Page last updated: 2024-12-05

bicuculline

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Description

Bicuculline is a selective competitive antagonist of GABA-A receptors. It was first isolated from the seeds of the climbing plant, *Dicentra cucullaria*, commonly known as Dutchman's breeches. Bicuculline's mechanism of action involves binding to the GABA binding site on the GABA-A receptor, thus blocking the effects of GABA. This blockage prevents the receptor from opening and allowing chloride ions to flow into the neuron, which ultimately results in neuronal excitation. Bicuculline is used as a research tool to study the role of GABA in the central nervous system. Its effects include increasing neuronal firing rates, inducing seizures, and blocking the inhibitory effects of GABAergic neurotransmission. Researchers use bicuculline to investigate the involvement of GABA in various neurological processes, including learning, memory, anxiety, and epilepsy. The study of bicuculline has provided valuable insights into the role of GABA in brain function and the development of new therapeutic strategies for treating neurological disorders.'

Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bicuculline : A benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
CorydalisgenusA plant genus of the family FUMARIACEAE (classified by some in PAPAVERACEAE) that contains isoquinoline alkaloids.[MeSH]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]
Adlumiagenus[no description available]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]
Cucullariagenus[no description available]Vochysiaceae[no description available]
DicentragenusA genus of herbaceous plants with asymmetrically-shaped flowers and finely divided leaves, native to east Asia and North America.[MeSH]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]
Adlumia fungosaspecies[no description available]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]
Dicentra cucullariaspecies[no description available]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]

Cross-References

ID SourceID
PubMed CID10237
CHEMBL ID417990
CHEBI ID3092
SCHEMBL ID8222
MeSH IDM0002466

Synonyms (97)

Synonym
smr001233241
MLS002153892
HMS3266A07
gtpl2312
(6r)-6-[(5s)-6-methyl-7,8-dihydro-5h-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-6h-furo[4,3-g][1,3]benzodioxol-8-one
nsc-32192
wln: t c566 do fo kn eh&&tj k1 j- et b565 cvo jo lo eh khj
NSC32192 ,
d-bicuculline
furo[3,3-benzodioxol-8(6h)-one, 6-(5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl)-, [r-(r*,s*)]-
bicculine
(+)-bicuculline
KBIO1_000609
DIVK1C_000609
PDSP2_000138
BPBIO1_000482
nsc 32192
brn 0098786
furo(3,4-e)-1,3-benzodioxol-8(6h)-one, 6-(5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)-, (r-(r*,s*))-
einecs 207-619-7
bicucullin
PRESTWICK_96
PRESTWICK2_000589
BIOMOL-NT_000252
PRESTWICK3_000589
BSPBIO_000438
485-49-4
bicuculline
C09364
NINDS_000609
PRESTWICK0_000589
SPBIO_002657
PRESTWICK1_000589
LOPAC0_000234
BPBIO1_000794
IDI1_000609
(6r)-6-[(5s)-6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinolin-5-yl]furo[3,4-e][1,3]benzodioxol-8(6h)-one
B-2400
B 9130
(6r)-6-[(5s)-6-methyl-7,8-dihydro-5h-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-6h-furo[3,4-g][1,3]benzodioxol-8-one
CHEMBL417990 ,
HMS501O11
HMS1569F20
bdbm50000693
(bicuculline) 6-methyl-5-(8-oxo-6,8-dihydro-furo[3'',4'':3,4]benzo[1,2-d][1,3]dioxol-6-yl)-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-6-ium
6-(6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-6h-furo[3'',4'':3,4]benzo[1,2-d][1,3]dioxol-8-one
(r)-6-((s)-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-6h-furo[3'',4'':3,4]benzo[1,2-d][1,3]dioxol-8-one
6-(6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-6h-furo[3'',4'':3,4]benzo[1,2-d][1,3]dioxol-8-one(bicuculline)
6-(6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-6h-furo[3'',4'':3,4]benzo[1,2-d][1,3]dioxol-8-one (bicuculline)
bicuculline,(+)
(r)-6-((s)-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)isobenzofuro[5,4-d][1,3]dioxol-8(6h)-one
CHEBI:3092 ,
HMS2096F20
(6r)-6-((5s)-6-methyl(5,6,7,8-tetrahydro-2h-1,3-dioxolano[4,5-g]isoquinolin-5- yl))-6-hydro-2h-1,3-dioxoleno[4,5-e]isobenzofuran-8-one
B1890 ,
CCG-204329
HMS2235H18
furo(3,4-e)-1,3-benzodioxol-8(6h)-one, 6-((5s)-5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)-, (6r)-
y37615dvkc ,
unii-y37615dvkc
4-27-00-06900 (beilstein handbook reference)
(6r)-6-[(5s)-5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo[4,5-g]lisoquinolin-5-yl]furo[3,4-e]-1,3-benzodioxol-8(6h)-one
furo[3,4-e]-1,3-benzodioxol-8(6h)-one, 6-[(5s)-5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl]-, (6r)-
S7071
SCHEMBL8222
bicuculline [mi]
(6r)-6-((5s)-6-methyl-5,6,7,8-tetrahydro(1,3)dioxolo(4,5-g)isoquinolin-5-yl)furo(3,4-e)(1,3benzodioxol-8(6h)-one
DTXSID3042687
AKOS024282673
[r-(r*,s*)]-6-(5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl)furo[3,4-e]-1,3-benzodioxol-8(6h)-one
HB0896
[r-(r*,s*)]-6-(5,6,7,8-tetrahydro-6 -methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl)furo[3, 4-e]-1,3-benzodioxol-8(6h)-one
AC-31293
mfcd00005006
CS-5493
HY-N0219
(+)-bicuculline, 98%
(+)-bicuculline, >=97.0% (tlc)
HMS3652N20
SR-01000075252-1
sr-01000075252
SR-01000075252-4
SR-01000075252-5
NCGC00017385-06
(r)-6-((s)-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-[1,3]dioxolo[4,5-e]isobenzofuran-8(6h)-one
SW196408-2
DB11562
H0Z ,
BCP04180
Q3639734
HMS3678D19
AS-17471
HMS3414D19
HMS3886N09
bicuculline-(+)
BB164251
(+)-bicuculline- bio-x

Research Excerpts

Overview

Bicuculline is an antagonist of gamma-aminobutyric acid (GABA) receptors. muscimol is an agonist of GABA receptors.

ExcerptReferenceRelevance
"If bicuculline was assumed to be a pure non-competitive antagonist, then the observed depression of the GABA curves at high GABA concentrations was underestimated."( A re-examination of the GABA-inhibitory action of bicuculline on lobster muscle.
Constanti, A; Smart, TG, 1981
)
1.03
"Bicuculline is an antagonist of gamma-aminobutyric acid (GABA) receptors, and muscimol is an agonist of GABA receptors. "( Comparison of effects of bilateral injections of bicuculline and muscimol into the caudate-putamen of amygdaloid-kindled rats.
Mori, N; Watanabe, M, 1994
)
1.99

Effects

Bicuculline methiodide has been shown to block mutual inhibition between these interneurons and to cause them to spike tonically while recorded intracellularly (Schmidt and Calabrese, 1992) The drug was applied electrophoretically from a fluid filled microelectrode at different depths within the primary somatosensory area of the cerebral cortex of rats anaesthetized with urethane.

