-
1
-
-
29244437830
-
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
-
16183706 10.1124/jpet.105.089920 1:CAS:528:DC%2BD28XhslCiug%3D%3D
-
Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A et al (2006) 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. J Pharmacol Exp Ther 316:410-422
-
(2006)
J Pharmacol Exp Ther
, vol.316
, pp. 410-422
-
-
Atack, J.R.1
Wafford, K.A.2
Tye, S.J.3
Cook, S.M.4
Sohal, B.5
Pike, A.6
-
2
-
-
79952149335
-
MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans
-
20147571 10.1177/0269881109354927 1:CAS:528:DC%2BC3MXksFWkurk%3D
-
Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K et al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J Psychopharmacol 25:314-328
-
(2011)
J Psychopharmacol
, vol.25
, pp. 314-328
-
-
Atack, J.R.1
Wafford, K.A.2
Street, L.J.3
Dawson, G.R.4
Tye, S.5
Van Laere, K.6
-
3
-
-
0034022348
-
Beta-CCT, a selective BZ-omega1 receptor antagonist, blocks the anti-anxiety but not the amnesic action of chlordiazepoxide in mice
-
10877117 10.1097/00008877-200004000-00004 1:CAS:528:DC%2BD3cXjvVWis7k%3D
-
Belzung C, Le Guisquet AM, Griebel G (2000) Beta-CCT, a selective BZ-omega1 receptor antagonist, blocks the anti-anxiety but not the amnesic action of chlordiazepoxide in mice. Behav Pharmacol 11:125-131
-
(2000)
Behav Pharmacol
, vol.11
, pp. 125-131
-
-
Belzung, C.1
Le Guisquet, A.M.2
Griebel, G.3
-
4
-
-
36749096756
-
The impact of sub-cellular location and intracellular neuronal proteins on properties of GABA(A) receptors
-
18045166 10.2174/138161207782341330 1:CAS:528:DC%2BD2sXhsVSgsb7N
-
Birnir B, Korpi ER (2007) The impact of sub-cellular location and intracellular neuronal proteins on properties of GABA(A) receptors. Curr Pharm Des 13:3169-3177
-
(2007)
Curr Pharm des
, vol.13
, pp. 3169-3177
-
-
Birnir, B.1
Korpi, E.R.2
-
5
-
-
0029664746
-
Stoichiometry of a recombinant GABAA receptor
-
8757254 1:CAS:528:DyaK28Xlt1eis74%3D
-
Chang Y, Wang R, Barot S, Weiss DS (1996) Stoichiometry of a recombinant GABAA receptor. J Neurosci 16:5415-5424
-
(1996)
J Neurosci
, vol.16
, pp. 5415-5424
-
-
Chang, Y.1
Wang, R.2
Barot, S.3
Weiss, D.S.4
-
6
-
-
0035122824
-
Molecular targets for the myorelaxant action of diazepam
-
11179437 1:CAS:528:DC%2BD3MXhs1Ojsro%3D
-
Crestani F, Löw K, Keist R, Mandelli M, Möhler H, Rudolph U (2001) Molecular targets for the myorelaxant action of diazepam. Mol Pharmacol 59:442-445
-
(2001)
Mol Pharmacol
, vol.59
, pp. 442-445
-
-
Crestani, F.1
Löw, K.2
Keist, R.3
Mandelli, M.4
Möhler, H.5
Rudolph, U.6
-
7
-
-
12344276536
-
Development of subtype selective GABAA modulators
-
15618944
-
Dawson GR, Collinson N, Atack JR (2005) Development of subtype selective GABAA modulators. CNS Spectr 10:21-27
-
(2005)
CNS Spectr
, vol.10
, pp. 21-27
-
-
Dawson, G.R.1
Collinson, N.2
Atack, J.R.3
-
8
-
-
84871909017
-
Psychiatry, the pharmaceutical industry, and the road to better therapeutics
-
22837348 10.1093/schbul/sbs073
-
Fibiger HC (2012) Psychiatry, the pharmaceutical industry, and the road to better therapeutics. Schizophr Bull 38:649-650
-
(2012)
Schizophr Bull
, vol.38
, pp. 649-650
-
-
Fibiger, H.C.1
-
9
-
-
0022570677
-
