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gamma-aminobutyric acid

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Description

gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4. [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]

Cross-References

ID SourceID
PubMed CID119
CHEMBL ID96
CHEBI ID16865
SCHEMBL ID4878
MeSH IDM0008927

Synonyms (246)

Synonym
gamma-amino butyric acid
gtpl1067
CHEBI:16865 ,
smr000058285
gamma-aminobutanoic acid
gamma-aminobuttersaeure
MLS000028505 ,
gamma aminobutyric acid
4abu ,
omega-aminobutyric acid
NSC51295 ,
nsc-51295
NSC45460 ,
nsc-45460
.gamma.-aminobutanoic acid
piperidinic acid
NSC27418 ,
piperidic acid
butyric acid, 4-amino-
aminalon
gammasol
mielomade
gammar
wln: z3vq
gammalone
mielogen
chemical name: .gamma.-aminobutanoic acid
gamarex
nsc-27418
nsc-32044
gaballon
.gamma.-aminobutyric acid
NSC32044 ,
gammalon
KBIO1_000616
DIVK1C_000616
acide amino-4- butyrique [french]
gammagee
gamastan
einecs 200-258-6
gamma-aminobuttersaeure [german]
nsc 27418
gamulin
gamma-aminobutyric acid [jan]
SGCUT00121
a-aminobutyric acid
EU-0100005
gamma-aminobutyric acid, >=99%
D00058
gammalon (tn)
gamma-aminobutyric acid (jan)
SPECTRUM_000049
SPECTRUM5_001425
lopac-a-2129
NCGC00015043-01
tocris-0344
NCGC00024546-01
4-amino-butanoic acid
LMFA01100039
PDSP2_001259
cid_119
4 aminobutyric acid
[3h]gaba
aminalone
4-amino-n-[2,3-3h]butyric acid
chembl96 ,
4 aminobutanoic acid
bdbm24183
IDI1_000616
BIOMOL-NT_000230
LOPAC0_000005
OPREA1_584567
BSPBIO_002970
PDSP1_001275
butanoic acid,4-amino 4-amino,butyric acid
butanoic acid, 4-amino-
inchi=1/c4h9no2/c5-3-1-2-4(6)7/h1-3,5h2,(h,6,7
epa pesticide chemical code 030802
reanal
immu-g
3-carboxypropylamine
gamma-aminobutryic acid
butanoic acid, 4-amino- (9ci)
ai3-26812
butyric acid, 4-amino- (7ci,8ci)
ccris 3721
df 468
gamma-amino-butanoic acid
STK301748
gamma-amino-n-butyric acid
56-12-2
4-aminobutanoic acid
4-AMINO-BUTYRATE ,
gaba
gamma-aminobutyric acid
4-amino-n-butyric acid
C00334
4-nh2-but
4-aminobutyric acid
4-nh3-but
g-aminobutyric acid
gamma-aminobutyric acid, bioxtra, >=99%
TO_000021
DB02530
gamma(amino)-butyric acid
NCGC00024546-03
NCGC00024546-04
NCGC00024546-06
KBIOSS_000429
KBIO2_000429
KBIO3_002190
KBIO2_005565
KBIOGR_001297
KBIO2_002997
NINDS_000616
SPECTRUM3_001385
SPECTRUM2_001208
SPECTRUM4_000809
SPBIO_000996
SPECTRUM1500678
NCGC00024546-02
NCGC00024546-05
A-5290
NCGC00015043-03
A 2129
C5C3DC27-C105-4D18-8A52-F51978B32D24
A0282
NCGC00015043-08
L000262
BMSE000340
aminobutanoic acid
butanoic acid,4-amino
.gamma.-amino-butyric acid
.gamma.-amino-n-butyric acid
aminobutyric acid, gamma-
factor i
vigabatrin impurity, .gamma.-aminobutyric acid-
HMS501O18
HMS1921C06
NCGC00015043-07
AKOS000119660
HMS3260A11
BMSE000871
2acz6ipc6i ,
acide amino-4- butyrique
unii-2acz6ipc6i
BMSE000820
BBL008590
nsc757426
nsc-757426
pharmakon1600-01500678
cas-56-12-2
dtxcid4015106
tox21_110071
dtxsid6035106 ,
4-amino-butyric acid
HMS2232P09
S4700
CCG-38515
NCGC00015043-04
NCGC00015043-05
NCGC00015043-09
NCGC00015043-06
NCGC00015043-02
piperidate
FT-0617569
AM20100372
LP00005
aminobutyric acid [inci]
.gamma.-aminobutyric acid [mi]
vigabatrin impurity, .gamma.-aminobutyric acid- [usp impurity]
gamma-aminobutyric acid [who-dd]
vigabatrin impurity d [ep impurity]
gamma-aminobutyric acid [usp-rs]
gamma-aminobutyric acid [mart.]
sodium alendronate trihydrate impurity a [ep impurity]
4-aminobutyric acid [fhfi]
aminobutyrate
gtpl5410
BP-21452
SCHEMBL4878
KS-5273
tox21_500005
NCGC00260690-01
4-aminobutyricacid
NCGC00015043-10
4-amino butyric acid
nh2-(ch2)3-cooh
aminobutyric acid,-4-
immuglobin
.omega.-aminobutyric acid
STR01523
CS-W020704
?-aminobutyric acid
HB0882
AB00052155_12
OPERA_ID_1152
mfcd00008226
y-aminobutyric acid
F2191-0196
sr-01000075618
SR-01000075618-1
20-79-1
gamma-aminobutyric acid, certified reference material, tracecert(r)
gamma-aminobutyric acid, united states pharmacopeia (usp) reference standard
gamma-aminobutyric acid, analytical standard
D70585
vigabatrin impurity d, european pharmacopoeia (ep) reference standard
SR-01000075618-6
SR-01000075618-3
SR-01000075618-7
SBI-0049994.P003
omega-aminobutyrate
w-aminobutyric acid
piperidinate
w-aminobutyrate
gamma aminobutyrate
4-aminobutyric
HY-N0067
4-aminobutyric-2,2-d2 acid
gamma-aminobutyric acid,(s)
Q210021
BRD-K77245796-001-19-2
A14934
SDCCGSBI-0049994.P004
gamma-aminobutyric acid pound>>(c)(3/4)?aminobutyric acid (gaba)
BCP34675
NCGC00015043-14
gamma-aminobutyric-acid
vigabatrin ep impurity d
4-aminobutanoic acid (gamma-aminobutyric acid)
vigabatrin impurity d
EN300-19823
gamma-aminobutyric acid (4-aminobutyric acid)
gamma-aminobutyric acid (mart.)
gaba phenolic
gaba (gamma-aminobutyric acid)
gamma.-aminobutyric acid
vigabatrin impurity, gamma-aminobutyric acid-(usp impurity)
gamma-amino-butyric acid
hydrocodone, acetaminophen, gamma-aminobutyric acid
gaba1519
acide amino-4-butyrique
gamma-aminobutyric acid (usp-rs)
gamma-aminobuttersaure
Z104475620

Research Excerpts

Overview

Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the central nervous system, synthesized by two isoforms of glutamate decarboxylase (GAD): GAD65 and GAD67. It is a nutritious bioactive compound that is also an antioxidant.

ExcerptReferenceRelevance
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the central nervous system, synthesized by two isoforms of glutamate decarboxylase (GAD): GAD65 and GAD67. "( GAD67-mediated GABA Synthesis and Signaling Impinges on Directing Basket Cell Axonal Projections Toward Purkinje Cells in the Cerebellum.
Hirai, S; Kobayashi, K; Miwa, H; Okado, H; Watanabe, M; Yamada, M; Yanagawa, Y, 2022
)
2.16
"Gamma-aminobutyric acid (GABA) is a non-proteinogenic amino acid act as a major neurotransmitter inhibitor in the nervous system of mammals. "( Gamma aminobutyric acid (GABA) production in Escherichia coli with pyridoxal kinase (pdxY) based regeneration system.
Ahn, J; Bhatia, SK; Choi, KY; Choi, YK; Gurav, R; Ham, S; Jeon, JM; Kim, HT; Yang, YH; Yoon, JJ, 2022
)
2.16
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid that possesses various physiological functions. "( Ultrasound accelerated γ-aminobutyric acid accumulation in coffee leaves through influencing the microstructure, enzyme activity, and metabolites.
Chen, X; Ji, D; Ma, H; Sun, Y, 2022
)
2.16
"Gamma-aminobutyric acid (GABA) is a nonproteinogenic amino acid that plays vital roles in plant growth and developmental processes. "( Physiological and proteomic analyses of γ-aminobutyric acid (GABA)-treated tubers reveals that StPOD42 promotes sprouting in potato.
Chen, J; Huang, XL; Li, LQ; Lu, LM; Lu, YF; Ren, B; Wang, Q; Wang, XY; Yu, LP; Zeng, FC, 2022
)
2.16
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid widely distributed in nature and extensively explored for its numerous physiological functions and effects on metabolic disorders. "( Strategies for improvement of gamma-aminobutyric acid (GABA) biosynthesis
Faizal Wong, FW; Halim, M; Mohamad, R; Mohamed, MS; Pannerchelvan, S; Rios-Solis, L; Tan, JS; Wasoh, H; Zaidan, UH, 2023
)
2.64
"Gamma-aminobutyric acid (GABA) is a crucial inhibitory neurotransmitter in the sympathetic nervous system that exerts regulatory effects on the blood, immune, and nervous systems. "( Genome sequences and functional analysis of Levilactobacillus brevis LSF9-1 and Pediococcus acidilactici LSF1-1 from fermented fish cake (Som-fak) with gamma-aminobutyric acid (GABA) production.
Kingkaew, E; Pakdeeto, A; Phuengjayaem, S; Somphong, A; Tanasupawat, S; Tunvongvinis, T, 2023
)
2.55
"Gamma-aminobutyric acid (GABA) is a nutritious bioactive compound that is also an antioxidant. "( Characterization of bioactive film from pectin incorporated with gamma-aminobutyric acid.
Meerasri, J; Sothornvit, R, 2020
)
2.24
"Gamma-Aminobutyric acid (GABA) is a non-protein amino acid widely distributed in nature. "( A Brief Review on the Non-protein Amino Acid, Gamma-amino Butyric Acid (GABA): Its Production and Role in Microbes.
Angayarkanni, J; Mahendran, R; Muthusamy, G; Sarasa, SB; Selta, DRF; Thankappan, B, 2020
)
2
"Gamma-aminobutyric acid (GABA) is an important metabolite which functions in plant growth, development, and stress responses. "( Induction of γ-aminobutyric acid plays a positive role to Arabidopsis resistance against Pseudomonas syringae.
Deng, X; Liu, Y; Xu, J; Xu, X; Yang, L; Zhang, S; Zhang, Y, 2020
)
2
"Gamma-aminobutyric acid (GABA) is a newly recognized signaling molecule participating in physiological processes, growth, and development of plants under optimal and stressful environments. "( GABA reverses salt-inhibited photosynthetic and growth responses through its influence on NO-mediated nitrogen-sulfur assimilation and antioxidant system in wheat.
AlAjmi, MF; Iqbal, N; Jahan, B; Khan, MIR; Khan, NA; Khanna, RR; Tabish Rehman, M, 2021
)
2.06
"Gamma-aminobutyric acid (GABA) is a ubiquitous four-carbon, non-protein amino acid. "( The versatile GABA in plants.
Dou, N; Li, L; Wu, C; Zhang, H, 2021
)
2.06
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter that is strongly and selectively synthesized in and secreted from pancreatic beta cells. "( Effects of sustained GABA releasing implants on pancreatic islets in mice.
Hagan, DW; Ling, KC; Phelps, EA; Santini-González, J, 2021
)
2.06
"Gamma-aminobutyric acid (GABA) is a principal inhibitory neurotransmitter in the central nervous system and is produced by irreversible decarboxylation of glutamate. "( Evaluation of GABA Production and Probiotic Activities of Enterococcus faecium BS5.
Angayarkanni, J; Bs, S; Femil Selta, DR; Mahendran, R; Muthusamy, G; Thankappan, B, 2021
)
2.06
"Gamma-aminobutyric acid (GABA) is a well-known feed supplement for its capability of reducing the adverse effect of stress in chickens. "( The effect of gamma-aminobutyric acid supplementation on growth performances, immune responses, and blood parameters of chickens reared under stressful environment: a meta-analysis.
Goel, A; Gupta, V; Jeong, C; Ncho, CM, 2021
)
2.42
"Gamma-aminobutyric acid (GABA) is a key inhibitory neurotransmitter that has been implicated in the aetiology of common mood and behavioural disorders. "( Kisspeptin modulates gamma-aminobutyric acid levels in the human brain.
Abbara, A; Comninos, AN; Demetriou, L; Dhillo, WS; Mills, EG; O'Callaghan, J; Owen, BM; Rabiner, EA; Thurston, L; Wall, MB; Wing, VC; Yang, L, 2021
)
2.38
"Gamma-aminobutyric acid (GABA) is an important bio-product used in pharmaceuticals and functional foods and as a precursor of the biodegradable plastic polyamide 4. "( Characterization of three glutamate decarboxylases from Bacillus spp. for efficient γ-aminobutyric acid production.
Bai, Y; Luo, H; Su, X; Sun, L; Tu, T; Wang, Y; Yao, B; Zhang, J; Zhang, X; Zhou, C, 2021
)
2.06
"Gamma-aminobutyric acid (GABA) is an amino that plays a major role as a neurotransmitter. "( In silico comparative genomics analysis of Lactiplantibacillus plantarum DW12, a potential gamma-aminobutyric acid (GABA)-producing strain.
Chukamnerd, A; Deachamag, P; Jeenkeawpiam, K; Kantachote, D; Surachat, K; Wonglapsuwan, M, 2021
)
2.28
"Gamma-aminobutyric acid (GABA) is a major modulator in brain maturation and its role in many different neurodevelopmental disorders has been widely reported. "( Gamma-aminobutyric acid levels in cerebrospinal fluid in neuropaediatric disorders.
Armstrong-Morón, J; Artuch, R; Casado, M; Cortès-Saladelafont, E; Cuadras, D; García-Cazorla, À; Molero-Luis, M; Montoya, J; Yubero, D, 2018
)
3.37
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter found in the central nervous system of mammals. "( Transcriptomic response to GABA-producing Lactobacillus plantarum CGMCC 1.2437T induced by L-MSG.
Dang, F; Feng, X; Jiang, Y; Li, L; Man, C; Zhang, W; Zhuang, K, 2018
)
1.92
"Gamma-aminobutyric acid (GABA) is a neurotransmitter that exerts several physiological functions and positive effects on human health. "( Characteristics of Potential Gamma-Aminobutyric Acid-Producing Bacteria Isolated from Korean and Vietnamese Fermented Fish Products.
Park, JH; Vo, T, 2019
)
2.25
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid with various health benefits. "( Physicochemical and functional properties of γ-aminobutyric acid-treated soy proteins.
Liu, C; Ma, T; Wang, Y; Zhao, J, 2019
)
1.96
"Gamma-aminobutyric acid (GABA) is a well-known neurotransmitter in the central nervous system, but additionally enhances the sperm acrosome reaction in the rat and cow."( Capacitation of mouse sperm is modulated by gamma-aminobutyric acid (GABA) concentration.
Hara, K; Hiradate, Y; Kurata, S; Tanemura, K; Umezu, K, 2019
)
1.5
"Gamma-aminobutyric acid (Gaba) is a non-proteinogenic amino acid that is widely present in microorganisms, plants, and vertebrates. "( An Updated Review on Pharmaceutical Properties of Gamma-Aminobutyric Acid.
Ngo, DH; Vo, TS, 2019
)
2.21
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid commonly present in all organisms. "( Genetic manipulation of the γ-aminobutyric acid (GABA) shunt in rice: overexpression of truncated glutamate decarboxylase (GAD2) and knockdown of γ-aminobutyric acid transaminase (GABA-T) lead to sustained and high levels of GABA accumulation in rice kern
Akama, K; Kainou, K; Oonishi, T; Ozaki, K; Shimajiri, Y, 2013
)
1.83
"Gamma-aminobutyric acid (GABA) is a precursor of one of the most promising heat-resistant biopolymers, Nylon-4, and can be produced by the decarboxylation of monosodium glutamate (MSG). "( Efficient gamma-aminobutyric acid bioconversion by employing synthetic complex between glutamate decarboxylase and glutamate/GABA antiporter in engineered Escherichia coli.
Hong, SH; Ko, JS; Le Vo, TD; Lee, SH; Park, SJ, 2013
)
2.23
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the cerebral cortex, and most cortical inhibitory synapses originate from non-pyramidal cells."( Untangling GABAergic wiring in the cortical microcircuit.
Kubota, Y, 2014
)
1.12
"Gamma-aminobutyric acid (GABA) is an important neurotransmitter, but recent reports have revealed the expression of GABAergic components in peripheral, non-neural tissues. "( Characteristic expressions of GABA receptors and GABA producing/transporting molecules in rat kidney.
Abe, A; Kimura, J; Sanada, H; Suzuki, Y; Takano, K; Watanabe, T; Yatabe, J; Yatabe, MS, 2014
)
1.85
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter of the retina and affects myopic development. "( Effects of electroacupuncture on the levels of retinal gamma-aminobutyric acid and its receptors in a guinea pig model of lens-induced myopia.
Bi, AL; Bi, HS; Ding, MH; Guo, DD; Guo, JG; Jiang, WJ; Sha, F; Wang, L; Wu, JF; Xu, CL; Ye, X; Zhao, W, 2015
)
2.11
"Gamma-aminobutyric acid (GABA) is an important bioactive compound biosynthesized by microorganisms through decarboxylation of glutamate by glutamate decarboxylase (GAD). "( Overexpression and optimization of glutamate decarboxylase in Lactobacillus plantarum Taj-Apis362 for high gamma-aminobutyric acid production.
Bakar, FA; Baradaran, A; Ebrahimpour, A; Manap, MY; Mohammed, AS; Rahim, RA; Saari, N; Tajabadi, N, 2015
)
2.07
"Gamma-aminobutyric acid (GABA) is a key neurotransmitter where it usually inhibits impulse transmission. "( Gamma-aminobutyric acid loaded halloysite nanotubes and in vitro-in vivo evaluation for brain delivery.
Çengelli Ünel, Ç; Erol, K; Kırımlıoğlu, GY; Yazan, Y, 2015
)
3.3
"Gamma-aminobutyric acid (GABA) is an amino acid which acts as a neurotransmitter in the central nervous system. "( Metabotropic GABAB receptors mediate GABA inhibition of acetylcholine release in the rat neuromuscular junction.
Malomouzh, AI; Nikolsky, EE; Nurullin, LF; Petrov, KA, 2015
)
1.86
"Gamma-aminobutyric acid (GABA) is an important bio-product, which is used in pharmaceutical formulations, nutritional supplements, and biopolymer monomer. "( Efficient production of gamma-aminobutyric acid using Escherichia coli by co-localization of glutamate synthase, glutamate decarboxylase, and GABA transporter.
Dung Pham, V; Hong, SH; Lee, SH; Park, SJ; Somasundaram, S, 2016
)
2.18
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid, which is an important inhibitor of neurotransmission in the human brain. "( Co-Localization of GABA Shunt Enzymes for the Efficient Production of Gamma-Aminobutyric Acid via GABA Shunt Pathway in Escherichia coli.
Hong, SH; Lee, SH; Park, SJ; Pham, VD; Somasundaram, S, 2016
)
2.11
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid widespread in Nature. "( Improved fermentative production of gamma-aminobutyric acid via the putrescine route: Systems metabolic engineering for production from glucose, amino sugars, and xylose.
Jorge, JM; Kind, S; Nguyen, AQ; Pérez-García, F; Wendisch, VF, 2017
)
2.17
"Gamma-aminobutyric acid (GABA) is a four-carbon non-protein amino acid that is widely distributed among various organisms. "( Biotechnological advances and perspectives of gamma-aminobutyric acid production.
Liu, J; Wei, L; Xu, N, 2017
)
2.16
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in animals that is also found in plants and has been associated with plant responses to stress. "( A validated method for gas chromatographic analysis of gamma-aminobutyric acid in tall fescue herbage.
Coe, BL; Dougherty, CT; Huo, CJ; Kagan, IA; Smith, LL; Strickland, JR, 2008
)
2.04
"Gamma-aminobutyric acid is a major inhibitory neurotransmitter in the central nervous system. "( [Gamma-aminobutyric acid--metabolism and its disorders].
Kowalski, A; Rebas, E; Zylińska, L, 2007
)
2.69
"Gamma-aminobutyric acid (GABA) is a four-carbon amino acid that is commonly present in living organisms and functions as a major inhibitory neurotransmitter in mammals. "( Seed-specific expression of truncated OsGAD2 produces GABA-enriched rice grains that influence a decrease in blood pressure in spontaneously hypertensive rats.
Akama, K; Kanetou, J; Kawakami, K; Shimosaki, S; Takaiwa, F; Tsuchikura, S, 2009
)
1.8
"gamma-aminobutyric acid (GABA) is a four-carbon non-protein amino acid presented in a wide range of organisms. "( Effects of exogenous GABA on gene expression of Caragana intermedia roots under NaCl stress: regulatory roles for H2O2 and ethylene production.
Jiang, ZP; Li, CX; Liu, JF; Qi, LW; Shi, SQ; Shi, Z; Sun, XM; Xiao, WF; Zhang, SG, 2010
)
1.8
"gamma-Aminobutyric acid (GABA) is an important bioactive regulator, and its biosynthesis is primarily through the alpha-decarboxylation of glutamate by glutamate decarboxylase (GAD). "( Purification of calmodulin from rice bran and activation of glutamate decarboxylase by Ca2+/calmodulin.
Liu, M; Lv, YG; Wang, L; Zhang, H, 2010
)
1.8
"Gamma-aminobutyric acid is a non-protein amino acid that is widely present in organisms. "( Lactic acid bacterial cell factories for gamma-aminobutyric acid.
Cao, Y; Li, H, 2010
)
2.07
"Gamma-aminobutyric acid is a major inhibitory neurotransmitter in mammalian brains, and has several well-known physiological functions. "( Production of gamma-aminobutyric acid by Lactobacillus brevis NCL912 using fed-batch fermentation.
Cao, Y; Huang, G; Li, H; Qiu, T, 2010
)
2.16
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the brain. "( In vivo magnetic resonance spectroscopy measurement of gray-matter and white-matter gamma-aminobutyric acid concentration in sensorimotor cortex using a motion-controlled MEGA point-resolved spectroscopy sequence.
Bhattacharyya, PK; Lowe, MJ; Phillips, MD; Stone, LA, 2011
)
2.04
"Gamma-aminobutyric acid (GABA) is a non-proteinaceous amino acid that is widely distributed in nature and acts as the major inhibitory neurotransmitter in the mammalian brain. "( Separation of gamma-aminobutyric acid from fermented broth.
Cao, Y; Chen, Y; Li, H; Qiu, T, 2011
)
2.17
"Gamma-aminobutyric acid (GABA) is a non-essential amino acid and a precursor of pyrrolidone, a monomer of nylon 4. "( Effects of glutamate decarboxylase and gamma-aminobutyric acid (GABA) transporter on the bioconversion of GABA in engineered Escherichia coli.
Hong, SH; Kim, TW; Le Vo, TD, 2012
)
2.09
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter. "( Reduced GAD(65/67) immunoreactivity in the hypothalamic paraventricular nucleus in depression: a postmortem study.
Bao, AM; Gao, SF; Klomp, A; Swaab, DF; Wu, JL, 2013
)
1.83
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter present almost exclusively in the central nervous system (CNS), distributed across almost all brain regions, and expressed in interneurons modulating local circuits."( GABAergic dysfunction in mood disorders.
Barale, F; Brambilla, P; Perez, J; Schettini, G; Soares, JC, 2003
)
1.04
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the mammalian central nervous system. "( Cleft palate by picrotoxin or 3-MP and palatal shelf elevation in GABA-deficient mice.
Ding, R; Obata, K; Tsunekawa, N,
)
1.57
"Gamma-aminobutyric acid (GABA) is an inhibitory amino acid and acts as an intercellular transmitter in the central nervous system and peripheral tissues. "( Vesicular inhibitory amino acid transporter is expressed in gamma-aminobutyric acid (GABA)-containing astrocytes in rat pineal glands.
Echigo, N; Moriyama, Y, 2004
)
2.01
"Gamma-aminobutyric acid (GABA) is a principal inhibitory neurotransmitter in the vertebrate nervous system. "( Gamma-aminobutiric acid immunostaining in trigeminal, nodose and spinal ganglia of the cat.
Stoyanova, II, 2004
)
1.77
"gamma-Aminobutyric acid (GABA) is a neurotransmitter with a demonstrated neuroregulatory role in reproduction in most representative species of vertebrate classes via the hypothalamus. "( In vitro and in vivo effects of GABA, muscimol, and bicuculline on lamprey GnRH concentration in the brain of the sea lamprey (Petromyzon marinus).
Kavanaugh, SI; Root, AR; Sanford, JD; Sower, SA, 2004
)
1.77
"gamma-Aminobutyric acid (GABA) is a neurotransmitter found in both the central and the peripheral nervous systems including the gastrointestinal tract. "( GABAergic mechanisms of gastroprotection in the rat: role of sensory neurons, prostaglandins, and nitric oxide.
Ancha, HR; Anderson, M; Harty, RF; Jazzar, A; Xia, Y,
)
1.57
"gamma-Aminobutyric acid (GABA), which is a major inhibitory neurotransmitter in the brain, is also found in many peripheral nonneuronal tissues, including male reproductive organs. "( Epithelial localization of green fluorescent protein-positive cells in epididymis of the GAD67-GFP knock-in mouse.
Abe, H; Azuma, H; Hayasaki, H; Kanbara, K; Katsuoka, Y; Maemura, K; Obata, K; Watanabe, M; Yabumoto, M; Yanagawa, Y,
)
1.57
"gamma-Aminobutyric acid (GABA) is an important regulatory factor of pituitary gland function, which in addition to hypothalamic neurons, can be derived from intrapituitary sources, ie, growth hormone (GH) cells of rat and monkey. "( Receptors and sites of synthesis and storage of gamma-aminobutyric acid in human pituitary glands and in growth hormone adenomas.
End, K; Gamel-Didelon, K; Gratzl, M; Jung, H; Lüdecke, D; Mayerhofer, A; Tolnay, M, 2005
)
2.03
"gamma-Aminobutyric acid (GABA) is an inhibitory transmitter in the central nervous system of mammals. "( Quantum dot-mediated detection of gamma-aminobutyric acid binding sites on the surface of living pollen protoplasts in tobacco.
He, Z; Liang, J; Sun, M; Yu, G, 2006
)
2.06
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter that is synthesized by two isoforms of glutamic acid decarboxylase (GAD), GAD65 and GAD67. "( GABAergic neurons in the lateral superior olive of the hamster are distinguished by differential expression of gad isoforms during development.
Jenkins, SA; Simmons, DD, 2006
)
1.78
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in the brain, but widely distributed in different peripheral organs. "( Possible expression of a particular gamma-aminobutyric acid transporter isoform responsive to upregulation by hyperosmolarity in rat calvarial osteoblasts.
Fujimori, S; Hinoi, E; Iemata, M; Takahata, Y; Takarada, T; Yoneda, Y, 2006
)
2.05
"Gamma-aminobutyric acid (GABA) is an important retinal neurotransmitter. "( Dark-rearing-induced reduction of GABA and GAD and prevention of the effect by BDNF in the mouse retina.
Gibo, TL; Grzywacz, NM; Lee, EJ, 2006
)
1.78
"Gamma-aminobutyric acid (GABA) is an important neurotransmitter that, through the subtype A GABA receptor (GABAAR), induces inhibition in the adult brain. "( A GABAergic system in airway epithelium is essential for mucus overproduction in asthma.
Fan, Y; Hirota, JA; Inman, MD; Ju, W; Kelly, MM; Li, J; Liu, M; Lu, WY; O'Byrne, PM; Orser, B; Wang, S; Xiang, YY; Yang, X; Ye, B, 2007
)
1.78
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in insects and is widely distributed in the central nervous system (CNS). "( gamma-Aminobutyric acid (GABA) signaling components in Drosophila: immunocytochemical localization of GABA(B) receptors in relation to the GABA(A) receptor subunit RDL and a vesicular GABA transporter.
Enell, L; Hamasaka, Y; Kolodziejczyk, A; Nässel, DR, 2007
)
3.23
"Gamma-aminobutyric acid (GABA) is a non-protein amino acid. "( Wound healing activity of gamma-aminobutyric Acid (GABA) in rats.
Hahm, DH; Han, D; Kim, HY; Lee, HJ; Shim, I, 2007
)
2.08
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter and also presumed to be a neurotrophic factor. "( GABA and synaptic inhibition of mouse cerebellum lacking glutamate decarboxylase 67.
Hirono, M; Itohara, S; Kawaguchi, Y; Kume, N; Obata, K; Yanagawa, Y, 2008
)
1.79
"Gamma-aminobutyric acid (GABA) is a candidate as a neurotransmitter in the vertebrate retina. "( Binding and uptake of the GABA analogue, 3H-muscimol, in the retinas of goldfish and chicken.
Brecha, N; Yazulla, S, 1980
)
1.7
"gamma-Aminobutyric acid (GABA) is a potent inhibitory neurotransmitter which is synthesized by the enteric bacterial flora and delivered into portal venous blood. "( Identification of an acceptor system for gamma-aminobutyric acid on isolated rat hepatocytes.
Ferenci, P; Jones, EA; Minuk, GY; Vergalla, J,
)
1.84
"gamma-Aminobutyric acid (GABA) is an important inhibitory neurotransmitter."( Biochemistry and the schizophrenia. Old concepts and new hypothesis.
Berger, PA, 1981
)
0.98
"gamma-Aminobutyric acid (GABA) is an important inhibitive neurotransmitter in central nervous system (CNS). "( [Morphologic study of GABA-ergic neurons in dissociated cell culture of spinal cord and dorsal root ganglion].
Pao, X; Tao, ZJ; Zha, XM, 1995
)
1.73
"Gamma-aminobutyric acid (GABA) is a potent amino acid neurotransmitter with various physiologic effects throughout the body. "( Gamma-aminobutyric acid and the liver.
Minuk, GY, 1993
)
3.17
"gamma-Aminobutyric acid (GABA) is a potent inhibitory neurotransmitter with growth-regulatory properties. "( The effect of gamma-aminobutyric acid on hepatic regenerative activity following partial hepatectomy in rats.
Gauthier, T; Minuk, GY, 1993
)
2.09
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter, synthesised from glutamate by glutamate decarboxylase (GAD), in the central nervous system. "( Transcription and translation of two glutamate decarboxylase genes in the ileum of rat, mouse and guinea pig.
Cram, DS; Faulkner-Jones, BE; Furness, JB; Harrison, LC; Williamson, S, 1995
)
1.73
"Gamma-aminobutyric acid (GABA) is a prominent inhibitory transmitter in both the central nucleus of the amygdala (Ce) and the medial nuclei of the solitary tracts (mNTS). "( GABAergic neurons in rat nuclei of solitary tracts receive inhibitory-type synapses from amygdaloid efferents lacking detectable GABA-immunoreactivity.
Cestari, DM; Chan, J; Pickel, VM; Van Bockstaele, EJ, 1996
)
1.74
"Gamma-aminobutyric acid (GABA) is a prevalent neurotransmitter in both vertebrate and invertebrate systems. "( GABA-induced synaptic facilitation at type B to A photoreceptor connections in Hermissenda.
Clark, GA; Schultz, LM, 1997
)
1.74
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the mammalian retina, and its physiological action is well established. "( GABA-gated Cl- channels in the rat retina.
Bormann, J; Feigenspan, A, 1998
)
1.74
"Gamma-aminobutyric acid (GABA) is an important inhibitory neurotransmitter in vertebrates and invertebrates (Sattelle [1990] Adv. "( Distribution of GABA-like immunoreactive neurons in insects suggests lineage homology.
Truman, JW; Witten, JL, 1998
)
1.74
"Gamma-aminobutyric acid (GABA) acts as an inhibitory neurotransmitter in the mature vertebrate retina, where it is localized predominantly in amacrine cells, and to a lesser extent in other cell types. "( GABA as a developmental signal in the inner retina and optic nerve.
Sandell, JH, 1998
)
1.74
"gamma-Aminobutyric acid (GABA) is a neurotransmitter that also occurs in a few non-neuronal cell types, where it may serve as a paracrine modulator. "( Immunocytochemical evidence suggesting that diamine oxidase catalyzes biosynthesis of gamma-aminobutyric acid in antropyloric gastrin cells.
Hardt, J; Hougaard, DM; Larsson, LI, 2000
)
1.97
"Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter that is elevated in inflamed human dental pulp. "( Evaluation of functional GABA(B) receptors in dental pulp.
Bowles, W; Hargreaves, KM; Richardson, JD; Wurm, C, 2001
)
1.75
"gamma-Aminobutyric acid (GABA) is a major neurotransmitter in AMG, and histamine receptor activation is also reported to stimulate GABA release."( Modulation of audiogenically kindled seizures by gamma-aminobutyric acid-related mechanisms in the amygdala.
Faingold, CL; Feng, HJ; Naritoku, DK; Randall, ME, 2001
)
1.29
"Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter of the mammalian brain and the enzyme responsible for catabolism (breakdown in the liver during regulation) is GABA-Transaminase (GABA-T). "( GABA-transaminase, the liver and infantile autism.
Cohen, BI, 2001
)
1.75
"gamma-Aminobutyric acid (GABA) is an inhibitory neurotransmitter in the peripheral nervous system of certain invertebrates and is thought to be a major transmitter in the vertebrate central nervous system. "( GABA may be a neurotransmitter in the vertebrate peripheral nervous system.
Burnstock, G; Dennison, ME; Jessen, KR; Mirsky, R, 1979
)
1.7
"Gamma-aminobutyric acid (GABA) is a putative inhibitory neurotransmitter in the vertebrate nervous system. "( GABA-immunoreactive terminals synapse on primate spinothalamic tract cells.
Carlton, SM; Westlund, KN; Willis, WD; Zhang, D, 1992
)
1.73
"gamma-Aminobutyric acid (GABA) acts as an inhibitory transmitter in the vertebrate central nervous system, often by interacting with the GABAA type of receptor. "( Activation and inactivation of the GABAA receptor: insights from comparison of native and recombinant subunit assemblies.
Mathers, DA, 1991
)
1.72
"gamma-Aminobutyric acid (GABA) is a regulator of uterine motility. "( Steroid control of uterine motility via gamma-aminobutyric acidA receptors in the rabbit: a novel mechanism?
Majewska, MD; Vaupel, DB, 1991
)
1.99
"gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the mammalian retina, where it serves many roles in establishing complex response characteristics of ganglion cells. "( Evidence for functionally distinct subclasses of gamma-aminobutyric acid receptors in rabbit retina.
Friedman, DL; Redburn, DA, 1990
)
1.98
"gamma-Aminobutyric acid (GABA) is an inhibitory transmitter found in the retinae of mammals largely within certain amacrine cells. "( The effects of gabaculine in vivo on the distribution of GABA-like immunoreactivity in the rat retina.
Cubells, JF; Makman, MH; Walkley, SU, 1988
)
1.72
"Gamma-aminobutyric acid (GABA) is a putative central neurotransmitter that depresses respiratory neurons and has a metabolism in the brain that is tied to CO2 fixation and H+ metabolism. "( Reversible depression of ventilation and cardiovascular function by ventriculocisternal perfusion with gamma-aminobutyric acid in dogs.
Hoop, B; Kazemi, H; Kneussl, MP; Pappagianopoulos, P, 1986
)
1.93
"Gamma-aminobutyric acid (GABA) is a potent amino acid neurotransmitter that suppresses normal neuronal activity in the central nervous system. "( Gamma-aminobutyric acid (GABA) production by eight common bacterial pathogens.
Minuk, GY, 1986
)
3.16