ExcerptReferenceRelevance
"Bicuculline methiodide has been shown to block mutual inhibition between these interneurons and to cause them to spike tonically while recorded intracellularly (Schmidt and Calabrese, 1992)."( Bursting in leech heart interneurons: cell-autonomous and network-based mechanisms.
Calabrese, RL; Cymbalyuk, GS; Gaudry, Q; Masino, MA, 2002
)
1.04
"Bicuculline has been applied electrophoretically from a fluid filled microelectrode at different depths within the primary somatosensory area of the cerebral cortex of rats anaesthetized with urethane. "( Bicuculline epileptogenesis in the rat.
Campbell, AM; Holmes, O, 1984
)
3.15
"Bicuculline alone has little or no influence on [35S]TBPS binding in the cerebral cortex, hippocampus, and cerebellum, but produces a dose-dependent enhancement of [35S]TBPS binding in the striatum, midbrain, and hypothalamus."( Anxiolytic cyclopyrrolone drugs allosterically modulate the binding of [35S]t-butylbicyclophosphorothionate to the benzodiazepine/gamma-aminobutyric acid-A receptor/chloride anionophore complex.
Snowman, AM; Snyder, SH; Trifiletti, RR, 1984
)
0.99
"Bicuculline alone has produced antinociception in the second phase and CGP35348 alone has had antinociception in both phases of the formalin test."( Effect of intracerebroventricular injection of GABA receptor agents on morphine-induced antinociception in the formalin test.
Mahmoudi, M; Zarrindast, MR, 2002
)
1.04

Actions

Bicuculline may disinhibit GABAergic efferents to the ventral pallidum resulting in a dramatic increase in glucose use within striatopallidal synaptic terminals as well as in local terminals of the pallidal projection neurons. Bicuculine did not increase blood pressure in 6-OHDA treated rats. The blood-brain barrier remained intact.

ExcerptReferenceRelevance
"Bicuculline led to an increase in the firing rate and a change in the firing pattern of GPe neurons."( Bicuculline-induced chorea manifests in focal rather than globalized abnormalities in the activation of the external and internal globus pallidus.
Bar-Gad, I; Belelovsky, K; Bronfeld, M; Bugaysen, J; Erez, Y; Korngreen, A, 2010
)
2.52
"Bicuculline alone did not produce an intrinsic effect in the paw-pressure test."( GABAergic mechanisms are involved in the antihyperalgesic effects of carbamazepine and oxcarbazepine in a rat model of inflammatory hyperalgesia.
Bosković, B; Kocev, N; Prostran, MS; Stepanović-Petrović, RM; Tomić, MA; Ugresić, ND; Vucković, SM, 2008
)
1.07
"The bicuculline produced an increase in both the visually evoked and the spontaneous unit activity."( Bicuculline and neuronal activity in motor cortex.
Chattha, AS; Fromm, GH; Glass, JD, 1980
)
2.18
"(+)-Bicuculline was used to suppress bicuculline sensitive GABA binding."( Bicuculline insensitive effects of baclofen.
Rägo, LK; Zarkovsky, AM, 1983
)
2.19
"Bicuculline prevented the increase in GABA levels induced by ether stress in both areas."( GABAA receptors mediate the changes produced by stress on GABA function and locomotor activity.
Acosta, GB; Rubio, MC, 1994
)
1.01
"Bicuculline did not increase blood pressure in 6-OHDA treated rats; thus the blood-brain barrier remained intact."( Neonatal 6-hydroxydopamine treatment increases the vulnerability of the blood-brain barrier to acute hypertension in conscious rats.
Johansson, BB, 1979
)
0.98
"Bicuculline may disinhibit GABAergic efferents to the ventral pallidum resulting in a dramatic increase in glucose use within striatopallidal synaptic terminals as well as in local terminals of the pallidal projection neurons."( Patterns of glucose use after bicuculline-induced convulsions in relationship to gamma-aminobutyric acid and mu-opioid receptors in the ventral pallidum--functional markers for the ventral pallidum.
Churchill, L; Cross, RS; Heimer, L; Kalivas, PW; Nelson, SR; Pazdernik, TL; Zahm, DS, 1992
)
1.29
"Bicuculline led to an increase in the size, duration, cortical extent, and, surprisingly, the latency of the evoked responses."( Optical recordings of the cortical response to whisker stimulation before and after the addition of an epileptogenic agent.
Cohen, LB; London, JA; Wu, JY, 1989
)
1

Treatment

Treatment with bicuculline to decrease GABA(A) receptor signaling from embryonic day (E) 10 to E17 resulted in fewer cells containing immunoreactive (ir) ERalpha in the region of the PVN vs. the hypothalamus. Treatment with gabazine to enhance neuronal activity promotes recruitment of wild-type 4GII, but not the4GII S1156A mutant or 4GI.