The pharmacokinetics of diazepam and desmethyldiazepam in rat brain and plasma
-
3083446 10.1007/BF00180822 1:CAS:528:DyaL28XhvF2mt7w%3D
-
Friedman H, Abernethy DR, Greenblatt DJ, Shader RI (1986) The pharmacokinetics of diazepam and desmethyldiazepam in rat brain and plasma. Psychopharmacology 88:267-270
-
(1986)
Psychopharmacology
, vol.88
, pp. 267-270
-
-
Friedman, H.1
Abernethy, D.R.2
Greenblatt, D.J.3
Shader, R.I.4
-
10
-
-
0032863732
-
New evidence that the pharmacological effects of benzodiazepine receptor ligands can be associated with activities at different BZ (omega) receptor subtypes
-
10525757 10.1007/s002130051108 1:CAS:528:DyaK1MXntlOmtbo%3D
-
Griebel G, Perrault G, Letang V, Granger P, Avenet P, Schoemaker H et al (1999) New evidence that the pharmacological effects of benzodiazepine receptor ligands can be associated with activities at different BZ (omega) receptor subtypes. Psychopharmacology 146:205-213
-
(1999)
Psychopharmacology
, vol.146
, pp. 205-213
-
-
Griebel, G.1
Perrault, G.2
Letang, V.3
Granger, P.4
Avenet, P.5
Schoemaker, H.6
-
11
-
-
0027761396
-
Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors
-
8264558 1:CAS:528:DyaK2cXhsFCnsrw%3D
-
Hadingham KL, Wingrove PB, Wafford KA, Bain C, Kemp JA, Palmer KJ et al (1993) Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors. Mol Pharmacol 44:1211-1218
-
(1993)
Mol Pharmacol
, vol.44
, pp. 1211-1218
-
-
Hadingham, K.L.1
Wingrove, P.B.2
Wafford, K.A.3
Bain, C.4
Kemp, J.A.5
Palmer, K.J.6
-
12
-
-
84874412750
-
Neurosteroid influences on sensitivity to ethanol
-
22654852 10.3389/fendo.2012.00010 1:CAS:528:DC%2BC3sXmvVCqtbw%3D
-
Helms CM, Rossi DJ, Grant KA (2012) Neurosteroid influences on sensitivity to ethanol. Frontiers in Endocrinology 3:10
-
(2012)
Frontiers in Endocrinology
, vol.3
, pp. 10
-
-
Helms, C.M.1
Rossi, D.J.2
Grant, K.A.3
-
13
-
-
0021239198
-
Absorption of diazepam and its transfer through the blood-brain barrier after intraperitoneal administration in the rat
-
6726659 1:CAS:528:DyaL2cXksVyit7k%3D
-
Hironaka T, Fuchino K, Fujii T (1984) Absorption of diazepam and its transfer through the blood-brain barrier after intraperitoneal administration in the rat. J Pharmacol Exp Ther 229:809-815
-
(1984)
J Pharmacol Exp Ther
, vol.229
, pp. 809-815
-
-
Hironaka, T.1
Fuchino, K.2
Fujii, T.3
-
14
-
-
0029867314
-
A review of the validity and variability of the elevated plus-maze as an animal model of anxiety
-
8728535 10.1016/0091-3057(95)02126-4 1:CAS:528:DyaK28XisVOisro%3D
-
Hogg S (1996) A review of the validity and variability of the elevated plus-maze as an animal model of anxiety. Pharmacol Biochem Behav 54:21-30
-
(1996)
Pharmacol Biochem Behav
, vol.54
, pp. 21-30
-
-
Hogg, S.1
-
15
-
-
84891597940
-
Benzodiazepine-induced spatial learning deficits in rats are regulated by the degree of modulation of α(1) GABA(A) receptors
-
22633616 10.1016/j.euroneuro.2012.05.003
-
Joksimović S, Divljaković J, Van Linn ML, Varagic Z, Brajković G, Milinković MM et al (2013) Benzodiazepine-induced spatial learning deficits in rats are regulated by the degree of modulation of α(1) GABA(A) receptors. Eur Neuropsychopharmacol 23:390-399
