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Results: 1 to 20 of 244

1.

A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Lewis RT, Blackaby WP, Blackburn T, Jennings AS, Pike A, Wilson RA, Hallett DJ, Cook SM, Ferris P, Marshall GR, Reynolds DS, Sheppard WF, Smith AJ, Sohal B, Stanley J, Tye SJ, Wafford KA, Atack JR.

J Med Chem. 2006 Apr 20;49(8):2600-10.

PMID:
16610803
[PubMed - indexed for MEDLINE]
2.

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Goodacre SC, Hallett DJ, Carling RW, Castro JL, Reynolds DS, Pike A, Wafford KA, Newman R, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1582-5. Epub 2005 Dec 27.

PMID:
16384707
[PubMed - indexed for MEDLINE]
3.

GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.

Atack JR.

Curr Top Med Chem. 2011;11(9):1176-202. Review.

PMID:
21050172
[PubMed - indexed for MEDLINE]
4.

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.

Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ.

J Med Chem. 2005 Nov 17;48(23):7089-92.

PMID:
16279764
[PubMed - indexed for MEDLINE]
5.

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site.

Atack JR.

Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32. Review.

PMID:
12871032
[PubMed - indexed for MEDLINE]
6.

TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.

Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM.

J Pharmacol Exp Ther. 2006 Jan;316(1):410-22. Epub 2005 Sep 23.

PMID:
16183706
[PubMed - indexed for MEDLINE]
Free Article
7.

Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL.

J Med Chem. 2006 Feb 23;49(4):1235-8.

PMID:
16480260
[PubMed - indexed for MEDLINE]
8.

The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics.

Atack JR.

Expert Opin Investig Drugs. 2005 May;14(5):601-18. Review.

PMID:
15926867
[PubMed - indexed for MEDLINE]
9.

Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Jennings AS, Lewis RT, Russell MG, Hallett DJ, Street LJ, Castro JL, Atack JR, Cook SM, Lincoln R, Stanley J, Smith AJ, Reynolds DS, Sohal B, Pike A, Marshall GR, Wafford KA, Sheppard WF, Tye SJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1477-80. Epub 2006 Jan 4.

PMID:
16386900
[PubMed - indexed for MEDLINE]
10.

gamma-Aminobutyrate-A receptor modulation by 3-aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines.

Rybczynski PJ, Combs DW, Jacobs K, Shank RP, Dubinsky B.

J Med Chem. 1999 Jul 1;42(13):2403-8.

PMID:
10395481
[PubMed - indexed for MEDLINE]
11.

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.

Carling RW, Russell MG, Moore KW, Mitchinson A, Guiblin A, Smith A, Wafford KA, Marshall G, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3550-4. Epub 2006 Apr 18.

PMID:
16621541
[PubMed - indexed for MEDLINE]
12.

GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement.

Atack JR.

Curr Top Med Chem. 2011;11(9):1203-14. Review.

PMID:
21050171
[PubMed - indexed for MEDLINE]
13.

Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.

Jacobsen EJ, Stelzer LS, TenBrink RE, Belonga KL, Carter DB, Im HK, Im WB, Sethy VH, Tang AH, VonVoigtlander PF, Petke JD, Zhong WZ, Mickelson JW.

J Med Chem. 1999 Apr 8;42(7):1123-44.

PMID:
10197957
[PubMed - indexed for MEDLINE]
14.

Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.

Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR.

J Med Chem. 2006 Jan 12;49(1):35-8.

PMID:
16392789
[PubMed - indexed for MEDLINE]
15.

Ligands for the benzodiazepine binding site--a survey.

Teuber L, Wätjens F, Jensen LH.

Curr Pharm Des. 1999 May;5(5):317-43. Review.

PMID:
10213798
[PubMed - indexed for MEDLINE]
16.

Bidirectional effects of benzodiazepine binding site ligands on active avoidance acquisition and retention: differential antagonism by flumazenil and beta-CCt.

Savić MM, Obradović DI, Ugresić ND, Cook JM, Sarma PV, Bokonjić DR.

Psychopharmacology (Berl). 2005 Jul;180(3):455-65. Epub 2005 Feb 18.

PMID:
15719222
[PubMed - indexed for MEDLINE]
17.

3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.

Collins I, Moyes C, Davey WB, Rowley M, Bromidge FA, Quirk K, Atack JR, McKernan RM, Thompson SA, Wafford K, Dawson GR, Pike A, Sohal B, Tsou NN, Ball RG, Castro JL.

J Med Chem. 2002 Apr 25;45(9):1887-900.

PMID:
11960500
[PubMed - indexed for MEDLINE]
18.

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10.

PMID:
20147571
[PubMed - indexed for MEDLINE]
19.

Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans.

Atack JR, Wong DF, Fryer TD, Ryan C, Sanabria S, Zhou Y, Dannals RF, Eng WS, Gibson RE, Burns HD, Vega JM, Vessy L, Scott-Stevens P, Beech JS, Baron JC, Sohal B, Schrag ML, Aigbirhio FI, McKernan RM, Hargreaves RJ.

J Pharmacol Exp Ther. 2010 Jan;332(1):17-25. doi: 10.1124/jpet.109.157909. Epub 2009 Sep 24.

PMID:
19779131
[PubMed - indexed for MEDLINE]
Free Article
20.

Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor.

Taliani S, Cosimelli B, Da Settimo F, Marini AM, La Motta C, Simorini F, Salerno S, Novellino E, Greco G, Cosconati S, Marinelli L, Salvetti F, L'Abbate G, Trasciatti S, Montali M, Costa B, Martini C.

J Med Chem. 2009 Jun 25;52(12):3723-34. doi: 10.1021/jm9001154.

PMID:
19469479
[PubMed - indexed for MEDLINE]
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