Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents

Neuropharmacology

Volumn 54, Issue 5, 2008, Pages 854-862

  Jacobson, Laura H ^a   Cryan, John F ^b,c  

^a NOVARTIS PHARMA AG   (Switzerland)

^b UNIVERSITY COLLEGE CORK   (Ireland)

^c UNIVERSITY COLLEGE CORK   (Ireland)

Author keywords

Anxiety; CGP7930; GABAB receptor; Mice; Positive modulator; Rotarod

Indexed keywords

2,6 DI TERT BUTYL 4 (3 HYDROXY 2,2 DIMETHYLPROPYL)PHENOL; 4 AMINOBUTYRIC ACID B RECEPTOR; BACLOFEN; CHLORDIAZEPOXIDE; N,N' DICYCLOPENTYL 2 METHYLTHIO 5 NITRO 4,6 PYRIMIDINEDIAMINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANXIETY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; DRUG SCREENING; HYPOTHERMIA; MALE; MOTOR COORDINATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; RODENT; STRESS; TRANQUILIZING ACTIVITY;

ANIMALS; ANTI-ANXIETY AGENTS; ANXIETY; BACLOFEN; BEHAVIOR, ANIMAL; BENZODIAZEPINES; BODY TEMPERATURE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION; FEVER; GABA AGONISTS; MALE; MAZE LEARNING; MICE; MODELS, ANIMAL; MOTOR ACTIVITY; PHENOLS; PHYSICAL ENDURANCE; PSYCHOMOTOR PERFORMANCE; RATS;

EID: 40849083238     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2008.01.004     Document Type: Article

References (36)