-
(2013)
Eur Neuropsychopharmacol
, vol.23
, pp. 390-399
-
-
Joksimović, S.1
Divljaković, J.2
Van Linn, M.L.3
Varagic, Z.4
Brajković, G.5
Milinković, M.M.6
-
16
-
-
78649709408
-
Quantitative localisation of synaptic and extrasynaptic GABAA receptor subunits on hippocampal pyramidal cells by freeze-fracture replica immunolabelling
-
21073549 10.1111/j.1460-9568.2010.07473.x
-
Kasugai Y, Swinny JD, Roberts JD, Dalezios Y, Fukazawa Y, Sieghart W et al (2010) Quantitative localisation of synaptic and extrasynaptic GABAA receptor subunits on hippocampal pyramidal cells by freeze-fracture replica immunolabelling. Eur J Neurosci 32:1868-1888
-
(2010)
Eur J Neurosci
, vol.32
, pp. 1868-1888
-
-
Kasugai, Y.1
Swinny, J.D.2
Roberts, J.D.3
Dalezios, Y.4
Fukazawa, Y.5
Sieghart, W.6
-
17
-
-
62749191456
-
Contribution of alpha1 subunit-containing gamma-aminobutyric acidA (GABAA) receptors to motor-impairing effects of benzodiazepines in squirrel monkeys
-
19031072 10.1007/s00213-008-1401-7 1:CAS:528:DC%2BD1cXhsVaisbvN
-
Licata SC, Platt DM, Cook JM, Van Linn ML, Rowlett JK (2009) Contribution of alpha1 subunit-containing gamma-aminobutyric acidA (GABAA) receptors to motor-impairing effects of benzodiazepines in squirrel monkeys. Psychopharmacology 203:539-546
-
(2009)
Psychopharmacology
, vol.203
, pp. 539-546
-
-
Licata, S.C.1
Platt, D.M.2
Cook, J.M.3
Van Linn, M.L.4
Rowlett, J.K.5
-
18
-
-
21044437177
-
Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator
-
15870187 10.1073/pnas.0502579102 1:CAS:528:DC%2BD2MXks12ntrw%3D
-
Lippa A, Czobor P, Stark J, Beer B, Kostakis E, Gravielle M et al (2005) Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator. Proc Natl Acad Sci USA 102:7380-7385
-
(2005)
Proc Natl Acad Sci USA
, vol.102
, pp. 7380-7385
-
-
Lippa, A.1
Czobor, P.2
Stark, J.3
Beer, B.4
Kostakis, E.5
Gravielle, M.6
-
19
-
-
0034108997
-
Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype
-
10816315 10.1038/75761 1:CAS:528:DC%2BD3cXjsF2nu70%3D
-
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
-
(2000)
Nat Neurosci
, vol.3
, pp. 587-592
-
-
McKernan, R.M.1
Rosahl, T.W.2
Reynolds, D.S.3
Sur, C.4
Wafford, K.A.5
Atack, J.R.6
-
20
-
-
84858708930
-
The role of α1 and α5 subunit-containing GABAA receptors in motor impairment induced by benzodiazepines in rats
-
22327019 10.1097/FBP.0b013e3283512c85
-
Milić M, Divljaković J, Rallapalli S, van Linn ML, Timić T, Cook JM, Savić MM (2012) The role of α1 and α5 subunit-containing GABAA receptors in motor impairment induced by benzodiazepines in rats. Behav Pharmacol 23:191-197
-
(2012)
Behav Pharmacol
, vol.23
, pp. 191-197
-
-
Milić, M.1
Divljaković, J.2
Rallapalli, S.3
Van Linn, M.L.4
Timić, T.5
Cook, J.M.6
Savić, M.M.7
-
21
-
-
33646692183
-
Both alpha2 and alpha3 GABAA receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the conditioned emotional response paradigm
-
16706856 10.1111/j.1460-9568.2006.04775.x 1:STN:280: DC%2BD28zlvFGmug%3D%3D
-
Morris HV, Dawson GR, Reynolds DS, Atack JR, Stephens DN (2006) Both alpha2 and alpha3 GABAA receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the conditioned emotional response paradigm. Eur J Neurosci 23:2495-2504