Effects

Gamma-aminobutyric acid (GABA) has a dual role as an inhibitory neurotransmitter in the adult central nervous system (CNS) and as a signaling molecule exerting largely excitatory actions during development.

gamma-aminobutyric acid (GABA) has been shown to depolarize the membranes of astrocytes and oligodendrocyte taken from different tissues and species. The GABA-transaminase (GAba-T) is the main GABA-degrading enzyme in the GABA shunt pathway. Gamma-amino acids have been hypothesized to play a role in tactile hypersensitivity.

ExcerptReferenceRelevance
"Gamma-aminobutyric acid (GABA) has a dual role as an inhibitory neurotransmitter in the adult central nervous system (CNS) and as a signaling molecule exerting largely excitatory actions during development. "( The spatiotemporal segregation of GAD forms defines distinct GABA signaling functions in the developing mouse olfactory system and provides novel insights into the origin and migration of GnRH neurons.
Erdélyi, F; Katarova, Z; Kwakowsky, A; Margolis, FL; Schwirtlich, M; Szabó, G; Vastagh, C; Yanagawa, Y, 2015
)
1.86
"gamma-Aminobutyric acid (GABA) has a pronounced effect on these events and elicits differentiation of neurons; that is, GABA acts as a trophic signal."( Effects of gamma-aminobutyric acid (GABA) on synaptogenesis and synaptic function.
Belhage, B; Elster, L; Hansen, GH; Schousboe, A, 1998
)
1.41
"Gamma-aminobutyric acid (GABA) has been reported to accumulate in plants when subjected to salt stress, and GABA-transaminase (GABA-T) is the main GABA-degrading enzyme in the GABA shunt pathway. "( Characterization of GABA-Transaminase Gene from Mulberry (
Fan, Y; Gai, Y; Ji, X; Li, Y; Liu, C; Liu, Z; Wang, H; Xin, Y; Zhang, M, 2022
)
2.16
"Gamma-aminobutyric acid (GABA) has been hypothesized to play a role in tactile hypersensitivity."( Tactile hypersensitivity and GABA concentration in the sensorimotor cortex of adults with autism.
Lamberton, F; Mattout, J; Sapey-Triomphe, LA; Schmitz, C; Sonié, S, 2019
)
1.24
"Gamma-aminobutyric acid (GABA) has a dual role as an inhibitory neurotransmitter in the adult central nervous system (CNS) and as a signaling molecule exerting largely excitatory actions during development. "( The spatiotemporal segregation of GAD forms defines distinct GABA signaling functions in the developing mouse olfactory system and provides novel insights into the origin and migration of GnRH neurons.
Erdélyi, F; Katarova, Z; Kwakowsky, A; Margolis, FL; Schwirtlich, M; Szabó, G; Vastagh, C; Yanagawa, Y, 2015
)
1.86
"Gamma-aminobutyric acid (GABA) has many biological functions, including the inhibition of blood pressure increases and acceleration of growth hormone secretion. "( Monitoring Technology for Gamma-Aminobutyric acid Production in Polished Mochi Barley Grains using a Carbon Dioxide Sensor.
Kawata, K; Watanabe, S; Watanabe, Y, 2015
)
2.16
"Gamma-aminobutyric acid (GABA) has been reported to inhibit the growth of cholangiocarcinoma QBC939 cells, but the mechanisms are still not fully understood."( Gamma-aminobutyric acid binds to GABAb receptor to inhibit cholangiocarcinoma cells growth via the JAK/STAT3 pathway.
Hu, SY; Huang, Q; Liu, CH; Xie, F; Zhu, CL; Zhu, K, 2013
)
3.28
"gamma-Aminobutyric acid (GABA) has been reported to enhance exocrine secretion evoked by intrinsic neuronal excitation in the pancreas."( Effects of gamma-aminobutyric acid on action of gastrin-releasing peptidergic neurons in exocrine secretion of isolated, perfused rat pancreas.
Cui, ZY; Park, HJ; Park, YD, 2002
)
2.15
"gamma-Aminobutyric acid (GABA) has been proposed to function as a paracrine signaling molecule in islets of Langerhans. "( Glucose inhibition of glucagon secretion from rat alpha-cells is mediated by GABA released from neighboring beta-cells.
Birnir, B; Braun, M; Buschard, K; Gromada, J; Rorsman, P; Salehi, A; Sewing, S; Wendt, A, 2004
)
1.77
"gamma-Aminobutyric acid (GABA) has been known to function as an autocrine/paracrine signal molecule in addition to its well-known inhibitory neurotransmitter function. "( Role of gamma-aminobutyric acid in early neuronal development: studies with an embryonic neuroectodermal stem cell clone.
Anderová, M; Jelitai, M; Kékesi, K; Koncz, P; Madarász, E; Markó, K; Syková, E, 2004
)
2.2
"Gamma-aminobutyric acid (GABA) has been implicated in cell proliferation and differentiation during development. "( Morphogenesis in the retina of a slow-developing teleost: emergence of the GABAergic system in relation to cell proliferation and differentiation.
Anadón, R; Candal, E; Ferreiro-Galve, S; Rodríguez-Moldes, I, 2008
)
1.79
"Gamma-aminobutyric acid (GABA) has several physiological functions in humans. "( Characterization of glutamate decarboxylase from a high gamma-aminobutyric acid (GABA)-producer, Lactobacillus paracasei.
Kimura, T; Komatsuzaki, N; Nakamura, T; Shima, J, 2008
)
2.03
"Gamma-aminobutyric acid also has been shown to have an inhibitory role in some studies."( Possible aminergic mediation of MSH release and of the CNS effects of MSH and MIF-I.
Kastin, AJ; Kostrzewa, RM; Schally, AV, 1980
)
0.98
"gamma-Aminobutyric acid (GABA) has been implicated in the development of hypertension and in the regulation of blood pressure. "( The GABA/benzodiazepine receptor complex in the nervous system of a hypertensive strain of rat.
Head, RA; Tunnicliff, G; Welborn, KL, 1984
)
1.71
"gamma-Aminobutyric acid has no effect on [3H]Ro 5-8464 binding, again in contrast to its marked effect on [3H]diazepam binding."( Characterization of peripheral-type benzodiazepine binding sites in brain using [3H]Ro 5-4864.
Boulenger, JP; Clark-Rosenberg, R; Marangos, PJ; Patel, J, 1982
)
0.99
"gamma-Aminobutyric acid (GABA) has been suggested to be a neurotransmitter of monophasic horizontal cells (a subtype of horizontal cells), which have direct connections with red-sensitive and green-sensitive cones."( gamma-Aminobutyric acid acts at axon terminals of turtle photoreceptors: difference in sensitivity among cell types.
Kaneko, A; Tachibana, M, 1984
)
2.43
"gamma-Aminobutyric acid (GABA) has been determined in rat brain by derivatization with 2,4,6-trinitrobenzenesulfonic acid. "( Determination of gamma-aminobutyric acid by liquid chromatography with electrochemical detection.
Caudill, WL; Houck, GP; Wightman, RM, 1982
)
2.05
"gamma-Aminobutyric acid (GABA) has been shown both to stimulate and inhibit LH secretion in vivo. "( Differential expression of gamma-aminobutyric acid receptors in immortalized luteinizing hormone-releasing hormone neurons.
Favit, A; Negro-Vilar, A; Wetsel, WC, 1993
)
2.03
"Gamma-Aminobutyric acid(GABA) has been established as a major inhibitory neurotransmitter in the brain. "( [GABA receptor chloride ion channel].
Hashimoto, T, 1998
)
1.74
"gamma-Aminobutyric acid (GABA) has a pronounced effect on these events and elicits differentiation of neurons; that is, GABA acts as a trophic signal."( Effects of gamma-aminobutyric acid (GABA) on synaptogenesis and synaptic function.
Belhage, B; Elster, L; Hansen, GH; Schousboe, A, 1998
)
1.41
"Gamma-aminobutyric acid (GABA) has been implicated in the regulation of reproduction, particularly in the developmental modulation of gonadotropin-releasing hormone (GnRH) secretion. "( GABA inhibition of immortalized gonadotropin-releasing hormone neuronal excitability involves GABA(A) receptors negatively coupled to cyclic adenosine monophosphate formation.
Beltrán-Parrazal, L; Clapp, C; Martínez de la Escalera, G; Noris, G, 2001
)
1.75
"Gamma-Aminobutyric acid (GABA) has been implicated in the neurochemistry of epilepsy. "( Low cerebrospinal fluid gamma-aminobutyric acid content in seizure patients.
Ballenger, JC; Glaeser, BS; Hare, TA; Post, RM; Wood, JH, 1979
)
2.01
"gamma-Aminobutyric acid (Gaba) has been shown to influence dopamine activity in the brain. "( gamma-Aminobutyric acid (Gaba) and the dopamine hypothesis of schizophrenia.
Van Kammen, DP, 1977
)
3.14
"Gamma-aminobutyric acid (GABA) has been proposed as a neurotransmitter of a subset of efferent nerve fibers in the mammalian cochlea. "( Potassium induced release of GABA and other substances from the guinea pig cochlea.
Bobbin, RP; Ceasar, G; Fallon, M, 1990
)
1.72
"gamma-Aminobutyric acid (GABA) has been identified in axon terminals innervating neurons of the supraoptic nucleus and has been shown to inhibit the electrical activity of supraoptic neurons when applied iontophoretically. "( gamma-Aminobutyric acid antagonists stimulate vasopressin release from organ-cultured hypothalamo-neurohypophyseal explants.
Armstrong, WE; Sladek, CD, 1987
)
3.16
"gamma-aminobutyric acid (GABA) has been reported to be an important neurotransmitter in the retinas of many species. "( Localization of GABA- and GAD-like immunoreactivity in the turtle retina.
Eldred, WD; Hurd, LB, 1989
)
1.72
"gamma-Aminobutyric acid (GABA) has been shown to depolarize the membranes of astrocytes and oligodendrocytes taken from different tissues and species. "( GABA triggers a Cl- efflux from cultured mouse oligodendrocytes.
Hoppe, D; Kettenmann, H, 1989
)
1.72
"The gamma-aminobutyric acid (GABA) system has been found to differentiate very early relative to other transmitter-identified neurons, such that by embryonic day 13 a well developed fiber network exists in the brainstem, mesencephalon and diencephalon, including a large projection in the posterior commissure and adjacent areas on the surface of the mesencephalon and tectum."( Prenatal ontogeny of the GABAergic system in the rat brain: an immunocytochemical study.
Han, VK; Henderson, P; Lauder, JM; Towle, AC; Verdoorn, T, 1986
)
0.75

Actions

Gamma-aminobutyric acid (GABA) plays a crucial role as a neurotransmitter in anxiety circuits, prominently in the hippocampus, amygdala, and prefrontal cortex. It also plays a key role in cytosolic regulation of pH, controlling of carbon and nitrogen metabolism, and protection against biotic and abiotic stresses.

ExcerptReferenceRelevance
"Gamma-aminobutyric acid (GABA) plays a crucial role in signal transduction and can function as a neurotransmitter. "( Gamma-Aminobutyric Acid Signaling in Damage Response, Metabolism, and Disease.
Kim, K; Yoon, H, 2023
)
3.8
"Gamma-aminobutyric acid (GABA) plays a crucial role as a neurotransmitter in anxiety circuits, prominently in the hippocampus, amygdala, and prefrontal cortex. "( Age-related changes in glutamic acid decarboxylase 1 gene expression in the medial prefrontal cortex and ventral hippocampus of fear-potentiated rats subjected to isolation stress.
Abbasnejad, M; Esmaili-Mahani, S; Hosseininasab, NS; Motaghi, S; Sepehri, G; Sirchi, MM, 2023
)
2.35
"Gamma-aminobutyric acid (GABA) plays a vital role in plant responses to multifarious stresses."( Gamma-aminobutyric acid enhances tolerance to iron deficiency by stimulating auxin signaling in cucumber (Cucumis sativusL.).
Du, N; Guo, Z; Li, Y; Piao, F; Shen, S; Zheng, S, 2020
)
2.72
"Gamma-aminobutyric acid (GABA) plays a key role in cytosolic regulation of pH, controlling of carbon and nitrogen metabolism, and protection against biotic and abiotic stresses."( Application of gamma-aminobutyric acid increased the level of phytohormones in Citrus sinensis.
Hijaz, F; Killiny, N; Nehela, Y, 2018
)
1.56
"Gamma-aminobutyric acid may act to inhibit brain areas involved in fear learning (e.g., the amygdala), and glutamate, acting at N-methyl-D-aspartate receptors, may play a role in the neural plasticity that permits this GABA-mediated inhibition to be exerted appropriately."( The role of glutamate and gamma-aminobutyric acid in fear extinction: clinical implications for exposure therapy.
Davis, M; Myers, KM, 2002
)
1.34
"Gamma-aminobutyric acid (GABA) plays a key role in the pathophysiology and treatment of depression and anxiety. "( Open-label tiagabine monotherapy for major depressive disorder with anxiety.
Carpenter, LL; Haggarty, R; Mello, AF; Mello, MF; Price, LH; Schecter, JM; Tyrka, AR, 2006
)
1.78
"Gamma-aminobutyric acid (GABA) plays a pivotal role in suppressing the origin and spread of seizure activity. "( Measuring human brain GABA in vivo: effects of GABA-transaminase inhibition with vigabatrin.
Petroff, OA; Rothman, DL, 1998
)
1.74
"The gamma-aminobutyric acid (GABA) system plays an important role in the early development of the hippocampal formation. "( Development of GABAergic neurons and their transporter in human temporal cortex.
Hachiya, Y; Takashima, S, 2001
)
0.87

Toxicity

The acute administration of an anticonvulsant dose of ethosuximide had no effect on brain gamma-aminobutyric acid (GABA) concentration. A toxic dose (400 mg/kg) increased significantly the concentration of brain GABA (1.5%)

