Dimerization of 8-OH-DPAT increases activity at serotonin 5-HT(1A) receptors

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 358, Issue 4, 1998, Pages 404-410

  Pauwels, Petrus J ^a   Dupuis, Delphine S ^a   Perez, Michel ^a   Halazy, Serge ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

5 HT(1A); 5 HT(1B) and 5 HT(1D) receptor; 8 OH DPAT dimer; 35S GTP S binding and autoradiography; Bivalent ligand; Guinea pig brain; Recombinant cell line

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); GUANOSINE DIPHOSPHATE; N [4 [5 [3 (2 AMINOETHYL) 1H INDOL 5 YL] 1,2,4 OXADIAZOL 3 YL]BENZYL]METHANESULFONAMIDE; SEROTONIN; SEROTONIN 1A RECEPTOR; SEROTONIN 1B RECEPTOR; SEROTONIN 1D RECEPTOR; SULFUR 35; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; CINGULATE GYRUS; CONTROLLED STUDY; DIMERIZATION; DORSAL RAPHE NUCLEUS; DRUG ACTIVITY; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; GLIA CELL; GUINEA PIG; HIPPOCAMPUS; HUMAN; HUMAN CELL; NONHUMAN; RAT; SEPTUM PELLUCIDUM;

8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN; ANIMALS; AUTORADIOGRAPHY; DIMERIZATION; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); GUINEA PIGS; HELA CELLS; HUMANS; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS;

EID: 0031657294     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/PL00005271     Document Type: Article

References (39)

1. 1D, receptor agonist. Br J Pharmacol 110:1196-1200
2. 1A receptor in Escherichia coli. J Biol Chem 267:8200-8206
3. Bradford MM (1976) A rapid and sensitive method for the quantification of microgram quantitites of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254
4. Cvejic S, Devi LA (1997) Dimerization of the δ opioid receptor: implication for a role in receptor internalizalion. J Biol Chem 272:26959-26964
5. 35S]GTPγS binding. J Neurochem 70:1258-1268
6. Erez M, Takemori AE, Portoghese PS (1982) Narcotic antagonist potency of bivalent ligands which contain β-naltrexamine. Evidence for bridging between proximal recognition sites. J Mod Chem 25:847-849
7. 1A receptor. J Biol Chem 264:14848-14852
8. 1A receptor. Biochemistry 33:4283-4290
9. 3H-PAT. Nature 305:140-142
10. 1B/1D agonist. J Med Chem 39:4920-4927
11. Hazum E, Chang KJ, Leighton HJ, William Lever O, Cuatrecasas OP (1982) Increased biological activity of dimers of oxymorphone and enkephalin: possible role of receptor cross-linking. Biochem Biophys Res Commun 104:347-353
12. 2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation. J Biol Chem 271:16384-16392
13. Hjorth S, Carlsson A, Lindberg P, Sanchez D, Wikströni H, Arvidsson LE, Hacksell U, Nilsson JLG (1982) 8-Hydroxy-2-(di-n-propylamino)tetralin, 8-OH-DPAT, a potent and selective simplified ergot congener with central 5-HT-receptor stimulating activity. J Neural Transm 55:169-188
14. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PPA (1994) International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev 46:157-203
15. Julius D (1991) Molecular biology of serotonin receptors. Annu Rev Neurosci 14:335-360
16. 2A-adrenergic receptor inhibition of stimulus-secretion coupling. Mol Pharmacol 50:96-103
17. Le Boulluec K, Mattson RJ, Mable CD, McGovern RT, Nowak HP, Gentile AJ (1995) Bivalent indoles exhibiting serotonergic binding affinity. Bioorg Med Chem Lett 5:123-126
18. 1A receptor directs signaling specificity. Mol Pharmacol 52:164-171
19. Milligan G (1988) Techniques used in the identification and analysis of function of pertussis toxin-sensitive guanine nucleotide binding G-proteins. Biochem J 255:1-13
20. 1A receptors. Eur J Pharmacol 307:107-111
21. 1A receptors by the inverse agonist, spiperone, but not the neutral antagonist. WAY 100,635. Br J Pharmacol 120:737-739
22. 1A receptors as a function of receptor: G-protein stoichiometry. Neuropharmacology 36:451-459
23. 1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol 355:682-688
24. 3 receptor dimers and tetramers in brain and in transfected cells. J Biol Chem 272:29229-29237
25. 1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells. Biochem Pharmacol 45:375-383
26. 1B receptors. Naunyn Schmiedebergs Arch Pharmacol 353:144-146
27. 1A receptor agonists in recombinant cell lines. Modulation of apparent efficacy by G-protein activation state. Naunyn Schmiedebergs Arch Pharmacol 356:551-561
28. 1B/D receptor ligands: an answer from GTPγS binding studies with stably transfected C6-glial cell lines. Neuropharmacology 36:499-512
29. 1A receptors: intrinsic activity and modulation by G-protein activation state. Naunyn Schmiedebergs Arch Pharmacol 357:490-499
30. Perez DM, Hwa J, Gaivin R, Mathur M, Brown F, Graham RM (1996) Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor. Mol Pharmacol 49:112-122
31. 1B/1D receptor subtypes. Bioorg Med Chem Lett 8:1407-1412
32. Portoghese PS (1989) Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. Trends Pharmacol Sci 10:230-235
33. Portoghese PS, Ronsisvalle G, Larson DL, Yim CB, Sayre LM, Takemori AH (1982) Opioid agonist and antagonist bivalent ligands as receptor probes. Life Sci 31:1283-1286
34. 1A receptors to inhibitory G protein α-subunits and lack of coupling to Gsα. Biochemistry 32:11064-11073
35. Nα has properties of a constitutively active receptor. J Biol Chem 273:5109-5116
36. Selley DE, Sim LJ, Xiao R, Liu Q, Childers SR (1997) μ-Opioid receptor-stimulated guanosine-5′-O-(γ-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist efficacy. Mol Pharmacol 51:87-96
37. 35S]thio]triphosphate binding. Proc Natl Acad Sci USA 92:7242-7246
38. 35S]GTPγS binding. Eur J Pharmacol 320:267-275
39. 1A receptor gene is sufficient for its in vitro expression. Neurosci Res Commun 19:75-82