-
(2006)
Eur J Neurosci
, vol.23
, pp. 2495-2504
-
-
Morris, H.V.1
Dawson, G.R.2
Reynolds, D.S.3
Atack, J.R.4
Stephens, D.N.5
-
22
-
-
54049137689
-
International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: Classification on the basis of subunit composition, pharmacology, and function. Update
-
18790874 10.1124/pr.108.00505 1:CAS:528:DC%2BD1MXmsVChtrY%3D
-
Olsen RW, Sieghart W (2008) International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol Rev 60:243-260
-
(2008)
Pharmacol Rev
, vol.60
, pp. 243-260
-
-
Olsen, R.W.1
Sieghart, W.2
-
23
-
-
0036918252
-
Selective antagonism of the ataxic effects of zolpidem and triazolam by the GABAA/alpha1-preferring antagonist beta-CCt in squirrel monkeys
-
12404077 10.1007/s00213-002-1189-9 1:CAS:528:DC%2BD38Xot1Ciurw%3D
-
Platt DM, Rowlett JK, Spealman RD, Cook J, Ma C (2002) Selective antagonism of the ataxic effects of zolpidem and triazolam by the GABAA/alpha1-preferring antagonist beta-CCt in squirrel monkeys. Psychopharmacology 164:151-159
-
(2002)
Psychopharmacology
, vol.164
, pp. 151-159
-
-
Platt, D.M.1
Rowlett, J.K.2
Spealman, R.D.3
Cook, J.4
Ma, C.5
-
24
-
-
77952675421
-
The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes
-
20303942 10.1016/j.ejphar.2010.03.015 1:CAS:528:DC%2BC3cXlvVaqu7k%3D
-
Ramerstorfer J, Furtmüller R, Vogel E, Huck S, Sieghart W (2010) The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes. Eur J Pharmacol 636:18-27
-
(2010)
Eur J Pharmacol
, vol.636
, pp. 18-27
-
-
Ramerstorfer, J.1
Furtmüller, R.2
Vogel, E.3
Huck, S.4
Sieghart, W.5
-
25
-
-
64549125587
-
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models
-
19275170 10.1021/jm801652d 1:CAS:528:DC%2BD1MXjtFyrsL8%3D
-
Rivas FM, Stables JP, Murphree L, Edwankar RV, Edwankar CR, Huang S et al (2009) Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. J Med Chem 52:1795-1798
-
(2009)
J Med Chem
, vol.52
, pp. 1795-1798
-
-
Rivas, F.M.1
Stables, J.P.2
Murphree, L.3
Edwankar, R.V.4
Edwankar, C.R.5
Huang, S.6
-
26
-
-
12344331438
-
Selective antagonism of GABAA receptor subtypes: An in vivo approach to exploring the therapeutic and side effects of benzodiazepine-type drugs
-
15618946
-
Rowlett JK, Cook JM, Duke AN, Platt DM (2005) Selective antagonism of GABAA receptor subtypes: an in vivo approach to exploring the therapeutic and side effects of benzodiazepine-type drugs. CNS Spectr 10:40-48
-
(2005)
CNS Spectr
, vol.10
, pp. 40-48
-
-
Rowlett, J.K.1
Cook, J.M.2
Duke, A.N.3
Platt, D.M.4
-
27
-
-
80052274158
-
Beyond classical benzodiazepines: Novel therapeutic potential of GABAA receptor subtypes
-
21799515 10.1038/nrd3502 1:CAS:528:DC%2BC3MXpsFKrtbc%3D
-
Rudolph U, Knoflach F (2011) Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes. Nat Rev Drug Discov 10:685-697
-
(2011)
Nat Rev Drug Discov
, vol.10
, pp. 685-697
-
-
Rudolph, U.1
Knoflach, F.2
-
28
-
-
1342344806
-
Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics
-
14744255 10.1146/annurev.pharmtox.44.101802.121429 1:CAS:528: DC%2BD2cXhvVCktb4%3D
-
Rudolph U, Möhler H (2004) Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics. Annu Rev Pharmacol Toxicol 44:475-498