ExcerptReferenceRelevance
"Bicuculline treatment significantly reduced demyelination extension and increased the level of MBP expression."( Inhibition of GABA A receptor improved spatial memory impairment in the local model of demyelination in rat hippocampus.
Afghani, A; Ashrafpour, M; Ashrafpour, S; Dehghan, S; Ebrahim Tabar, F; Gol, M; Mousavi Majd, A; Pourabdolhossein, F, 2018
)
1.2
"Bicuculline pretreatment blocked D-AP5-induced anxiolytic-like behaviors and contradicted its effect on avoidance memory."( The role of CA3 GABAA receptors on anxiolytic-like behaviors and avoidance memory deficit induced by NMDA receptor antagonists.
Farahizadeh, M; Nasehi, M; Zarrabian, S; Zarrindast, MR, 2016
)
1.16
"Bicuculline treatment also leads to an increase in the levels of the transcriptional repressor MeCP2, which binds to the GluR2 promoter along with the corepressors HDAC1 and mSin3A."( The Rett syndrome protein MeCP2 regulates synaptic scaling.
Ghosh, A; Lieberman, DN; Liu, XY; Qiu, Z; Sylwestrak, EL; Zhang, Y, 2012
)
1.1
"Bicuculline pretreatment reduced SKF38393- and/or progesterone-mediated increases in lordosis of E2-primed hamsters."( In the ventral tegmental area, progestins have actions at D1 receptors for lordosis of hamsters and rats that involve GABA A receptors.
Frye, CA; Petralia, SM; Walf, AA, 2006
)
1.06
"Bicuculline treatment of pentobarbital-anesthetized rats (n = 5) restores small pressor responses to subfornical organ stimulation (t test, p < 0.05), suggesting that potentiated GABA inhibition underlies this modified state under pentobarbital anesthesia."( Cardiovascular and single-unit responses to subfornical organ stimulation are abolished by pentobarbital anesthesia.
Ferguson, AV; Loucks, C, 1994
)
1.01
"In bicuculline-treated arthritic animals in which joint inflammation was minimal, concentrations of ASP and GLU did not increase above base line."( Inflammation-induced release of excitatory amino acids is prevented by spinal administration of a GABAA but not by a GABAB receptor antagonist in rats.
Sluka, KA; Westlund, KN; Willis, WD, 1994
)
0.8
"Bicuculline treatment led to a disorganized distribution of GnRH cells in the forebrain and a concomitant dissociation of GnRH cells from fibers of guidance."( Effects of gamma-aminobutyric acid(A) receptor manipulation on migrating gonadotropin-releasing hormone neurons through the entire migratory route in vivo and in vitro.
Bless, EP; Schwarting, GA; Tobet, SA; Westaway, WA, 2000
)
1.03
"Bicuculline treatment induced tonic/clonic seizures and status epilepticus in sham operated animals; these effects were drastically diminished at various time points after BCCA."( Transient reduction of cerebral blood flow leads to longlasting increase in GABA content in vulnerable structures and decreased susceptibility to bicuculline induced seizures.
Block, F; Heim, C; Sieklucka, M; Sontag, KH, 1992
)
1.21
"5. Bicuculline, and pretreatment with GABA or (+/-)-baclofen had no effect on the NANC-evoked relaxations to electrical stimulation and acetylcholine."( GABAA receptor-mediated stimulation of non-adrenergic non-cholinergic neurones in the dog ileocolonic junction.
Boeckxstaens, GE; Herman, AG; Pelckmans, PA; Rampart, M; Ruytjens, IF; Van Maercke, YM; Verbeuren, TJ, 1990
)
0.79
"Bicuculline pretreatment, however, did not alter the basal secretion of TSH in either the normal or the uremic animals, and it also did not augment the TRH-stimulated TSH response in the normal animals."( Gamma-aminobutyric acid and dysregulation of TSH secretion in uremic male rats.
Ansari, MA; Elias, AN; Iyer, K; Pandian, MR; Vaziri, ND, 1987
)
0.99
"Treatment with bicuculline, a GABAA receptor antagonist, decreased DHHC9 expression in somatostatin-positive interneurons and membrane localization of an H-Ras reporter in a manner that depended on miR-134."( MicroRNA-134 activity in somatostatin interneurons regulates H-Ras localization by repressing the palmitoylation enzyme, DHHC9.
Cambronne, XA; Chai, S; Eichhorn, SW; Goodman, RH, 2013
)
0.73
"Treatment with bicuculline normalized GABAergic tone and restored the increase in cGMP that was induced by activation of N-methyl-D-aspartate receptors and learning ability in hyperammonemic rats."( Hyperammonemia increases GABAergic tone in the cerebellum but decreases it in the rat cortex.
Agusti, A; Cauli, O; Felipo, V; Mansouri, MT, 2009
)
0.69
"Treatment with bicuculline to decrease GABA(A) receptor signaling from embryonic day (E) 10 to E17 resulted in fewer cells containing immunoreactive (ir) ERalpha in the region of the PVN vs."( Roles for gamma-aminobutyric acid in the development of the paraventricular nucleus of the hypothalamus.
McClellan, KM; Stratton, MS; Tobet, SA, 2010
)
0.7
"Treatment with bicuculline, which is an antagonist of the gamma-aminobutyric acid A (GABA(A)) receptor, increased the BOLD signal intensity in the regions that had shown decreases in the BOLD signal after the IG infusion of 10% ethanol solution, but it did not affect the BOLD signal increase in the hypothalamus."( The role of the GABAergic and dopaminergic systems in the brain response to an intragastric load of alcohol in conscious rats.
Torii, K; Tsurugizawa, T; Uematsu, A; Uneyama, H, 2010
)
0.7
"Treatment with bicuculline or gabazine to enhance neuronal activity promotes recruitment of wild-type 4GII, but not the 4GII S1156A mutant or 4GI, to the heterotrimeric eIF4F (4F) complex that assembles at the 5' cap structure (m⁷GTP) of mRNA to initiate ribosomal scanning."( Regulation of neuronal mRNA translation by CaM-kinase I phosphorylation of eIF4GII.
Edelman, AM; Fortin, DA; Kaech, S; Nygaard, S; Soderling, TR; Sonenberg, N; Srivastava, T, 2012
)
0.72
"Treatment with bicuculline and 4-aminopyridine (Bic + 4-AP), which induced burst firing, inhibited metabotropic-induced suppression of excitation (MSE) and prolonged the duration of depolarization-induced suppression of excitation (DSE)."( Epileptic stimulus increases Homer 1a expression to modulate endocannabinoid signaling in cultured hippocampal neurons.
Krogh, KA; Li, Y; Thayer, SA, 2012
)
0.72
"Pretreatment with bicuculline (3 mg/kg IP) significantly attenuated the intensity of circling behavior induced by intranigral injections of GABA or muscimol."( Circling behavior induced by intranigral injections of GABA and muscimol in rats.
Kaakkola, S; Kääriäinen, I, 1980
)
0.58
"Pretreatment with bicuculline (3 mg/kg i.p.) significantly attenuated the intensity of the circling behaviour induced by intranigral baclofen but failed to prevent it completely."( Circling behaviour induced by intranigral injection of baclofen in rats.
Kaakkola, S, 1980
)
0.58
"Pretreatment with bicuculline (3 mg/kg intraperitoneally) or strychnine (0.25 mg/kg intraperitoneally) significantly inhibited the taurine-induced circling."( Contralateral circling behaviour induced by intranigral injection of taurine in rats.
Kaakkola, S; Kääriäinen, I, 1980
)
0.58
"Pretreatment with bicuculline (0.3 mg/kg, i.v.), a GABA antagonist, or semicarbazide (200 mg/kg, i.v.), an inhibitor of GABA synthesis, accelerated the recovery of PSR potentials after the removal of the arterial occlusion."( Effects of GABAergic drugs on the recovery of reflex potentials after spinal cord ischemia in cats.
Moriya, H; Murayama, S; Nakaya, H; Nemoto, T; Okamoto, Y; Sekikawa, T; Suzuki, T, 1995
)
0.61
"Pretreatment with bicuculline (30 micrograms kg-1; i.p.), a GABAA antagonist, but not phaclofen (1 mg kg-1) a GABAB antagonist, reversed the effect of valproate and increased c-fos positive cells within lamina I, IIo."( Attenuation by valproate of c-fos immunoreactivity in trigeminal nucleus caudalis induced by intracisternal capsaicin.
Ayata, G; Cutrer, FM; Limmroth, V; Moskowitz, MA, 1995
)
0.61
"Pretreatment with bicuculline and flumazenil were effective in ameliorating the memory deficits caused by diazepam, and consolidated memory function in saline-treated controls following strong and weak aversant training."( The role of the benzodiazepine-GABA system in the memory processes of the day-old chick.
Crowe, SF; Farkas, L, 2000
)
0.63
"Pretreatment with bicuculline at 0.5, 1, and 2.5 pmol reduced the sedative action of GABA on locomotor activity by 10, 20, and 41%, respectively."( Nitrogen at raised pressure interacts with the GABA(A) receptor to produce its narcotic pharmacological effect in the rat.
Abraini, JH; Balon, N; David, HN; Rostain, JC, 2001
)
0.63
"Pretreatment with bicuculline (GABAA antagonist) turned them to relaxation."( gamma-Aminobutyric acid enhances the tone of human internal anal sphincter.
Fujita, S; Kusunoki, M; Sakanoue, Y; Shoji, Y; Utsunomiya, J; Yamamura, T; Yanagi, H, 1991
)
0.6
"Pretreatment with bicuculline (68 pmol) blocked the suppressive effects of muscimol (12 pmol) upon affective defense behavior."( GABA-mediated regulation of feline aggression elicited from midbrain periaqueductal gray.
Shaikh, MB; Siegel, A, 1990
)
0.6
"Pretreatment with bicuculline, a GABAA-receptor antagonist, in the doses of 1 and 3 mg/kg, subcutaneously, had no influence on the gastric acid response to baclofen."( Effects of GABA antagonists and structural GABA analogues on baclofen stimulated gastric acid secretion in the rat.
Goto, Y; Hara, N; Hara, Y, 1990
)
0.6
"Treatment with bicuculline or picrotoxin results in depression of biphasic GABA responses that appears selective for the depolarizing portion of the potential."( In vitro studies of the role of gamma-aminobutyric acid in inhibition in the lateral septum of the rat.
Gallagher, JP; Shinnick-Gallagher, P; Stevens, DR, 1987
)
0.61