ExcerptReferenceRelevance
" Pronounced [3H]GABA release could already be evoked on day 3 by N-methyl-D-aspartate, quisqualate and kainate, whereas toxic cell death could first be induced on day 7, in vitro."( Developmental dissociation of pharmacological and neurotoxic effects of excitatory amino acids.
Cai, NS; Erdö, SL, 1992
)
0.28
" To characterize better the selectivity of the toxic action of MPP+, other parameters were measured reflecting survival and function of dopaminergic or nondopaminergic neurons."( Toxicity of 1-methyl-4-phenylpyridinium for rat dopaminergic neurons in culture: selectivity and irreversibility.
Dandapani, BK; Hefti, F; Knusel, B; Michel, PP; Sanchez-Ramos, J, 1990
)
0.28
" GABA increases glutamate toxicity in a dose-dependent fashion, but NMDA and kainic acid were not toxic in the presence or absence of GABA."( gamma-Aminobutyric acid (GABA) enhances glutamate cytotoxicity in a cerebellar cell line.
Simantov, R, 1990
)
1.72
" One hundred to 300 microM was toxic for all cell types, and concentrations above 300 microM resulted in fixation."( Toxicity of 6-hydroxydopamine and dopamine for dopaminergic neurons in culture.
Hefti, F; Michel, PP, 1990
)
0.28
" Immature cortical neurons are insensitive to the toxic effects of glutamate receptor stimulation."( Glutamate toxicity in immature cortical neurons precedes development of glutamate receptor currents.
Baraban, JM; Murphy, TH, 1990
)
0.28
" THIP, even at toxic doses, did not alter the anti-PTZ activity of either pentobarbital or phenobarbital."( Effects of gamma-aminobutyric acid (GABA) receptor agonists on the neurotoxicity and anticonvulsant activity of barbiturates in mice.
Chweh, AY; Swinyard, EA; Ulloque, RA, 1986
)
0.66
"The acute administration of an anticonvulsant dose of ethosuximide (150 mg/kg) had no effect on brain gamma-aminobutyric acid (GABA) concentration, whereas a toxic dose (400 mg/kg) increased significantly the concentration of brain GABA (1."( Effect of ethosuximide alone and in combination with gamma-aminobutyric acid receptor agonists on brain gamma-aminobutyric acid concentration, anticonvulsant activity and neurotoxicity in mice.
Chweh, AY; Lin-Michell, E; Swinyard, EA, 1986
)
0.74
" These behavioral and neurochemical results are identical to those observed following concomitant destruction of striatonigral GABA and mesostriatal dopamine projections, and indicate that MPP+ may be toxic to GABAergic as well as to A10 and A9 dopaminergic neurons."( 1-Methyl-4-phenylpyridine (MPP+): regional dopamine neuron uptake, toxicity, and novel rotational behavior following dopamine receptor proliferation.
Altar, CA; Heikkila, RE; Manzino, L; Marien, MR, 1986
)
0.27
" The LD50 associated with seizure activity was lower in mice receiving MMT in propylene glycol (152 mg/kg) than in those receiving MMT in corn oil (999 mg/kg)."( Neurotoxic effects of methylcyclopentadienyl manganese tricarbonyl (MMT) in the mouse: basis of MMT-induced seizure activity.
Fishman, BE; Gianutsos, G; McGinley, PA, 1987
)
0.27
" Only ALA (10 microM) and glutamic acid (1 mM) were toxic towards neurons in culture, as measured by cell survival after 5 days' exposure."( [Mechanism of delta-aminolevulinic acid neurotoxicity].
Lamm, MC; McCarthy, BW; Neethling, AC; Percy, VA; Taljaard, JJ; Truter, L, 1981
)
0.26
" These findings argue strongly for a direct toxic effect of ethanol, and are furthermore compatible with behavioural changes in chronic alcoholics, dominated by memory impairment."( The neurotoxicity of ethanol.
Melgaard, B, 1983
)
0.27
" In an initial non-blinded study, L-glutamic acid (15 mM) exerted a significant toxic effect on HD fibroblasts, decreasing viability by approximately 60% after 48 h exposure."( Effects of L-glutamate on viabilities of cultured diploid skin fibroblasts and lymphocytes. Increased toxicity not observed in Huntington's disease.
Bird, TD; Casper, JB; Stahl, WL; Ward, CB,
)
0.13
"Plasma and brain levels of chlordecone in chlordecone-induced motor impairment, lethal levels of chlordecone, and cumulative LD50 of chlordecone in the mouse are presented."( Neurochemical evaluation of chlordecone toxicity in the mouse.
Chang-Tusi, H; Fujimori, K; Ho, IK; Huang, TP,
)
0.13
" However, results obtained with dispersed cells in culture may not necessarily reflect the situation in vivo where the cell may have a far greater resistance to the effects of toxic agents."( delta-Aminolaevulinic acid uptake, toxicity, and effect on [14C]gamma-aminobutyric acid uptake into neurons and glia in culture.
Lamm, MC; Percy, VA; Taljaard, JJ, 1981
)
0.5
" In order to demonstrate the existence of such a selective vulnerability, the toxic effects of rotenone, an inhibitor of complex I of the respiratory chain, and of glutamate, which is very likely involved in the neurotoxicity induced by an energetic stress, were analyzed on cultured mouse mesencephalic neurons."( A selective toxicity toward cultured mesencephalic dopaminergic neurons is induced by the synergistic effects of energetic metabolism impairment and NMDA receptor activation.
Gelman, M; Lévi-Strauss, M; Marey-Semper, I, 1995
)
0.29
" Finally, gabapentin is a very safe add-on medication."( The new anticonvulsant drugs. Implications for avoidance of adverse effects.
Krämer, G; Schmidt, D, 1994
)
0.29
" No adverse maternal or fetal effects were observed in mice or rats given doses up to 1500 or 3000 mg/kg, respectively."( Developmental toxicity studies in mice, rats, and rabbits with the anticonvulsant gabapentin.
Anderson, JA; Petrere, JA, 1994
)
0.29
" polylepis were toxic as determined by all four test methods."( Toxicity of four potentially ichthyotoxic marine phytoflagellates determined by four different test methods.
Edvardsen, B; Fonnum, F; Meldahl, AS, 1994
)
0.29
" Although adverse events occur in most patients receiving gabapentin as adjunctive therapy, they are transient and mild to moderate in severity."( Clinical efficacy and safety of gabapentin.
Ramsay, RE, 1994
)
0.29
" At the time of data cutoff, 30% of patients had withdrawn from the study due to lack of efficacy, and 4% due to adverse events."( The long-term safety and efficacy of gabapentin (Neurontin) as add-on therapy in drug-resistant partial epilepsy. The US Gabapentin Study Group.
, 1994
)
0.29
" Discontinuation resulting from adverse events were infrequent, occurring in 15% of patients receiving TGB compared to 5% receiving placebo."( Tiagabine: the safety landscape.
Leppik, IE, 1995
)
0.29
" It is well tolerated, with transient somnolence and dizziness being the most frequent adverse effects."( Gabapentin: pharmacokinetics, efficacy, and safety.
Beydoun, A; Sackellares, JC; Uthman, BM, 1995
)
0.29
" Adverse effects of antiepileptic treatment may affect the patient's quality of life to an even greater extent than the occurrence of seizures."( Adverse effects of established and new antiepileptic drugs: an attempted comparison.
Gram, L; Rogvi-Hansen, B, 1995
)
0.29
"Copper and manganese, two essential metals involved in physiological and physiopathological processes in the brain, were measured in corpora striata of rats 7 days after intrastriatal injection of quinolinic acid (QUIN, 240 nmol/l microliters), an N-methyl-D-aspartate (NMDA) receptor agonist with toxic activity."( Quinolinic acid neurotoxicity: in vivo increased copper and manganese content in rat corpus striatum after quinolinate intrastriatal injection.
Flores, A; Galván-Arzate, S; Osorio-Rico, L; Pérez, P; Ríos, C; Santamaría, A; Solís, F, 1996
)
0.29
"Standard antiepileptic drugs (AEDs) are associated with a wide variety of acute and chronic adverse events and with many interactions with each other and with non-AEDs that complicate patient management."( Overview of the safety of newer antiepileptic drugs.
Shorvon, S; Stefan, H, 1997
)
0.3
"We suggest that, in patients with mental retardation and epilepsy, involuntary movements may either occur as reversible side effects of gabapentin therapy or result from a previously undescribed adverse drug interaction with other antiepileptic agents."( Choreoathetosis as a side effect of gabapentin therapy in severely neurologically impaired patients.
Chudnow, RS; Dewey, RB; Lawson, CR, 1997
)
0.3
" One general rule that may reduce the risks of toxic drug interactions is to add medication to the patient's current regimen in modest doses and increase the dose slowly."( Mood stabilizer combinations: a review of safety and efficacy.
Freeman, MP; Stoll, AL, 1998
)
0.3
" Gabapentin is a new antiepileptic drug not appreciably metabolized by the liver in humans, and it appears to be safe and effective in the maintenance therapy of epilepsy in these patients."( Treatment of seizures in acute intermittent porphyria: safety and efficacy of gabapentin.
Brambilla, A; Erli, LC; Grandi, R; Mirabile, D; Zadra, M, 1998
)
0.3
" Two analyses of adverse events are presented: tolerability and safety."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
" Within these 281 patients, two mutually exclusive groups were compared (a) those reporting adverse events at only < or =1,800 mg/day (low dose); and (b) those reporting adverse events at only >1,800 mg/day (high dose)."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
"Gabapentin doses >1,800 mg/day were as well tolerated as doses < or =1,800 mg/day and were not associated with more adverse events."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
" We investigated whether this drug was comparable to standard first-line monotherapy in efficacy and incidence of adverse events."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.3
" After initial maintenance doses were reached, doses were adjusted downwards (in the case of adverse events) or upwards (in the case of seizures) by the clinician."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.3
"Time to withdrawal for lack of efficacy or adverse events did not differ between groups (p=0."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.3
"Although gabapentin seems also to be safe in children, the efficacy in refractory partial seizures was disappointing."( Gabapentin in childhood epilepsy: a prospective evaluation of efficacy and safety.
Boenigk, HE; Borusiak, P; Korn-Merker, E, 2000
)
0.31
" It has a relatively benign side effect profile, but little data exists on massive overdoses with this agent."( A case of sustained massive gabapentin overdose without serious side effects.
Radtke, RA; St Clair, EW; Verma, A, 1999
)
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
"Water hemlock, Cicuta virosa, belonging to the Umbelliferae, is well-known as a toxic plant responsible for lethal poisonings in humans as well as animals, causing tonic and clonic convulsions and respiratory paralysis."( Exploring the structural basis of neurotoxicity in C(17)-polyacetylenes isolated from water hemlock.
Kisara, K; Ohashi, K; Ohta, T; Oshima, Y; Sakakibara, R; Shibusawa, K; Tadano, T; Takaya, Y; Uwai, K, 2000
)
0.31
" However, on rare occasions, they can progress to more severe cutaneous disorders, including Stevens-Johnson syndrome and toxic epidermal necrolysis."( Therapeutic safety monitoring: what to look for and when to look for it.
Harden, CL, 2000
)
0.31
"The purpose of the present investigation was to determine whether the sensitivity to systemic toxic effects of cocaine is altered in genetically epilepsy-prone rats (GEPRs)."( Phenotypic expression of the systemic toxicity of cocaine in genetically epilepsy-prone rats.
Heavner, JE; Kao, YJ; Kaye, AD; Reigel, CE; Shi, B, 2000
)
0.31
" Serious adverse events were assessed individually."( Adverse event monitoring in lamotrigine patients: a pharmacoepidemiologic study in the United Kingdom.
Mawer, GE; Sander, JW; Wong, IC, 2001
)
0.31
" The adverse events with LTG reported by this study were similar to those reported in the literature."( Adverse event monitoring in lamotrigine patients: a pharmacoepidemiologic study in the United Kingdom.
Mawer, GE; Sander, JW; Wong, IC, 2001
)
0.31
" Life-threatening adverse reactions were rare."( Adverse event monitoring in lamotrigine patients: a pharmacoepidemiologic study in the United Kingdom.
Mawer, GE; Sander, JW; Wong, IC, 2001
)
0.31
" Weight gain, somnolence, nystagmus, and dizziness were the major adverse events in these patients, whereas ataxia, tremor, and diplopia were found with gabapentin in a dose higher than 1,800 mg/day."( Efficacy and safety of gabapentin as an add-on therapy in refractory partial epileptic patients.
Rungreangyingyod, L; Suthisisang, C; Towanabut, S, 2001
)
0.31
" The most frequent adverse events were dizziness (31%), fatigue (29%), somnolence (27%), headache (21%), and ataxia (20%), with no major increase seen in adverse events necessitating discontinuation as the dose of GBP was titrated upward."( AUStralian study of titration to effect profile of safety (AUS-STEPS): high-dose gabapentin (neurontin) in partial seizures.
Beran, R; Berkovic, S; Black, A; Danta, G; Dunne, J; Frasca, J; Grainger, K; Kilpatrick, C; McKenzie, R; McLaughlin, D; Schapel, G; Somerville, E, 2001
)
0.31
"We reviewed the reports in the literature on the safety, adverse effects and tolerance of GBP as treatment, used as monotherapy or associated with other drugs, in epilepsies in patients of all age groups, including children, adults and the elderly."( [Safety and tolerability of gabapentin].
Viteri, C,
)
0.13
" The commonest adverse effects seen were somnolence, fainting, ataxia, nystagmus, tremor and headache."( [Safety and tolerability of gabapentin].
Viteri, C,
)
0.13
" Mild adverse effects were seen in 62 patients (37."( [Effectiveness and safety of gabapentin in the preventive treatment of migraine].
Friera Acebal, G; Jiménez-Hernández, MD; Torrecillas Nárvaez, MD,
)
0.13
"Gabapentin can be considered an effective and safe drug in the preventive treatment of migraine."( [Effectiveness and safety of gabapentin in the preventive treatment of migraine].
Friera Acebal, G; Jiménez-Hernández, MD; Torrecillas Nárvaez, MD,
)
0.13
" Five hundred micromolar GABA and 50 microM tiagabine were not toxic in the presence or absence of light."( Acute vigabatrin retinotoxicity in albino rats depends on light but not GABA.
Benz, AM; Ishikawa, M; Izumi, M; Izumi, Y; Thio, LL; Zorumski, CF, 2004
)
0.32
"3 the corresponding values for phepyrone (irrespective of the LD50 values)."( [Functional-behavioral profile of new cyclic GABA analogs in acute toxicity tests].
Bugaeva, LI; Spasov, AA; Verovskiĭ, VE,
)
0.13
" It is assumed that adverse events occurring with gabapentin are dose related, their frequency and severity increasing with increasing doses."( Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia.
Huang, S; Parsons, B; Tive, L, 2004
)
0.32
"The aim of this study was to assess the dose dependence of adverse events with gabapentin by determining the relationship between increasing doses of gabapentin and the onset and/or worsening of adverse events in patients with PHN."( Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia.
Huang, S; Parsons, B; Tive, L, 2004
)
0.32
" The analysis of adverse events was based on 3 distinct groups: patients who received gabapentin <1800 mg/d, those who received gabapentin >or=1800 mg/d, and those who received placebo."( Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia.
Huang, S; Parsons, B; Tive, L, 2004
)
0.32
" The 3 most common adverse events were dizziness, somnolence, and peripheral edema."( Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia.
Huang, S; Parsons, B; Tive, L, 2004
)
0.32
" Dizziness and somnolence, the other most commonly occurring adverse events, were transient and did not occur more frequently or worsen with titration to >or=1800 mg/d."( Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia.
Huang, S; Parsons, B; Tive, L, 2004
)
0.32
" Safety/tolerability assessments included adverse events (AEs), physical and neurologic examinations, and clinical laboratory evaluation."( Safety and efficacy of two pregabalin regimens for add-on treatment of partial epilepsy.
Beydoun, A; Garofalo, EA; Greiner, MJ; Knapp, LE; Kugler, AR; Uthman, BM, 2005
)
0.33
"Fetal exposure to SSRI are associated to transient toxic symptoms of the neonates, likely to be an expression of excess serotonin activity in the CNS."( [SSRI during pregnancy and risk of fetal neurotoxicity. Follow precautions and look for other therapeutic alternatives].
Högberg, U; Wang, M,
)
0.13
" The aim of the study was to evaluate the frequency of AED utilisation and reported adverse events, in a cohort of MS patients."( Antiepileptic medications in multiple sclerosis: adverse effects in a three-year follow-up study.
Battaglia, MA; Brichetto, G; Mancardi, GL; Messmer Uccelli, M; Solaro, C, 2005
)
0.33
" The increased activities of ASS and ASL suggest the increased and effective recycling of citrulline to arginine in acute ammonia toxicity, making NO production more effective and contributing to its toxic effects."( Effects of acute ammonia toxicity on nitric oxide (NO), citrulline-NO cycle enzymes, arginase and related metabolites in different regions of rat brain.
Govindasamy, C; Nadiger, HA; Sirajudeen, KN; Swamy, M; Zakaria, AZ, 2005
)
0.33
" There is also a fairly broad consensus that gabapentin is safe and well tolerated, but the side-effect profile of gabapentin has not been adequately assessed in pain populations."( Adverse effects of gabapentin and lack of anti-allodynic efficacy of amitriptyline in the streptozotocin model of painful diabetic neuropathy.
Bourin, C; Chen, P; Hogan, JB; Leet, JE; Lindner, MD; Machet, F; McElroy, JF; Stock, DA, 2006
)
0.33
" Discontinuation rates due to associated adverse events were greatest in the venlafaxine treatment group: venlafaxine, 20."( Efficacy and safety of pregabalin in the treatment of generalized anxiety disorder: a 6-week, multicenter, randomized, double-blind, placebo-controlled comparison of pregabalin and venlafaxine.
Kasper, S; Montgomery, SA; Pande, AC; Tobias, K; Zornberg, GL, 2006
)
0.33
" Toxic potencies for MZ and MB were similar and no difference in sensitivity between the DA and GABA populations was observed with the fungicides."( Acute neurotoxic effects of mancozeb and maneb in mesencephalic neuronal cultures are associated with mitochondrial dysfunction.
Bernard, LP; Cooper, KR; Domico, LM; Zeevalk, GD, 2006
)
0.33
"A growing body of experimental evidence suggests that anaesthetics, by influencing GABAergic and glutaminergic neural signalling, can have adverse effects on the developing central nervous system."( Potentially toxic effects of anaesthetics on the developing central nervous system.
Gascon, E; Kiss, JZ; Klauser, P; Vutskits, L, 2007
)
0.34
"Polychlorinated biphenyls (PCBs) are persistent environmental contaminants that are highly toxic to the developing nervous system, particularly via their disruption of dopamine (DA) function."( Polychlorinated biphenyl-induced neurotoxicity in organotypic cocultures of developing rat ventral mesencephalon and striatum.
Lyng, GD; Seegal, RF; Snyder-Keller, A, 2007
)
0.34
" In this study we evaluated randomized, controlled trials examining the analgesic efficacy, adverse effects, and clinical value of gabapentinoids in postoperative pain."( Do surgical patients benefit from perioperative gabapentin/pregabalin? A systematic review of efficacy and safety.
Hamunen, K; Kalso, E; Kontinen, VK; Tiippana, EM, 2007
)
0.34
" Gabapentin reduced opioid-related adverse effects, such as nausea, vomiting, and urinary retention (number-needed-to-treat 25, 6, and 7, respectively)."( Do surgical patients benefit from perioperative gabapentin/pregabalin? A systematic review of efficacy and safety.
Hamunen, K; Kalso, E; Kontinen, VK; Tiippana, EM, 2007
)
0.34
"Gabapentinoids effectively reduce postoperative pain, opioid consumption, and opioid-related adverse effects after surgery."( Do surgical patients benefit from perioperative gabapentin/pregabalin? A systematic review of efficacy and safety.
Hamunen, K; Kalso, E; Kontinen, VK; Tiippana, EM, 2007
)
0.34
" As clinicians face a broader spectrum of efficacious treatments, side-effect profiles play an increasingly important role in the development of a pain management regimen."( Safety profile of treatment in diabetic peripheral neuropathic pain.
Robinson-Papp, J; Simpson, DM, 2007
)
0.34
" The most frequently reported adverse events were dizziness and somnolence, although tolerance to these developed within a few weeks."( Pregabalin: its efficacy, safety and tolerability profile in generalized anxiety.
Owen, RT, 2007
)
0.34
" It is known that dopamine (DA) enhances this toxic effect."( Endogenous dopamine enhances the neurotoxicity of 3-nitropropionic acid in the striatum through the increase of mitochondrial respiratory inhibition and free radicals production.
Cano, J; de Pablos, RM; Herrera, AJ; Machado, A; Navarro, A; Santiago, M; Tomás-Camardiel, M; Villarán, RF, 2008
)
0.35
" Overall, pregabalin was well tolerated with no new adverse events emerging that have not been reported with its use in other indications."( Pregabalin: its efficacy, safety and tolerability profile in fibromyalgia syndrome.
Owen, RT, 2007
)
0.34
" A global improvement, especially in anxious and depressive symptomatology, was observed; no adverse events were reported."( [Efficacy and safety of gabapentin in Borderline Personality Disorder: a six-month, open-label study].
Peris, L; Ruíz, M; Szerman, N,
)
0.13
" The adverse effects of gabapentin seem to vary from person to person and should be viewed with a high degree of suspicion, especially in patients taking this drug at the beginning."( Gabapentin toxicity: an important cause of altered consciousness in patients with uraemia.
Chen, CC; Chong, CF; Hung, TY; Seow, VK; Wang, TL, 2008
)
0.35
" The most common treatment-emergent adverse events were dizziness, somnolence, and peripheral edema."( Efficacy, safety, and tolerability of pregabalin treatment for painful diabetic peripheral neuropathy: findings from seven randomized, controlled trials across a range of doses.
Durso-Decruz, E; Emir, B; Freeman, R, 2008
)
0.35
" An additional four patients dropped out during the study, and one stopped taking medication due to adverse events."( Efficacy and safety of pregabalin in alcohol dependence.
Bria, P; Di Nicola, M; Janiri, L; Martinotti, G; Mazza, M; Tedeschi, D, 2008
)
0.35
" Pregabalin was well-tolerated, with almost all adverse events in the mild-to-moderate range, and self-limiting (median duration of 4-16 days)."( Efficacy and safety of pregabalin in elderly people with generalised anxiety disorder.
Baldinetti, F; Chatamra, K; Montgomery, S; Pauer, L; Whalen, E, 2008
)
0.35
"Pregabalin, in doses of 150-600 mg/day, was a safe and effective treatment of generalised anxiety disorder in patients 65 years and older."( Efficacy and safety of pregabalin in elderly people with generalised anxiety disorder.
Baldinetti, F; Chatamra, K; Montgomery, S; Pauer, L; Whalen, E, 2008
)
0.35
" Patients administering lidocaine plaster experienced fewer drug-related adverse events (3."( Efficacy and safety of 5% lidocaine (lignocaine) medicated plaster in comparison with pregabalin in patients with postherpetic neuralgia and diabetic polyneuropathy: interim analysis from an open-label, two-stage adaptive, randomized, controlled trial.
Baron, R; Binder, A; Leijon, G; Mayoral, V; Serpell, M; Steigerwald, I, 2009
)
0.35
"After 4 weeks, 5% lidocaine medicated plaster treatment was associated with similar levels of analgesia in patients with PHN or DPN but substantially fewer frequent adverse events than pregabalin."( Efficacy and safety of 5% lidocaine (lignocaine) medicated plaster in comparison with pregabalin in patients with postherpetic neuralgia and diabetic polyneuropathy: interim analysis from an open-label, two-stage adaptive, randomized, controlled trial.
Baron, R; Binder, A; Leijon, G; Mayoral, V; Serpell, M; Steigerwald, I, 2009
)
0.35
" Safety evaluation included adverse events (AEs), drug-related AEs (DRAEs), and withdrawal due to AEs."( Efficacy and safety of combination therapy with 5% lidocaine medicated plaster and pregabalin in post-herpetic neuralgia and diabetic polyneuropathy.
Baron, R; Binder, A; Leijon, G; Mayoral, V; Serpell, M; Steigerwald, I, 2009
)
0.35
"In patients with PHN and painful DPN failing to respond to monotherapy, combination therapy with 5% lidocaine medicated plaster and pregabalin provides additional clinically relevant pain relief and is safe and well-tolerated."( Efficacy and safety of combination therapy with 5% lidocaine medicated plaster and pregabalin in post-herpetic neuralgia and diabetic polyneuropathy.
Baron, R; Binder, A; Leijon, G; Mayoral, V; Serpell, M; Steigerwald, I, 2009
)
0.35
"Gabapentin was found to be partially effective and safe in symptomatic treatment of CTS patients."( The efficacy and safety of gabapentin in carpal tunnel patients: open label trial.
Erdemoglu, AK,
)
0.13
" Acute human toxicity related to adverse neuronal function is usually a result of over-excitation or depression of the nervous system."( GABAA receptor and cell membrane potential as functional endpoints in cultured neurons to evaluate chemicals for human acute toxicity.
Babot, Z; Forsby, A; Galofré, M; García, DA; Iraola, S; Rodríguez-Farré, E; Suñol, C,
)
0.13
"The incidence of constipation as an adverse effect of pregabalin has previously been reported as low, with all cases described as either mild or moderate."( Severe and disabling constipation: an adverse effect of pregabalin.
Cook, MJ; D'Souza, WJ; Kamel, JT, 2010
)
0.36
" The proportions of patients with any adverse event, somnolence or dizziness were also significantly greater with pregabalin than with placebo."( Pregabalin in fibromyalgia: meta-analysis of efficacy and safety from company clinical trial reports.
Derry, S; McQuay, HJ; Moore, RA; Straube, S, 2010
)
0.36
"8%); toxic manifestations were more severe in group III than in group II."( Gabapentin toxicity in patients with chronic kidney disease: a preventable cause of morbidity.
McKian, KP; Qian, Q; Zand, L, 2010
)
0.36
" Titration (dose escalation) regimens based on clinical judgment were implemented to mitigate this adverse event and reduce patient dropout across clinical trials."( Modeling dropout from adverse event data: impact of dosing regimens across pregabalin trials in the treatment of generalized anxiety disorder.
Frame, B; Hutmacher, M; Lalovic, B; Miller, R, 2011
)
0.37
" The commonly reported adverse events were dizziness, somnolence, peripheral edema and weight gain, and most of them were mild to moderate in intensity."( [Long-term efficacy and safety of pregabalin in patients with postherpetic neuralgia: results of a 52-week, open-label, flexible-dose study].
Arakawa, A; Ogawa, S; Suzuki, M; Yoshiyama, T, 2010
)
0.36
" Treatments were generally well tolerated; discontinuation rates due to adverse events were 4%, 2%, 5%, 0%, and 1% with standard- and low-dose pregabalin/tolterodine ER, pregabalin, tolterodine ER, and placebo, respectively."( Investigation of the clinical efficacy and safety of pregabalin alone or combined with tolterodine in female subjects with idiopathic overactive bladder.
Cossons, NH; Darekar, A; Marencak, J; Mills, IW, 2011
)
0.37
" Safety was based on adverse events (AEs)."( Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 clinical studies.
Cheung, R; Emir, B; Murphy, TK; Semel, D; Zlateva, G, 2010
)
0.36
" Pregabalin was well tolerated; somnolence (26%), dizziness (24%), peripheral oedema (13%) and weight gain (11%) were the most common adverse events and generally were reported as mild to moderate."( Efficacy and safety of pregabalin for treating neuropathic pain associated with diabetic peripheral neuropathy: a 14 week, randomized, double-blind, placebo-controlled trial.
Arakawa, A; Baba, M; Satoh, J; Shoji, S; Suzuki, M; Yagihashi, S; Yoshiyama, T, 2011
)
0.37
" Adverse events were more frequent with pregabalin than with placebo and caused discontinuation in 9 (8."( Safety and efficacy of pregabalin in patients with central post-stroke pain.
Bashford, G; Cheung, R; Dror, V; Kim, JS; Martin, A; Murphy, KT, 2011
)
0.37
" We aimed at identifying treatment emergent adverse events (AEs) associated with pregabalin through a systematic review and meta-analysis of all available RCTs."( The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials.
Gangemi, P; Perucca, P; Specchio, L; Zaccara, G, 2011
)
0.37
"Information about the time course of adverse drug reactions (ADRs) is often lacking."( Longitudinal monitoring of the safety of drugs by using a web-based system: the case of pregabalin.
Grootheest, K; Härmark, L; Puijenbroek, E, 2011
)
0.37
" Safety was evaluated using adverse events (AEs)."( Pregabalin or placebo used adjunctively with levetiracetam in refractory partial-onset epilepsy: a post hoc efficacy and safety analysis in combined clinical trials.
Almas, M; Emir, B; Giordano, S; Leon, T; Uthman, BM, 2011
)
0.37
" Adverse events were typical of pregabalin and, in general, did not vary as the number of concomitant AEDs increased."( The impact of background antiepileptic drugs on the efficacy and safety of pregabalin in treating partial-onset seizures: a post hoc analysis of combined clinical trials.
Almas, M; Cabrera, J; Giordano, S; Tomson, T, 2011
)
0.37
"To report a case of acute elevation of hepatic enzyme levels as a probable adverse reaction associated with pregabalin."( Pregabalin-induced hepatotoxicity.
Junyent, TT; Pellicer, MJ; Sendra, JM, 2011
)
0.37
" Reported adverse effects were also analysed."( Efficacy and safety of perioperative pregabalin for post-operative pain: a meta-analysis of randomized-controlled trials.
Cateloy, F; Engelman, E, 2011
)
0.37
"Efficacious and safe monotherapy options are needed for adult patients with newly diagnosed epilepsy."( Efficacy and safety of pregabalin versus lamotrigine in patients with newly diagnosed partial seizures: a phase 3, double-blind, randomised, parallel-group trial.
Brodie, MJ; Kälviäinen, R; Knapp, LE; Kwan, P; Weaver, J; Yurkewicz, L, 2011
)
0.37
" The overall incidence of adverse events was similar between the groups and consistent with that in previous studies; dizziness (55 [17%] vs 45 [14%] patients), somnolence (29 [9%] vs 14 [4%]), fatigue (27 [8%] vs 19 [6%]), and weight increase (21 [6%] vs 7 [2%]) were numerically more common in the pregabalin group than in the lamotrigine group."( Efficacy and safety of pregabalin versus lamotrigine in patients with newly diagnosed partial seizures: a phase 3, double-blind, randomised, parallel-group trial.
Brodie, MJ; Kälviäinen, R; Knapp, LE; Kwan, P; Weaver, J; Yurkewicz, L, 2011
)
0.37