-
(2004)
Annu Rev Pharmacol Toxicol
, vol.44
, pp. 475-498
-
-
Rudolph, U.1
Möhler, H.2
-
29
-
-
11144336626
-
Bidirectional effects of benzodiazepine binding site ligands in the elevated plus-maze: Differential antagonism by flumazenil and beta-CCt
-
15501303 10.1016/j.pbb.2004.07.013
-
Savić MM, Obradović DI, Ugrešić ND, Cook JM, Yin W, Bokonjić DR (2004) Bidirectional effects of benzodiazepine binding site ligands in the elevated plus-maze: differential antagonism by flumazenil and beta-CCt. Pharmacol Biochem Behav 79:279-290
-
(2004)
Pharmacol Biochem Behav
, vol.79
, pp. 279-290
-
-
Savić, M.M.1
Obradović, D.I.2
Ugrešić, N.D.3
Cook, J.M.4
Yin, W.5
Bokonjić, D.R.6
-
30
-
-
77649270051
-
The differential role of alpha1- and alpha5-containing GABA(A) receptors in mediating diazepam effects on spontaneous locomotor activity and water-maze learning and memory in rats
-
19265570 10.1017/S1461145709000108
-
Savić MM, Milinković MM, Rallapalli S, Clayton T Sr, Joksimović S, Van Linn M, Cook JM (2009) The differential role of alpha1- and alpha5-containing GABA(A) receptors in mediating diazepam effects on spontaneous locomotor activity and water-maze learning and memory in rats. Int J Neuropsychopharmacol 12:1179-1193
-
(2009)
Int J Neuropsychopharmacol
, vol.12
, pp. 1179-1193
-
-
Savić, M.M.1
Milinković, M.M.2
Rallapalli, S.3
Clayton, Sr.T.4
Joksimović, S.5
Van Linn, M.6
Cook, J.M.7
-
31
-
-
23844550957
-
Heterogeneity of GABAA receptors: Revived interest in the development of subtype-selective drugs
-
10.2174/1568015054863837 1:CAS:528:DC%2BD2MXovFSjs74%3D
-
Sieghart W, Ernst M (2005) Heterogeneity of GABAA receptors: revived interest in the development of subtype-selective drugs. Curr Med Chem Cent Nerv Syst Agents 5:217-242
-
(2005)
Curr Med Chem Cent Nerv Syst Agents
, vol.5
, pp. 217-242
-
-
Sieghart, W.1
Ernst, M.2
-
32
-
-
84867861360
-
Anxioselective anxiolytics: On a quest for the Holy Grail
-
22981367 10.1016/j.tips.2012.08.003 1:CAS:528:DC%2BC38XhtlKrtrjK
-
Skolnick P (2012) Anxioselective anxiolytics: on a quest for the Holy Grail. Trends Pharmacol Sci 33:611-620
-
(2012)
Trends Pharmacol Sci
, vol.33
, pp. 611-620
-
-
Skolnick, P.1
-
33
-
-
84861959996
-
Benzodiazepine-induced anxiolysis and reduction of conditioned fear are mediated by distinct GABAA receptor subtypes in mice
-
22465203 10.1016/j.neuropharm.2012.03.001 1:CAS:528:DC%2BC38Xls1elurw%3D
-
Smith KS, Engin E, Meloni EG, Rudolph U (2012) Benzodiazepine-induced anxiolysis and reduction of conditioned fear are mediated by distinct GABAA receptor subtypes in mice. Neuropharmacology 63:250-258
-
(2012)
Neuropharmacology
, vol.63
, pp. 250-258
-
-
Smith, K.S.1
Engin, E.2
Meloni, E.G.3
Rudolph, U.4
-
34
-
-
77957976870
-
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse
-
20888240 10.1016/j.bmc.2010.08.049 1:CAS:528:DC%2BC3cXhtlSms73K
-
Yin W, Majumder S, Clayton T, Petrou S, Van Linn ML, Namjoshi OA et al (2010) Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. Bioorg Med Chem 18:7548-7564
-
(2010)
Bioorg Med Chem
, vol.18
, pp. 7548-7564
-
-
Yin, W.1
Majumder, S.2
Clayton, T.3
Petrou, S.4
Van Linn, M.L.5
Namjoshi, O.A.6
|