Toxicity

ExcerptReferenceRelevance
" PRM is a relatively nontoxic anticonvulsant with a different action than PB, and PEMA is both a weak and a relatively toxic anticonvulsant."( Primidone, phenobarbital, and PEMA: I. Seizure protection, neurotoxicity, and therapeutic index of individual compounds in mice.
Bourgeois, BF; Dodson, WE; Ferrendelli, JA, 1983
)
0.27
" From these observations, it is proposed that intrinsic functional inhibition in hippocampal circuits can reduce adverse effects of Abeta on the excitatory component."( Inhibitory neuronal activity can compensate for adverse effects of beta-amyloid in hippocampal neurons.
Graf, RA; Kater, SB, 1998
)
0.3
" The toxic effect of gamma-vinyl-GABA was mimicked by a 24-h treatment with GABA (100 microM) and the GABA(A) receptor agonist, muscimol (10 microM), but not the GABA(B) receptor agonist, baclofen (10 microM)."( GABA(A)-mediated toxicity of hippocampal neurons in vitro.
Lukasiuk, K; Pitkänen, A, 2000
)
0.31
"Neurotoxicity is the dose-limiting side-effect of vincristine in cancer therapy."( Effect of thiopental, propofol, and etomidate on vincristine toxicity in PC12 cells.
Chen, JT; Cheng, JT; Chou, AK; Lee, TC; Lin, CR; Lin, FC; Yang, LC, 2002
)
0.31
"Lethal intestinal tissue toxicity is a common side effect and a dose-limiting factor in chemoradiotherapy."( Inhibition of GABAA receptors in intestinal stem cells prevents chemoradiotherapy-induced intestinal toxicity.
Chen, D; Guo, W; Hu, H; Jiang, W; Li, J; Li, Y; Liu, H; Mu, K; Ning, N; Yu, X; Zhang, C; Zheng, J; Zhou, Y, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" The method was successfully applied to the pharmacokinetic study after gavage administration of 15mg/kg bicuculline in rats."( Determination of bicuculline in rat plasma by liquid chromatography mass spectrometry and its application in a pharmacokinetic study.
Lin, C; Ma, J; Wang, X; Wen, C; Xiang, Z; Yang, X, 2014
)
0.96

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of enoxacin, a new quinolone antibacterial agent, and its combination with 4-biphenylacetate (BPA), an active metabolite of the non-steroidal antiinflammatory agent fenbufen, were examined on population spikes induced by electrical stimulation of the stratum radiatum in the CA1 pyramidal cell layer in rat hippocampal slices."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
" The anxiolytic effect of dibunol alone and combined with phenazepam is attended by a decrease in the content of malonic dialdehyde in rat blood and brain, evidence of the reduction of the lipid peroxidation intensity."( [Effect of the antioxidant dibunol and its combination with phenazepam on the behavior of rats in a conflict situation].
Molodavkin, GM; Poiurovskiĭ, MV, 1985
)
0.27

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The actions of Sl 75 102 were in nearly all respects identical to those of GABA. parameters examined were the effects on membrane potential and input conductance, desensitization, dose-response characteristics and sensitivity to the GABA antagonists. Neither bicuculline nor strychnine antagonized the taurine effect, as revealed by absence.

