The 5HT(1A) receptor ligand, S15535, antagonises G-protein activation: A [35S]GTPγS and [3H]S15535 autoradiography study

European Journal of Pharmacology

Volumn 384, Issue 2-3, 1999, Pages 111-121

  Newman Tancredi, Adrian ^a   Rivet, Jean Michel ^a   Chaput, Christine ^a   Touzard, Manuelle ^a   Verrièle, Laurence ^a   Millan, Mark J ^a  

^a INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

(+) 8 Hydroxy dipropyl aminotetralin; 5 HT(1A) receptor; 35S GTP S; Autoradiography; G protein; S15535

Indexed keywords

1 (1,4 BENZODIOXAN 5 YL) 4 (2 INDANYL)PIPERAZINE; 2 DIPROPYLAMINO 8 HYDROXYTETRALIN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; RECEPTOR SUBTYPE; SEROTONIN 1A RECEPTOR; SEROTONIN RECEPTOR;

ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BRAIN CORTEX; BRAIN REGION; CAUDATE NUCLEUS; DORSAL RAPHE NUCLEUS; DRUG RECEPTOR BINDING; HIPPOCAMPUS; IN VITRO STUDY; MALE; MESENCEPHALON; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR DENSITY; SUBSTANTIA NIGRA;

8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN; ANIMALS; AUTORADIOGRAPHY; BINDING, COMPETITIVE; BRAIN; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); LIGANDS; MALE; PIPERAZINES; RATS; RATS, WISTAR; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN; SEROTONIN AGONISTS; SULFUR RADIOISOTOPES; TRITIUM;

EID: 0033404538     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(99)00491-4     Document Type: Article

References (52)

