55. The activation process of the α(1B)-adrenergic receptor: Potential role of protonation and hydrophobicity of a highly conserved aspartate
56. Hydrophobic amino acid in the i2 loop plays a key role in receptor-G protein coupling
57. Agonist-promoted down-regulation and functional desensitization in two naturally occurring variants of the human serotonin(1A) receptor
58. Modified ligand binding to the naturally occurring Cys-124 variant of the human 5-HT(1B) receptor
59. Coronary side-effect potential of current and prospective antimigraine drugs
60. 2 receptor influences amplitude and timing of intracellular calcium mobilization
61. Serotonin receptor variants in disease: New therapeutics opportunities?
62. Agonist-independent activation of G(z) by the 5-hydroxytryptamine(1A) receptor co-expressed in Spodoptera frugiperda cells. Distinguishing inverse agonists from neutral antagonists
63. Inhibition of the constitutive activity of human 5-HT(1A) receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100.635
64. 35S]GTPγS binding
65. 7 receptor (long form); antagonist profile of SB-258719
66. How efficacious are 5-HT(1B/D) receptor ligands: An answer from GTPγS binding studies with stably transfected C6-glial cell lines
67. Activation of constitutive 5-hydroxytryptamine(1B) receptor by a series of mutations in the BBXXB motif: Positioning of the third intracellular loop distal junction and its G(αo) protein interactions
68. Creation of a constitutively activated state of the 5-hydroxytryptamine(2A) receptor by site-directed mutagenesis: Inverse agonist activity of antipsychotic drugs
69. Constitutively active 5-hydroxytryptamine 2C (5-HT(2C)) receptors reveal novel inverse agonist activity of receptor ligands
70. Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists
71. Activating mutations of the serotonin 5-HT(2C) receptor
72. 4 receptor antagonist ML10375 inhibits the constitutive activity of human 5-HT(4(C)) receptor
73. 35S]GTPγS binding to Chinese hamster ovary cell membranes stably expressing cloned human 5-HT(1D) receptor subtypes