" International Restless Legs Syndrome Scale (IRLS) score, investigator- and patient-rated Clinical Global Impression (CGI) scores, Pittsburgh Sleep Quality Index (PSQI) total scores and subscores, and short form (SF)-36 subscores were assessed, and adverse events (AEs) were monitored."( Long-term efficacy and safety of gabapentin enacarbil in Japanese restless legs syndrome patients.
Hattori, N; Hirata, K; Inoue, Y; Kuroda, K; Uchimura, N, 2012
)
0.38
"Pregabalin and placebo were equally safe and well tolerated."( Efficacy and safety of pregabalin in the treatment of alcohol withdrawal syndrome: a randomized placebo-controlled trial.
Förg, A; Hein, J; Heinz, A; Müller, CA; Richter, C; Volkmar, K; Winter, M,
)
0.13
"In a recent meta-analysis of 38 double-blind randomized controlled trials (RCTs) comparing pregabalin (PGB) to placebo, we found 20 adverse events (AEs) to be significantly associated with PGB treatment."( The adverse event profile of pregabalin across different disorders: a meta-analysis.
Gangemi, PF; Perucca, P; Zaccara, G, 2012
)
0.38
" The most common adverse reactions (incidence ≥ 20%) with single-agent use are fatigue, nausea, and anorexia."( Pemetrexed-induced cellulitis: a rare toxicity in non-small cell lung cancer treatment.
Katsenos, S; Panagou, C; Psara, A, 2013
)
0.39
"The adverse effect profile of this medication from controlled, randomized studies as well as open and long-term studies is described with consideration of the evidence-based results for pregabalin's clinical use."( Drug safety evaluation of pregabalin.
Toth, C, 2012
)
0.38
" Pregabalin use is associated with benign central nervous system and systemic adverse effects with very limited metabolic, idiosyncratic, or teratogenic adverse effects."( Drug safety evaluation of pregabalin.
Toth, C, 2012
)
0.38
"9%) permanently discontinued study participation due to treatment-emergent adverse events (all causality) at 12 weeks (pooled data) and 53 of 429 (12."( Safety profile and tolerability of up to 1 year of pregabalin treatment in 3 open-label extension studies in patients with fibromyalgia.
Arnold, LM; Emir, B; Murphy, TK; Pauer, L; Petersel, D; Scott, G; Zeiher, BG, 2012
)
0.38
"The data from these extension studies suggest that the adverse event safety profile and tolerability of patients with FM treated with open-label pregabalin (75-300 mg BID) for up to 1 year were stable and were consistent with those of previous studies."( Safety profile and tolerability of up to 1 year of pregabalin treatment in 3 open-label extension studies in patients with fibromyalgia.
Arnold, LM; Emir, B; Murphy, TK; Pauer, L; Petersel, D; Scott, G; Zeiher, BG, 2012
)
0.38
" The relative scarcity and controversial evidential status of available pharmacological interventions for the treatment of patients' acute withdrawal syndrome and/or relapse prevention call for the clinical investigation of novel safe and efficacious agents."( Efficacy and safety of pregabalin in the treatment of alcohol and benzodiazepine dependence.
Konstantakopoulos, G; Oulis, P, 2012
)
0.38
"Available evidence suggests that monotherapy with pregabalin, within the dosage range of 150 - 600 mg/d, is a promising "novel" option for the safe and efficacious relapse prevention of both AD and BD."( Efficacy and safety of pregabalin in the treatment of alcohol and benzodiazepine dependence.
Konstantakopoulos, G; Oulis, P, 2012
)
0.38
"Pregabalin is one of the first-line treatments for painful diabetic peripheral neuropathy in many countries, and we have administered it to relieve the neurotoxicity associated with adverse effects of VCR in a DLBCL patient treated with the R-CHOP regimen."( [A case of neurotoxicity reduced with pregabalin in R-CHOP chemotherapy for diffuse large B-cell lymphoma].
Hosokawa, A; Ito, T; Kiba, T; Kido, M; Kimura, A; Kozawa, K; Nakashima, T; Niimi, H; Ogawa, Y; Okada, Y; Okikawa, Y; Saito, A; Shintani, H; Taniguchi, T; Taniyama, K, 2012
)
0.38
" We found no differences in the offspring mice with regard to their cognitive function and mood or mRNA neurotransmitter receptor gene expression in several brain areas, including 5-HT(1A), MOR₁ and GABA(Aα1), suggesting the absence of adverse effects of postnatal exposure to ∑6 NDL-PCBs under these conditions."( Neurodevelopmental and behavioral toxicity via lactational exposure to the sum of six indicator non-dioxin-like-polychlorinated biphenyls (∑6 NDL-PCBs) in mice.
Bouayed, J; Desor, F; Diesel, B; Elnar, AA; Feidt, C; Kiemer, AK; Soulimani, R, 2012
)
0.38
" The 2 most commonly reported adverse events were somnolence and dizziness."( A randomized, double-blind, placebo-controlled, dose-response study to assess the pharmacokinetics, efficacy, and safety of gabapentin enacarbil in subjects with restless legs syndrome.
Atluri, H; Bonzo, D; Chen, D; Cundy, KC; Ellenbogen, A; Hurt, J; Lal, R; Lassauzet, ML; Luo, W; Tovera, J; Vu, A; Zomorodi, K,
)
0.13
" Efficacy data showed that a once-daily dose of GEn 600 to 2400 mg provides greater relief of RLS symptoms than placebo; GEn was generally well tolerated with an adverse event profile consistent with gabapentin."( A randomized, double-blind, placebo-controlled, dose-response study to assess the pharmacokinetics, efficacy, and safety of gabapentin enacarbil in subjects with restless legs syndrome.
Atluri, H; Bonzo, D; Chen, D; Cundy, KC; Ellenbogen, A; Hurt, J; Lal, R; Lassauzet, ML; Luo, W; Tovera, J; Vu, A; Zomorodi, K,
)
0.13
" Descriptive safety data from the original trials were reviewed and the most commonly reported adverse events (AEs; dizziness, somnolence, peripheral oedema and weight gain) were identified to be of primary interest."( Pregabalin treatment for peripheral neuropathic pain: a review of safety data from randomized controlled trials conducted in Japan and in the west.
Arakawa, A; Ogawa, S; Satoh, J; Suzuki, M; Yoshiyama, T, 2012
)
0.38
" After the treatment, more than 95% of the initial blue product was removed from the waste solution and the treated waste was proven to be safe for aquatic organisms, as studied in brine shrimp and guppy fishes."( "From safe source to safe sink" development of colorimetric assay for gabapentin in bulk drug and capsules using naturally derived genipin.
Dejpittayanunt, S; Kongpakwattana, K; Nuntharatanapong, N; Pathomcharoensukchai, S; Rojanarata, T; Suksaran, U; Winotapun, W, 2012
)
0.38
" Treatment was generally well tolerated, with somnolence and dizziness the most frequently reported adverse events."( A randomized, double-blind, multicenter, placebo-controlled phase III trial to evaluate the efficacy and safety of pregabalin in Japanese patients with fibromyalgia.
Nishioka, K; Ohkura, M; Ohta, H; Oka, H; Suzuki, M; Usui, C, 2012
)
0.38
"Treatment options for postherpetic neuralgia (PHN), a complication of herpes zoster, are commonly unsatisfactory and associated with adverse events."( Once-daily gastroretentive gabapentin for postherpetic neuralgia: integrated efficacy, time to onset of pain relief and safety analyses of data from two phase 3, multicenter, randomized, double-blind, placebo-controlled studies.
Irving, GA; Rauck, RL; Sweeney, M; Vanhove, GF; Wallace, MS, 2013
)
0.39
" The most frequently reported adverse events were dizziness (G-GR, 11%; placebo, 2%) and somnolence (G-GR, 5%; placebo, 3%)."( Once-daily gastroretentive gabapentin for postherpetic neuralgia: integrated efficacy, time to onset of pain relief and safety analyses of data from two phase 3, multicenter, randomized, double-blind, placebo-controlled studies.
Irving, GA; Rauck, RL; Sweeney, M; Vanhove, GF; Wallace, MS, 2013
)
0.39
" The most common treatment-related adverse events were somnolence, dizziness, increased weight, and constipation."( An open-label long-term phase III extension trial to evaluate the safety and efficacy of pregabalin in Japanese patients with fibromyalgia.
Nishioka, K; Ohkura, M; Ohta, H; Oka, H; Suzuki, M; Usui, C, 2013
)
0.39
"These data indicate that the long-term treatment of Japanese FM patients with pregabalin may be both safe and effective."( An open-label long-term phase III extension trial to evaluate the safety and efficacy of pregabalin in Japanese patients with fibromyalgia.
Nishioka, K; Ohkura, M; Ohta, H; Oka, H; Suzuki, M; Usui, C, 2013
)
0.39
" Despite its essentiality, at excessive levels Mn is toxic to the central nervous system (CNS)."( Manganese toxicity in the central nervous system: the glutamine/glutamate-γ-aminobutyric acid cycle.
Aschner, M; Sidoryk-Wegrzynowicz, M, 2013
)
0.39
" Safety assessments included the incidence and severity of adverse events (AEs), the occurrence of serious AEs, changes in physical and neurological examination findings, clinical laboratory assessments, and changes in weight."( Long-term safety of gastroretentive gabapentin in postherpetic neuralgia patients.
Irving, G; Jensen, MP; Rauck, R; Sweeney, M; Vanhove, GF; Wallace, M, 2013
)
0.39
" The primary endpoint was a ≥1/3 reduction in pain (NRS); secondary endpoints included the time to analgesia and adverse effects."( Randomised phase II trial (NCT00637975) evaluating activity and toxicity of two different escalating strategies for pregabalin and oxycodone combination therapy for neuropathic pain in cancer patients.
Bianchi, A; Bramati, A; Carbone, C; Farina, G; Febbraro, A; Ganzinelli, M; Garassino, MC; Gentili, M; Iorno, V; La Verde, N; Marabese, M; Moretti, A; Piva, S; Spagnoletti, I; Torri, V, 2013
)
0.39
" The most commonly reported adverse events were dizziness and somnolence."( A randomized, double-blind, placebo-controlled trial to assess the efficacy and safety of gabapentin enacarbil in subjects with neuropathic pain associated with postherpetic neuralgia (PXN110748).
Bell, CF; Chen, C; Freeman, R; Graff, O; Harden, RN; Harding, K; Hunter, S; Kavanagh, S; Laurijssens, B; McClung, C; Rainka, M; Schwartzbach, C; Warren, S; Zhang, L, 2013
)
0.39
"5%) was the only treatment-related adverse event (AE) occurring ≥10%."( Long-term treatment of anxiety disorders with pregabalin: a 1 year open-label study of safety and tolerability.
Emir, B; Haswell, H; Montgomery, S; Prieto, R, 2013
)
0.39
" Weight loss and numbness were common adverse effects in the topiramate group."( Comparison of efficacy and safety of topiramate with gabapentin in migraine prophylaxis: randomized open label control trial.
Ahmed, S; Alam, R; Khan, M; Zafar, I; Zain, S, 2013
)
0.39
" While there was a decrease in total patient-reported adverse events in the once nightly arm, the lack of specificity in relation to a particular adverse event suggested no real difference in adverse events."( Twice daily versus once nightly dosing of pregabalin for fibromyalgia: a double-blind randomized clinical trial of efficacy and safety.
Kivitz, AJ; Maricic, MJ; Nasser, K; Silver, DS; Silverman, SL, 2014
)
0.4
" Adverse events (AEs) were also compared between treatment groups."( Efficacy and safety of pregabalin in patients with spinal cord injury: a pooled analysis.
Emir, B; Juhn, M; Parsons, B; Sanin, L; Yang, R, 2013
)
0.39
" Endpoints were responder rate, seizure frequency, adverse events, and anxiety symptoms."( Efficacy and safety of pregabalin in refractory focal epilepsy with and without comorbid anxiety disorders - results of an open-label, parallel group, investigator-initiated, proof-of-concept study.
Brandt, C; Fueratsch, N; May, TW; Pohlmann-Eden, B; Schoendienst, M; Schrecke, M; Trentowska, M; Witte-Boelt, K, 2013
)
0.39
" A total of 12 subjects in the gabapentin group and 15 subjects in the amitriptyline group experienced adverse events which were of mild to moderate grades."( A comparative study of efficacy and safety of gabapentin versus amitriptyline as coanalgesics in patients receiving opioid analgesics for neuropathic pain in malignancy.
Banerjee, M; Basu, J; Bhattacharya, B; Ghosh, B; Mondal, S; Pal, S,
)
0.13
"This paper presents a new analytical method for the simultaneous determination of baclofen and gabapentin in feeds based on two modified quick, easy, cheap, effective, rugged and safe (QuEChERS) sample preparation methods and liquid chromatography tandem mass spectrometry (LC-MS/MS)."( Evaluation of two modified quick, easy, cheap, effective, rugged and safe (QuEChERS) sample preparation methods for the analysis of baclofen and gabapentin in feeds by liquid chromatography tandem mass spectrometry.
Chen, RX; Hou, XL; Lv, Y; Wu, YL; Xu, XQ; Zhu, Y, 2014
)
0.4
" In 28-37% of patients, pregabalin was associated with adverse events, with drowsiness and dizziness being frequently observed."( [Efficacy and safety of pregabalin for oxaliplatin- and paclitaxel-induced peripheral neuropathy].
Itabashi, T; Kashiwaba, M; Kudo, K; Nihei, S; Sato, J; Takahashi, K, 2013
)
0.39
"Treatment of postherpetic neuralgia (PHN) is more complicated in elderly patients, and multiple daily dosing, complex titration, and high incidences of adverse events can be limiting for many pharmacological treatment options."( Safety and efficacy of once-daily gastroretentive gabapentin in patients with postherpetic neuralgia aged 75 years and over.
Gupta, A; Li, S, 2013
)
0.39
" We chose the number of patients experiencing = 50% reduction in pain and number of patient withdrawals due to adverse events (AE) as primary outcomes for efficacy and safety, respectively."( Comparative efficacy and safety of six antidepressants and anticonvulsants in painful diabetic neuropathy: a network meta-analysis.
Bansal, D; Bhansali, A; Ghai, B; Gudala, K; Hota, D; Rudroju, N; Talakokkula, ST,
)
0.13
"Gabapentin was found to be most efficacious and amitriptyline to be least safe among the treatments included in the study."( Comparative efficacy and safety of six antidepressants and anticonvulsants in painful diabetic neuropathy: a network meta-analysis.
Bansal, D; Bhansali, A; Ghai, B; Gudala, K; Hota, D; Rudroju, N; Talakokkula, ST,
)
0.13
" Gabapentin misuse is possible, similar to other medications not typically considered drugs of abuse, but it should be considered safe and appropriate for use in patients with all types of SUDs, including patients who take opioid drugs."( Gabapentin for Substance Use Disorders: Is it Safe and Appropriate?
Howland, RH, 2014
)
0.4
" However, gabapentin increased the somnolence (RR 2·03; 95% CI 1·39, 2·98; I(2)  = 2%), dizziness (RR 2·68; 95% CI 1·95, 3·69; I(2)  = 15%), peripheral oedema (RR 9·10; 95% CI 3·23, 25·60; I(2)  = 2%), total adverse effects (RR 1·28; 95% CI 1·16, 1·42; I(2)  = 0%) and withdrawal due to adverse events (RR 1·51; 95% CI 1·06, 2·16; I(2)  = 6%), but these adverse effects were often mild to moderate."( Efficacy and safety of gabapentin 1800 mg treatment for post-herpetic neuralgia: a meta-analysis of randomized controlled trials.
Cao, H; Fan, H; Hu, X; Li, J; Shao, Y; Wang, J; Yu, W; Zhang, Q, 2014
)
0.4
" Gabapentin 1800 mg appeared safe in treating PHN for up to 24 weeks."( Efficacy and safety of gabapentin 1800 mg treatment for post-herpetic neuralgia: a meta-analysis of randomized controlled trials.
Cao, H; Fan, H; Hu, X; Li, J; Shao, Y; Wang, J; Yu, W; Zhang, Q, 2014
)
0.4
" Discontinuation because of adverse events was significantly greater in the duloxetine (19."( Comparative safety and tolerability of duloxetine vs. pregabalin vs. duloxetine plus gabapentin in patients with diabetic peripheral neuropathic pain.
Irving, G; Malcolm, S; Raskin, J; Risser, RC; Tanenberg, RJ, 2014
)
0.4
"Duloxetine, pregabalin and duloxetine plus gabapentin were generally safe and tolerable for the treatment of DPNP."( Comparative safety and tolerability of duloxetine vs. pregabalin vs. duloxetine plus gabapentin in patients with diabetic peripheral neuropathic pain.
Irving, G; Malcolm, S; Raskin, J; Risser, RC; Tanenberg, RJ, 2014
)
0.4
"Lead (Pb) is a heavy metal that is toxic to numerous physiological processes."( Novel dose-dependent alterations in excitatory GABA during embryonic development associated with lead (Pb) neurotoxicity.
Cannon, JR; Freeman, JL; Lee, JW; Weber, GJ; Wirbisky, SE, 2014
)
0.4
"Pregabalin administration is occasionally abandoned due to adverse events such as somnolence, dizziness, unsteadiness, weight gain and edema."( Factors predicting adverse events associated with pregabalin administered for neuropathic pain relief.
Hosokawa, T; Kanbayashi, Y; Onishi, K,
)
0.13
"To identify factors predicting adverse events associated with pregabalin administered for neuropathic pain."( Factors predicting adverse events associated with pregabalin administered for neuropathic pain relief.
Hosokawa, T; Kanbayashi, Y; Onishi, K,
)
0.13
" Variables were extracted from the clinical records for regression analysis of factors related to the occurrence of adverse events associated with pregabalin administration."( Factors predicting adverse events associated with pregabalin administered for neuropathic pain relief.
Hosokawa, T; Kanbayashi, Y; Onishi, K,
)
0.13
"The results of the present study indicate that care is warranted regarding long durations of therapy for somnolence, advanced age rather than dose-dependent adverse events for unsteadiness, elevated serum creatinine level for weight gain, and elevated serum creatinine level and combination use of neurotropin for edema."( Factors predicting adverse events associated with pregabalin administered for neuropathic pain relief.
Hosokawa, T; Kanbayashi, Y; Onishi, K,
)
0.13
" The aim of this review was to provide an update of current knowledge of adverse events (AE) associated with the most common perioperative non-opioid analgesics: paracetamol, non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticoids (GCCs), gabapentinoids and their combinations."( Adverse effects of perioperative paracetamol, NSAIDs, glucocorticoids, gabapentinoids and their combinations: a topical review.
Dahl, JB; Hamunen, K; Hansen, MS; Kjer, JJ; Kontinen, VK; Mathiesen, O; Nikolajsen, L; Pommergaard, HC; Rosenberg, J; Wetterslev, J, 2014
)
0.4
" If future pregnancy registry data confirm this positive safety profile, gabapentin therapy would likely be a safe and effective treatment for RLS during pregnancy."( Potential maternal symptomatic benefit of gabapentin and review of its safety in pregnancy.
Guttuso, T; Shaman, M; Thornburg, LL, 2014
)
0.4
" Safety assessments included adverse events (AEs), clinical laboratory tests, and electrocardiograms."( Efficacy and safety of mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study.
Feins, K; Hsu, C; Merante, D; Rosenstock, J; Sharma, U; Vinik, A, 2014
)
0.4
" Delayed corneal reepithelialization was a common side effect of both topical anesthetics and topical NSAIDs."( Efficacy and safety of pain relief medications after photorefractive keratectomy: review of prospective randomized trials.
Faktorovich, EG; Melwani, K, 2014
)
0.4
" Two children experienced serious adverse events, one of whom received pregabalin 15 mg/kg/day."( Safety, tolerability, and pharmacokinetics of pregabalin in children with refractory partial seizures: a phase 1, randomized controlled study.
Alvey, CW; Bockbrader, H; Chew, ML; Liu, J; Mann, D; Pellock, J; Pitman, VW; Zegarac, E, 2014
)
0.4
" However, narcotics can have significant adverse effects."( Safety and tolerability of gabapentin for aneurysmal subarachnoid hemorrhage (sah) headache and meningismus.
Dhakal, LP; Freeman, WD; Hodge, DO; Mayes, M; Nagal, J; Nagel, J; Ng, LK; Richie, A, 2015
)
0.42
"GBP appears to be relatively safe and tolerable in SAH patients with headache and may be a useful narcotic-sparing agent to prevent narcotics-associated complications, such as gastrointestinal immobility, ileus, and constipation."( Safety and tolerability of gabapentin for aneurysmal subarachnoid hemorrhage (sah) headache and meningismus.
Dhakal, LP; Freeman, WD; Hodge, DO; Mayes, M; Nagal, J; Nagel, J; Ng, LK; Richie, A, 2015
)
0.42
"Weight gain and alopecia were the most common patient-reported CSEs in this study, and weight gain was the most likely cosmetic side effect to result in dosage adjustment or medication discontinuation."( Cosmetic side effects of antiepileptic drugs in adults with epilepsy.
Buchsbaum, R; Chen, B; Choi, H; Detyniecki, K; Hirsch, LJ; Javed, A; Kato, K; Legge, A; Moeller, J, 2015
)
0.42
" Despite its essentiality, at excessive levels Mn is toxic to the central nervous system."( Impairment of glutamine/glutamate-γ-aminobutyric acid cycle in manganese toxicity in the central nervous system.
Sidoryk-Wegrzynowicz, M, 2014
)
0.4
" A discussion of pregabalin dosing and adverse events is also presented."( Pregabalin for painful diabetic peripheral neuropathy: strategies for dosing, monotherapy vs. combination therapy, treatment-refractory patients, and adverse events.
Juhn, MS; Parsons, B; Sadosky, A; Varvara, R, 2015
)
0.42
"To characterize risk factors for occurrence of adverse events (AEs) and treatment discontinuations due to AEs for improving safety and tolerability of treatment of postherpetic neuralgia (PHN)."( Relationships Among Adverse Events, Disease Characteristics, and Demographics in Treatment of Postherpetic Neuralgia With Gastroretentive Gabapentin.
Bucior, I; Nalamachu, S; Shaparin, N; Slattum, PW, 2015
)
0.42
" Otherwise, it has been described to produce a large number of adverse effects among them cell death mediated mainly by blockage of K(+) channels."( Neuroprotective or neurotoxic effects of 4-aminopyridine mediated by KChIP1 regulation through adjustment of Kv 4.3 potassium channels expression and GABA-mediated transmission in primary hippocampal cells.
Baselga, MJA; Capo, MA; Del Pino, J; Díaz, MJ; Frejo, MT; García, JM; Moyano, P, 2015
)
0.42
" Considering that GAB was found in raw drinking water, the formation of toxic PTPs during drinking water treatment with UV light might be possible."( Identification of phototransformation products of the antiepileptic drug gabapentin: Biodegradability and initial assessment of toxicity.
Herrmann, M; Kümmerer, K; Menz, J; Olsson, O, 2015
)
0.42
" To gather information on prevalence of use, desired effects and/or adverse effects, we searched grey literature (online drug discussion forums) and medical literature (PubMed and abstracts from selected International Toxicology conferences)."( Phenibut (4-amino-3-phenyl-butyric acid): Availability, prevalence of use, desired effects and acute toxicity.
Archer, JR; Dargan, PI; Owen, DR; Wood, DM, 2016
)
0.43
" According to the grey literature, phenibut is taken for its anxiolytic and euphoric properties, with tolerance and withdrawal syndromes commonly reported adverse effects."( Phenibut (4-amino-3-phenyl-butyric acid): Availability, prevalence of use, desired effects and acute toxicity.
Archer, JR; Dargan, PI; Owen, DR; Wood, DM, 2016
)
0.43
" Its desired and adverse effects appear similar to other gamma-aminobutyric acid receptor agonists."( Phenibut (4-amino-3-phenyl-butyric acid): Availability, prevalence of use, desired effects and acute toxicity.
Archer, JR; Dargan, PI; Owen, DR; Wood, DM, 2016
)
0.68
" Although the adverse effects of this compound are well documented in various species, the full modes of action (MoAs) are still not well characterized."( Whole-Organism Transcriptomic Analysis Provides Mechanistic Insight into the Acute Toxicity of Emamectin Benzoate in Daphnia magna.
Evenseth, LM; Gomes, T; Høgåsen, T; Iguchi, T; Rundberget, JT; Song, Y; Tollefsen, KE; Xie, L, 2016
)
0.43
" Removal of this potential adverse effect with adjuvant intervention(s) would represent a significant advance in epilepsy therapeutics."( Aberrant mTOR signaling and disrupted autophagy: The missing link in potential vigabatrin-associated ocular toxicity?
Ainslie, GR; Gibson, KM; Pearl, PL; Vogel, KR, 2017
)
0.46
" Adverse event were monitored and summarized."( Efficacy and Safety of Gabapentin in Comparison to Solifenacin Succinate in Adult Overactive Bladder Treatment.
Balingit, JC; Chua, ME; Esmeňa, EB; Morales, ML; See, MC, 2018
)
0.48
" Summary effect for migraine headache days, headache frequency, at least 50% reduction in headache attacks, all-adverse events, nausea, somnolence, dizziness, withdrawal and withdrawal due to adverse events were produced by synthesizing both direct and indirect evidence."( Unveiling the relative efficacy, safety and tolerability of prophylactic medications for migraine: pairwise and network-meta analysis.
He, A; Li, C; Song, D; Zhang, L, 2017
)
0.46
" Patients' demographic and clinical characteristics, resource utilization data and adverse drug reactions (ADRs) as described in the leaflet were extracted."( Characteristics, resource utilization and safety profile of patients prescribed with neuropathic pain treatments: a real-world evidence study on general practices in Europe - the role of the lidocaine 5% medicated plaster.
Katz, P; Liedgens, H; Pegoraro, V, 2017
)
0.46
" These results raise the possibility that the phenobarbital-induced adverse effects could be reduced by a co-treatment with caffeine."( Caffeine Protects Against Anticonvulsant-Induced Neurotoxicity in the Developing Rat Brain.
Bendix, I; Bührer, C; Endesfelder, S; Schiller, C; Sifringer, M; Weichelt, U, 2017
)
0.46
"Although propofol is a widely used intravenous general anaesthetic, many studies report its toxic potential, particularly on the developing central nervous system."( Neurotoxicity of propofol on rat hypoglossal motoneurons in vitro.
Corsini, S; Ghezzi, F; Monni, L; Nistri, A, 2017
)
0.46
"This meta-analysis of randomized controlled trials (RCTs) was performed to compare the use of gabapentin with placebo in open hysterectomy regarding (1) the mean difference (MD) of postoperative opioid requirements; (2) the changes of visual analogue scale (VAS) scores in two groups; and (3) incidence rate of adverse effects."( Is gabapentin effective and safe in open hysterectomy? A PRISMA compliant meta-analysis of randomized controlled trials.
Han, C; Li, XD; Yu, WL, 2017
)
0.46
" They necessitate prolonged use and are associated with adverse effects and increased cost."( Benefits and safety of gabapentinoids in chronic low back pain: A systematic review and meta-analysis of randomized controlled trials.
AlAmri, R; Bhandari, M; Devereaux, PJ; Gilron, I; Kamath, S; Rajarathinam, M; Shanthanna, H; Thabane, L, 2017
)
0.46
"Existing evidence on the use of gabapentinoids in CLBP is limited and demonstrates significant risk of adverse effects without any demonstrated benefit."( Benefits and safety of gabapentinoids in chronic low back pain: A systematic review and meta-analysis of randomized controlled trials.
AlAmri, R; Bhandari, M; Devereaux, PJ; Gilron, I; Kamath, S; Rajarathinam, M; Shanthanna, H; Thabane, L, 2017
)
0.46
" The present research was to test the hypothesis that Mn causes putrescine accumulation over a physiologically adequate to toxic concentration range in a neuronal cell line."( Putrescine as indicator of manganese neurotoxicity: Dose-response study in human SH-SY5Y cells.
Chandler, JD; Fernandes, J; Go, YM; Jones, DP; Liu, KH; Uppal, K, 2018
)
0.48
"0001], but were more likely to experience incidence of adverse events, such as somnolence, dizziness, and peripheral edema."( A Meta-Analysis of Therapeutic Efficacy and Safety of Gabapentin in the Treatment of Postherpetic Neuralgia from Randomized Controlled Trials.
Dai, ZG; Gao, CX; Li, L; Ma, KT; Si, JQ; Wang, S; Zhang, M, 2018
)
0.48
" Number and type of adverse events were similar between the three groups."( Safety and efficacy of GABA
Audoli-Inthavong, ML; Bassetti, CL; Chabriat, H; Hermann, DM; Lambert, E; Marx, U; Sors, A; Wattez, M, 2020
)
0.56
" elegans did not cause significant toxic reaction in the rats after long-term exposure."( A comprehensive toxicity evaluation in rats after long-term oral Gelsemium elegans exposure.
Huang, CY; Huang, SJ; Liu, ZY; Wang, N; Wang, ZY; Wu, Y; Yu, H; Zhao, XJ; Zuo, MT, 2021
)
0.62
" The application of GABA had a significant effect on alleviating the adverse effect of ammonia poisoning, and 80-100 mg/kg treatment exerted the best effect."( Effects of ammonia toxicity on the histopathology, detoxification, oxidative stress, and immune response of the cuttlefish Sepia pharaonis and the mitigation of γ-aminobutyric acid.
Chen, S; Jiang, M; Jiang, X; Li, J; Liang, Y; Lin, J; Peng, R; Wu, Y, 2022
)
0.72
"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
"4 mg/kg/h was safe and well tolerated by all mild or moderate hepatic impairment subjects and normal hepatic function subjects."( Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment.
Chen, H; Ding, Y; Hu, Y; Li, C; Li, X; Liu, J; Liu, X; Lou, J; Ma, S; Wang, X; Wu, M; Wu, N; Xuan, C; Yan, P; Zhang, H; Zheng, W; Zhu, X, 2022
)
0.72
"Acrolein (ACR) and formaldehyde (FA) are toxic aldehydes co-produced in foods."( Cytotoxicity of a Novel Compound Produced in Foods via the Reaction of Amino Acids with Acrolein along with Formaldehyde.
Hu, J; Ou, J; Ou, S, 2022
)
0.72
" The majority of adverse events pertained to the nervous system (7 effects) or psychiatric (3 effects) disorders."( The safety and efficacy of gabapentinoids in the management of neuropathic pain: a systematic review with meta-analysis of randomised controlled trials.
Eldabe, S; Meaadi, J; Nazar, H; Obara, I, 2023
)
0.91
"Despite RCTs documenting the adverse events of gabapentionoids on the nervous system, there was no evidence of gabapentinoid use leading to addiction, suggesting an urgent need to design studies investigating their abusive potential."( The safety and efficacy of gabapentinoids in the management of neuropathic pain: a systematic review with meta-analysis of randomised controlled trials.
Eldabe, S; Meaadi, J; Nazar, H; Obara, I, 2023
)
0.91
"Although gamma-aminobutyric acid-benzodiazepine (GABA-BZ) receptor agonists are used to treat insomnia, their long-term or high-dosage use causes adverse events."( Efficacy and safety of lemborexant as an alternative drug for patients with insomnia taking gamma-aminobutyric acid-benzodiazepine receptor agonists or suvorexant.
Inamoto, A; Iwanami, A; Kawai, K; Okino, K; Sanada, K; Suzuki, H; Tomioka, H, 2023
)
1.55
"The novel dual orexin receptor antagonist lemborexant (LEM) has fewer adverse effects than GABA-BZ receptor agonists."( Efficacy and safety of lemborexant as an alternative drug for patients with insomnia taking gamma-aminobutyric acid-benzodiazepine receptor agonists or suvorexant.
Inamoto, A; Iwanami, A; Kawai, K; Okino, K; Sanada, K; Suzuki, H; Tomioka, H, 2023
)
1.13
" The safety and tolerability of GABA-BZ receptor agonists and SUX were high, and no serious adverse effects were observed after switching to LEM."( Efficacy and safety of lemborexant as an alternative drug for patients with insomnia taking gamma-aminobutyric acid-benzodiazepine receptor agonists or suvorexant.
Inamoto, A; Iwanami, A; Kawai, K; Okino, K; Sanada, K; Suzuki, H; Tomioka, H, 2023
)
1.13