ExcerptRelevanceReference
"3 PB, tested at concentrations up to 80 muM, produced variable effects on the dose-response curve to GABA."( Reversal of the action of amino acid antagonists by barbiturates and other hypnotic drugs.
Bowery, NG; Dray, A, 1978
)
0.26
" Their actions were transient and were 'occluded' by GABA; also the dose-response curve in each case was parallel to that of GABA."( A comparison of gamma-aminobutyric acid and the semi-rigid analogues 4-aminotetrolic acid, 4-aminocrotonic acid and imidazole-4-acetic acid on the isolated superior cervical ganglion of the rat.
Bowery, NG; Jones, GP, 1976
)
0.26
" Neither bicuculline nor strychnine antagonized the taurine effect, as revealed by absence of a shift to right, a change in slope or in the taurine IC50 value in the dose-response curve."( Taurine induces bicuculline/strychnine-insensitive dose-dependent inhibition of cortical visual evoked responses.
Cañas, P; Hernández, A; Pérez, H,
)
0.89
" In the present study, we determined, in rat pups, the effect of nigral infusions of gamma-vinyl-GABA (GVG) on clonic-tonic seizures induced by flurothyl, generated a dose-response curve of the GVG effect and investigated the possible role of the nigral GABAA receptor in mediating the GVG effect."( Is the anticonvulsant effect of substantia nigra infusion of gamma-vinyl-GABA (GVG) mediated by the GABAA receptor in rat pups?
Moshé, SL; Sperber, EF; Xu, SG, 1991
)
0.28
" 4-PIOL antagonized the response to isoguvacine with a parallel shift to the right of the dose-response curve."( Electrophysiological studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones.
Falch, E; Kristiansen, U; Krogsgaard-Larsen, P; Lambert, JD, 1991
)
0.28
"In order to test the GABA hypothesis of kindling, GABA-complex antagonists were administered in a dose-response paradigm to rats that had been implanted with indwelling forebrain electrodes, but not kindled."( Secondary generalization in non-kindled rats following acute administration of GABA-complex and adenosine antagonists.
Burnham, WM; Mingo, NS, 1990
)
0.28
" The dose-response relationships showed that the effect of enoxacin was 100 times potentiated in the presence of BPA (10(-5) M)."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
" The dose-response curve with the dissociation constant 2 x 10(-3) mol/l was obtained."( [Taurine-activated currents in isolated neurons of the rat cerebellum].
Dashkin, AN; Garashchuk, OA; Valeev, AE, 1990
)
0.28
" The dose-response curve of R-(--)-baclofen for its inhibitory effect on the electrically-induced vasopressor response was shifted to the right by the GABAB-receptor antagonist 2-hydroxysaclofen, but was not affected by the GABAA-receptor antagonist bicuculline."( GABAB receptor-mediated inhibition of the neurogenic vasopressor response in the pithed rat.
Kohlenbach, A; Schlicker, E, 1990
)
0.46
" Flumazenil (Ro 15-1788) administration caused a parallel shift to the right of the dose-response curve for midazolam spinal analgesia."( On the mechanism by which midazolam causes spinally mediated analgesia.
Edwards, M; Gent, JP; Goodchild, CS; Serrao, JM, 1990
)
0.28
" The inhibitory effect of GABA was mimicked by the type B GABA agonist baclofen, displaying a similar dose-response relationship as GABA."( Presynaptic effects of gamma-aminobutyric acid on norepinephrine release and uptake in rat pineal gland.
Cardinali, DP; Chuluyan, HE; Rosenstein, RE, 1990
)
0.28
" Dose-response curves generated during acoustic stimulation by varying GABA ejection current were sigmoidal at all ages studied, and the range of slopes relating discharge rate to applied currents increased during the first 10 postnatal days."( GABA actions within the caudal cochlear nucleus of developing kittens.
Fitzakerley, JL; McGee, J; Walsh, EJ, 1990
)
0.28
" The dose-response relationship followed simple Michaelis-Menten kinetics, with a half-maximal response elicited at approximately 110 microM."( Effects of gamma-aminobutyric acid on skate retinal horizontal cells: evidence for an electrogenic uptake mechanism.
Malchow, RP; Ripps, H, 1990
)
0.28
" Dose-response curves were shifted to the right in a parallel fashion."( Electrophysiological study of SR 42641, a novel aminopyridazine derivative of GABA: antagonist properties and receptor selectivity of GABAA versus GABAB responses.
Desarmenien, M; Desaulles, E; Feltz, P; Hamann, M, 1987
)
0.27
" Hill coefficients, determined from dose-response data, indicated that binding of at least two GABA molecules was required to activate the chloride channel."( GABA receptors on the cell-body membrane of an identified insect motor neuron.
David, JA; Pinnock, RD; Sattelle, DB; Wafford, KA, 1988
)
0.27
"Using isolated, internally perfused bullfrog dorsal root ganglion cells we have studied the dose-response curves for gamma-aminobutyric acid (GABA) in the presence of internally or externally applied GABA antagonists."( Bicuculline and picrotoxin block gamma-aminobutyric acid-gated Cl- conductance by different mechanisms.
Akaike, N; Carpenter, DO; Hattori, K; Oomura, Y, 1985
)
1.71
" Bicuculline 1 microM shifted the dose-response curve of GABA to the right and the excitatory effect was also enhanced."( Excitatory and inhibitory action of GABA on synaptic transmission in slices of guinea pig superior colliculus.
Arakawa, T; Okada, Y, 1988
)
1.19
" The effect of GABA was mimicked by (-)-baclofen, which gave a dose-response curve overlapping that of GABA, while (+)-baclofen was about one hundred times less potent."( Modulatory activity of GABAB receptors on cholinergic tone in guinea-pig distal colon.
Giotti, A; Luzzi, S; Maggi, CA; Spagnesi, S; Zilletti, L, 1985
)
0.27
" These advantages are: the composition of fluids supplying the preparation is under control; the oxygen supply to the cord is no longer dependent on the cardiovascular function, which may be impaired by the substance under study; a complete dose-response curve may be obtained from each animal; washout experiments may be performed; the action of substances can be studied in the presence of extreme concentrations of drugs, ions, etc."( The in situ perfused spinal cord of the rat. Applicability of drugs and chemicals, sodium-lithium exchange, and calcium reduction to functional intact central nervous system tissue.
Deutschmann, W; Wellhöner, HH, 1986
)
0.27
" Dose-response and time course studies of Ro 15-4513 against gamma-aminobutyric acid (GABA) antagonists were performed."( Interactions of the imidazodiazepine Ro 15-4513 with chemical convulsants.
Lister, RG; Nutt, DJ, 1988
)
0.27
"835 and a parallel shift of the probit-log dosage regression line to the right."( Delta-aminovaleric acid antagonizes the pharmacological actions of baclofen in the central nervous system.
Klockgether, T; Schwarz, M; Sontag, KH; Turski, L; Wüllner, U, 1988
)
0.27
" Prednisolone shifted the dose-response curve of the GABA current downward."( Voltage-clamp studies of the inhibition of gamma-aminobutyric acid response by glucocorticoids in bullfrog primary afferent neurons.
Akasu, T; Ariyoshi, M, 1987
)
0.27
" Muscimol (2 mg/kg) and THIP (5 and 10 mg/kg) exerted the antiimmobility effect even after single dosing 1 h before the test."( Effect of GABAergic drugs in the behavioral 'despair' test in rats.
Borsini, F; Evangelista, S; Meli, A, 1986
)
0.27
" PB shifted the dose-response curve for GABA in the presence of bicuculline methochloride to the left without altering the slope or the dose ratio, and not only displaced the dose-response curve for GABA in the presence of picrotoxinin but also restored the slope and the maximum response towards that of the control GABA-induced response."( Potentiation of GABAA-receptor-mediated responses by barbiturates in the guinea-pig ileum.
Kerr, DI; Ong, J, 1984
)
0.51
" 5 Methohexitone and thiopentone produced a biphasic dose-response on the K+-stimulated release of both amino acids; low concentrations enhanced release, high concentrations depressed release."( The effects of anaesthetics on the uptake and release of amino acid neurotransmitters in thalamic slices.
Kendall, TJ; Minchin, MC, 1982
)
0.26
" It means that over this dosage range haloperidol potentiates GABA-induced effects."( [Participation of GABA-ergic structures in producing the effects of haloperidol].
