Are GABAA receptors containing α5 subunits contributing to the sedative properties of benzodiazepine site agonists?

Neuropsychopharmacology

Volumn 33, Issue 2, 2008, Pages 332-339

  Savić, Miroslav M ^a   Huang, Shengming ^b   Furtmüller, Roman ^c   Clayton, Terry ^b   Huck, Sigismund ^c   Obradović, Dragan I ^a   Ugrešić, Nenad D ^a   Sieghart, Werner ^c   Bokonjić, Dubravko R ^d   Cook, James M ^b  

^a UNIVERSITY OF BELGRADE   (Serbia)

^b UNIVERSITY OF WISCONSIN MILWAUKEE   (United States)

^c MEDICAL UNIVERSITY OF VIENNA   (Austria)

^d UNIVERSITY OF DEFENCE   (Serbia)

Author keywords

Anxiety; Ataxia; Benzodiazepine; GABAA; Sedation; Subtype selectivity

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 8 ETHINYL 4 METHYL 6 PHENYL 4H 25,10B TRIAZABENZO[E]AZULENE 3 CARBOXYLIC ACID ETHYL ESTER; 8 ETHINYL 6 (2 FLUOROPHENYL) 4 METHYL 4H 2,5,10B TRIAZABENZO[E]AZULENE 3 CARBOXYLIC ACID ETHYL ESTER; BENZODIAZEPINE RECEPTOR STIMULATING AGENT; DIAZEPAM; RECEPTOR SUBTYPE; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG; BENZODIAZEPINE DERIVATIVE; PROTEIN SUBUNIT;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; ATAXIA; BEHAVIOR; CONTROLLED STUDY; DRUG SELECTIVITY; ELECTRODE; FEMALE; IN VIVO STUDY; LOCOMOTION; MALE; MAZE TEST; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; ROTAROD TEST; SEDATION; TRANQUILIZING ACTIVITY; VOLTAGE CLAMP; XENOPUS; ANALYSIS OF VARIANCE; ANIMAL; DRUG EFFECT; MOTOR ACTIVITY; PHYSIOLOGY; WISTAR RAT;

ANALYSIS OF VARIANCE; ANIMALS; BENZODIAZEPINES; MALE; MAZE LEARNING; MOTOR ACTIVITY; PROTEIN SUBUNITS; RATS; RATS, WISTAR; RECEPTORS, GABA-A;

EID: 36949012960     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.npp.1301403     Document Type: Article

References (41)

