Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: Effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties

Neuropharmacology

Volumn 48, Issue 3, 2005, Pages 343-353

  Urwyler, Stephan ^a   Gjoni, Tina ^a   Koljatić, Jelena ^a   Dupuis, Delphine S ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Affinity; Allosteric modulation; CGP7930; Efficacy; GABAB receptor; GS39783

Indexed keywords

3 AMINOPROPYL(DIETHOXYMETHYL)PHOSPHINIC ACID; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID B RECEPTOR STIMULATING AGENT; CGP 7930; CYCLIC AMP; FORSKOLIN; GS 39783; GUANOSINE TRIPHOSPHATE DERIVATIVE; LIGAND; RADIOLIGAND; RECOMBINANT RECEPTOR; SACLOFEN; SULFUR 35;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL LINE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; FEMALE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION;

EID: 13844275284     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2004.10.013     Document Type: Article

References (37)

1. A.S. Bessis, P. Rondard, F. Gaven, I. Brabet, N. Triballeau, L. Prézeau, F. Acher, and J.P. Pin Closure of the Venus flytrap module of mGlu8 receptor and the activation process: insights from mutations converting antagonists into agonists Proceedings of the National Academy of Sciences of the United States of America 99 2002 11097 11102
2. B receptor Journal of Biological Chemistry 279 2004 29085 29091
3. D.C. Bolser, D.J. Blythin, R.W. Chapman, R.W. Egan, J.A. Hey, C. Rizzo, S.C. Kuo, and W. Kreutner The pharmacology of SCH50911: a novel, orally active GABA-beta receptor antagonist Journal of Pharmacology and Experimental Therapeutics 274 1995 1393 1398
4. B receptors: structure and function Pharmacological Reviews 54 2002 247 264
5. 50) of an enzymatic reaction Biochemical Pharmacology 22 1973 3099 3108
6. A. Christopoulos Allosteric binding sites on cell-surface receptors: novel targets for drug discovery Nature Reviews Drug Discovery 1 2002 198 210
7. A. Christopoulos, and T. Kenakin G protein-coupled receptor allosterism and complexing Pharmacological Reviews 54 2002 323 374
8. A. De Lean, J.M. Stadel, and R.J. Lefkowitz A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor Journal of Biological Chemistry 255 1980 7108 7117
9. B agonists Journal of Medicinal Chemistry 38 1995 3297 3312
10. B modulators S.J. Enna N.G. Bowery The GABA Receptors 1997 Humana Press Inc. Totowa, NJ 271 296
11. B receptor extracellular domain support a Venus flytrap mechanism for ligand binding Journal of Biological Chemistry 274 1999 13362 13369
12. B receptors Journal of Biological Chemistry 275 2000 41166 41174
13. 3 adenosine receptors by a series of imidazoquinoline derivatives Molecular Pharmacology 62 2002 81 89
14. B receptor C-termini for G-protein coupling Molecular Pharmacology 61 2003 1070 1080
15. D.A. Hall Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation Molecular Pharmacology 58 2000 1412 1423
16. B2 receptor subunits Biochemical Pharmacology 65 2003 1103 1113
17. A.A. Jensen, and T.A. Spalding Allosteric modulation of G-protein coupled receptors European Journal of Pharmaceutical Sciences 21 2004 407 420
18. E.W. Karbon, and S.J. Enna Characterization of the relationship between gamma-aminobutyric acid B agonists and transmitter-coupled cyclic nucleotide-generating systems in rat brain Molecular Pharmacology 27 1985 53 59
19. T. Kenakin Efficacy as a vector: the relative prevalence and paucity of inverse agonism Molecular Pharmacology 65 2004 2 11
20. B receptors Neuroscience Letters 92 1988 92 96
21. B receptors in rat brain slices Neuropharmacology 35 1996 703 712
22. F. Knoflach, V. Mutel, S. Jolidon, J.N.C. Kew, P. Malherbe, E. Vieira, J. Wichmann, and J.A. Kemp Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site Proceedings of the National Academy of Sciences of the United States of America 98 2001 13402 13407
23. A. Laurenza, Y. Khandelwal, N.J. De Souza, R.H. Rupp, H. Metzger, and K.B. Seamon Stimulation of adenylate cyclase by water-soluble analogues of forskolin Molecular Pharmacology 32 1987 133 139
24. P. Leff The two-state model of receptor activation Trends in Pharmacological Sciences 16 1995 89 97
25. R.J. Lefkowitz, S. Cotecchia, P. Samama, and T. Costa Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins Trends in Pharmacological Sciences 14 1993 303 307
26. M. Maj, V. Bruno, Z. Dragic, R. Yamamoto, G. Battaglia, W. Inderbitzin, N. Stoehr, T. Stein, F. Gasparini, I. Vranesic, R. Kuhn, F. Nicoletti, and P.J. Flor (-)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection Neuropharmacology 45 2003 895 906
27. J.M. Mathiesen, N. Svendsen, H. Bräuner-Osborne, C. Thomsen, and M.T. Ramirez Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP British Journal of Pharmacology 138 2003 1026 1030
28. G. Milligan Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective Molecular Pharmacology 64 2003 1271 1276
29. B receptors European Journal of Pharmacology 187 1990 27 38
30. B receptors dually coupled to cyclic AMP by the allosteric agent CGP7930 European Journal of Pharmacology 471 2003 77 84
31. J.-P. Pin, T. Galvez, and L. Prézeau Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors Pharmacology & Therapeutics 98 2003 325 354
32. H. Schaffhauser, B.A. Rowe, S. Morales, L.E. Chavez-Noriega, R. Yin, C. Jachec, S.P. Rao, G. Bain, A.B. Pinkerton, J.M. Vernier, L.J. Bristow, M.A. Varney, and L.P. Daggett Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2 Molecular Pharmacology 64 2003 798 810
33. P.G. Strange Mechanisms of inverse agonism at G-protein-coupled receptors Trends in Pharmacological Sciences 23 2002 89 95
34. B receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501 Molecular Pharmacology 60 2001 963 971
35. B receptor function Journal of Pharmacology and Experimental Therapeutics 307 2003 322 330
36. B receptors European Journal of Pharmacology 483 2004 147 153
37. W.J. Wojcik, and N.H. Neff γ-Aminobutyric acid B receptors are negatively coupled to adenylate cyclase in brain, and in the cerebellum these receptors may be associated with granule cells Molecular Pharmacology 25 1984 24 28