Molodavkin, GM; Ostrovskaia, RU, 1980
)
0.26
" The log dose-response curves for GABA and muscimol appeared to be parallel, but were not parallel to that for dopamine."( GABA and muscimol inhibit the release of prolactin from dispersed rat anterior pituitary cells.
Besser, GM; Delitala, G; Grossman, A; Yeo, T, 1981
)
0.26
" For MES testing, mice were injected with either reserpine, yohimbine, propranolol, haloperidol or metergoline prior to dosing with TET."( Pharmacological and biochemical evaluation of triethyltin's anticonvulsant effects.
Fox, DA,
)
0.13
" GABA dose-response curves were obtained for SC neurons by pressure applying known concentrations of GABA from micropipettes with large tips (miniperfusion pipettes)."( GABA and bicuculline actions on mouse spinal cord and cortical neurons in cell culture.
Macdonald, RL; Nowak, LM; Young, AB, 1982
)
0.68
" Dose-response curves show that EDA differs from GABA with respect to both potency and efficacy."( Ethylenediamine and GABA potentiation of [3H]diazepam binding to benzodiazepine receptors in rat cerebral cortex.
Morgan, PF; Stone, TW, 1982
)
0.26
" In animals implanted with chronically indwelling cannulae, a muscimol (25-400 ng) dose-response analysis confirmed the greater sensitivity of the MR site."( Intra-raphe muscimol induced hyperactivity depends on ascending serotonin projections.
Lorens, SA; Sainati, SM, 1982
)
0.26
" Limiting the opportunity to gnaw on inanimate objects shifted the dose-response curve for muscimol-induced self-injurious behavior (SIB) to the left and increased the maximum incidence of SIB."( Self-injurious behavior in rats produced by intranigral microinjection of GABA agonists.
Baumeister, AA; Frye, GD, 1984
)
0.27
" Amphetamine induces a dose-response partial reversal of the GBL effect."( gamma-Butyrolactone effects on behavior induced by dopamine agonists.
Dougherty, GG; Ellinwood, EH; Gonzalez, AE, 1983
)
0.27
" In contrast, neither the dose-response nor the time course of TMT-induced hypothermia were affected by any of the drugs tested."( Antinociceptive and hypothermic effects of trimethyltin.
Costa, LG; Doctor, SV; Murphy, SD, 1982
)
0.26
" Anisatin shifted the dose-response curve for GABA-induced depolarization in the primary afferent terminal to the right and also reduced the maximum response to GABA."( Anisatin, a potent GABA antagonist, isolated from Illicium anisatum.
Kudo, Y; Oka, JI; Yamada, K, 1981
)
0.26
" When applied topically to cortex, muscimol blocks focal penicillin, bicuculline, and picrotoxin discharges in a dose-response relationship."( Anticonvulsant effects of muscimol.
Collins, RC, 1980
)
0.5
"Experiments on isolated mice (CC57W males) have demonstrated that GABA antagonists (bicuculline, picrotoxin, thiosemicarbazide) increase the desocializing effects of isolation (enhance aggression and reduce intraspecies sociability), while GABA-positive drugs (muscimol, gamma-acetylenic GABA) within a certain dosage range diminish aggression and favour a temporary recovery of sociability."( [GABA-ergic correlates of aggression and intraspecies sociability of mice subjected to isolation].
Poshivalov, VP, 1981
)
0.49
" 3 The actions of Sl 75 102 were in nearly all respects identical to those of GABA; parameters examined were the effects on membrane potential and input conductance, desensitization, dose-response characteristics and sensitivity to the GABA antagonists, bicuculline and picrotoxin."( SL 75 102 as a gama-aminobutyric acid agonist: experiments on dorsal root ganglion neurones in vitro.
Desarmenien, M; Feltz, P; Headley, PM; Santangelo, F, 1981
)
0.44
" This anti-MES activity is achieved with nontoxic doses, with the optimal effect recorded in rats dosed orally with anti-MES ED50 and protective index (PI) values of 25."( Comparative anticonvulsant activity and neurotoxicity of 4-amino-N-(2,6-dimethylphenyl)phthalimide and prototype antiepileptic drugs in mice and rats.
Bailleux, V; Hamoir, G; Nuyts, JP; Poupaert, JH; Stables, JP; Vallée, L; Vamecq, J, 1995
)
0.29
" Morphine, pethidine and fentanyl, which showed a biphasic dose-response relationship with respect to seizure modulation, abolished the anticonvulsant activity of propofol to exhibit their own intrinsic activity in proconvulsant doses."( Interactions between opioid drugs and propofol in laboratory models of seizures.
Ahmad, I; Pleuvry, BJ, 1995
)
0.29
" Repeated treatment with diazepam produced tolerance to its anticonvulsant activities as indicated by shifts of the dose-response curves by a factor of 3-5."( Repeated treatment with alpidem, a new anxiolytic, does not induce tolerance or physical dependence.
Morel, E; Perrault, G; Sanger, DJ; Zivkovic, B, 1993
)
0.29
" Diazepam shifted the dose-response curve for muscimol-stimulated flux to about 4-fold lower concentrations without affecting the maximum response."( Reconstitution of purified GABAA receptors: ligand binding and chloride transporting properties.
Dunn, SM; Thuynsma, RP, 1994
)
0.29
" Thus, bicuculline not only produced a rightward shift of the dose-response curves of the central depressant drugs in the cortex, but also increased the maximal stimulation of 35S-TBPS binding."( Bicuculline-produced regional differences in the modulation of 35S-TBPS binding by GABA, pentobarbital and diazepam in mouse cerebellum and cortex.
Liljequist, S; Tabakoff, B, 1993
)
2.18
" These two current components have different dose-response characteristics for GABA, with the nondesensitizing component being activated more effectively and reaching its peak amplitude at lower agonist concentrations than the desensitizing one."( GABA responses and their partial occlusion by glycine in cultured rat medullary neurons.
Faber, DS; Lewis, CA, 1993
)
0.29
"4 nmol) of bicuculline produced dose-response relationships simply without any reversal effect."( Heterogeneous characteristics of mitral cells in the rat olfactory bulb.
Kaba, H; Saito, H; Seto, K; Yu, GZ, 1993
)
0.68
" Dose-response curves yielded an EC50 of about 50 microM."( Patch-clamp analysis of glycine-induced currents in chick ciliary ganglion neurons.
Berg, DK; Zhang, ZW, 1995
)
0.29
" The idazoxan dose-response curve for this suppression of fentanyl antinociception assessed with tail flick latency was the same as that for suppression of xylazine."( Antinociceptive actions of intrathecal xylazine: interactions with spinal cord opioid pathways.
Davies, A; Gent, JP; Goodchild, CS; Guo, Z, 1996
)
0.29
" The results indicate that bicuculline (GABA antagonist), SKF38393 (DA agonist), and ST587 (NE agonist) facilitated retention with little change in the dose-response curves for P8 mice 4, 8, and 12 months of age."( Age-related changes in hippocampal drug facilitation of memory processing in SAMP8 mice.
Flood, JF; Harris, FJ; Morley, JE,
)
0.43
" In bicuculline, the dose-response curve for GABA was fitted with a sigmoidal curve with an EC50 value of 209 microM."( Functionally distinct chloride-mediated GABA responses in rat cerebellar granule cells cultured in a low-potassium medium.
Cherubini, E; Martina, M; Virginio, C, 1997
)
0.86
" Evoked inhibitory postsynaptic currents (IPSCs) were decreased by kainate by up to 90%, showing a bell-shaped dose-response curve similar to that of native kainate-selective receptors."( Kainate receptors presynaptically downregulate GABAergic inhibition in the rat hippocampus.
Herreras, O; Lerma, J; Rodríguez-Moreno, A, 1997
)
0.3
", with a U-shape dose-response relationship."( Inhibition by levetiracetam of a non-GABAA receptor-associated epileptiform effect of bicuculline in rat hippocampus.
Margineanu, DG; Wülfert, E, 1997
)
0.52
" Thus, from the present study it may be concluded that: (a) caffeine-induced stimulation of LA is dependent on dose and duration of caffeine treatment, (b) development of tolerance to caffeine is dependent on the dosage of caffeine, and (c) the reduction of central GABAergic activity in the caffeine-nontolerant condition pushed up and restored the LA to the control level on the development of tolerance to caffeine."( Is GABA involved in the development of caffeine tolerance?
Mukhopadhyay, S; Poddar, MK, 1998
)
0.3