1. Atack JR, Bayley PJ, Fletcher SR, McKernan RM, Wafford KA, Dawson GR (2006a). The proconvulsant effects of the GABA(A) alpha5 subtype-selective compound RY-080 may not be alpha5-mediated. Eur J Pharmacol 548: 77-82.
2. Atack JR, Pike A, Marshall G, Stanley J, Lincoln R, Cook SM et al (2006b). The in vivo properties of pagoclone in rat are most likely mediated by 5′-hydroxy pagoclone. Neuropharmacology 50: 677-689.
3. A receptors, is a nonsedating anxiolytic in rodents and primates. J Pharmacol Exp Ther 316: 410-422.
4. Basile AS, Lippa AS, Skolnick P (2004). Anxioselective anxiolytics: can less be more? Eur J Pharmacol 500: 441-451.
5. A-receptor subtypes in the spinal cord: an immunohistochemical study. J Neurosci 16: 283-297.
6. Bourin M, Briley M (2004). Sedation, an unpleasant, undesirable and potentially dangerous side-effect of many psychotropic drugs. Hum Psychopharmacol 19: 135-139.
7. A receptor. J Neurosci 16: 5415-5424.
8. A receptor. J Neurosci 22: 5572-5580.
9. Crestani F, Keist R, Fritschy JM, Benke D, Vogt K, Prut L et al (2002). Trace fear conditioning involves hippocampal alpha5 GABA(A) receptors. Proc Natl Acad Sci USA 99: 8980-8985.
10. A receptor mutant mouse studies. Nat Neurosci 3: 1059.
11. Dailly E, Hascoet M, Colombel MC, Jolliet P, Bourin M (2002). Relationship between cerebral pharmacokinetics and anxiolytic activity of diazepam and its active metabolites after a single intra-peritoneal administration of diazepam in mice. Hum Psychopharmacol 17: 239-245.
12. A receptors in mediating the anxiolytic effects of benzodiazepines. J Neurosci 25: 10682-10688.
13. Facklam M, Schoch P, Bonetti EP, Jenck F, Martin JR, Moreau JL et al (1992). Relationship between benzodiazepine receptor occupancy and functional effects in vivo of four ligands of differing intrinsic efficacies. J Pharmacol Exp Ther 261: 1113-1121.
14. 3H]flunitrazepam binding in human embryonic kidney cell line 293. Eur J Pharmacol 289: 87-95.
15. Griebel G, Perrault G, Simiand J, Cohen C, Granger P, Decobert M et al (2001). SL651498: an anxioselective compound with functional selectivity for alpha2-and alpha3-containing gamma-aminobutyric acid(A) (GABA(A)) receptors. J Pharmacol Exp Ther 298: 753-768.
16. He X, Huang Q, Ma C, Yu S, McKernan R, Cook JM (2000). Pharmacophore/receptor models for GABA(A)/BzR α2β3γ2, α3β3γ2 and α4β3γ2 recombinant subtypes. Included volume analysis and comparison to α1β3γ2, α5β3γ2, and α6β3γ2 subtypes. Drug Des Discov 17: 131-171.
17. Jennings AS, Lewis RT, Russell MG, Hallett DJ, Street LJ, Castro JL et al (2006). Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety. Bioorg Med Chem Lett 16: 1477-1480.
18. Kelley AE (1993). Locomotor activity and exploration. In: van Haaren F (ed). Techniques in the Behavioral and Neural Sciences, vol 10. Methods in Behavioral Pharmacology. Elsevier: New York. pp 499-518.
19. Lader MH (1999). Limitations on the use of benzodiazepines in anxiety and insomnia: are they justified? Eur Neuropsychopharmacol 9(Suppl 6): S399-S405.
20. A receptor subtypes to the anxiolytic-like, motor, and discriminative stimulus effects of benzodiazepines: studies with the functionally selective ligand SL651498 [6-fluoro-9-methyl-2-phenyl-4- (pyrrolidin-1-yl-carbonyl)-2,9-dihydro-1H-pyridol[ 3,4-b]indol-1-one]. J Pharmacol Exp Ther 313: 1118-1125.
21. A/benzodiazepine receptor subtype. Med Chem Res 5: 700-709.
22. Low K, Crestani F, Keist R, Benke D, Brunig I, Benson JA et al (2000). Molecular and neuronal substrate for the selective attenuation of anxiety. Science 290: 131-134.
23. McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR et al (2000). Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype. Nat Neurosci 3: 587-592.
24. Porsolt RD, McArthur RA, Lenegre A (1993). Psychotropic screening procedures. In: van Haaren F (ed). Techniques in the Behavioral And Neural Sciences, vol 10. Methods in Behavioral Pharmacology. Elsevier: New York. pp 23-51.
25. A receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates. Proc Natl Acad Sci USA 102: 915-920.
26. Rudolph U, Crestani F, Benke D, Brunig I, Benson JA, Fritschy JM et al (1999). Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. Nature 401: 796-800.
27. A receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics. Annu Rev Pharmacol Toxicol 44: 475-498.
28. Rudolph U, Möhler H (2006). GABA-based therapeutic approaches: GABA(A) receptor subtype functions. Curr Opin Pharmacol 6: 18-23.
29. Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E et al (2006). Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. J Med Chem 49: 1235-1238.
30. Sanger D, Willner P, Bergman J (2003). Applications of behavioural pharmacology in drug discovery. Behav Pharmacol 14: 363-367.
31. Sanger DJ, Morel E, Perrault G (1996). Comparison of the pharmacological profiles of the hypnotic drugs, zaleplon and zolpidem. Eur J Pharmacol 313: 35-42.
32. Savić MM, Obradoviæ DI, Ugrešiæ ND, Bokonjiæ DR (2003). The influence of diazepam on atropine reversal of behavioural impairment in dichlorvos-treated rats. Pharmacol Toxicol 93: 211-218.
33. Savić MM, Obradović DI, Ugrešiæ ND, Cook JM, Yin W, Van Linn M et al (2006). Benzodiazepine site inverse agonists and locomotor activity in rats: bimodal and biphasic influence. Pharmacol Biochem Behav 84: 35-42.
34. A receptor subtypes. Curr Opin Med Chem 2: 795-816.
35. Sigel E (1987). Properties of single sodium channels translated by Xenopus oocytes after injection with messenger ribonucleic acid. J Physiol 386: 73-90.
36. A receptors on channel function. Neuron 5: 703-711.
37. A receptors. Trends Pharmacol Sci 18: 425-429.
38. A receptors for the development of tolerance to the sedative action of diazepam in mice. J Neurosci 24: 6785-6790.
39. Vogel HG (2002). Drug Discovery and Evaluation. Springer: Berlin.
40. Whiting PJ (2006). GABA-A receptors: a viable target for novel anxiolytics? Curr Opin Pharmacol 6: 24-29.
41. Zhang W, Koehler KF, Zhang P, Cook JM (1995). Development of a comprehensive pharmacophore model for the benzodiazepine receptor. Drug Des Discov 12: 193-248.