Pharmacokinetics

ExcerptReferenceRelevance
"The influence of progabide, a new antiepileptic drug, on the pharmacokinetic profiles of phenobarbital, phenytoin, carbamazepine, and valproic acid was evaluated in four separate studies, each including six young healthy volunteers."( Pharmacokinetic interactions of progabide with other antiepileptic drugs.
Bianchetti, G; Morselli, PL; Padovani, P; Thénot, JP; Thiercelin, JF,
)
0.13
" The present study was, therefore, planned to confirm blood-barrier crossing by Ca AOTA and to study the drug's physicochemical and pharmacokinetic characteristics."( Physicochemical, pharmacological and pharmacokinetic study of a new GABAergic compound, calcium acetylhomotaurinate.
Andre, D; Boismare, F; Boucly, P; Chabenat, C; Chretien, P; Daoust, M; Lhuintre, JP; Moore, N; Saligaut, C, 1988
)
0.27
"This paper describes the pharmacokinetic studies of 1-(aminomethyl)-cyclohexane acetic acid (gabapentin, Gö 3450, CI-945) conducted with the 14C-labelled substance following intravenous and intragastric administration to rats and dogs and oral administration to humans."( Pharmacokinetics and metabolism of gabapentin in rat, dog and man.
Kölle, EU; Vollmer, KO; von Hodenberg, A, 1986
)
0.27
"The pharmacokinetic profile of progabide was investigated in five chronically catheterized male rhesus monkeys."( Pharmacokinetic profile of progabide, a new gamma-aminobutyric acid-mimetic drug, in rhesus monkey.
Johno, I; Levy, RH; Ludwick, BT, 1982
)
0.53
" Pharmacodynamic interactions take place at the level of receptor sites, where they may have additive or potentiating effects."( Pharmacokinetic and pharmacodynamic drug interactions during treatment with vigabatrin.
Richens, A, 1995
)
0.29
" Pharmacokinetic parameters were calculated by standard noncompartmental methods."( Pharmacokinetics of tiagabine, a gamma-aminobutyric acid-uptake inhibitor, in healthy subjects after single and multiple doses.
Gustavson, LE; Mengel, HB, 1995
)
0.57
"Only valproyl glycinamide showed a good anticonvulsant profile in both mice and rats due to its better pharmacokinetic profile."( Pharmacokinetic analysis and antiepileptic activity of N-valproyl derivatives of GABA and glycine.
Bialer, M; Hadad, S, 1995
)
0.29
" The current study demonstrates the benefit of the SPPR approach in developing and selecting a potent antiepileptic compound in intact animals based not only on its intrinsic pharmacodynamic activity, but also on its better pharmacokinetic profile."( Pharmacokinetic analysis and antiepileptic activity of N-valproyl derivatives of GABA and glycine.
Bialer, M; Hadad, S, 1995
)
0.29
" The plasma VGB concentration-time data were analyzed by mixed-effects modeling to estimate population pharmacokinetic parameters and to identify any significant demographic covariates."( A comparison of population and standard two-stage pharmacokinetic analyses of vigabatrin data.
Bhargava, VO; Hutcheson, SJ; Wei, G; Weir, SJ; Yu, DK, 1994
)
0.29
"With the introduction of three new anti-epileptic drugs (AEDs) in the UK during the past 4 years as adjunctive add-on therapy, the possibility of AED pharmacokinetic interactions has become a relevant consideration."( Phenobarbitone to gabapentin: a guide to 82 years of anti-epileptic drug pharmacokinetic interactions.
Patsalos, PN, 1994
)
0.29
" The elimination half-life is approximately 5 to 9 hours."( Clinical pharmacokinetics of gabapentin.
McLean, MJ, 1994
)
0.29
" Apparent oral plasma clearance (CL/F) and renal clearance (CLR) of gabapentin decreased and maximum plasma concentration, time to reach maximum concentration, and half-life values increased as renal function diminished."( Pharmacokinetics of gabapentin in subjects with various degrees of renal function.
Blum, RA; Bockbrader, H; Busch, JA; Comstock, TJ; Keller, E; Reece, PA; Reetze, P; Schultz, RW; Sica, DA; Tuerck, D, 1994
)
0.29
" Three of the new drugs, gabapentin, topiramate and vigabatrin, are more promising on the basis of their pharmacokinetic features."( Comparative pharmacokinetics of the newer antiepileptic drugs.
Bialer, M, 1993
)
0.29
"To assess the possible occurrence of pharmacokinetic interactions between the antiepileptic agents felbamate and vigabatrin, two randomized, double-blind, placebo-controlled, crossover studies were conducted in healthy male volunteers."( Pharmacokinetic interaction studies between felbamate and vigabatrin.
Banfield, C; Colucci, R; Glue, P; Lim, J; Lin, C; Meehan, J; Nomeir, A; Radwanski, E; Reidenberg, P; Rey, E, 1995
)
0.29
" The terminal elimination half-life (t1/2z) is relatively long in neonates; it then decreases during the first postnatal month to lower values than in adults, and then progressively increases with age due to an age-dependent decrease in the metabolic rate."( Clinical pharmacokinetics of antiepileptic drugs in paediatric patients. Part II. Phenytoin, carbamazepine, sulthiame, lamotrigine, vigabatrin, oxcarbazepine and felbamate.
Avanzini, G; Battino, D; Estienne, M, 1995
)
0.29
"Antiepileptic drugs (AEDs) in broad use today have a number of pharmacokinetic liabilities, including a propensity for clinically meaningful drug interactions."( Pharmacokinetic profile of topiramate in comparison with other new antiepileptic drugs.
Perucca, E, 1996
)
0.29
"Gabapentin is a new antiepileptic drug (AED) with an attractive pharmacokinetic profile."( Gabapentin: pharmacokinetics, efficacy, and safety.
Beydoun, A; Sackellares, JC; Uthman, BM, 1995
)
0.29
" The BBB influx (CL1) and efflux (CL2) permeabilities of GBP were estimated with a hybrid pharmacokinetic model assuming that transport between intra- and extracellular space was more rapid than transport across the BBB."( The simultaneous estimation of the influx and efflux blood-brain barrier permeabilities of gabapentin using a microdialysis-pharmacokinetic approach.
Wang, Y; Welty, DF, 1996
)
0.29
" All the drugs can be conveniently given as a twice daily dosage apart from gabapentin, which has a short half-life and a midday dose is needed."( Clinical pharmacokinetics of newer antiepileptic drugs. Lamotrigine, vigabatrin, gabapentin and oxcarbazepine.
Binnie, CD; Elwes, RD, 1996
)
0.29
" Calculated pharmacokinetic parameters included Cmax' Tmax' AUC and T1/2."( Effect of a high-protein meal on gabapentin pharmacokinetics.
Budde, J; Gidal, BE; Jones, JC; Lensmeyer, GL; Maly, MM; Pitterle, ME, 1996
)
0.29
"This article surveys the pharmacokinetic parameters for the new antiepileptic drugs (AEDs): felbamate, gabapentin, lamotrigine, oxcarbazepine, tiagabine, topiramate, and vigabatrin."( Pharmacokinetics of new antiepileptic drugs.
Gram, L, 1996
)
0.29
" The pharmacokinetic parameters of the two enantiomers have been studied after administration of a single oral 125 mg dose of the racemate to six neonates."( Pharmacokinetics of the individual enantiomers of vigabatrin in neonates with uncontrolled seizures.
Chiron, C; d'Athis, P; Dulac, O; Dumas, C; Olive, G; Pons, G; Rey, E; Vauzelle-Kervroëdan, F, 1996
)
0.29
" Plasma tiagabine concentrations were determined by high-performance liquid chromatography; pharmacokinetic parameters were calculated using noncompartmental methods."( Pharmacokinetics of tiagabine as add-on therapy in patients taking enzyme-inducing antiepilepsy drugs.
Cascino, GD; Graves, NM; Gustavson, LE; Leppik, IE; Pixton, GC; So, EL; Wolff, D, 1995
)
0.29
"Standard antiepileptic drugs (AEDs) have a number of pharmacokinetic shortcomings, and AEDs with more favorable profiles would be preferred."( Pharmacokinetics and interaction profile of topiramate: review and comparison with other newer antiepileptic drugs.
Johannessen, SI, 1997
)
0.3
" A pharmacokinetic study of the S(+) and R(-) enantiomers of vigabatrin was performed before and during dialysis."( Pharmacokinetics of the S(+) and R(-) enantiomers of vigabatrin during chronic dosing in a patient with renal failure.
Chiron, C; Guillonneau, M; Jacqz-Aigrain, E; Loirat, C; Macher, MA; Montes, C; Rey, E, 1997
)
0.3
" This study examined the single-dose pharmacokinetic profiles of Li in 13 patients receiving placebo and then steady-state gabapentin (mean daily dose: 3,646."( Gabapentin does not alter single-dose lithium pharmacokinetics.
Corá-Locatelli, G; Dunn, RT; Frye, MA; Grothe, D; Ketter, TA; Kimbrell, TA; Piscitelli, S; Post, RM; Vanderham, E, 1998
)
0.3
" GBP concentrations in plasma and urine were measured by high-performance liquid chromatography, and pharmacokinetic parameters were calculated by noncompartmental methods."( Effects of age and gender on single-dose pharmacokinetics of gabapentin.
Abel, RB; Bockbrader, HN; Boyd, RA; Sedman, AJ; Türck, D, 1999
)
0.3
" No change in maximal GBP plasma concentration (Cmax), time at which Cmax occurred (tmax), or apparent volume of distribution (V/F) with age was noted."( Effects of age and gender on single-dose pharmacokinetics of gabapentin.
Abel, RB; Bockbrader, HN; Boyd, RA; Sedman, AJ; Türck, D, 1999
)
0.3
" For all drugs that are metabolized, half-life is shortened and clearance is increased when patients receive concomitant enzyme-inducing agents such as barbiturates, phenytoin, and carbamazepine."( The clinical pharmacokinetics of the new antiepileptic drugs.
Perucca, E, 1999
)
0.3
" Orally administered GBP did not significantly alter the pharmacokinetic parameters of parenteral PT."( Effect of vigabatrin and gabapentin on phenytoin pharmacokinetics in the dog.
Al-Hassan, MI; Bawazir, SA; Matar, KM; Nicholls, PJ; Tekle, A, 2000
)
0.31
"5-30 Hz) of the EEG as derived by fast Fourier transformation analysis was used as pharmacodynamic endpoint."( Pharmacokinetic-pharmacodynamic modelling of tiagabine CNS effects upon chronic treatment in rats: lack of change in concentration-EEG effect relationship.
Altorf, BA; Cleton, A; Danhof, M; Voskuyl, RA, 2000
)
0.31
" Plots of pharmacokinetic parameters versus age suggested significant differences between younger (1 month to < 5 years) and older (> or =5 to 12 years) subjects."( Single-dose gabapentin pharmacokinetics and safety in healthy infants and children.
Bockbrader, HN; Boellner, SW; Brown, RR; Haig, GM; Ouellet, D; Posvar, EL; Randinitis, EJ; Wesche, DL, 2001
)
0.31
" Orally administered GBP did not significantly alter the pharmacokinetic parameters of parental PT."( Effect of vigabatrin and gabapentin on phynytoin pharmacokinetics in the dog.
al-Hassan, MI; Bawazir, SA; Matar, KM; Nicholls, PJ; Tekle, A,
)
0.13
" In the meantime, a review of the established pharmacokinetic and pharmacodynamic activities of these agents is the first step in defining their optimal uses and limitations in the psychiatric setting."( Pharmacokinetics of new anticonvulsants in psychiatry.
Morris, HH, 1998
)
0.3
" Pregabalin pharmacokinetic parameters were evaluated by established noncompartmental methods."( Pharmacokinetics of pregabalin in subjects with various degrees of renal function.
Alvey, CW; Bockbrader, HN; Cook, JA; Posvar, EL; Randinitis, EJ; Sedman, AJ, 2003
)
0.32
"The pharmacokinetic properties of a drug are the primary deter-minant of the extent and duration of drug action, and influence susceptibility to clinically important drug interactions."( The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come?
Johannessen, SI; Perucca, E, 2003
)
0.32
" Pharmacokinetic parameters for gabapentin were determined by non-compartment methods using multivariate regression analysis."( Pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures.
Lo, W; Nahata, MC; Tallian, KB; Tsao, CY, 2004
)
0.32
"Data from nine patients were suitable for pharmacokinetic analysis."( Pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures.
Lo, W; Nahata, MC; Tallian, KB; Tsao, CY, 2004
)
0.32
" Likewise, PGB steady-state pharmacokinetic parameter values were similar among patients receiving CBZ, PHT, LTG, or VPA and, in general, were similar to those observed historically in healthy subjects receiving PGB alone."( Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy.
Alvey, CW; Bockbrader, HN; Brodie, MJ; Bron, NJ; Gibson, GL; Hounslow, NJ; Posvar, EL; Randinitis, EJ; Wesche, DL; Wilson, EA, 2005
)
0.33
" The pharmacokinetic parameters such as AUC(0."( Pharmacokinetics and bioequivalence evaluation of two gabapentin preparations after a single oral dose in healthy Korean volunteers.
Cho, HY; Kang, HA; Lee, YB, 2006
)
0.33
" No statistically significant difference was found for tmax and t1/2 values."( Pharmacokinetics and bioequivalence evaluation of two gabapentin preparations after a single oral dose in healthy Korean volunteers.
Cho, HY; Kang, HA; Lee, YB, 2006
)
0.33
" For drugs that are eliminated renally completely unchanged (gabapentin, pregabalin and vigabatrin) or mainly unchanged (levetiracetam and topiramate), the pharmacokinetic variability is less pronounced and more predictable."( Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed?
Johannessen, SI; Tomson, T, 2006
)
0.33
" The pharmacokinetic profile of GBP was examined."( The effect of MDR1 G2677T/A polymorphism on pharmacokinetics of gabapentin in healthy Korean subjects.
Cho, HY; Kang, HA; Lee, YB, 2007
)
0.34
"A sensitive validated liquid chromatography-tandem mass spectrometric method (LC-MS/MS) for gabapentin (GB) in human plasma has been developed and applied to pharmacokinetic (PK) and bioequivalence (BE) studies in human."( Validated LC-MS/MS method for quantification of gabapentin in human plasma: application to pharmacokinetic and bioequivalence studies in Korean volunteers.
Jhee, OH; Kang, JS; Kim, KH; Kim, YS; Lee, JH; Lee, JS; Lee, MH; Park, JH; Park, SH; Shaw, LM, 2007
)
0.34
" A single dose (600 mg) of each formulation was orally administered to four beagle dogs under fasted conditions, and the pharmacokinetic parameters were calculated."( In Vitro/in vivo relationship of gabapentin from a sustained-release tablet formulation: a pharmacokinetic study in the beagle dog.
Han, SB; Jeon, JW; Lee, DS; Lee, TW; Nam, TY; Oh, TO; Park, CW; Park, ES; Park, S; Rhee, YS, 2008
)
0.35
"To investigate the pharmacokinetic interrelationship of vigabatrin in blood and the brain (frontal cortex vs."( Vigabatrin extracellular pharmacokinetics and concurrent gamma-aminobutyric acid neurotransmitter effects in rat frontal cortex and hippocampus using microdialysis.
Patsalos, PN; Ratnaraj, N; Tong, X, 2009
)
0.6
" In contrast, levetiracetam was without affect on tiagabine or vigabatrin concentrations and co-administration with gabapentin, tiagabine or vigabatrin had no effect on levetiracetam brain concentrations, indicating the pharmacodynamic nature of interaction between these antiepileptic drugs in the mouse pentylenetetrazole model."( Pharmacodynamic and pharmacokinetic interaction profiles of levetiracetam in combination with gabapentin, tiagabine and vigabatrin in the mouse pentylenetetrazole-induced seizure model: an isobolographic analysis.
Andres-Mach, MM; Czuczwar, SJ; Dudra-Jastrzebska, M; Luszczki, JJ; Patsalos, PN; Ratnaraj, N; Sielski, M, 2009
)
0.35
" Inclusion of such a pharmacokinetic compartment into the patch model introduced a slow kinetic component in the extracellular exchange time course, thereby providing recapitulation of divergent whole cell results."( Pentobarbital produces activation and block of {alpha}1{beta}2{gamma}2S GABAA receptors in rapidly perfused whole cells and membrane patches: divergent results can be explained by pharmacokinetics.
Burkat, PM; Gingrich, KJ; Roberts, WA, 2009
)
0.35
" The focus of this study was to determine the influence of sildenafil on the pharmacokinetics (PK) of pregabalin with the objective of informing the design of a quantitative pharmacodynamic (PD) study."( Population pharmacokinetic model of the pregabalin-sildenafil interaction in rats: application of simulation to preclinical PK-PD study design.
Bender, G; Bies, R; Danhof, M; DeJongh, J; Field, M; Florian, J; Gosset, J; Marshall, S; Tan, K, 2009
)
0.35
" Noncompartmental analysis was used to estimate pharmacokinetic variables."( Pharmacokinetics of single-dose oral pregabalin administration in normal dogs.
Badgley, BL; Dewey, CW; Gleed, RD; Horne, W; Ludders, JW; Salazar, V; Schwark, W, 2009
)
0.35
" The median (range) pharmacokinetic parameters were: Area under the curve from time 0 to 36 hours = 81."( Pharmacokinetics of single-dose oral pregabalin administration in normal dogs.
Badgley, BL; Dewey, CW; Gleed, RD; Horne, W; Ludders, JW; Salazar, V; Schwark, W, 2009
)
0.35
" Pharmacokinetic parameters were determined with computer software."( Pharmacokinetics of oral gabapentin in greyhound dogs.
Cohen, RL; Kukanich, B, 2011
)
0.37
" We demonstrate that diazepam variously modulates theta (4-7 Hz), alpha (7-14 Hz), beta (15-25 Hz), and gamma (30-80 Hz) frequency oscillations in specific regions of the cortex, with a pharmacodynamic profile consistent with that of drug uptake."( Neuronal network pharmacodynamics of GABAergic modulation in the human cortex determined using pharmaco-magnetoencephalography.
Barnes, GR; Furlong, PL; Hall, SD; Hillebrand, A; Seri, S, 2010
)
0.36
" Data from all subjects were used for pharmacokinetic and safety analyses unless stated otherwise."( The effect of food with varying fat content on the clinical pharmacokinetics of gabapentin after oral administration of gabapentin enacarbil.
Cundy, KC; Huff, FJ; Lal, R; Luo, W; Sukbuntherng, J; Zou, J, 2010
)
0.36
" Pregabalin elimination half-life is approximately 6 hours and steady state is achieved within 1 to 2 days of repeated administration."( Clinical pharmacokinetics of pregabalin in healthy volunteers.
Alvey, CW; Bockbrader, HN; Boyd, RA; Busch, JA; Corrigan, BW; Haig, GM; Posvar, EL; Radulovic, LL; Randinitis, EJ; Strand, JC; Wesche, DL, 2010
)
0.36
" The pharmacokinetics of gabapentin delivered from this extended-release formulation allows a reduced dosing frequency while maintaining bioavailability and possibly diminishing the occurrence of adverse events attributable to a slower increase to the peak concentration compared with the immediate-release dosage form."( Pharmacokinetics of gabapentin in a novel gastric-retentive extended-release formulation: comparison with an immediate-release formulation and effect of dose escalation and food.
Chen, C; Cowles, VE; Hou, E, 2011
)
0.37
" After IV administration, the mean +/- SEM apparent volume of the central compartment, apparent volume of distribution at steady state, and clearance and the harmonic mean +/- jackknife pseudo-SD for terminal half-life were 90."( Pharmacokinetics of gabapentin in cats.
Ilkiw, JE; Pypendop, BH; Siao, KT, 2010
)
0.36
"Pregabalin and gabapentin share a similar mechanism of action, inhibiting calcium influx and subsequent release of excitatory neurotransmitters; however, the compounds differ in their pharmacokinetic and pharmacodynamic characteristics."( A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin.
Bockbrader, HN; Burger, P; Chapel, S; Janiczek, N; Miller, R; Wesche, D, 2010
)
0.36
"Gabapentin is being used in horses although its pharmacokinetic (PK) profile, pharmacodynamic (PD) effects and safety in the equine are not fully investigated."( Pharmacokinetic profile and behavioral effects of gabapentin in the horse.
Driessen, B; Liu, Y; McDonnell, SM; Moate, PJ; Soma, LR; Terry, RL; Uboh, CE; Van Eps, AW, 2010
)
0.36
" Plasma drug concentrations were determined over 48h post-administration by liquid chromatography/mass spectrometry followed by non-compartmental pharmacokinetic analysis."( Pharmacokinetics of oral gabapentin alone or co-administered with meloxicam in ruminant beef calves.
Coetzee, JF; Cull, CA; Kelly, LL; Kohake, LE; KuKanich, B; Mosher, RA; Mueting, SL, 2011
)
0.37
" The aim of this study was to develop a population pharmacokinetic model and quantify the influence of covariates on the parameters."( Population pharmacokinetics of pregabalin in healthy subjects and patients with post-herpetic neuralgia or diabetic peripheral neuropathy.
Bockbrader, HN; Matsui, S; Shoji, S; Suzuki, M; Tomono, Y, 2011
)
0.37
"This pregabalin population pharmacokinetic analysis was conducted on data from 14 clinical trials involving healthy subjects, subjects with impaired renal function and patients with post-herpetic neuralgia or diabetic peripheral neuropathy (n= 616)."( Population pharmacokinetics of pregabalin in healthy subjects and patients with post-herpetic neuralgia or diabetic peripheral neuropathy.
Bockbrader, HN; Matsui, S; Shoji, S; Suzuki, M; Tomono, Y, 2011
)
0.37
" To evaluate if pregabalin coadministration affects pharmacokinetics of other antiepileptic drugs, population pharmacokinetic analyses using NONMEM software were performed on data from three epilepsy trials involving seven antiepileptic drugs with pregabalin as add-on therapy."( Pregabalin effect on steady-state pharmacokinetics of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, valproate, and tiagabine.
Bockbrader, HN; Burger, P; Knapp, L, 2011
)
0.37
"The objective of this study was to describe a population pharmacokinetic analysis of gabapentin enacarbil in patients with varying degrees of renal function, using data from an open-label study of gabapentin enacarbil in patients with renal impairment (XenoPort, Inc."( Clinical pharmacokinetics of gabapentin after administration of gabapentin enacarbil extended-release tablets in patients with varying degrees of renal function using data from an open-label, single-dose pharmacokinetic study.
Blumenthal, R; Chen, D; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J, 2012
)
0.38
" Pharmacokinetic data were compared with those from Phase I-III studies in subjects with normal renal function to evaluate the relationship between gabapentin oral clearance (CL/F) and CrCL."( Clinical pharmacokinetics of gabapentin after administration of gabapentin enacarbil extended-release tablets in patients with varying degrees of renal function using data from an open-label, single-dose pharmacokinetic study.
Blumenthal, R; Chen, D; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J, 2012
)
0.38
" The method was proved to be selective, sensitive, rapid and suitable for pharmacokinetic study of gabapentin in human plasma."( [LC-MS/MS method for quantification and pharmacokinetic study of gabapentin in human plasma].
He, JF; Li, FM; Qin, F; Xiong, ZL; Yu, J, 2011
)
0.37
" Plasma and milk drug concentrations were determined over 7 days postadministration by HPLC/MS followed by noncompartmental pharmacokinetic analyses."( Pharmacokinetics and milk secretion of gabapentin and meloxicam co-administered orally in Holstein-Friesian cows.
Coetzee, JF; Gehring, R; Kukanich, B; Malreddy, PR, 2013
)
0.39
" Therefore, pharmacokinetic of gabapentin is essential for patients who have to receive gabapentin 600 mg."( Pharmacokinetic of gabapentin 600 mg tablet in Thai healthy subjects.
Chompootaweep, S; Khemsri, W; Prompila, N; Punyasang, W; Sayankuldilok, N; Thaworn, N; Wittayalertpanya, S, 2012
)
0.38
"To investigate the pharmacokinetic of gabapentin 600 mg in Thai healthy subjects."( Pharmacokinetic of gabapentin 600 mg tablet in Thai healthy subjects.
Chompootaweep, S; Khemsri, W; Prompila, N; Punyasang, W; Sayankuldilok, N; Thaworn, N; Wittayalertpanya, S, 2012
)
0.38
" The relevant pharmacokinetic parameters were determined."( Pharmacokinetic of gabapentin 600 mg tablet in Thai healthy subjects.
Chompootaweep, S; Khemsri, W; Prompila, N; Punyasang, W; Sayankuldilok, N; Thaworn, N; Wittayalertpanya, S, 2012
)
0.38
"The data show the pharmacokinetic parameters of gabapentin 600 mg."( Pharmacokinetic of gabapentin 600 mg tablet in Thai healthy subjects.
Chompootaweep, S; Khemsri, W; Prompila, N; Punyasang, W; Sayankuldilok, N; Thaworn, N; Wittayalertpanya, S, 2012
)
0.38
" Pharmacokinetic sampling was conducted over a 24-hour period at the end of each study period."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
"The pharmacokinetic profile of gabapentin-ER may allow for once- or twice-daily dosing while maintaining bioavailability and thus efficacy."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
" Two different gabapentin to pregabalin transition designs were simulated based on their respective population pharmacokinetic profiles."( Gabapentin to pregabalin therapy transition: a pharmacokinetic simulation.
Bockbrader, HN; Budhwani, MN; Wesche, DL, 2013
)
0.39
"Pregabalin , the S-enantiomer of 3-aminomethyl-5-methylhaxanoic acid, is a second-generation antiepileptic drug (AED) developed after gabapentin with improved pharmacokinetic and pharmacodynamics properties."( Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy.
Schulze-Bonhage, A, 2013
)
0.39
" The article also looks at its clinical application as a combination therapy with particular respect to its pharmacokinetic profile."( Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy.
Schulze-Bonhage, A, 2013
)
0.39
"This review aims to analyze pharmacokinetic profile, plasma level variations so as the metabolism, interactions and possible relation to clinical effect of several drugs which are used primarily as anxiolytics."( Understanding the pharmacokinetics of anxiolytic drugs.
Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013
)
0.39
"There is a need for a more balanced assessment of the benefits and risks associated with benzodiazepine use, particularly considering pharmacokinetic profile of the drugs to ensure that patients, who would truly benefit from these agents, are not denied appropriate treatment."( Understanding the pharmacokinetics of anxiolytic drugs.
Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013
)
0.39
" The differences in the dosing frequency and tolerability between G-IR and GR are mainly because of the difference in formulations and thus pharmacokinetic properties."( Pharmacokinetics, efficacy, and tolerability of a once-daily gastroretentive dosage form of gabapentin for the treatment of postherpetic neuralgia.
Chen, C; Cowles, VE; Han, CH; Sweeney, M, 2013
)
0.39
" Using plasma gabapentin concentration data obtained after administration of GEn in 12 phase 1 to 3 GEn studies in healthy adults or patients with RLS (dose range, 300-2400 mg/d), a population pharmacokinetic (PK) model was developed by nonlinear mixed-effect modeling using NONMEM."( Population pharmacokinetics and pharmacodynamics of gabapentin after administration of gabapentin enacarbil.
Cundy, KC; Lal, R; Lassauzet, ML; Luo, W; Sukbuntherng, J; Tovera, J, 2013
)
0.39
" In this study, we compared the pharmacokinetic parameters and effect of preemptive analgesics administered to calves subjected to dehorning with local anesthesia."( The pharmacokinetics and effects of meloxicam, gabapentin, and flunixin in postweaning dairy calves following dehorning with local anesthesia.
Allen, KA; Bergamasco, LL; Coetzee, JF; Dockweiler, JC; Edwards-Callaway, LN; Fraccaro, E; Glynn, HD; Jones, M; KuKanich, B; Lubbers, B, 2013
)
0.39
" Pharmacokinetic variables were estimated by means of noncompartmental analysis."( Pharmacokinetics of single-dose intragastric and intravenous pregabalin administration in clinically normal horses.
Divers, TJ; Mullen, KR; Schwark, W, 2013
)
0.39
"These data suggest that diet-drug pharmacokinetic interactions may occur during co-exposure to gabapentin and mushroom constituents."( Effect of mushroom diet on pharmacokinetics of gabapentin in healthy Chinese subjects.
Goh, BC; Lee, EJ; Limenta, LM; Murray, M; Toh, DS; Wang, LZ; Yee, JY, 2014
)
0.4
"The pharmacokinetic properties of the immediate-release (IR) and the recently developed controlled-release (CR) formulation of pregabalin are dose proportional."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
" The objectives of this analysis were: (1) to evaluate the effect of administration time and fat or caloric content of an accompanying meal on the pharmacokinetic properties of a single dose of pregabalin CR (330 mg) relative to a single dose of pregabalin IR (300 mg); (2) to evaluate the pharmacokinetic properties of a single dose of pregabalin CR administered fasted relative to a single dose of pregabalin CR administered immediately after food; and (3) to determine the safety and tolerability of single-dose administration of pregabalin CR and IR with and without food."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
"The effect of food on the pharmacokinetic properties of pregabalin CR was determined in five phase I, open-label, single-dose, crossover studies (24-28 participants/study)."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
"Time of day of administration and the fat and caloric content of the accompanying meal had minimal overall effect on the pharmacokinetic properties and bioavailability of the pregabalin CR formulation."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
"The pharmacokinetic properties of pregabalin CR were determined in four phase I, open-label, multiple-dose crossover studies (18-24 participants/study)."( Pregabalin controlled-release pharmacokinetics in healthy volunteers: analysis of four multiple-dose randomized clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
" Pregabalin CR pharmacokinetic parameters were dose proportional following administration of 82."( Pregabalin controlled-release pharmacokinetics in healthy volunteers: analysis of four multiple-dose randomized clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
" The primary goal of the study reported here was to describe endogenous concentrations of GABA in horses and the pharmacokinetics, selected pharmacodynamic effects, and CSF concentrations following administration of a GABA-containing product."( Endogenous concentrations, pharmacokinetics, and selected pharmacodynamic effects of a single dose of exogenous GABA in horses.
Knych, HK; McKemie, DS; Steinmetz, SJ, 2015
)
0.42
"Vigabatrin pharmacokinetic data from six randomized controlled clinical trials and one open-label study were analyzed using nonlinear mixed-effects modeling."( Population pharmacokinetics analysis of vigabatrin in adults and children with epilepsy and children with infantile spasms.
Karim, A; Kowalski, KG; Nielsen, JC; Patel, M; Tolbert, D; Wesche, DL, 2014
)
0.4
" Covariate analysis indicated that age, creatinine clearance (CLCR), and body weight were important predictors of vigabatrin pharmacokinetic parameters."( Population pharmacokinetics analysis of vigabatrin in adults and children with epilepsy and children with infantile spasms.
Karim, A; Kowalski, KG; Nielsen, JC; Patel, M; Tolbert, D; Wesche, DL, 2014
)
0.4
"The model adequately described vigabatrin pharmacokinetic and enabled predictions of systemic exposures in pediatric patients 1-12 months of age."( Population pharmacokinetics analysis of vigabatrin in adults and children with epilepsy and children with infantile spasms.
Karim, A; Kowalski, KG; Nielsen, JC; Patel, M; Tolbert, D; Wesche, DL, 2014
)
0.4
"5, 3, 4, 5, 6, 8, 10, 12, 15, and 24 hours after dosing, to evaluate pharmacokinetic parameters of the single dose administration, ie, the area under the plasma concentration-time curve (AUC) from time zero to 24 hours (AUCt), AUC from time zero to infinity (AUC(inf)), the peak plasma concentration of the drug (Cmax), time needed to achieve Cmax (tmax), and the elimination half-life (t1/2)."( Single dose pharmacokinetic equivalence study of two gabapentin preparations in healthy subjects.
Amalia, F; Putri, RS; Setiawati, E; Susanto, LW; Tjandrawinata, RR; Yunaidi, DA, 2014
)
0.4
" The differences in tmax and t1/2 values between the test and reference drug products for gabapentin were not statistically significant."( Single dose pharmacokinetic equivalence study of two gabapentin preparations in healthy subjects.
Amalia, F; Putri, RS; Setiawati, E; Susanto, LW; Tjandrawinata, RR; Yunaidi, DA, 2014
)
0.4
" Pharmacodynamic measures were limited to subject assessment of somnolence, dizziness, and nausea conducted by using a visual analog scale (VAS)."( Gabapentin enacarbil and morphine administered in combination versus alone: a double-blind, randomized, pharmacokinetic, and tolerability comparison.
Arumugham, T; Chen, C; Davy, M; Stier, B; Upward, J, 2015
)
0.42
"No significant pharmacokinetic interaction between the 2 drugs was seen in this study."( Gabapentin enacarbil and morphine administered in combination versus alone: a double-blind, randomized, pharmacokinetic, and tolerability comparison.
Arumugham, T; Chen, C; Davy, M; Stier, B; Upward, J, 2015
)
0.42
" Pharmacokinetic parameters were estimated from plasma concentration-time data using standard non-compartmental methods."( Pharmacokinetic effects of simultaneous administration of single-dose gabapentin 500 mg and zolpidem tartrate 10 mg in healthy volunteers: a randomized, open-label, crossover trial.
Furey, SA; Galitz, LA; Jayawardena, S, 2015
)
0.42
" The method was successfully applied to a pharmacokinetic study of GABA tablets in healthy Chinese volunteers."( [Determination of γ-aminobutyric acid in human plasma by LC-MS/MS and its preliminary application to a human pharmacokinetic study].
Chen, XY; Chen, Y; Dai, XJ; Du, JB; Zhong, DF; Zhong, K, 2014
)
0.4
" Plasma gabapentin concentrations were estimated by noncompartmental pharmacokinetic analysis."( PHARMACOKINETIC PROPERTIES OF A SINGLE ADMINISTRATION OF ORAL GABAPENTIN IN THE GREAT HORNED OWL (BUBO VIRGINIANUS).
Coetzee, JF; Gall, A; Olds, JE; Papastavros, E; Wulf, L; Yaw, TJ; Zaffarano, BA, 2015
)
0.42
" Plasma samples were analyzed for gabapentin concentration, and pharmacokinetic parameters were calculated with both a nonlinear mixed-effect approach and a noncompartmental analysis."( Pharmacokinetics of Compounded Intravenous and Oral Gabapentin in Hispaniolan Amazon Parrots ( Amazona ventralis ).
Baine, K; Cox, S; Jones, MP; Martín-Jiménez, T, 2015
)
0.42
" Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions."( Population Pharmacokinetic Modelling of Morphine, Gabapentin and their Combination in the Rat.
Gabel-Jensen, C; Juul, RV; Kreilgaard, M; Lund, TM; Papathanasiou, T, 2016
)
0.43
" The combination did not lead to pharmacokinetic interactions for morphine or gabapentin but resulted in an estimated ~33% diminished morphine-3-glucuronide formation."( Population Pharmacokinetic Modelling of Morphine, Gabapentin and their Combination in the Rat.
Gabel-Jensen, C; Juul, RV; Kreilgaard, M; Lund, TM; Papathanasiou, T, 2016
)
0.43
"The finding of a lack of pharmacokinetic interaction strengthens the notion that the combination of the two drugs leads to better efficacy in pain treatment due to interaction at the pharmacodynamic level."( Population Pharmacokinetic Modelling of Morphine, Gabapentin and their Combination in the Rat.
Gabel-Jensen, C; Juul, RV; Kreilgaard, M; Lund, TM; Papathanasiou, T, 2016
)
0.43
" To validate the pharmacodynamic biomarkers for GABA-ergic anxiolytics, this study determined the pharmacodynamics of two anxiolytics and a nonanxiolytic control, and linked them to their anxiolytic and sedative effects, during an anxiety-challenge study day."( Pharmacodynamic response profiles of anxiolytic and sedative drugs.
Baas, J; Broeyer, F; Chen, X; Cohen, A; de Kam, M; van Gerven, J, 2017
)
0.46
" Thus, the potential influence of anxiety on CNS pharmacodynamic markers could be examined."( Pharmacodynamic response profiles of anxiolytic and sedative drugs.
Baas, J; Broeyer, F; Chen, X; Cohen, A; de Kam, M; van Gerven, J, 2017
)
0.46
" This was a prospective pharmacokinetic study in elderly nursing home patients (≥60 years) receiving GBP for the management of chronic pain or epilepsy from seven nursing homes."( Pharmacokinetics and Saturable Absorption of Gabapentin in Nursing Home Elderly Patients.
Ahmed, GF; Bathena, SP; Birnbaum, AK; Brundage, RC; Conway, JM; Leppik, IE; Schwartz, JB, 2017
)
0.46
" With 2-L exchanges every 2 hours, we document an apparent elimination half-life of 41."( Treatment of Gabapentin Toxicity With Peritoneal Dialysis: Assessment of Gabapentin Clearance.
Edwards, JC; Ibrahim, H; Oman, Z; Schuelke, M, 2017
)
0.46
" The purpose of this study was to quantitatively characterize the pharmacodynamic interaction between the two drugs and to identify the optimal concentration-effect relationship of the combination."( Quantification of the Pharmacodynamic Interaction of Morphine and Gabapentin Using a Response Surface Approach.
Gabel-Jensen, C; Heegaard, AM; Juul, RV; Kreilgaard, M; Lund, TM; Papathanasiou, T, 2017
)
0.46
" Pharmacokinetic analysis was based on plasma and urine data concentrations."( The role of organic cation transporter 2 inhibitor cimetidine, experimental diabetes mellitus and metformin on gabapentin pharmacokinetics in rats.
Baviera, AM; Benzi, JRL; de Moraes, NV; Stevens, JH; Yamamoto, PA, 2018
)
0.48
"No differences in pharmacokinetic parameters were observed between vehicle + GAB × cimetidine + GAB and vehicle + GAB × metformin + GAB groups."( The role of organic cation transporter 2 inhibitor cimetidine, experimental diabetes mellitus and metformin on gabapentin pharmacokinetics in rats.
Baviera, AM; Benzi, JRL; de Moraes, NV; Stevens, JH; Yamamoto, PA, 2018
)
0.48
" This is the first pharmacokinetic (PK) comparison of all three formulations using FDA-recommended doses for PHN."( Pharmacokinetics of immediate release, extended release, and gastric retentive gabapentin formulations in healthy adults
.
Aronoff, GM; Ciric, S; Lal, R; Swearingen, D, 2018
)
0.48
" The brain concentration-time profiles of diazepam that correspond to these effects are unknown, but can be estimated with physiologically based pharmacokinetic (PBPK) modeling."( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points.
Burkat, PM, 2022
)
0.72
" This study utilized physiologically based pharmacokinetic (PK) and pharmacodynamic (PD) modelling to further examine the underlying mechanisms of anxiety treatment and addiction."( Physiologically based pharmacokinetic and pharmacodynamic modelling of alprazolam: Implications for anxiety and addiction.
Burkat, PM, 2023
)
0.91
" With repetitive administrations, peak concentration is 59 nM for a 2-mg alprazolam immediate-release dose and 122 nM for a 10-mg extended-release dose."( Physiologically based pharmacokinetic and pharmacodynamic modelling of alprazolam: Implications for anxiety and addiction.
Burkat, PM, 2023
)
0.91
" In this study, we investigated locomotor behavior as well as metabolic and pharmacokinetic interactions following co-administration of GHB and ethanol in rats."( Alcohol perturbed locomotor behavior, metabolism, and pharmacokinetics of gamma-hydroxybutyric acid in rats.
Bae, JW; Choi, B; Ji, M; Kim, M; Kim, S; Lee, S; Lee, YS; Oh, S; Paik, MJ, 2023
)
0.91