" Sigmoid dose-response curves were plotted, and the IC50s were calculated."( Comparison of the effects of M1 and M2 muscarinic receptor activation in the absence of GABAergic inhibition in immature rat hippocampal CA3 area.
Beaucher, J; Harnois, C; Psarropoulou, C, 1998
)
0.3
" The dose-response relationship pooled from nine progenitor cells was best fit by a logistic function of EC50=113 microM and Hill coefficient=0."( Properties of GABA(A) receptors in cultured rat oligodendrocyte progenitor cells.
Grant, AL; Mellor, JR; Randall, AD; Williamson, AV, 1998
)
0.3
" Muscarine shifted the GABA dose-response curve to the left, with the GABA EC50 decreased from 45 +/- 2 to 13 +/- 2 microM."( Enhancement of GABA-activated current by muscarine in rat dorsal root ganglion neurons.
Hu, HZ; Li, ZW; Shao, M, 1999
)
0.3
" In fact it showed: (1) very sensitive dose-response not affected by TTX in the bath; (2) an equilibrium potential compatible with Cl-channel conductance; (3) a massive reduction with the competitive GABA(A) antagonist bicuculline; (4) a small reduction, if any, with the potent competitive GABA(B) antagonist CGP55845A; (5) persistence of the responses under 4-AP (4-aminopyridine), the potassium channel blocker, and inhibition of the 4-AP-induced calcium bursts of spikes."( Purkinje cell inhibitory responses to 3-APPA (3-aminopropylphosphinic acid) in RAT cerebellar slices.
Batini, C; Vigot, R, 1999
)
0.49
" We investigated the dose-response relationship for each alcohol and determined that the order of potency was methanol < EtOH << octanol, with EC(50) values of 291 mM, 39."( Effect of ethanol upon respiratory-related hypoglossal nerve output of neonatal rat brain stem slices.
Berger, AJ; Gibson, IC, 2000
)
0.31
" increased the percentage of loss of the righting reflex in a dose-dependent manner with an ED50 value of 140 (95% confidence limits 123-160) mg kg-1 (n = 40; eight animals per dose, five doses per dose-response curve)."( Propofol anaesthesia in mice is potentiated by muscimol and reversed by bicuculline.
Dohi, T; Irifune, M; Kawahara, M; Maeoka, K; Nishikawa, T; Shimizu, Y; Sugimura, M; Takarada, T, 1999
)
0.54
" The excitatory effects of L-Glu and BIC and the inhibitory effects of GABA showed a dose-response relationship."( [Effects of L-glutamic acid, gamma-aminobutyric acid and their respective antagonists on spontaneous discharge of nucleus paragigantocellularis lateralis neurons in rats].
Li, L; Xu, M; Zheng, Y, 1997
)
0.3
" The area under the field potentials was reduced only at a dosage of 60micromol/l (n=11)."( Effects of nifedipine on rhythmic synchronous activity of human neocortical slices.
Ebner, A; Höhling, JM; Köhling, R; Lücke, A; Oppel, F; Pannek, H; Speckmann, EJ; Straub, H; Tuxhorn, I; Wolf, P, 2000
)
0.31
" Muscimol increased responsiveness to formalin and reduced the slope of the formalin dose-response relation."( GABAergic modulation of descending inhibitory systems from the rostral ventromedial medulla (RVM). Dose-response analysis of nociception and neurological deficits.
Franklin, KB; Gilbert, AK, 2001
)
0.31
"4 microg) dose-response curves confirmed a supra-additive interaction between BIC and STR in this model."( Coadministration of intrathecal strychnine and bicuculline effects synergistic allodynia in the rat: an isobolographic analysis.
Hefferan, MP; Khandwala, H; Loomis, CW; Osmond, G, 2001
)
0.57
" BK shifted the GABA dose-response curve downward obviously and depressed the maximal response to GABA by 1/3 or more while the Kd value was unchanged."( [Inhibition of GABA-activated currents in isolated rat DRG neurons by bradykinin].
Li, ZW; Lu, CY; Si, JQ, 1998
)
0.3
" Parallel dose-response curves suggest that TMPP acts by a competitive antagonism of GABA inhibition, and are consistent with reported patch-clamp analysis of TMPP-induced reduction of inhibitory postsynaptic current amplitudes."( Characterization of acute neurotoxic effects of trimethylolpropane phosphate via neuronal network biosensors.
Gramowski, A; Gross, GW; Keefer, EW; Pancrazio, JJ; Stenger, DA, 2001
)
0.31
" In a separate series of in vivo electrophysiological experiments, administration of the same dosage of the taurine antagonist into the supraoptic nucleus via microdialysis resulted in an increased electrical activity of identified vasopressinergic, but not oxytocinergic, neurons."( Taurine selectively modulates the secretory activity of vasopressin neurons in conscious rats.
Ebner, K; Engelmann, M; Landgraf, R; Lubec, G; Ludwig, M; Sabatier, N; Singewald, N; Wotjak, CT, 2001
)
0.31
" VS-3 neuron GABA receptors were activated by muscimol and inhibited by picrotoxin but not bicuculline, and their dose-response relationship had an EC(50) of 103."( Peripheral GABAergic inhibition of spider mechanosensory afferents.
French, AS; Panek, I; Sekizawa, S; Seyfarth, EA; Torkkeli, PH, 2002
)
0.54
" In Experiment 4, a high dosage of 5alpha-dihydrotestosterone was more anxiolytic than a high dosage of estradiol benzoate, suggesting that testosterone action may require 5alpha-reduction."( Testosterone rapidly reduces anxiety in male house mice (Mus musculus).
Aikey, JL; Anmuth, DM; James, PJ; Nyby, JG, 2002
)
0.31
" In contrast, in human neocortical preparations obtained from epilepsy surgery, in approximately 20% of the slices spontaneous epileptiform activity appeared with this bicuculline dosage without SDs."( Differential sensitivity to induction of spreading depression by partial disinhibition in chronically epileptic human and rat as compared to native rat neocortical tissue.
Hagemann, G; Koch, UR; Köhling, R; Redecker, C; Speckmann, EJ; Straub, H, 2003
)
0.51
" Using a dose-response model, we evaluated the effectiveness of adenosine application for focal seizure prophylaxis in 12 rats."( Focally injected adenosine prevents seizures in the rat.
Anschel, DJ; Fisher, RS; Kraus, AC; Ortega, EL, 2004
)
0.32
" AMI-193, a 5-HT(2A) antagonist (10(-10) to 10(-5) M), reduced GABA release in a dose-response manner, while it induced an increase of 5-HT outflow."( A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone.
Garrone, B; Luparini, MR; Pazzagli, M; Pepeu, G; Pinza, M, 2004
)
0.32
" Confirmation that different levels of GABA affect different receptor subtypes was demonstrated by the shift in the GABA dose-response curves to the selective antagonists."( Opposing roles for GABAA and GABAC receptors in short-term memory formation in young chicks.
Gibbs, ME; Johnston, GA, 2005
)
0.33
" Dose-response analysis of the antagonistic effect of the TRPV1 receptor antagonist, capsazepine administered peripherally, shows that the capsaicin-evoked inflammation was inhibited in a dose-dependent manner, and nearly completely abolished by capsazepine at doses between 30-150 mug."( Roles of TRPV1 and neuropeptidergic receptors in dorsal root reflex-mediated neurogenic inflammation induced by intradermal injection of capsaicin.
Fang, L; Li, D; Lin, Q; Xu, X; Zou, X, 2007
)
0.34
" Sleep EEG studies demonstrated lack of tolerance and withdrawal effects after 28 daily doses with gaboxadol, whereas zolpidem produced both tolerance and withdrawal effects under a similar dosing regimen."( Gaboxadol -- a different hypnotic profile with no tolerance to sleep EEG and sedative effects after repeated daily dosing.
Anderson, NJ; Cremers, TI; Ebert, B; Fahey, JM; Rasmussen, S; Sánchez, C; Vogel, V, 2008
)
0.35
" Microinjection of dynamin-DN and ConA also decreased the antinociceptive potency of the unlabeled opioid agonist dermorphin when microinjected into the vlPAG as demonstrated by rightward shifts in the dose-response curves."( Opioid receptor internalization contributes to dermorphin-mediated antinociception.
Aicher, SA; Arttamangkul, S; Bobeck, EN; Hegarty, DM; Ingram, SL; Macey, TA; Morgan, MM, 2010
)
0.36
"Overdose of γ-hydroxybutyrate (GHB) frequently causes respiratory depression, occasionally resulting in death; however, little is known about the dose-response relationship or effects of potential overdose treatment strategies on GHB-induced respiratory depression."( γ-Hydroxybutyrate (GHB)-induced respiratory depression: combined receptor-transporter inhibition therapy for treatment in GHB overdose.
Morris, ME; Morse, BL; Vijay, N, 2012