1. 1A receptor in Escherichia coli. J. Biol. Chem. 267:1992;8200-8206.
2. Boess F.G., Martin I.L. Molecular biology of 5-HT receptors. Neuropharmacology. 33:1994;275-317.
3. 2A receptor mRNA in human brain. Brain Res. 676:1995;157-168.
4. 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia. Neurochem. Int. 30:1997;565-574.
5. 1A binding in rat brain: a combined in situ hybridisation/in vitro receptor autoradiographic study. Brain Res. 561:1991;51-60.
6. 1A-mediated inhibition of adenylyl cyclase in dorsal raphe of male and female rats. J. Pharmacol. Exp. Ther. 277:1996;1259-1266.
7. Coplan J.D., Gorman J.M., Klein D.F. Serotonin related functions in panic-anxiety: a critical overview. Neuropsychopharmacology. 6:1992;189-200.
8. De Vivo M., Maayani S. Characterization of the 5-hydroxytryptamine1A receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes. J. Pharmacol. Exp. Ther. 238:1986;248-253.
9. 1A receptor agonists: recent developments and controversial issues. Psychopharmacology. 121:1995;1-26.
10. 35S]GTPγS binding. J. Neurochem. 70:1998;1258-1268.
11. 1A receptor-stimulated responses in the human and monkey brain. Eur. J. Neurosci. 11:1999;1809-1817.
12. 1A receptor to both adenylyl cyclase and phospholipase C is mediated via the same Gi protein. Cellular Signalling. 3:1991;547-557.
13. 1A receptor antagonist. Behav. Brain. Res. 73:1996;337-353.
14. iα3. J. Biol. Chem. 272:1997;7770-7776.
15. Gobert A., Lejeune F., Rivet J.-M., Audinot V., Newman-Tancredi A., Millan M.J. Modulation of the activity of central serotoninergic neurons by novel serotonin1A receptor agonists and antagonists: a comparison to adrenergic and dopaminergic neurons in rats. J. Pharmacol. Exp. Ther. 273:1995;1032-1046.
16. 1A receptors. Fozard J.R., Saxena P.R. Serotonin: Molecular Biology, Receptors and Functional Effects. 1991;95-106 Birkhauser Verlag, Basle.
17. 1A receptors are linked to a Gi-adenylate cyclase complex in rat hippocampus. Eur. J. Pharmacol. 154:1988;95-98.
18. 1A and GABAB receptor-mediated inhibition of serotonergic neurons. Eur. J. Pharmacol. 143:1987;195-204.
19. 1A receptor antagonist. Eur. J. Pharmacol. 360:1998;219-225.
20. 3H]8-OH-DPAT labels a 5-HT site coupled to inhibition of phosphoinositide hydrolysis in the dorsal raphe. Eur. J. Pharmacol. 329:1997;99-106.
21. 1A receptors in the acutely dissociated rat dorsal raphe neurons. Brain Res. 745:1997;283-292.
22. Kelly J.S., Larkman P., Penington N.J., Rainnie D.G., McAllister-Williams H., Hodgkiss J. Serotonin receptor heterogeneity and the role of potassium channels in neuronal excitability. Adv. Exp. Med. Biol. 287:1991;177-191.
23. 1A receptor antagonist. Brain Res. 673:1995;217-225.
24. Kia H., Miquel M.-C., Brisorgueil M.-J., Daval G., Riad M., El Mestikawy S., Hamon M., Vergé D. Immunocytochemical licalisation of serotonin1A receptors in the rat central nervous system. J. Comp. Neurol. 365:1996;289-305.
25. 125I]p-MPPI) as a new selective radioligand of serotonin-1A sites in rat brain: in vitro binding and autoradiographic studies. J. Pharmacol. Exp. Ther. 272:1995;429-437.
26. 1A receptors: WAY100,635-reversible actions of the highly selective ligands, flesinoxan and S15535. Synapse. 30:1998;172-180.
27. 1A receptors and their modulation of the activity of serotonergic and dopaminergic neurones in rats. J. Pharmacol. Exp. Ther. 280:1997;1241-1249.
28. Marcinkiewicz M., Vergé D., Gozlan H., Pichat L., Hamon M. Autoradiographic evidence for the heterogeneity of 5-HT1 sites in the rat brain. Brain Res. 291:1984;159-163.
29. 1A agonists. Mol. Pharmacol. 37:1990;231-237.
30. 1A antagonists. J. Pharmacol. Exp. Ther. 268:1994;337-351.
31. 1A receptors: II. Modulation of hippocampal serotonin release in relation to potential anxiolytic properties. J. Pharmacol. Exp. Ther. 282:1997;148-161.
32. 1D receptors to G-protein coupling and function in corticolimbic structures. Neuropsychopharmacology. 1999;. (in press).
33. 1A receptor mRNA in the rat brain. Mol. Brain Res. 14:1992;357-362.
34. 1A receptors. Eur. J. Pharmacol. 307:1996;107-111.
35. 3H]S15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn-Schmiedeberg's Arch. Pharmacol. 357:1998;205-217.
36. 1A receptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 358:1998;404-410.
37. Paxinos G., Watson C. The Rat Brain in Stereotaxic Coordinates. 4th edn. 1998;Academic Press, London.
38. Pazos A., Probst A., Palacios J.M. Serotonin receptors in the human brain - III. Autoradiographic mapping of serotonin-1 receptors. Neuroscience. 21:1987;97-122.
39. 1A receptors on dorsal raphe neurones of the adult rat. J. Physiol. 469:1993;387-405.
40. 1A receptor in the rat brain: correlation with receptor binding. J. Neurosci. 12:1992;440-453.
41. 1A receptors and differential coupling to second messengers in CHO cells. Naunyn-Schmiedeberg's Arch. Pharmacol. 346:1992;127-137.
42. sα. Biochemistry. 32:1993;11064-11073.
43. 1B receptor selectivity for 5-HT terminal autoreceptor activity: an in vivo microdialysis study in the freely-moving guinea-pig. Neuropharmacology. 36:1997;549-557.
44. 35S]GTPγS binding in rat brain. Br. J. Pharmacol. 120:1997;. 297 pp.
45. 1 binding sites: a comparative autoradiographic study between rat and guinea pig. Brain Res. 555:1991;295-304.
46. 35S]thio]-triphosphate binding. Proc. Natl. Acad. Sci. U.S.A. 92:1995;7242-7246.
47. Sim L.J., Selley D.E., Xiao R., Childers S.R. Differences in G-protein activation by μ- and δ-opioid and cannabinoid receptors in rat striatum. Eur. J. Pharmacol. 307:1996;97-105.
48. 1A receptor-activated G-proteins in the rat brain. Brain Res. Bull. 44:1997;39-45.
49. 1B agonists. Synapse. 1:1987;3-9.
50. Steckler T., Sahgal A. The role of serotonergic-cholinergic interactions in the mediation of cognitive behaviour. Behav. Brain Res. 67:1995;165-199.
51. 35S]guanosine-5′-O-(3-thio)triphosphate binding to rodent brain sections as visualised by in vitro autoradiography. Mol. Pharmacol. 52:1997;623-631.
52. 1A receptors negatively coupled to adenylyl cyclase activity in rat hippocampal membranes. Mol. Pharmacol. 41:1992;1066-1072.