Compound-Compound Interactions

The distribution of gamma-aminobutyric acid (GABA)-ergic elements in 3 forebrain regions of two-day-old domestic chicks was investigated using light and electron microscope autoradiography.

ExcerptReferenceRelevance
"The distribution of gamma-aminobutyric acid (GABA)-ergic elements in 3 forebrain regions (medial mid-telencephalic hyperstriatum ventrale; paleostriatum augmentatum; lobus parolfactorius) of two-day-old domestic chicks was investigated using (1) light and electron microscope autoradiography following [3H]GABA uptake in vitro in combination with pre-embedding GABA immunocytochemistry and (2) Golgi impregnation and 'gold-toning' combined with postembedding GABA immunocytochemistry."( GABAergic structures in the chick telencephalon: GABA immunocytochemistry combined with light and electron microscope autoradiography, and Golgi impregnation.
Csillag, A; Curtis, EM; Stewart, MG, 1987
)
0.6
"To assess the roles of substance P in neurologic or psychiatric illnesses, effects of acute or chronic (40- or 80-day dietary) treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content were investigated in the rat brain."( Effects of chronic treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content in rat brain: a possible implication of substance P in affective disorders.
Mataga, N; Mitsushio, H; Takashima, M; Toru, M, 1988
)
0.27
"The distribution of GABA-like immunoreactivity (GABA-LI) in the ectostriatal core (Ec) of domestic chicks (one to two days old) was investigated using (1) preembedding GABA immunocytochemistry and (2) Golgi impregnation and gold-toning combined with postembedding GABA immunocytochemistry."( Localization of GABA-like immunoreactivity in the ectostriatum of domestic chicks: GABA immunocytochemistry combined with Golgi impregnation.
Bourne, RC; Csillag, A; Patel, SN; Stewart, MG; Tömböl, T, 1989
)
0.28
"In order to associate specific fiber projections in the central nervous system with specific target neurons, procedures were developed in which the anterograde neuroanatomical tracing technique utilizing Phaseolus vulgaris-leucoagglutinin (PHA-L) is combined with immunocytochemistry of three (different) neuronal markers: gamma-amino butyric acid, choline acetyltransferase, and serotonin."( Anterograde neuroanatomical tracing with Phaseolus vulgaris-leucoagglutinin combined with immunocytochemistry of gamma-amino butyric acid, choline acetyltransferase or serotonin.
Wouterlood, FG, 1988
)
0.27
" 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
"A pharmacohistochemical method for GABA-transaminase (GABA-T), the key enzyme for GABA metabolism, has been combined with retrograde tracing by horseradish peroxidase, to a study of projections to the lateral habenula."( Retrograde HRP tracing combined with a pharmacohistochemical method for GABA transaminase for the identification of presumptive GABAergic projections to the habenula.
Araki, M; McGeer, EG; McGeer, PL, 1984
)
0.27
" To address this issue in cats, anterograde tracing with Phaseolus vulgaris-leucoagglutinin (PHA-L) was combined with postembedding immunocytochemistry for gamma-aminobutyric acid (GABA) and glutamate."( Intra-amygdaloid projections of the lateral nucleus in the cat: PHA-L anterograde labeling combined with postembedding GABA and glutamate immunocytochemistry.
Paré, D; Smith, Y, 1994
)
0.49
" For the labeling of the septal neurons we used a double immunocytochemical method combined with retrograde transport of wheatgerm agglutinin apo-horseradish peroxidase-gold (WAHG) injected unilaterally into the hippocampus."( Cholinergic and GABAergic septo-hippocampal projection neurons in mice: a retrograde tracing study combined with double immunocytochemistry for choline acetyltransferase and parvalbumin.
Boldyreva, M; Linke, R; Schwegler, H, 1994
)
0.29
"To verify the possibility that the pedunculopontine nucleus is a source of glutamatergic terminals in contact with midbrain dopaminergic neurons in the squirrel monkey, we used the anterograde transport of Phaseolus vulgaris-leucoagglutinin in combination with preembedding immunohistochemistry for tyrosine hydroxylase and for calbindin D-28k and postembedding immunocytochemistry for glutamate and for gamma-aminobutyric acid."( Glutamatergic inputs from the pedunculopontine nucleus to midbrain dopaminergic neurons in primates: Phaseolus vulgaris-leucoagglutinin anterograde labeling combined with postembedding glutamate and GABA immunohistochemistry.
Charara, A; Parent, A; Smith, Y, 1996
)
0.46
"Electric impedance measurements on awake rabbits with electrodes implanted into cortex, thalamus, and hypothalamus showed that modeling of the noise and general (wide-band) vibration, as well as their combination with sea-sickness action, leads to disturbances in the aqueous-electrolyte balance in brain."( [Effects of pikamilon on the brain water-electrolyte balance and in models of responses to the noise and vibration exposure, and their combination with motion sickness].
Sapegin, ID,
)
0.13
" The aim of the study was to investigate the influence of PP alone and in combination with various doses of vigabatrin (VGB) on brain GABA levels."( Influence of pyridoxal 5'-phosphate alone and in combination with vigabatrin on brain GABA measured by 1H-NMR-spectroscopy.
Boesiger, P; Mueller, SG; Weber, OM; Wieser, HG, 2001
)
0.31
"To investigate the effect of propofol combined with diazepam on the gamma-aminobutyric acid (GABA)-activated chloride current (IGABA) evoked in rat sensory neurons."( Propofol combined with diazepam synergistically potentiates the GABA-activated chloride current in rat sensory neurons.
Luo, A; Sugiyama, K, 2000
)
0.54
"Our results suggest that propofol combined with diazepam synergistically potentiates the IGABA."( Propofol combined with diazepam synergistically potentiates the GABA-activated chloride current in rat sensory neurons.
Luo, A; Sugiyama, K, 2000
)
0.31
" In the present study, the effect of gabapentin (GBP) on seizure score and memory is evaluated when it is given alone and in combination with some antidepressants, such as sertraline (SERTR) and alprazolam (ALP)."( Effects of gabapentin and antidepressant drug combinations on convulsions and memory in mice.
Ali, A; Dua, Y; Pal, SN; Pillai, KK; Rizwan, AN,
)
0.13
" The effect of SNP was tested alone and in combination with phenobarbitone (PB), the GABA potentiating antiepileptic drug, against picrotoxin (PCT) (5 mg/kg)-induced convulsions in rats."( Effects of sodium nitroprusside, a nitric oxide donor, on gamma-aminobutyric acid concentration in the brain and on picrotoxin-induced convulsions in combination with phenobarbitone in rats.
Ekambaram, P; Paul, V, 2005
)
0.57
" Patients received PGB, 600 mg/day (200 mg q8h) for 7 days, in combination with their individualized maintenance monotherapy with valproate (VPA), phenytoin (PHT), lamotrigine (LTG), or carbamazepine (CBZ)."( Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy.
Alvey, CW; Bockbrader, HN; Brodie, MJ; Bron, NJ; Gibson, GL; Hounslow, NJ; Posvar, EL; Randinitis, EJ; Wesche, DL; Wilson, EA, 2005
)
0.33
" PGB may be added to VPA, LTG, PHT, or CBZ therapy without concern for pharmacokinetic drug-drug interactions."( Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy.
Alvey, CW; Bockbrader, HN; Brodie, MJ; Bron, NJ; Gibson, GL; Hounslow, NJ; Posvar, EL; Randinitis, EJ; Wesche, DL; Wilson, EA, 2005
)
0.33
"Acute gabapentin administration was well tolerated in combination with alcohol, but did not alter the effects of alcohol."( The acute effects of gabapentin in combination with alcohol in heavy drinkers.
Bisaga, A; Evans, SM, 2006
)
0.33
"We report the successful management of anesthesia in a patient with stiff-person syndrome (SPS) undergoing a thymectomy using a volatile anesthetic combined with epidural anesthesia."( Considerations for general anesthesia combined with epidural anesthesia in a patient with stiff-person syndrome.
Hara, K; Horishita, T; Sata, T; Yamamoto, K, 2007
)
0.34
" We investigated the analgesic effect of pregabalin and dexamethasone in combination with paracetamol after abdominal hysterectomy."( Pregabalin and dexamethasone in combination with paracetamol for postoperative pain control after abdominal hysterectomy. A randomized clinical trial.
Dahl, JB; Dierking, G; Fomsgaard, JS; Hilsted, KL; Lech, K; Lose, G; Mathiesen, O; Rasmussen, ML, 2009
)
0.35
" Measurement of total brain antiepileptic drug concentrations revealed that levetiracetam in combination with gabapentin at the fixed-ratio of 1:4 significantly elevated (21%) total brain gabapentin concentrations."( Pharmacodynamic and pharmacokinetic interaction profiles of levetiracetam in combination with gabapentin, tiagabine and vigabatrin in the mouse pentylenetetrazole-induced seizure model: an isobolographic analysis.
Andres-Mach, MM; Czuczwar, SJ; Dudra-Jastrzebska, M; Luszczki, JJ; Patsalos, PN; Ratnaraj, N; Sielski, M, 2009
)
0.35
" We, therefore, investigated the analgesic effect of gabapentin, dexamethasone and low-dose ketamine in combination with paracetamol and ketorolac as compared with paracetamol and ketorolac alone after hip arthroplasty."( Multimodal analgesia with gabapentin, ketamine and dexamethasone in combination with paracetamol and ketorolac after hip arthroplasty: a preliminary study.
Christensen, BV; Dahl, JB; Dierking, G; Hilsted, KL; Larsen, TK; Mathiesen, O; Rasmussen, ML, 2010
)
0.36
"Preoperative gabapentin, dexamethasone and ketamine combined with paracetamol and ketorolac reduced overall pain scores in patients after hip arthroplasty as compared with paracetamol and ketorolac alone."( Multimodal analgesia with gabapentin, ketamine and dexamethasone in combination with paracetamol and ketorolac after hip arthroplasty: a preliminary study.
Christensen, BV; Dahl, JB; Dierking, G; Hilsted, KL; Larsen, TK; Mathiesen, O; Rasmussen, ML, 2010
)
0.36
"To evaluate the effects of high-frequency electrical stimulation (HFS) in both ventral hippocampi, alone and combined with a subeffective dose of antiepileptic drugs, during the status epilepticus (SE) induced by lithium-pilocarpine (LP)."( Antiepileptic drugs combined with high-frequency electrical stimulation in the ventral hippocampus modify pilocarpine-induced status epilepticus in rats.
Alcantara-Gonzalez, D; Cuellar-Herrera, M; Neri-Bazan, L; Peña, F; Rocha, L, 2010
)
0.36
" One minute following pilocarpine injection, HFS (pulses of 60 mus width at 130 Hz at subthreshold intensities and applied during 3 h) was applied alone or combined with subeffective doses of antiepileptic drugs."( Antiepileptic drugs combined with high-frequency electrical stimulation in the ventral hippocampus modify pilocarpine-induced status epilepticus in rats.
Alcantara-Gonzalez, D; Cuellar-Herrera, M; Neri-Bazan, L; Peña, F; Rocha, L, 2010
)
0.36
" This effect was not evident when HFS was combined with phenytoin (33."( Antiepileptic drugs combined with high-frequency electrical stimulation in the ventral hippocampus modify pilocarpine-induced status epilepticus in rats.
Alcantara-Gonzalez, D; Cuellar-Herrera, M; Neri-Bazan, L; Peña, F; Rocha, L, 2010
)
0.36
" The aim of this study was to see whether low-dose gabapentin is effective in treating cancer-related neuropathic pain when combined with low-dose imipramine."( Low-dose gabapentin as useful adjuvant to opioids for neuropathic cancer pain when combined with low-dose imipramine.
Arai, YC; Arakawa, M; Hayashi, R; Kinoshita, A; Kobayashi, K; Kondo, M; Matsubara, S; Matsubara, T; Nishida, K; Nishihara, M; Shimo, K; Suetomi, K; Suzuki, C; Tohyama, Y; Ushida, T, 2010
)
0.36
"Low-dose gabapentin-antidepressant combination with opioids was effective in managing neuropathic cancer pain without severe adverse effects."( Low-dose gabapentin as useful adjuvant to opioids for neuropathic cancer pain when combined with low-dose imipramine.
Arai, YC; Arakawa, M; Hayashi, R; Kinoshita, A; Kobayashi, K; Kondo, M; Matsubara, S; Matsubara, T; Nishida, K; Nishihara, M; Shimo, K; Suetomi, K; Suzuki, C; Tohyama, Y; Ushida, T, 2010
)
0.36
"Three-phase hollow fiber microextraction technique combined with high performance liquid chromatography-ultra violet (HPLC-UV) was applied for the extraction and determination of gabapentin in biological fluids."( Hollow fiber-based liquid phase microextraction combined with high-performance liquid chromatography for the analysis of gabapentin in biological samples.
Ebrahimzadeh, H; Firozjaei, HA; Kamarei, F; Rouini, MR; Tavassoli, N; Yamini, Y, 2010
)
0.36
" To examine the potential for drug-drug interactions at these two transporters, the pharmacokinetics of gabapentin enacarbil were evaluated in healthy adults after administration alone or in combination with either naproxen (an MCT-1 substrate) or cimetidine (an OCT2 substrate)."( Clinical pharmacokinetic drug interaction studies of gabapentin enacarbil, a novel transported prodrug of gabapentin, with naproxen and cimetidine.
Blumenthal, R; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J; Vicente, V, 2010
)
0.36
" This study determined the pharmacokinetics of oral (PO) gabapentin alone or in combination with meloxicam in ruminant calves."( Pharmacokinetics of oral gabapentin alone or co-administered with meloxicam in ruminant beef calves.
Coetzee, JF; Cull, CA; Kelly, LL; Kohake, LE; KuKanich, B; Mosher, RA; Mueting, SL, 2011
)
0.37
"To assess the efficacy and safety of pregabalin alone or in combination with tolterodine extended release (ER) in subjects with idiopathic OAB."( Investigation of the clinical efficacy and safety of pregabalin alone or combined with tolterodine in female subjects with idiopathic overactive bladder.
Cossons, NH; Darekar, A; Marencak, J; Mills, IW, 2011
)
0.37
" Using a double-blind, randomized, crossover design, 16 healthy volunteers were administered (in separate sessions) capsules containing placebo, 75 mg pregabalin, 150 mg pregabalin, 10 mg oxycodone, and 75 mg pregabalin combined with 10 mg oxycodone."( Subjective, psychomotor, and physiological effects of pregabalin alone and in combination with oxycodone in healthy volunteers.
Coalson, DW; Paice, JA; Zacny, JP, 2012
)
0.38
" We performed unilateral ventralis caudalis deep brain stimulation combined with stereotactic bilateral cingulotomy to maximize the effects of treatment for 3 patients with intractable post-stroke pain."( Impact of ventralis caudalis deep brain stimulation combined with stereotactic bilateral cingulotomy for treatment of post-stroke pain.
Chang, JW; Chang, WS; Kim, JP; Park, YS, 2012
)
0.38
" Below we describe the preliminary evaluation of support vector machine in the regression mode (SVR) application for the prediction of maximal antiallodynic effect of a new derivative of dihydrofuran-2-one (LPP1) used in combination with pregabalin (PGB) in the streptozocin-induced neuropathic pain model in mice."( The application of support vector regression for prediction of the antiallodynic effect of drug combinations in the mouse model of streptozocin-induced diabetic neuropathy.
Sałat, K; Sałat, R, 2013
)
0.39
"25), although this enhancement was not observed when morphine was combined with 17 mg/kg pregabalin."( Assessment of the antinociceptive effects of pregabalin alone or in combination with morphine during acetic acid-induced writhing in mice.
Keyhanfar, F; Shamsi Meymandi, M, 2013
)
0.39
"The frequency and financial impact of potential drug-drug interactions (DDIs) and drug-condition interactions (DCIs) in patients with painful diabetic peripheral neuropathy (DPN) treated with either pregabalin or duloxetine were compared."( Cost comparison of drug-drug and drug-condition interactions in patients with painful diabetic peripheral neuropathy treated with pregabalin versus duloxetine.
Cappelleri, JC; Chu, BC; Johnson, BH; Johnston, SS; Shrady, G; Silverman, SL; Udall, M, 2013
)
0.39
"Potential DDI measured using clinical software that identifies co-prescription of medications that potentially interact with pregabalin or duloxetine."( Potential drug-drug and drug-condition interactions among fibromyalgia patients initiating pregabalin or duloxetine: prevalence and health care expenditure impact.
Cappelleri, JC; Chu, BC; Johnson, BH; Johnston, SS; Shrady, G; Silverman, SL; Udall, M, 2014
)
0.4
" The objective of the present study was to evaluate the efficacy and safety of OROS® hydromorphone combined with pregabalin in patients with chronic non-cancer neuropathic pain."( Long-term efficacy of OROS® hydromorphone combined with pregabalin for chronic non-cancer neuropathic pain.
Casali, M; Dauri, M; Lazzari, M; Sabato, AF; Sabato, E; Tufaro, G, 2014
)
0.4
"This study examined the pharmacokinetics and analgesic effect of oral meloxicam (MEL) administered alone or in combination with gabapentin (GABA) in an experimental bovine lameness model."( Impact of oral meloxicam administered alone or in combination with gabapentin on experimentally induced lameness in beef calves.
Anderson, DE; Coetzee, JF; Gehring, R; Kohake, LE; Kukanich, B; Mosher, RA; Robert, B; Wang, C; White, BJ, 2014
)
0.4
"To evaluate the analgesic effect of pregabalin combined with intrathecal sufentanil infusion for the treatment of breakthrough pain in patients with bone metastases."( [Pregabalin combined with intrathecal sufentanil infusion for breakthrough pain in patients with bone metastases].
Cao, Q; Gu, S; Huang, D; Wu, L; Xu, H, 2014
)
0.4
"A total of 60 breakthrough pain patients with bone metastases were randomly divided to 3 groups: group A (pregabalin combined with intrathecal sufentanil infusion group, n=20), group B (placebo combined with intrathecal sufentanil infusion group, n=20) and group C (oral morphine sulfate controlled-release tablet group, n=20)."( [Pregabalin combined with intrathecal sufentanil infusion for breakthrough pain in patients with bone metastases].
Cao, Q; Gu, S; Huang, D; Wu, L; Xu, H, 2014
)
0.4
"Pregabalin combined with intrathecal sufentanil infusion can effectively relieve breakthrough pain in patients with bone metastases."( [Pregabalin combined with intrathecal sufentanil infusion for breakthrough pain in patients with bone metastases].
Cao, Q; Gu, S; Huang, D; Wu, L; Xu, H, 2014
)
0.4
"We sought to compare a group (Group L) (n=21) of patients that underwent total knee arthroplasty and received a single preoperative dose of pregabalin combined with a COX-2 inhibitor with a control group (Group C) (n=20) that only received a COX-2 inhibitor in terms of (1) acute postoperative pain intensity, (2) analgesic consumption, and (3) functional recovery."( The effect of a single dose of preemptive pregabalin administered with COX-2 inhibitor: a trial in total knee arthroplasty.
Choi, CH; Chung, KS; Lee, JK, 2015
)
0.42
"This paper aimed to discuss the curative effect and safety of curing intercostal neuralgia through paravertebral nerve block combined with pregabalin."( Curative effect research on curing intercostal neuralgia through paravertebral nerve block combined with pregabalin.
Wu, X; Xiao, P; Zhu, X, 2014
)
0.4
" Gas release-based prescreening combined with reversed-phase HPLC confirmation was an efficient and cost-effective method to identify high-GABA-producing LAB, which could be good candidates for probiotics."( Gas release-based prescreening combined with reversed-phase HPLC quantitation for efficient selection of high-γ-aminobutyric acid (GABA)-producing lactic acid bacteria.
Shah, NP; Wu, Q, 2015
)
0.42
" In this study, we tested the hypothesis that HIV gp120 combined with antiretroviral therapy reduces spinal GABAergic inhibitory tone and that restoration of GABAergic inhibitory tone will reduce HIV-related NP in a rat model."( Gene Transfer of Glutamic Acid Decarboxylase 67 by Herpes Simplex Virus Vectors Suppresses Neuropathic Pain Induced by Human Immunodeficiency Virus gp120 Combined with ddC in Rats.
Candiotti, KA; Hao, S; Huang, W; Kanao, M; Kanda, H; Levitt, RC; Liu, S; Lubarsky, DA; Yi, H, 2015
)
0.42
"To explore the effects of electrical stimulation at acupoints in the distribution area of auricular vagus nerve combined with sound masking on auditory brainstem response (ABR) and contents of neurotransmitters of γ-aminobutyric acid (γ-GABA), 5-hydroxytryptamine (5-HT) and acetyl choline (Ach) in inferior colliculus of tinnitus rats."( [Effects of electrical stimulation at acupoints in the distribution area of auricular vagus nerve combined with sound masking method on auditory brainstem response and neurotransmitters of inferior colliculus in rats of tinnitus].
Cai, S; Huang, K; Li, T; Ma, W; Mei, Z; Tan, L; Wang, Z; Yang, S; Zhang, D, 2016
)
0.43
" Rats in the 7-d treatment group and 15-d treatment group were treated with electrical stimulation at "Shenmen (TF₄)" and "Yidan (CO₁₁)" in the distribution area of auricular vagus nerve combined with sound masking, once a day, for 7 days and 15 days."( [Effects of electrical stimulation at acupoints in the distribution area of auricular vagus nerve combined with sound masking method on auditory brainstem response and neurotransmitters of inferior colliculus in rats of tinnitus].
Cai, S; Huang, K; Li, T; Ma, W; Mei, Z; Tan, L; Wang, Z; Yang, S; Zhang, D, 2016
)
0.43
"Electrical stimulation at auricular vagus nerve combined with sound masking) could regulate the threshold of ABR, especially in the 15-d treatment group."( [Effects of electrical stimulation at acupoints in the distribution area of auricular vagus nerve combined with sound masking method on auditory brainstem response and neurotransmitters of inferior colliculus in rats of tinnitus].
Cai, S; Huang, K; Li, T; Ma, W; Mei, Z; Tan, L; Wang, Z; Yang, S; Zhang, D, 2016
)
0.43
" Previous studies showed that opioids combined with gabapentin for management of cancer pain reduced the dosage of opioids."( The research on long-term clinical effects and patients' satisfaction of gabapentin combined with oxycontin in treatment of severe cancer pain.
Chen, DL; Li, YH; Wang, ZJ; Zhu, YK, 2016
)
0.43
" To understand whether taurine-ethanol combined toxicity is exclusively connected to taurine or whether other inhibitory amino acids may have similar effects when combined with ethanol, we tested different doses of gamma-aminobutyric acid (GABA) in combination with ethanol in 7-day-old mice."( Comparison of Toxicity of Taurine and GABA in Combination with Alcohol in 7-Day-Old Mice.
Gunnar, T; Kiianmaa, K; Oja, SS; Saransaari, P; Taranukhin, AG,
)
0.32
" In order to monitor the neural activities in cortex under gamma-aminobutyric acid (GABA) and glutamate (Glu) modulation, an implantable microelectrode array (MEA) was combined with microinjection capillary."( Electrophysiological Detection of Cortical Neurons under Gamma-Aminobutyric Acid and Glutamate Modulation Based on Implantable Microelectrode Array Combined with Microinjection.
Cai, X; Gao, F; Li, Z; Song, Y; Wang, M; Xiao, G; Xu, S, 2018
)
0.97
"The study did not provide any evidence of clinical efficacy for AZD5213 when combined with pregabalin in the treatment of painful diabetic neuropathy."( A 3-way Cross-over Study of Pregabalin, Placebo, and the Histamine 3 Receptor Inverse Agonist AZD5213 in Combination With Pregabalin in Patients With Painful Diabetic Neuropathy and Good Pain-reporting Ability.
Alexander, RC; Katz, N; Raudibaugh, K; Spierings, ELH, 2021
)
0.62
" This anxiety animal model was established by intraperitoneal injection of FG7142 combined with restraint stress."( FG7142 combined with restraint stress induces anxiogenic-like effects via downregulation gamma-aminobutyric acid type A receptor subunit alpha1 and 5-hydroxytryptamine 1A receptors expression in the hippocampus.
Chen, S; Gao, J; Wang, K; Wei, X; Zeng, S; Zhao, Y, 2022
)
0.94
"Compared with the control group and restraint stress group, intraperitoneal injection of FG7142 combined with restraint stress model group was found to induce anxiogenic-like behavior in elevated plus maze and marble burying test."( FG7142 combined with restraint stress induces anxiogenic-like effects via downregulation gamma-aminobutyric acid type A receptor subunit alpha1 and 5-hydroxytryptamine 1A receptors expression in the hippocampus.
Chen, S; Gao, J; Wang, K; Wei, X; Zeng, S; Zhao, Y, 2022
)
0.94
"These results indicated that FG7142 combined with restraint stress is sufficient to induce anxiety, and its mechanism is associated with downregulation of hippocampal gamma-aminobutyric acid type A receptor subunit alpha1 and 5-hydroxytryptamine 1A receptors."( FG7142 combined with restraint stress induces anxiogenic-like effects via downregulation gamma-aminobutyric acid type A receptor subunit alpha1 and 5-hydroxytryptamine 1A receptors expression in the hippocampus.
Chen, S; Gao, J; Wang, K; Wei, X; Zeng, S; Zhao, Y, 2022
)
1.14
"This study aimed to evaluate the efficacy of gamma-aminobutyric acid (GABA) alone or combined with praziquantel (PZQ) against Schistosoma (S) mansoni infection in a murine model."( Schistosomicidal and hepatoprotective activity of gamma-aminobutyric acid (GABA) alone or combined with praziquantel against Schistosoma mansoni infection in murine model.
Fahmy, AM; Hegab, A; Tm, D; William, S, 2022
)
1.23
" Significant improvement in hepatic oxidative stress levels, serum albumin and total protein in response to GABA treatment alone or combined with PZQ."( Schistosomicidal and hepatoprotective activity of gamma-aminobutyric acid (GABA) alone or combined with praziquantel against Schistosoma mansoni infection in murine model.
Fahmy, AM; Hegab, A; Tm, D; William, S, 2022
)
0.97

