Inverse agonists and serotonergic transmission: From recombinant, human serotonin (5-HT)1Breceptors to G-protein coupling and function in corticolimbic structures in vivo

Neuropsychopharmacology

Volumn 21, Issue , 1999, Pages 61S-67S

  Millan, M J ^a   Gobert, A ^a   Audinot, V ^a   Dekeyne, A ^a   Newman Tancredi, A ^a  

^a INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

5 HT1B receptor; Constitutive activity; Intrinsic activity; Inverse agonist; 35S GTP S France

Indexed keywords

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 (1,2,5,6 TETRAHYDRO 4 PYRIDYL)PYRROLO[3,2 B]PYRIDIN 5 ONE; 3 [3 (2 DIMETHYLAMINOETHYL) 1H INDOL 5 YL] N (4 METHOXYBENZYL)ACRYLAMIDE; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); 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; RECOMBINANT RECEPTOR; S 18127; SEROTONIN 1A ANTAGONIST; SEROTONIN 1B AGONIST; SEROTONIN 1B ANTAGONIST; SEROTONIN 1B RECEPTOR; UNCLASSIFIED DRUG;

CHINESE HAMSTER; CORE TEMPERATURE; DRUG BINDING; DRUG INHIBITION; DRUG MECHANISM; DRUG RECEPTOR BINDING; IN VIVO STUDY; LIGAND BINDING; LIMBIC SYSTEM; NONHUMAN; PRIORITY JOURNAL; RECEPTOR INTRINSIC ACTIVITY; REVIEW; SEROTONINERGIC TRANSMISSION;

ANIMALS; CEREBRAL CORTEX; CHO CELLS; CRICETINAE; GTP-BINDING PROTEINS; HUMANS; LIMBIC SYSTEM; RATS; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; TRANSFECTION;

EID: 0032818914     PISSN: 0893133X     EISSN: 1740634X     Source Type: Journal    
DOI: 10.1016/S0893-133X(99)00007-X     Document Type: Article

References (37)