1. Bettler B., Kaupmann K., Mosbacher J., and Gassmann M. Molecular structure and physiological functions of GABA(B) receptors. Physiol. Rev. 84 (2004) 835-867
2. Binet V., Goudet C., Brajon C., Le Corre L., Acher F., Pin J.P., and Prezeau L. Molecular mechanisms of GABA(B) receptor activation: new insights from the mechanism of action of CGP7930, a positive allosteric modulator. Biochem. Soc. Trans. 32 (2004) 871-882
3. Boissier J., and Simon P. L'utilisation du test de la traction pour l'étude des psycholeptiques. Thérapie 15 (1960) 1170-1174
4. Calver A.R., Davies C.H., and Pangalos M. GABA(B) receptors: from monogamy to promiscuity. Neurosignals 11 (2002) 299-314
5. Carai M.A., Colombo G., Froestl W., and Gessa G.L. In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. Eur. J. Pharmacol. 504 (2004) 213-216
6. Christopoulos A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat. Rev. Drug Discov. 1 (2002) 198-210
7. Cryan J.F., and Holmes A. The ascent of mouse: advances in modelling human depression and anxiety. Nat. Rev. Drug Discov. 4 (2005) 775-790
8. Cryan J.F., and Kaupmann K. Don't worry 'B' happy!: a role for GABA(B) receptors in anxiety and depression. Trends Pharmacol. Sci. 26 (2005) 36-43
9. Cryan J.F., Kelly P.H., Neijt H.C., Sansig G., Flor P.J., and van Der Putten H. Antidepressant and anxiolytic-like effects in mice lacking the group III metabotropic glutamate receptor mGluR7. Eur. J. Neurosci. 17 (2003) 2409-2417
10. B receptor-positive modulator GS39783 (N,N′-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines. J. Pharmacol. Exp. Ther. 310 (2004) 952-963
11. Dunham N.W., and Miya T.S. A note on a simple apparatus for detecting neurological deficit in rats and mice. J. Am. Pharm. Assoc. (Balt.) 46 (1957) 208-209
12. B1 subunit. Mol. Pharmacol. 70 (2006) 2027-2036
13. Gjoni T., Desrayaud S., Imobersteg S., and Urwyler S. The positive allosteric modulator GS39783 enhances GABA(B) receptor-mediated inhibition of cyclic AMP formation in rat striatum in vivo. J. Neurochem. 96 (2006) 1416-1422
14. Handley S.L., and Mithani S. Effects of alpha-adrenoceptor agonists and antagonists in a maze-exploration model of 'fear'-motivated behaviour. Naunyn Schmiedebergs Arch. Pharmacol. 327 (1984) 1-5
15. Jacobson L.H., and Cryan J.F. Differential sensitivity to the motor and hypothermic effects of the GABA B receptor agonist baclofen in various mouse strains. Psychopharmacology (Berlin) 179 (2005) 688-699
16. B receptor agonist-induced changes in mice. J. Pharmacol. Exp. Ther. 319 (2006) 1317-1326
17. Jacobson L.H., Bettler B., Kaupmann K., and Cryan J.F. Behavioral evaluation of mice deficient in GABA(B(1)) receptor isoforms in tests of unconditioned anxiety. Psychopharmacology (Berlin) 190 (2007) 541-553
18. Kaufman E.E., Porrino L.J., and Nelson T. Pyretic action of low doses of gamma-hydroxybutyrate in rats. Biochem. Pharmacol. 40 (1990) 2637-2640
19. Kaupmann K., Cryan J.F., Wellendorph P., Mombereau C., Sansig G., Klebs K., Schmutz M., Froestl W., van der Putten H., Mosbacher J., Brauner-Osborne H., Waldmeier P., and Bettler B. Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice. Eur. J. Neurosci. 18 (2003) 2722-2730
20. Liang J.H., Chen F., Krstew E., Cowen M.S., Carroll F.Y., Crawford D., Beart P.M., and Lawrence A.J. The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 50 (2006) 632-639
21. Millan M.J. The neurobiology and control of anxious states. Prog. Neurobiol. 70 (2003) 83-244
22. Mohler H., Fritschy J.M., and Rudolph U. A new benzodiazepine pharmacology. J. Pharmacol. Exp. Ther. 300 (2002) 2-8
23. Mombereau C., Kaupmann K., van der Putten H., and Cryan J.F. Altered response to benzodiazepine anxiolytics in mice lacking GABA B(1) receptors. Eur. J. Pharmacol. 497 (2004) 119-120
24. Mombereau C., Kaupmann K., Froestl W., Sansig G., van der Putten H., and Cryan J.F. Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacology 29 (2004) 1050-1062
25. Mombereau C., Kaupmann K., Gassmann M., Bettler B., van der Putten H., and Cryan J.F. Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits. Neuroreport 16 (2005) 307-310
26. Orru A., Lai P., Lobina C., Maccioni P., Piras P., Scanu L., Froestl W., Gessa G.L., Carai M.A., and Colombo G. Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur. J. Pharmacol. 525 (2005) 105-111
27. Pilc A., and Nowak G. GABAergic hypotheses of anxiety and depression: focus on GABA-B receptors. Drugs Today (Barc.) 41 (2005) 755-766
28. Rodgers R.J. Animal models of 'anxiety': where next?. Behav. Pharmacol. 8 (1997) 477-496
29. Shepherd J.K., Grewal S.S., Fletcher A., Bill D.J., and Dourish C.T. Behavioural and pharmacological characterisation of the elevated "zero-maze" as an animal model of anxiety. Psychopharmacology (Berlin) 116 (1994) 56-64
30. Simiand J., Keane P.E., and Morre M. The staircase test in mice: a simple and efficient procedure for primary screening of anxiolytic agents. Psychopharmacology (Berlin) 84 (1984) 48-53
31. Smith M.A., Yancey D.L., Morgan D., Liu Y., Froestl W., and Roberts D.C. Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats. Psychopharmacology (Berlin) 173 (2004) 105-111
32. Soudijn W., Van Wijngaarden I., and IJzermann A.P. Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. Drug Discov. Today 9 (2004) 752-758
33. Urwyler S., Gjoni T., Koljatic J., and Dupuis D.S. Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties. Neuropharmacology 48 (2005) 343-353
34. Urwyler S., Mosbacher J., Lingenhoehl K., Heid J., Hofstetter K., Froestl W., Bettler B., and Kaupmann K. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol. Pharmacol. 60 (2001) 963-971
35. B receptor function. J. Pharmacol. Exp. Ther. 307 (2003) 322-330
36. Van der Heyden J.A., Zethof T.J., and Olivier B. Stress-induced hyperthermia in singly housed mice. Physiol. Behav. 62 (1997) 463-470