Bioavailability

ExcerptReferenceRelevance
" The drug bioavailability at oral administration to mice is 21."( [Pikamilon pharmacokinetics in animals].
Dorofeev, BF; Kholodov, LE,
)
0.13
" The substance is well absorbed after oral administration and penetrates the blood-brain barrier."( Intestinal absorption of gabapentin in rats.
Maurer, HH; Rump, AF, 1991
)
0.28
" The data obtained indicate that the gastric pH and gastric emptying rate will have a profound effect on the oral bioavailability of Progabide."( The stability and solubility of progabide and its related metabolic derivatives.
Davis, SS; Farraj, NF; Parr, GD; Stevens, HN, 1988
)
0.27
" Gabapentin is well absorbed in rats, dogs and in humans, with maximum blood levels, reached within 1-3 h after peroral administration."( Pharmacokinetics and metabolism of gabapentin in rat, dog and man.
Kölle, EU; Vollmer, KO; von Hodenberg, A, 1986
)
0.27
" Several issues pertaining to the bioavailability of progabide were addressed: first-pass effect, incomplete dissolution, and dose and time dependency."( Disposition of progabide and valproic acid following intraperitoneal administration in rhesus monkey.
Bialer, M; Johno, I; Levy, RH; Nickelson, SA, 1984
)
0.27
" The mean bioavailability was attributed principally to a first-pass effect."( Pharmacokinetic profile of progabide, a new gamma-aminobutyric acid-mimetic drug, in rhesus monkey.
Johno, I; Levy, RH; Ludwick, BT, 1982
)
0.53
" The results show that the compound is well absorbed and retained by the organism."( Absorption, distribution and excretion of DL-gamma-amino-beta-hydroxybutyric acid-1-14C (GABOB-1-14C) in the rat.
Bonardi, G; Mondino, A; Silvestri, S; Zanolo, G, 1981
)
0.26
" Oral bioavailability was 40% in monkeys administered 25 mg/kg, 79% in mice and rats receiving 50 mg/kg, and 80% in dogs administered 50 mg/kg."( Disposition of gabapentin (neurontin) in mice, rats, dogs, and monkeys.
Bockbrader, HN; Chang, T; DeHart, PD; Hanson, BJ; McNally, WP; Radulovic, LL; Türck, D; Vollmer, KO; von Hodenberg, A, 1995
)
0.29
" These results indicate a marked behavioral difference in the effects of haloperidol in drug-naive and chronically treated rats which is not related to an altered bioavailability of the drug and which is dissociated from both basal and haloperidol induced effects on dopamine and acetylcholine release in both brain regions."( Acute versus chronic haloperidol: relationship between tolerance to catalepsy and striatal and accumbens dopamine, GABA and acetylcholine release.
Beck, O; O'Connor, WT; Osborne, PG; Ungerstedt, U, 1994
)
0.29
" This drug is rapidly absorbed and exhibits dose-dependent bioavailability as a result of a saturable transport mechanism."( Clinical pharmacokinetics of gabapentin.
McLean, MJ, 1994
)
0.29
" Furthermore, ofloxacin competes with other fluoroquinolones or P-glycoprotein substrates for a common secretory pathway, resulting in an increased rate of absorption for both ofloxacin isomers; this is probably an indirect result of their reduced efflux from the apical side of intestinal cells."( Absorption of ofloxacin isomers in the rat small intestine.
Carbon, C; Colas-Linhart, N; Dautrey, S; Farinotti, R; Rabbaa, L, 1997
)
0.3
" However, GBP concentrations were much lower after rectal administration; therefore, we concluded that the aqueous solution was poorly absorbed rectally."( Failure of absorption of gabapentin after rectal administration.
Birnbaum, AK; Caruso, KJ; Cloyd, JC; Jones Saete, C; Kriel, RL; Ricker, BJ, 1997
)
0.3
" The following kinetic parameters were calculated: area under the concentration time curve from zero time to 24 h after the dose, AUC 0-24 h; maximal serum concentration, Cmax; time to the maximal serum concentration, Tmax; absorption rate constant, ka; elimination rate constant, beta; elimination half-time, t1/2beta."( Oral gabapentin disposition in patients with epilepsy after a high-protein meal.
Baraldo, M; Benetello, P; Fortunato, M; Furlanut, M; Pea, F; Testa, G; Tognon, A, 1997
)
0.3
" At large daily doses, oral bioavailability (F) may be improved by giving the daily dose more frequently."( Gabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsy.
Bockbrader, HN; DeCerce, J; Gidal, BE; Gonzalez, J; Kruger, S; Pitterle, ME; Ramsay, RE; Rutecki, P, 1998
)
0.3
" After oral administration, absorption is rapid and relatively efficient for the new AEDs, the most notable exception being gabapentin, whose bioavailability decreases with increasing dosage."( The clinical pharmacokinetics of the new antiepileptic drugs.
Perucca, E, 1999
)
0.3
"Study A: 400-mg single dose, randomized, cross-over study to assess bioavailability of four different gabapentin formulations (n=20, 9 males, 11 females; mean age and weight 41 years, 75."( Inter- and intra-subject variability in gabapentin absorption and absolute bioavailability.
Bockbrader, HN; Gidal, BE; Kruger, S; Pitterle, M; Radulovic, LL; Rutecki, P, 2000
)
0.31
" When administered orally as enteric-coated tablets at relatively high doses, this drug has a bioavailability of about 11%; however, the intestinal absorption mechanism has not been studied in depth."( Kinetic study of acamprosate absorption in rat small intestine.
Granero, L; Guerri, C; Martín-Algarra, RV; Más-Serrano, P; Polache, A,
)
0.13
" Both pulsed emission with a specific absorption rate (SAR) of 4 W/kg and continuous emission with high SAR (32 W/kg) were tested."( Effects of radiofrequency exposure on the GABAergic system in the rat cerebellum: clues from semi-quantitative immunohistochemistry.
de Seze, R; Mausset, AL; Montpeyroux, F; Privat, A, 2001
)
0.31
" Intersubject variability was approximately 30% for oral clearance and volume of distribution and was larger for the absorption rate constant and lag time."( Population pharmacokinetics of gabapentin in infants and children.
Bockbrader, HN; Garofalo, E; Ouellet, D; Shapiro, DY; Wesche, DL, 2001
)
0.31
" It is well absorbed when administered orally and displays linear kinetics up to doses of 1,800 mg/day."( [Characteristics and indications of gabapentin].
Sancho-Rieger, J, 2002
)
0.31
" It has been suggested that this transportation is capacity limited, thus decreasing GBP bioavailability at higher doses."( The absorption of gabapentin following high dose escalation.
Beran, RG; Berry, DJ; Clarke, LA; Hung, WT; Plunkeft, MJ, 2003
)
0.32
" In healthy volunteers, it is rapidly absorbed with peak blood concentrations within 1 h and it has a bioavailability of approximately 90%."( Pregabalin: a new anxiolytic.
Lauria-Horner, BA; Pohl, RB, 2003
)
0.32
" In monkeys, oral bioavailability of gabapentin from XP13512 capsules was 84."( XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys.
Annamalai, T; Barrett, RW; Bu, L; Cundy, KC; De Vera, J; Estrela, J; Gallop, MA; Luo, W; Shirsat, P; Torneros, A; Yao, F; Zou, J, 2004
)
0.32
" The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies."( Rapid quantification of gabapentin in human plasma by liquid chromatography/tandem mass spectrometry.
Chidambara, J; Koteshwara, M; Manoj, S; Ramakrishna, NV; Santosh, M; Sumatha, B; Varma, DP; Vishwottam, KN, 2006
)
0.33
" Together, these data support the idea that the synthesis of estrogen can be rapidly regulated in the brain, thus producing rapid changes in local estrogen bioavailability that could rapidly modify brain function with a time course similar to what has previously been described for neurotransmitters and neuromodulators."( Rapid control of brain aromatase activity by glutamatergic inputs.
Baillien, M; Ball, GF; Balthazart, J, 2006
)
0.33
" Peak plasma levels occur approximately 1 hour after oral doses and oral bioavailability is about 90%."( Pregabalin: a new agent for the treatment of neuropathic pain.
Zareba, G, 2005
)
0.33
" Unlike gabapentin, pregabalin was well absorbed (> 90%), and its absorption was dose independent."( Pregabalin in neuropathic pain: a more "pharmaceutically elegant" gabapentin?
Guay, DR, 2005
)
0.33
" Oral bioavailability of gabapentin was not affected by OCTN1 genotype."( Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin.
Brett, CM; Brown, C; Burchard, EG; Castro, RA; Giacomini, KM; Huang, Y; Mercer, R; Shah, N; Urban, TJ, 2008
)
0.35
" Gabapentin ER is based on the company's proprietary AcuForm drug delivery technology, which is part of the Gastric Retention (GR) family of technologies; this offers improved drug absorption and bioavailability compared with the existing immediate-release formulation of gabapentin (Neurontin), making gabapentin ER suitable for twice-daily dosing."( Gabapentin Extended-Release - Depomed: Gabapentin ER, Gabapentin Gastric Retention, Gabapentin GR.
, 2007
)
0.34
" XP13512 immediate-release (up to 2800 mg single dose and 2100 mg twice daily) was well absorbed (>68%, based on urinary recovery of gabapentin), converted rapidly to gabapentin, and provided dose-proportional exposure, whereas absorption of oral gabapentin declined with increasing doses to <27% at 1200 mg."( Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin.
Canafax, DM; Cundy, KC; Luo, W; Moors, TL; Sastry, S; Zou, J, 2008
)
0.35
" Bioavailability was included in the models as a function of dose by using a hyperbolic function derived from data previously reported in the literature."( A population pharmacokinetic model of gabapentin developed in nonparametric adaptive grid and nonlinear mixed effects modeling.
Carlsson, KC; Eriksen, HO; Hoem, NO; Karlsson, MO; Moberg, ER; van de Schootbrugge, M, 2009
)
0.35
" Additionally, present knowledge of bioavailability and in-vivo actions of the peptides in fermented milk are discussed."( Does fermented milk possess antihypertensive effect in humans?
Ibsen, H; Jensen, LT; Usinger, L, 2009
)
0.35
" The bioavailability of released GABA at the GABA(A) receptor improved when the release took place from m-OCF3 (2) but decreased for m-CF3 (3) when compared with the parent pHP derivative."( Competing pathways in the photo-Favorskii rearrangement and release of esters: studies on fluorinated p-hydroxyphenacyl-caged GABA and glutamate phototriggers.
Givens, RS; Heger, D; Kandler, K; Noh, J; Stensrud, K; Wirz, J, 2009
)
0.35
" Mean (standard deviation) bioavailability (based on urinary recovery) of gabapentin from gabapentin enacarbil was 42."( The effect of food with varying fat content on the clinical pharmacokinetics of gabapentin after oral administration of gabapentin enacarbil.
Cundy, KC; Huff, FJ; Lal, R; Luo, W; Sukbuntherng, J; Zou, J, 2010
)
0.36
" Pregabalin oral bioavailability is approximately 90% and is independent of dose and frequency of administration."( Clinical pharmacokinetics of pregabalin in healthy volunteers.
Alvey, CW; Bockbrader, HN; Boyd, RA; Busch, JA; Corrigan, BW; Haig, GM; Posvar, EL; Radulovic, LL; Randinitis, EJ; Strand, JC; Wesche, DL, 2010
)
0.36
" The pharmacokinetics of gabapentin delivered from this extended-release formulation allows a reduced dosing frequency while maintaining bioavailability and possibly diminishing the occurrence of adverse events attributable to a slower increase to the peak concentration compared with the immediate-release dosage form."( Pharmacokinetics of gabapentin in a novel gastric-retentive extended-release formulation: comparison with an immediate-release formulation and effect of dose escalation and food.
Chen, C; Cowles, VE; Hou, E, 2011
)
0.37
" The absolute bioavailability of gabapentin drops from 60% to 33% as the dosage increases from 900 to 3600 mg/day, while the absolute bioavailability of pregabalin remains at > or = 90% irrespective of the dosage."( A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin.
Bockbrader, HN; Burger, P; Chapel, S; Janiczek, N; Miller, R; Wesche, D, 2010
)
0.36
" The mean oral bioavailability of gabapentin (± SD) was 16."( Pharmacokinetic profile and behavioral effects of gabapentin in the horse.
Driessen, B; Liu, Y; McDonnell, SM; Moate, PJ; Soma, LR; Terry, RL; Uboh, CE; Van Eps, AW, 2010
)
0.36
" Our study investigated whether a single 300-mg dose of pregabalin in patients has sufficient central nervous system bioavailability to be useful under acute conditions where brain or spinal cord excitability may lead to long-term disease, such as chronic pain."( Can a single dose of 300 mg of pregabalin reach acute antihyperalgesic levels in the central nervous system?
Buvanendran, A; Kari, M; Kroin, JS; Tuman, KJ,
)
0.13
"This pharmacostatistical model showed that: (1) pregabalin oral clearance (CL/F) was directly proportional to creatinine clearance (CLcr), but was independent of gender, race, age, female hormonal status, daily dose, and dosing regimen; (2) apparent volume of distribution was dependent on body weight and gender; (3) absorption rate was decreased when given with food; and (4) coadministration with marketed antiepileptic drugs (AEDs) had no significant effect on pregabalin CL/F."( Population pharmacokinetics of pregabalin in healthy subjects and patients with chronic pain or partial seizures.
Bockbrader, HN; Burger, P; Corrigan, BW; Knapp, L, 2011
)
0.37
"The pharmaceutical properties, including the physical and chemical properties, and the bioavailability are greatly influenced by their polymorphism."( [The crystalline polymorph control and selection of gabapentin with polymer heteronuclei].
Lang, MD; Ru, ML; Yang, L, 2010
)
0.36
" Oral bioavailability (BA) of gabapentin was estimated by 24-h urine collection."( Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects.
Kawakami, J; Mino, Y; Naito, T; Umemura, K; Yagi, T, 2012
)
0.38
" These interactions may have important implications on the absorption and metabolism and thus the overall oral bioavailability of atazanavir."( Interactions between phytochemical components of Sutherlandia frutescens and the antiretroviral, atazanavir in vitro: implications for absorption and metabolism.
Bendayan, R; Kanfer, I; Kis, O; Müller, AC; Patnala, S, 2012
)
0.38
" The oral bioavailability of gabapentin displays dose-dependence."( Pharmacokinetic of gabapentin 600 mg tablet in Thai healthy subjects.
Chompootaweep, S; Khemsri, W; Prompila, N; Punyasang, W; Sayankuldilok, N; Thaworn, N; Wittayalertpanya, S, 2012
)
0.38
" Pregabalin is well absorbed in patients with chronic pancreatitis, and the pharmacokinetic profile of pregabalin is not extensively affected by chronic pancreatitis."( The absorption profile of pregabalin in chronic pancreatitis.
Andresen, T; Dahan, A; Drewes, AM; Olesen, AE; Olesen, SS; Olofsen, E; Staahl, C, 2012
)
0.38
"Gabapentin exposure at steady state, as measured by AUC(24), increased with doses from 600 mg/day to 3000 mg/day, although there was a slight decrease in gabapentin's relative bioavailability with increasing dose compared with the 600 mg dose."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
"The pharmacokinetic profile of gabapentin-ER may allow for once- or twice-daily dosing while maintaining bioavailability and thus efficacy."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
" It includes the following aspects: 1) the mechanism of gastroretention of gabapentin GR tablets, 2) in vitro dissolution profiles of the GR and IR formulations, 3) site of absorption of gabapentin in the human intestine, 4) studies of the mechanism of gabapentin absorption using intestinal tissue preparations, 5) human PK studies to examine the effects of dose and formulations on PK profiles and the bioavailability of gabapentin at therapeutically relevant doses, and 6) efficacy and safety of gastroretentive gabapentin in patients with PHN."( The intestinal absorption mechanism of gabapentin makes it appropriate for gastroretentive delivery.
Chen, C; Cowles, VE; Sweeney, M, 2013
)
0.39
" Pregabalin has a linear uptake without transporter saturation at therapeutic dosages, high bioavailability with rapid absorption independent of food intake."( Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy.
Schulze-Bonhage, A, 2013
)
0.39
"To determine the oral bioavailability of a pregabalin capsule relative to a pregabalin solution."( Bioequivalence assessment of a pregabalin capsule and oral solution in fasted healthy volunteers: a randomized, crossover study.
Alvey, CW; Bockbrader, HN; Corrigan, BW; Radulovic, LL, 2013
)
0.39
"To investigate the so-called "drift" with generic-generic drug substitution, a single-dose, four-way crossover comparative bioavailability study was performed involving 24 healthy subjects and three generic and one branded formulation of a tablet containing 800 mg gabapentin as test medication."( Interchangeability of gabapentin generic formulations in the Netherlands: a comparative bioavailability study.
Burger, D; Maliepaard, M; Neef, C; Teerenstra, S; Vanmolkot, F; Yu, Y, 2013
)
0.39
" Bioavailability was 97."( Pharmacokinetics of single-dose intragastric and intravenous pregabalin administration in clinically normal horses.
Divers, TJ; Mullen, KR; Schwark, W, 2013
)
0.39
" Human and animal experiments have shown that tissue-plasminogen activator participates in many mechanisms of action of electroconvulsive therapy or its animal variant, electroconvulsive stimulus, including improved N-methyl-D-aspartate receptor-mediated signaling, activation of both brain-derived neurotrophic factor and vascular endothelial growth factor, increased bioavailability of zinc, purinergic release, and increased mobility of dendritic spines."( Pivotal role of tissue plasminogen activator in the mechanism of action of electroconvulsive therapy.
Hoirisch-Clapauch, S; Mezzasalma, MA; Nardi, AE, 2014
)
0.4
" Absolute bioavailability was 64%."( Study of the absolute bioavailability of citrocard, a new GABA derivative.
Lebedeva, SA; Perfilova, VN; Ryabukha, AF; Smirnova, LA; Suchkov, EA; Tyurenkov, IN, 2013
)
0.39
" Overall, pregabalin is characterized by higher potency, quicker absorption rates and greater bioavailability levels than gabapentin."( Misuse and abuse of pregabalin and gabapentin: cause for concern?
Schifano, F, 2014
)
0.4
" Bioavailability is greater in gabapentin enacarbil as compared to gabapentin."( New treatment options for the management of restless leg syndrome.
Toro, BE, 2014
)
0.4
" Bioequivalence criteria for comparison of pregabalin CR after a low- or medium-calorie breakfast relative to pregabalin IR were not met; however, bioavailability of the pregabalin CR vs."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
"Time of day of administration and the fat and caloric content of the accompanying meal had minimal overall effect on the pharmacokinetic properties and bioavailability of the pregabalin CR formulation."( Pharmacokinetics of pregabalin controlled-release in healthy volunteers: effect of food in five single-dose, randomized, clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
" Relative bioavailability of pregabalin CR was 93-97 % of pregabalin IR, and bioequivalence criteria with respect to the 24-h steady-state exposure (area under the plasma concentration-time curve from 0 to 24 h [AUC24]) were met."( Pregabalin controlled-release pharmacokinetics in healthy volunteers: analysis of four multiple-dose randomized clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
"1 %) and relative bioavailability (F) (26."( Population pharmacokinetics analysis of vigabatrin in adults and children with epilepsy and children with infantile spasms.
Karim, A; Kowalski, KG; Nielsen, JC; Patel, M; Tolbert, D; Wesche, DL, 2014
)
0.4
"Gabapentin was selected to formulate oral controlled release dry suspension because of short biological half life of 5-7 h and low bioavailability (60%)."( Nanosponge-based pediatric-controlled release dry suspension of Gabapentin for reconstitution.
Bhingole, RC; Rao, MR, 2015
)
0.42
"To formulate and evaluate controlled release dry suspension for reconstitution to increase the bioavailability and to control bitter taste of drug."( Nanosponge-based pediatric-controlled release dry suspension of Gabapentin for reconstitution.
Bhingole, RC; Rao, MR, 2015
)
0.42
" The results of in vivo studies showed increase in bioavailability of controlled release suspension by 24."( Nanosponge-based pediatric-controlled release dry suspension of Gabapentin for reconstitution.
Bhingole, RC; Rao, MR, 2015
)
0.42
"The plasma/brain ECF concentration-time profiles of gabapentin were adequately described with a two-compartment plasma model with saturable intestinal absorption rate (K m  = 44."( Pharmacokinetic/Pharmacodynamic Relationship of Gabapentin in a CFA-induced Inflammatory Hyperalgesia Rat Model.
Holm, R; Keizer, R; Kreilgaard, M; Larsen, MS; Munro, G; Mørk, A; Savic, R, 2016
)
0.43
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43
" Dose dependencies were found for morphine absorption rate and gabapentin bioavailability."( Population Pharmacokinetic Modelling of Morphine, Gabapentin and their Combination in the Rat.
Gabel-Jensen, C; Juul, RV; Kreilgaard, M; Lund, TM; Papathanasiou, T, 2016
)
0.43
" Since brain-derived neurotrophic factor (BDNF) promotes GABAergic synaptogenesis, we hypothesized that individual differences in this vulnerability may arise from differences in the link between BDNF bioavailability and FR-evoked wheel running."( Variant BDNF-Val66Met Polymorphism is Associated with Layer-Specific Alterations in GABAergic Innervation of Pyramidal Neurons, Elevated Anxiety and Reduced Vulnerability of Adolescent Male Mice to Activity-Based Anorexia.
Aoki, C; Chen, YW; Lee, F; Rana, BS; Surgent, O, 2017
)
0.46
" Dose-dependent bioavailability of GBP was demonstrated, and the saturable absorption profile was described by a nonlinear hyperbolic function."( Pharmacokinetics and Saturable Absorption of Gabapentin in Nursing Home Elderly Patients.
Ahmed, GF; Bathena, SP; Birnbaum, AK; Brundage, RC; Conway, JM; Leppik, IE; Schwartz, JB, 2017
)
0.46
" Existing functional substances have been assessed as fermentation substrates for better component bioavailability or other functions."( Bioconversion Using Lactic Acid Bacteria: Ginsenosides, GABA, and Phenolic Compounds.
Lee, NK; Paik, HD, 2017
)
0.46
" A significant higher bioavailability of gabapentin administered 30min after meal, compared to fasting conditions or to dose administration 10min before meal, argued in favor of the gastro-retention of gabapentin prolonged release layer."( Multi-kinetics and site-specific release of gabapentin and flurbiprofen from oral fixed-dose combination: in vitro release and in vivo food effect.
Barchielli, M; Bettini, R; Buttini, F; Colombo, G; Colombo, P; Conti, C; Leoni, B; Loprete, L; Rossi, A; Sonvico, F, 2017
)
0.46
"The aim of this study is to enhance solubility and bioavailability via utilizing nanotechnology in the formulation of intranasal Zaleplon nano-emulsion (ZP-NE) to bypass the barriers and deliver an effective therapy to the brain."( Brain Targeted Intranasal Zaleplon Nano-emulsion: In-Vitro Characterization and Assessment of Gamma Aminobutyric Acid Levels in Rabbits' Brain and Plasma at Low and High Doses.
Abd-Elrasheed, E; El-Ashmoony, MM; El-Helaly, SN; Salah, S, 2018
)
0.48
"A NE composed of 10% Miglyol® 812, 40% Cremophor® RH40 40%Transcutol® HP and 10% water successfully enhanced the bioavailability and brain targeting in the rabbits, showing a three to four folds increase than the marketed product."( Brain Targeted Intranasal Zaleplon Nano-emulsion: In-Vitro Characterization and Assessment of Gamma Aminobutyric Acid Levels in Rabbits' Brain and Plasma at Low and High Doses.
Abd-Elrasheed, E; El-Ashmoony, MM; El-Helaly, SN; Salah, S, 2018
)
0.48
"Intranasal zaleplon solid dispersion was formulated to enhance the solubility, bioavailability and deliver an effective therapy."( Brain-targeted intranasal zaleplon solid dispersion in hydrophilic carrier system; 2
Abd-Elrasheed, E; El-Ashmoony, MM; Nageeb El-Helaly, S; Salah, S, 2018
)
0.48
"Gabapentin (GBP), an antiepileptic and anti-neuropathic agent, suffers from short half-life (5-7 h), has narrow absorption window, and is absorbed via carrier-mediated mechanism resulting in frequent dosing, poor compliance, and poor bioavailability (<60%)."( Gastroretentive raft liquid delivery system as a new approach to release extension for carrier-mediated drug.
Aboelwafa, AA; Abouelatta, SM; El-Gazayerly, ON, 2018
)
0.48
" The cooking and taste qualities of GBR were improved by the degradation of the crude fibre of the cortex and the increase in GBR water absorption rate under cyclic cellulase conditioning."( Effects of cyclic cellulase conditioning and germination treatment on the γ-aminobutyric acid content and the cooking and taste qualities of germinated brown rice.
Lan, H; Liu, N; Liu, Y; Wang, S; Zhang, Q, 2019
)
0.51
"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
" The bioavailability of organic iron is higher than that of inorganic iron."( Gamma Aminobutyric Acid Increases Absorption of Glycine-Bound Iron in Mice with Iron Deficiency Anemia.
Ko, HS; Lim, YH; Park, KT; Sim, I, 2020
)
0.56
" Despite its potent anticonvulsant activity, ZP is not commonly used for the treatment of convulsion since ZP is characterized by its low oral bioavailability as a result of poor solubility and extensive liver metabolism."( Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity.
Abosalha, AK; Donia, AA; El-Gizawy, SA; Essa, EA; Haggag, YA; Osman, EY; Tambuwala, MM, 2021
)
0.62
"The absorption and bioavailability of oral gabapentin are associated with a high degree of interindividual variability."( Interindividual Variability in the Bioavailability of Gabapentin Enacarbil Extended Release in Healthy Adults: An Analysis of Data From 6 Phase I Studies.
Ellenbogen, A; Gidal, B; Lal, R, 2022
)
0.72
" The distribution of bioavailability values was assessed in all studies."( Interindividual Variability in the Bioavailability of Gabapentin Enacarbil Extended Release in Healthy Adults: An Analysis of Data From 6 Phase I Studies.
Ellenbogen, A; Gidal, B; Lal, R, 2022
)
0.72
"4 μg·h/mL, and bioavailability range: 64."( Interindividual Variability in the Bioavailability of Gabapentin Enacarbil Extended Release in Healthy Adults: An Analysis of Data From 6 Phase I Studies.
Ellenbogen, A; Gidal, B; Lal, R, 2022
)
0.72
" Soy fermentation can improve the bioavailability of these precious nutrients."( Soy yoghurts produced with efficient GABA (γ-aminobutyric acid)-producing
Chen, LG; Chu, C; Hsieh, CW; Weng, BB; Yuan, HD, 2023
)
0.91