1. Barker EL, Westphal RS, Schmidt D, Sanders-Bush E (1994): Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands. J BiolChem 269:11687-11690
2. Bond RA, Leff P, Johnson TD, Milano CA, Rockman HA, McMinn TR, Apparsundaram S, Hyek MF, Kenakin TP, Allen LF, Lefkowitz RJ (1995): Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the ß2-adrenoceptor. Nature 374:272-274
3. Boess FG, Martin IL (1994): Molecular biology of 5-HT receptors. Neuropharmacology 33:275-317
4. Burgisser E, DeLean A, Lefkowitz RJ (1982): Reciprocal modulation of agonist and antagonist binding to mus-carinic cholinergic receptors by guanine nucleotides. ProcNatlAcadSci USA 79:1732-1736
5. Costa T, Herz A (1989): Antagonists with negative intrinsic activity at S-opioid receptors coupled to GTP-binding proteins. ProcNatlAcadSci USA 86:7321-7325
6. Costa T, Ogino Y, Munson PJ, Onaran HO, Rodbard D (1992): Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: Thermodynamic interpretation of negative antagonism of receptor activity in the absence of ligands. MolPharmacol 41:549-560
7. Creese I, Burt DR, Snyder SH (1975): Dopamine receptor binding: Differentiation of agonist and antagonist states with [3H]-dopamine and [3H]-haloperidol. Life Sci 17: 993-1003
8. Dupuis DS, Palmier C, Colpaert FC, Pauwels PJ (1998): Autoradiography of serotonin 5-HT1A receptor-acti-vated G proteins in guinea pig sections by agonist-stim-ulated [35S]-GTP7S binding. J Neurochem 70:1258-1268
9. Egan CT, Herrick-Davis K, Teitler M (1998): Creation of a con-stituvely activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: Inverse agonist activity of antipsychotic drugs. J PharmacolExpTher286:85-90
10. Fibiger HC, Grewaal DS (1974): Neurochemical evidence for denervation supersensitivity: The effect of unilateral sub-stantianigra lesions on apomorphine-induced increases in neostriatal acetylcholine levels. Life Sci 15: 57-63
11. Gaster LM, Blaney FE, Davies S, Duckworth M, Ham P, Jen-kins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD (1998): The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1, 2, 4-oxa-diazol-3-yl)biphenyl-4-yl]-2, 3, 6, 7-tetrahydro-spiro[furo [2, 3-f]indole-3, 4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem 41:1218-1235
12. Gobert A, Rivet J-M, Audinot V, Newman-Tancredi A, Cistarelli L, Millan MJ (1998): Simultaneous quantifica-tion of serotonin, dopamine and noradrenaline levels in single frontal cortex dialysates of freely-moving rats reveals a complex pattern of reciprocal auto- and hetero receptor-mediated control of release. Neuroscience84:413-429
13. Hagan JJ, Slade PD, Gaster L, Jeffrey P, Hatcher JP, Middle-miss DN (1997): Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig. Eur J Pharmacol331:169-174
14. Hall DA, Strange PG (1997): Evidence that antipsychotic drugs are inverse agonists at D2 dopamine receptors. Br J Pharmacol 121:731-736
15. Kenakin T (1996): The classification of seven transmembrane receptors in recombinant expression systems. Pharma-col Rev 48:413-463
16. Maes M, Meltzer HY (1995): The serotonin hypothesis of major depression. In Bloom FE, Kupfer DJ (eds), Psy-chopharmacology: The Fourth Generation in Progress. pp 933-944. Raven Press, New York
17. Millan MJ, Audinot V, Newman-Tancredi A, Dekeyne A, Gobert A, Lochon S, Rivet J-M, Goument B, Peglion J-L(1998): S18127: A novel and selective, aminopiperidine antagonist at serotonin (5-HT)1B/1Dreceptors. AmSoc Neurosci 24:1364
18. Milligan G, Bond RA, Lee M (1995): Inverse agonism: Phar-macological curiosity or potential therapeutic strategy? Trends PharmacolSci 16:10-13
19. Milligan G, Bond RA (1997): Inverse agonism and the regulation of receptor number. Trends PharmacolSci 18:468-474
20. Moret C, Briley M (1993): The unique effect of methiothepin on the terminal serotonin autoreceptor in the rat hypothalamus could be an example of inverse agonism. J Psychopharmacol 7:331-337
21. Morris BJ, Millan MJ (1991): Inability of an opioid antagonist lacking negative intrinsic activity to induce opioid recep-tor up-regulation in vivo. Br J Pharmacol 102:883-886
22. Newman-Tancredi A, Conte C, Chaput C, Spedding M, Millan MJ (1997a): Inhibition of the constitutive activity of human 5-HT1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100, 635. Br J Pharmacol 120:737-739
23. Newman-Tancredi A, Conte C, Chaput C, Verriele L, Millan MJ (1997b): Agonist and inverse agonist efficacy at human recombinant serotonin 5-HT1A receptors as a function of receptor: G-protein stoichiometry. Neuropharmacology36:451-459
24. Nilsson CL, Ekman A, Hellstrand M, Eriksson E (1996): Inverse agonism at dopamine D2 receptors. Haloperi-dol-induced prolactin release from GH4C1 cells trans-fected with the human D2 receptor is antagonized by R(-)-n-propylnorapomorphine, raclopride and phen-oxybenzamine. Neuropsychopharmacology 15:54-61
25. Pauwels PJ, Wurch T, Palmier C, Colpaert FC (1998): Phar-macological analysis of G-protein activation mediated by guinea-pig recombinant 5-HT1B receptors in C6-glial cells: Similarities with the human 5-HT1Breceptor. Br J Pharmacol 123:51-62
26. Pineyro G, de Montigny C, Blier P (1995): 5-HT1D receptors regulate 5-HT release in the rat raphe nuclei: in vivo vol-tametry and in vitro superfusion studies. Neuropsy-chopharmacology 13:249-260
27. Price GW, Roberts C, Watson J, Burton MJ, Mulholland K, Middlemiss DN, Jones B (1996): Species differences in 5-HT autoreceptors. Behav Brain Res 73:79-82
28. Roberts C, Price GW, Gaster L, Jones BJ, Middlemiss DN, Routledge C (1997): Importance of h5-HT1B receptor selectivity for 5-HT terminal autoreceptor activity: An in vivo microdialysis study in the freely-moving guinea-pig. Neuropharmacology 36:549-557
29. Schütz W, Freissmuth M (1992): Reverse intrinsic activity of antagonists on G protein-coupled receptors. Trends PharmacolSci 13:376-379
30. Sim LJ, Selley DE, Childers SR (1995): In vitro autoradiogra-phy of receptor-activated G-proteins in rat brain by ago-nist-stimulated guanylyl 5'-[-[35S]thio]-triphosphate binding. ProcNatlAcadSci USA 92:7242-7246
31. Skingle M, Beattie DT, Scopes DIC, Starkey SJ, Connor HE, Feniuk W, Tyers MB (1996): GR127935: A potent and selective 5-HT1D receptor antagonist. Behav Brain Res73:157-161
32. Smit MJ, Leurs R, Alewijnse AE, Blauw J, Van NieuwAmerongen GP, Van de Vrede Y, Roovers E, Timmer-man H (1996): Inverse agonism of histamine H2 antago-nists accounts for upregulation of spontaneously active histamine H2 receptors. ProcNatlAcadSci USA93:6802-6807
33. Stanton JA, Handford EJ, Beer MS (1997): In vitro visualisa-tion of 5-HT receptors in rat brain using p5S]-GTP7S binding. Br J Pharmacol 120(suppl):121P
34. Starkey SJ, Skingle M (1994): 5-HT1D as well as 5-HT1A autoreceptors modulate 5-HT release in the guinea pig dorsal raphe nucleus. Neuropharmacology 33:393-402
35. Thomas DR, Faruq SA, Balcarek JM, Brown AM (1995): Phar-macologicalcharacterisation of [35S]-GTP7S binding to Chinese hamster ovary cell membranes stably expressing cloned human 5-HT1D receptor subtypes. J Recept Signal Transduct Res 15:199-211
36. Thomas DR, Gittins S, Collin LL, Middlemiss DN, Riley G, Hagan J, Gloger I, Ellis CE, Forbes IT, Brown AM (1998): Functional characterization of the human cloned 5-HT7 receptor (long form): Antagonist profile of SB-258719. Br J Pharmacol 124:1300-1306
37. Watson JM, Burton MJ, Price GW, Jones BJ, Middlemiss DN (1996): GR127935 acts as a partial agonist at recombinant human 5-HT1D and 5-HT1D receptors. Eur J Phar-macol 314:365-372