)
0.38
" The doses of modulators were selected on the basis of dose-response studies."( Effects of agomelatine in a murine model of obsessive-compulsive disorder: interaction with meta-chlorophenylpiperazine, bicuculline, and diazepam.
Bhutada, P; Deshmukh, P; Dixit, P; Kaulaskar, S; Thakur, K, 2013
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
agrochemicalAn agrochemical is a substance that is used in agriculture or horticulture.
central nervous system stimulantAny drug that enhances the activity of the central nervous system.
GABA-gated chloride channel antagonistnull
neurotoxinA poison that interferes with the functions of the nervous system.
GABAA receptor antagonistnull
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
isoquinoline alkaloidAny alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine.
isoquinolinesA class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
benzylisoquinoline alkaloidAny isoquinoline alkaloid based on a benzylisoquinoline skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.79460.100020.879379.4328AID588453
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency25.11890.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
importin subunit beta-1 isoform 1Homo sapiens (human)Potency70.79465.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency70.79465.804836.130665.1308AID540263
gemininHomo sapiens (human)Potency2.31090.004611.374133.4983AID624296
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)15.00000.00011.14948.0000AID72298
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50 (µMol)15.00000.00011.03936.0000AID72298
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)15.00000.00011.29158.0000AID72298
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50 (µMol)15.00000.00011.30188.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50 (µMol)15.00000.00010.98006.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)15.00000.00011.19936.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)15.00000.00010.93746.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)15.00000.00011.01936.0000AID72298
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50 (µMol)15.00000.00011.02016.0000AID72298
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
chloride transmembrane transportGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
monoatomic ion transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to toxic substanceGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
central nervous system neuron developmentGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to progesteroneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ovulation cycleGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
roof of mouth developmentGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
behavioral fear responseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
associative learningGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
negative regulation of chloride transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
response to xenobiotic stimulusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neurotransmitter transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
GABA-A receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signaling receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane signaling receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter transmembrane transporter activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
apical plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
axonGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
nuclear envelopeGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
presynaptic active zone membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
nucleoplasmGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cytosolGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuronal cell body membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
cerebellar Golgi cell to granule cell synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
nucleolusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
microtubule cytoskeletonGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1224817Assays to identify small molecules inhibitory for eIF4E expression2015Chemistry & biology, Jul-23, Volume: 22, Issue:7
Internal Ribosome Entry Site-Based Bicistronic In Situ Reporter Assays for Discovery of Transcription-Targeted Lead Compounds.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID385598Activity of human GABA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as induction of ethanol induced GABA current2007The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
AID1576638Antagonist activity at GABAA receptor in electrically stimulated Sprague-Dawley rat dentate gyrus hippocampal granule neurons assessed as reduction in GABA induced IPSC at 20 uM at holding potential of -65 mV by whole-cell patch-clamp method2019Journal of natural products, 05-24, Volume: 82, Issue:5
Ferulic Acid Esters and Withanolides: In Search of Withania somnifera GABA
AID72298Displacement of [3H]GABA from gamma-aminobutyric-acid A (GABA-A) receptor1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Structure and molecular modeling of GABAA receptor antagonists.
AID71674In vitro displacement of [35S]TBPS from Gamma-aminobutyric acid A receptor of rat brain membrane preparations at 100 uM2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID72155Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
AID71427Percent displacement of [3H]GABA at Gamma-aminobutyric acid receptor in rat brain membranes at 0.01 uM1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
(+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID72724Percent GABA current elicited in Xenopus laevis oocytes expressing rat GABA-A alpha-1-beta-2-gamma-2 subunits at 100 uM [(-)inhibition, (+)stimulation]2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor.
AID72153Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
AID71681In vitro displacement of [3H]muscimol from Gamma-aminobutyric acid A receptor of rat brain membrane preparations at 10 uM2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID385597Activity of human GABA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as inhibition of ethanol induced GABA current at 30 uM2007The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
AID71679Displacement of [3H]flunitrazepam from GABA-A receptor of rat brain membrane preparations at 100 uM2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor.
AID71571Relative binding affinity for sodium-independent Gamma-aminobutyric acid receptor synaptic membrane binding site in rat brain tissue1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
(+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid.
AID385599Activity of human GABA alpha-1-beta-2-gamma-2L S327A mutant in HEK293 cells expressing as-PKCepsilon assessed as inhibition of ethanol induced GABA current at 30 uM2007The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
AID496866Anticonvulsant activity in po dosed mouse assessed as inhibition of MES-induced tonic seizures2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346449Human KCa2.1 (Calcium- and sodium-activated potassium channels)2000British journal of pharmacology, Mar, Volume: 129, Issue:5
Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
AID1346438Rat KCa2.2 (Calcium- and sodium-activated potassium channels)2000British journal of pharmacology, Mar, Volume: 129, Issue:5
Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,041)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901588 (26.29)18.7374
1990's1847 (30.57)18.2507
2000's1705 (28.22)29.6817
2010's816 (13.51)24.3611
2020's85 (1.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.37

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index52.37 (24.57)
Research Supply Index8.74 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index91.77 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (52.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (0.05%)5.53%
Reviews65 (1.04%)6.00%
Case Studies1 (0.02%)4.05%
Observational0 (0.00%)0.25%
Other6,184 (98.90%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]