Interaction of 1,2,4-substituted piperazines, new serotonin receptor ligands, with 5-HT1A and 5-HT2A receptors

Farmaco

Volumn 57, Issue 4, 2002, Pages 285-301

  Chilmonczyk, Zdzisław ^a,b   Cybulski, Marcin ^c   Iskra Jopa, Joanna ^c   Chojnacka Wójcik, Ewa ^d   Tatarczyńska, Ewa ^d   Kłodzińska, Aleksandra ^d   Leś, Andrzej ^c,e   Bronowska, Agnieszka ^e   Sylte, Ingebrigt ^f  

^a NATIONAL MEDICINES INSTITUTE   (Poland)

^b UNIVERSITY OF BIALYSTOK   (Poland)

^c INDUSTRIAL CHEMISTRY RESEARCH INSTITUTE   (Poland)

^d INSTITUTE OF PHARMACOLOGY   (Poland)

^e UNIVERSITY OF WARSAW   (Poland)

^f UNIVERSITY OF TROMSØ   (Norway)

Author keywords

5 HT1A and 5 HT2A receptors; Affinity; Intrinsic activity; Ligands; Molecular modelling

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; BUSPIRONE; KETANSERIN; N TERT BUTYL 3 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL] 2 PHENYLPROPIONAMIDE; PARTIAL AGONIST; PIPERAZINE DERIVATIVE; POSTSYNAPTIC RECEPTOR; PRESYNAPTIC RECEPTOR; RESERPINE; RITANSERIN; SEROTONIN 1A RECEPTOR; SEROTONIN 2A RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BEHAVIOR; BINDING COMPETITION; BIOCHEMISTRY; BODY TEMPERATURE; BRAIN; CONTROLLED STUDY; DRUG RECEPTOR BINDING; LIGAND BINDING; MALE; MOLECULAR DYNAMICS; MOLECULAR MODEL; MOUSE; NONHUMAN; RAT; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY; SEROTONIN SYNDROME;

ANIMALS; BEHAVIOR, ANIMAL; BINDING, COMPETITIVE; BODY TEMPERATURE; BRAIN; LIGANDS; MALE; MICE; MODELS, MOLECULAR; PIPERAZINES; RADIOLIGAND ASSAY; RATS; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0036533726     PISSN: 0014827X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-827X(02)01205-3     Document Type: Article

References (68)

1. Serotonergic antidepressants: current and future perspectives
2. 1A agonists, partial agonists and antagonists in anxiety and depression: a lost cause
3. 1A selective ligand and its effects in animal models of anxiety: comparison with buspirone, 8-OH-DPAT and diazepam
4. 1A receptor agonists: recent developments and controversial issues
5. Drug status update
6. 2 antagonist WY-50,324 in pigeons
7. 1A receptors
8. Flibanserin
9. 1A receptor ligands
10. 1A receptor. 1. The molecular structure of buspirone and its two analogues
11. 1A receptor ligands from crystallographic data. Updated model of the receptor pharmacophore
12. 1 recognition site
13. 2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-carbolines
14. 1A receptors induces lower lip retraction in rats
15. 1a receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino)tetralin in the rat
16. Ipsapirone, a new anxiolytic drug, stimulates catecholamine turnover in various regions of the rat brain
17. 1A agonist 8-OH-DPAT
18. The MIDAS display system
19. Application of RESP charges to calculate conformational energies, hydrogen bond energies and free energies of solvation
20. 2A receptors
21. A theoretical study of the dielectric constant of protein
22. 1A serotonin receptor
23. 1A receptor
24. Crystal structure of rhodopsin: a G protein-coupled receptor
25. Projection structure of rhodopsin
26. Low resolution structure of bovine rhodopsin determined by electron cryo-microscopy
27. The probable arrangement of the helices in G protein-coupled receptors
28. An α-carbon template for the transmembrane helices in the rhodopsin family of G-protein coupled receptors
29. 2A receptor
30. Requirement of rigid body motion of transmembrane helices for light activation of rhodopsin
31. Molecular mechanisms involved in muscarinic acetylcholine receptor-mediated G protein activation studied by insertion mutagenesis
32. Ab initio modeling and molecular dynamics simulation of the alpha 1b-adrenergic receptor activation
33. 1A receptor: a site-directed mutagenesis study
34. 1A receptors
35. 2A receptors
36. 2C receptor gene (HTR2C)
37. Five-transmembrane domains appear sufficient for a G-protein coupled receptor: functional five-transmembrane domain chemokine receptors
38. A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor
39. Transducin activation by rhodopsin without a covalent bond to the 11-cis-retinal chromophore
40. Involvement of Asn-293 in stereospecific agonist recognition and in activation of the β2-adrenergic receptor
41. Agonists induce conformational changes in transmembrane domains III and VI of the β2 adrenoreceptors
42. How receptors talk to trimeric G protein
43. Identification of a receptor/G-protein contact site critical for signalling specificity and G-protein activation
44. 2A receptor
45. 2 receptor in Xenopus laevis oocytes
46. Identification of Gs coupling domain in the amino acid terminus of the third intracellular loop of the α2A-adrenergic receptor. Evidence for distinct structural determinants that confer Gs versus Gi coupling
47. 2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin
48. Site-directed mutagenesis of a single residue changes the binding properties of the serotonin 5-HT2 receptor from a human to a rat pharmacology
49. 2 receptor activation
50. Antagonism of (+)-WAY 100135 to behavioural, hypothermic and corticosterone effects induced by 8-OH-DPAT
51. 1A receptor antagonist, and its analogues
52. The pharmacology of the hypothermic response in mice response to 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH DPAT)
53. 1A autoreceptor function
54. 1A receptor ligand with the same activity profile as buspirone
55. Differential effects 5-hydroxytryptamine selective drugs on the 5-HT behavioral syndrome
56. Central action of ipsapirone, a new anxiolytic drug, on serotonergic, noradrenergic and dopaminergic function
57. 1A autoreceptors of the dorsal and median raphé nuclei
58. 1A receptor agonists in vitro with different properties in vivo
59. In vivo biochemical characterization of 8-OH-DPAT: evidence for 5-HT receptor selectivity and agonist action in rat CNS
60. 1A receptor site
61. 1 recognition site
62. 5-Hydroxytryptamine receptors