Dosage Studied

Daily dosing increased brain gamma-aminobutyric acid (GABA) in patients with epilepsy. GABA and glycine are likely to activate the same receptors.

ExcerptRelevanceReference
" 4 The dose-response curve for the pressor action of Wy 20051 was potentiated in reserpine-treated anaesthetized rats."( The evaluation of the novel pressor activity of gamma-piperidinobutyramide (WY 20051, DF480).
Alps, BJ; Devoy, PW; Waterfall, JF, 1976
)
0.26
" In this case, however, the dosage of GABA required to produce a given depression was significantly less than the required dosage of glycine."( Effects of excitatory and inhibitory amino acids on phasic respiratory neurons.
Boyarsky, LL; Toleikis, JR; Wang, L, 1979
)
0.26
" No acitvity was detected in other brain areas at various dosed or incubation times."( Effects of kainic acid, a cyclic analogue of glutamic acid, on cyclic nucleotide accumulation in slices of rat cerebellum.
Molloy, BB; Ryan, JJ; Schmidt, MJ, 1976
)
0.26
" In addition, our preparation did not demonstrate the long-lasting responses to bromoaTT-induced depression of the nicotinic responses was studied on the dose-response curves; the mode of receptor inhibition was rather complexed, being neither type of competitive nor non-competitive."( Effects of disulfide bond reduction on the excitatory and inhibitory postsynaptic responses of Aplysia ganglion cells.
Sato, M; Sato, T; Sawada, M, 1976
)
0.26
"Intraperitoneal injection of diazepam in moderate dosage (1--10mg/kg) to rats caused a decrease in dopa and 5-hydroxytryptophan (5-HTP) formation, measured as the accumulation of these intermediates induced by inhibition of the aromatic L-aminoacid decarboxylase by means of NSD 1015 (3-hydroxybenzylhydrazine (HCl), in limbic forebrain, striatum and the remaining hemisphere portion."( On the mode of action of diazepam on brain catecholamine metabolism.
Biswas, B; Carlsson, A, 1978
)
0.26
"Log dose-response curves for induction of contralateral rotational behaviour in the rat by unilateral intranigral injections of the GABA agonist muscimol and the GABA analogue baclofen have been compared."( Baclofen and muscimol: behavioural and neurochemical sequelae of unilateral intranigral administration and effects on 3H-GABA receptor binding.
Cross, AJ; Waddington, JL, 1979
)
0.26
" The dose-response relationship and specifity of this effect were investigated."( Transient apnoea after systemic injection of GABA in the rat.
Hagmüller, K; Holzer, P, 1979
)
0.26
" GABA derivatives in the used dosage caused similar changes in the sleep patterns in case of its disturbances, with a relatively more pronounced action of sodium oxybutyrate."( [Effect of gamma-aminobutyric acid derivatives on sleep disorders in neuroses].
Vlasov, NA, 1978
)
0.65
" Using voltage--clamp technique and local drug application, the dose-response relationships were studied during selective activation either of two kinds of cholinoreceptors available on the identified neuron membrane."( [Study of the chemoreceptor membrane of identified neurons of the gastropod mollusk Planorbarius corneus with different technics of applying chemicals].
Frolova, EV; Gapon, SA; Kachman, AN,
)
0.13
" Pentobarbitone reversibly enhanced the conductance increase produced by GABA with a variable slowing of response kinetics, shifting GABA dose-response curves to the left."( Pentobarbitone pharmacology of mammalian central neurones grown in tissue culture.
Barker, JL; Ransom, BR, 1978
)
0.26
" GABA depressed motor and exploratory activity in rats in a degree dependent on its dosage and inborn exploratory of the rats, and this effect was accompanied by changes in the cerebral cholinergic system."( The central action of gamma-aminobutyric acid in rats.
Bień, E; Herman, ZS; Kmieciak-Kolada, K; Kozok, J; Szwed, A, 1977
)
0.57
" There was a significant progressive loss of GABA with increasing dosage of DPH."( Effect of diphenylhydantoin on gamma aminobutyric acid (GABA) and succinate activity in rat Purkinje cells.
Gabra-Sanders, T; Hitchcock, E, 1977
)
0.26
" GABA both in DA- and in NA-predominated brain regions, the dose-response relations being complex."( The effect of intraperitoneally administered GABA on brain monoamine metabolism.
Biswas, B; Carlsson, A, 1977
)
0.26
" 4 In the frog spinal cord GABA depolarized the dorsal roots presumably by mimicking the activity of the transmitter depolarizing the primary afferents; sigmoidal log dose-response curves for GABA were obtained."( A comparative study of the action of gamma-aminobutyric acid and piperazine on the lobster muscle fibre and the frog spinal cord.
Constanti, A; Nistri, A, 1976
)
0.53
" Relatively specific patterns of action of different drugs in vivo may prove to be largely dependent on their customary rates and routes of administration, and on summation of minor differences in the dose-response curves with different types of neuron, even though the basic types of molecular action may be essentially similar."( Direct effects of ethanol on the nervous system.
Kalant, H, 1975
)
0.25
" 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
)
0.6
" The benzodiazepine effect was evaluated by the shift in the isoguvacine dose-response curve in the absence, then presence, of diazepam."( Reduction in potency of selective gamma-aminobutyric acidA agonists and diazepam in CA1 region of in vitro hippocampal slices from chronic flurazepam-treated rats.
Tietz, EI; Xie, XH, 1992
)
0.56
" The dose-response curve for GABA was shifted to the right by 3 x 10(-3) M 3-aminopropanesulfonic acid."( GABAB receptor-mediated mechanisms in human intestine in vitro.
Cortesini, C; Franchi-Micheli, S; Gentilini, G; Pantalone, D; Zilletti, L, 1992
)
0.28
" At acute dosing of 500 mg/kg, vigabatrin slightly decreased behavioral activity of rats through decreasing the number of trials completed and percent of correct responses."( Effects of single and repeated administration of vigabatrin on the performance of rats in a 5-choice serial reaction time task.
Mazurkiewicz, M; Riekkinen, P; Sirviö, J, 1992
)
0.28
" 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,
)
0.13
" The GABAB receptor antagonist 2-hydroxy-saclofen caused a 10 fold rightward shift of the baclofen dose-response curve, whereas the GABAA receptor antagonist bicuculline (10-50 microM) was ineffective."( Presynaptic GABAB receptor activation attenuates synaptic transmission to rat sympathetic preganglionic neurons in vitro.
Dun, NJ; Wu, SY, 1992
)
0.28
" Unilateral injections of L-glutamate (10 pmol to 100 nmol), or bilateral injections of GABA (1 nmol to 125 nmol), were made into the CVLM, and dose-response effects on arterial pressure determined."( Effect of nucleus tractus solitarius lesions on cardiovascular responses elicited from the caudal ventrolateral medulla.
Blessing, WW; Gieroba, ZJ, 1992
)
0.28
", reduced Feulgen-DNA reactivity), irrespective of the dosage employed and the delay prior to sacrifice."( Cytophotometric analysis of magnocellular azure B-RNA and Feulgen-DNA following chronic GABA infusion into the nucleus basalis of rats.
Anthony, A; Ballough, G; Kan, R; Majchrzak, M; Strauss, J; Will, B, 1992
)
0.28
" Bicuculline (1 microM) shifted the dose-response inhibitory curve of GABA to the right, while the excitatory effect was enhanced."( The distribution and function of gamma-aminobutyric acid (GABA) in the superior colliculus.
Okada, Y, 1992
)
0.56
" A significant improvement was found in the symptomatology of these patients, but relapses occurred when CLZ dosage was reduced."( Sodium valproate and clonazepam for treatment-resistant panic disorder.
Fontaine, R; Ontiveros, A, 1992
)
0.28
"Time- and dose-response studies were carried out on the effects of the monoamine oxidase-inhibiting antidepressant and antipanic drug phenelzine on GABA levels in rat whole brain."( Effects of the antidepressant phenelzine on brain levels of gamma-aminobutyric acid (GABA).
Baker, GB; Coutts, RT; Wong, JT; Yeung, JM, 1991
)
0.52
" The dose-response curve for inhibition of the GABA response by Zn is shifted to the right at a high GABA concentration but is unaffected by the presence of chlordiazepoxide, pentobarbital, or 5 beta-pregnan-3 alpha-ol-20-one."( Negative modulation of the gamma-aminobutyric acid response by extracellular zinc.
Celentano, JJ; Farb, DH; Gibbs, TT; Gyenes, M, 1991
)
0.58
" Dose-response curves for GABA obtained in different preparations were highly reproducible."( The intact central nervous system of the newborn opossum in long-term culture: fine structure and GABA-mediated inhibition of electrical activity.
Møllgård, K; Nicholls, JG; Saunders, NR; Stewart, RR; Treherne, JM; Zou, DJ, 1991
)
0.28
" The relationship held over an extensive range of experimental conditions including different drugs, different dosage levels of the same drug, different time intervals after administration of the same drug, and both single and multiple injections of drugs."( Regulation of the GABAA receptor/ion channel complex by intracellular GABA levels.
Davies, M; Wood, JD, 1991
)
0.28
" An enhancing dose of La3+ shifted the dose-response curve for kainate to lower concentrations of agonist without changing the maximum evoked current, and a similar leftward shift of the quisqualate dose-response curve occurred at non-saturating concentrations of quisqualate."( Lanthanum actions on excitatory amino acid-gated currents and voltage-gated calcium currents in rat dorsal horn neurons.
MacDermott, AB; Reichling, DB, 1991
)
0.28
" The dose-response relation for LY171555 was bell-shaped, with a maximal effect being obtained with 10(-9) M) LY171555."( Opposing effects of dopamine D2 receptor stimulation on the spontaneous and the electrically evoked release of [3H]GABA on rat prefrontal cortex slices.
Besson, MJ; Penit-Soria, J; Rétaux, S, 1991
)
0.28
" Its anticonvulsant effects against 3-mercaptopropionic acid (MPA)-induced seizures in mice is related to the elevation of whole brain GABA concentrations: The mentioned doses of MDL 72483 which cause a decrease of GABA-T activity by 50%, produce within 5 h after dosing an increase of GABA concentration by about 3 mumol."( (4S)-4-amino-5,6-heptadienoic acid (MDL 72483): a potent anticonvulsant GABA-T inhibitor.
Casara, P; Knödgen, B; Sarhan, S; Seiler, N, 1991
)
0.28
" The GBP dosage of 900 mg appeared to be ineffective."( Double-blind study of Gabapentin in the treatment of partial seizures.
Kälviäinen, R; Riekkinen, P; Sivenius, J; Ylinen, A,
)
0.13
" Fischer 344 rats were separated into multiple groups and underwent two dose-response evaluations."( Cerebral radioprotection by pentobarbital: dose-response characteristics and association with GABA agonist activity.
Delaney, T; Friedman, R; Oldfield, EH; Olson, JJ; Orr, K, 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
)
0.28
" The antagonist properties of 6-cyano-2,3-dihydroxy-7-nitroquinoxaline, kynurenate, and gamma-D-glutamylglycine were competitive in nature, inducing parallel rightward shifts of the KA dose-response curves."( Kainate receptors coupled to the evoked release of [3H]-gamma-aminobutyric acid from striatal neurons in primary culture: potentiation by lithium ions.
Bauce, L; Kemp, DE; Tse, FW; Weiss, S, 1990
)
0.53
" Also, Ro5-4864 caused a rightward shift in GABA dose-response curves, increasing the IC50 value for GABA more than 6 fold."( Dependence on gamma-aminobutyric acid of pyrethroid and 4'-chlorodiazepam modulation of the binding of t-[35S]butylbicyclophosphorothionate in piscine brain.
Eshleman, AJ; Murray, TF, 1990
)
0.64
" As in the in vitro experiments, the dose-response curve for the antagonist was shifted rightward in a parallel fashion when D-serine was coinjected."( Activity of 5,7-dichlorokynurenic acid, a potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site.
Baron, BM; Harrison, BL; McDonald, IA; Miller, FP; Palfreyman, MG; Salituro, FG; Schmidt, CJ; Sorensen, SM; White, HS, 1990
)
0.28
" The GABA-A receptor agonist muscimol (25-200 nmol) ICV produced an increase in food intake in which the dose-response relation was most obvious 30-60 min after dosing."( Effects of intracerebroventricular injection of muscimol or GABA on operant feeding in pigs.
Baldwin, BA; De La Riva, C; Ebenezer, IS, 1990
)
0.28
" Although absolute tissue concentrations are not known, dose-response curves constructed using pressure-ejection doses as previously described we found that FG 7142 was more efficacious, but less potent than Ro 15-4513."( GABAergic mechanisms in the electrophysiological actions of ethanol on cerebellar neurons.
Hoffer, BJ; Palmer, MR, 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
)
0.59
" 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
)
0.67
" Histologically, GABA at the high dosage and baclofen at both dosages significantly decreased the labeling index of the antral mucosa and significantly increased the serum gastrin level."( Inhibition by gamma-amino-n-butyric acid and baclofen of gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats.
Baba, M; Ichii, M; Iishi, H; Nakaizumi, A; Taniguchi, H; Tatsuta, M, 1990
)
0.28
" The presence of these different ICl components explains why the dose-response relationship cannot be fitted well by a single Hill equation; the fitting requires a synthesis of 3 suitable Hill equations."( GABA activates different types of chloride-conducting receptor-ionophore complexes in a dose-dependent manner.
Akaike, N; Ishizuka, S; Yasui, S, 1985
)
0.27
" The dose-response curve for GABA-induced Cl- conductance was sigmoidal with the GABA concentration producing a half-maximum response (4."( Interactions of gamma-aminobutyric acid (GABA), pentobarbital, and homopantothenic acid (HOPA) on internally perfused frog sensory neurons.
Akaike, N; Oomura, Y, 1985
)
0.62
" In the presence of DZP, the GABA dose-response curve shifted to the left without changing the maximum current, indicating that DZP modifies the interaction between GABA and its receptor rather than affecting directly the channel activation step."( Diazepam action on gamma-aminobutyric acid-activated chloride currents in internally perfused frog sensory neurons.
Akaike, N; Hattori, K; Oomura, Y, 1986
)
0.6
" The GABA dose-response curve was shifted to the right without changing the maximum response by increasing [Ca2+]i."( Different actions of intracellular free calcium on resting and GABA-gated chloride conductances.
Akaike, N; Inoue, M; Sadoshima, J, 1987
)
0.27
"4 mM Ca2+, the degree of depression was inversely related to the Ca2+ concentration, with an increased sensitivity and sinistral shift of the dose-response curve at lower Ca2+ concentrations."( Calcium dependence of baclofen- and GABA-induced depression of responses to transmural stimulation in the guinea-pig isolated ileum.
Johnston, GA; Kerr, DI; Ong, J, 1987
)
0.27
" A preceding ICa shifted the GABA dose-response curve to the right without affecting the maximum current or the Hill coefficient (n = 2)."( Modulation of the gamma-aminobutyric acid-gated chloride current by intracellular calcium in frog sensory neurones.
Akaike, N; Inoue, M; Tokutomi, N, 1987
)
0.61
" 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
" GABA dose-response measurements were made with and without external Na+."( Sodium-dependent suppression of gamma-aminobutyric-acid-gated chloride currents in internally perfused frog sensory neurones.
Akaike, N; Maruyama, T; Sikdar, SK; Yasui, S, 1987
)
0.27
"We have investigated the effects of an aryl-aminopyridazine derivative of GABA (SR 95531) on dose-response curves of GABA-induced depolarizations from dorsal root ganglion neurones recorded intracellularly."( Quantitative evaluation of the properties of a pyridazinyl GABA derivative (SR 95531) as a GABAA competitive antagonist. An electrophysiological approach.
Bader, MF; Desarmenien, M; Desaulles, E; Feltz, P; Hamann, M, 1988
)
0.27
" However, the dose-response curve for the substance P effect had a biphasic shape."( Differential modulation of striatal dopamine release by intranigral injection of gamma-aminobutyric acid (GABA), dynorphin A and substance P.
Herrera-Marschitz, M; Hökfelt, T; Reid, M; Terenius, L; Ungerstedt, U, 1988
)
0.5
" The Cl- -selective channels were activated after the sequential binding of two GABA molecules to the receptor, as deduced from the slope of the dose-response curve."( Patch-clamp study of gamma-aminobutyric acid receptor Cl- channels in cultured astrocytes.
Bormann, J; Kettenmann, H, 1988
)
0.59
" Dose-response experiments at a holding potential of -45 mV showed that 1) maximal peak responses to glutamate were on the average approximately 40% of those to GABA, 2) the dose-peak response curve for glutamate was steeper than that for GABA, and 3) time-to-peak (risetime) and desensitization half-time decreased monotonically with dose for GABA but were relatively insensitive to dose and more variable for glutamate."( Voltage-clamp characterization of Cl- conductance gated by GABA and L-glutamate in single neurons of Aplysia.
Carpenter, DO; King, WM, 1989
)
0.28
" Lumbar punctures were carried out prior to treatment and at the end of each dosage regimen and cerebrospinal fluid (CSF) evaluated for concentrations of free and total GABA, homocarnosine (GABA-histidine dipeptide), homovanillic acid (HVA), 5-hydroxyindole acetic acid (5-HIAA) and vigabatrin."( The effect of different vigabatrin treatment regimens on CSF biochemistry and seizure control in epileptic patients.
Ben-Menachem, E; Dahlgren, L; Haegele, KD; Hardenberg, J; Huebert, N; Mumford, JP; Persson, LI; Schechter, PJ, 1989
)
0.28
" ACTH(1-24) and 8-bromocyclic AMP both provoked a dose-related release of putrescine-derived GABA, although the dose-response curve for the latter differed somewhat from that for the release of corticosterone by this secretogogue."( Formation of releasable gamma-aminobutyrate from putrescine by rat adrenal slices in vitro.
Gillham, B; Oon, BB; Scraggs, PR, 1989
)
0.28
"5 mM shifted the dose-response curve for GABA to the left."( The effect of GABA on neurotransmission in frog tectal slices.
Arakawa, T; Okada, Y, 1989
)
0.28
" Licking episodes elicited by amphetamine in 11-day-old pups can be magnified by muscimol if the dosage of the former is relatively too potent."( Functional maturation of the GABAergic inhibition on dopamine-mediated behaviours during the neonatal period in the mouse.
Tirelli, E, 1989
)
0.28
" The dose-response curve for GABA was shifted to the right without affecting the maximum response."( Influences of external Ca2+ on the GABA-induced chloride current and the efficacy of diazepam in internally perfused frog sensory neurons.
Akaike, N; Oyama, Y; Yakushiji, T, 1989
)
0.28
" Extracellular Br- [( Br-]o) shifted the dose-response curves of GABA-induced inward anion currents to the left without affecting the maximum values, whereas [Cl-]o, [I-]o, [No3-]o, [HCOO-]o, and [CH3COO-]o altered the rate of desensitization differently without shifting the GABA dose-response curves, indicating that the kinetics of desensitization phase are affected differently by various extracellular anions."( Differential effects of extra- and intracellular anions on GABA-activated currents in bullfrog sensory neurons.
Akaike, N; Inomata, N; Yakushiji, T, 1989
)
0.28
" Data from dose-response curves show that glutamate enhances the GABAA conductance without significantly changing GABA binding affinity."( GABAA responses in hippocampal neurons are potentiated by glutamate.
Stelzer, A; Wong, RK, 1989
)
0.28
" The apparent KD = 417 nM and Bmax = 1083 fmol/mg of membrane protein were calculated using a computer program for dose-response curve fitting."( Further characterisation of the [35S]-TBPS binding site of the GABA receptor complex in locust (Schistocerca gregaria) ganglia membranes.
Brown, MC; Lunt, GC; Stapleton, A, 1989
)
0.28
" The dose-response curve of the GABA-evoked catecholamine release was shifted to the left by midazolam without affecting the maximal response to GABA."( Benzodiazepines facilitate the stimulatory action of gamma-aminobutyric acid (GABA) on basal and veratridine-evoked catecholamine release from cultured bovine adrenal chromaffin cells.
Dohi, T; Kitayama, S; Morita, K; Tsujimoto, A,
)
0.38
"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
)
0.76
" Thus (-)-baclofen (100 microM) shifted the dose-response curve to forskolin to the right 5 fold in an apparently parallel fashion."( GABAB receptor modulation of adenylate cyclase activity in rat brain slices.
Hill, DR, 1985
)
0.27
" The dose-response curve has a slope of 2 in the Hill plot, indicating a bimolecular binding reaction of GABA to the receptor."( gamma-Aminobutyric acid receptor channels in adrenal chromaffin cells: a patch-clamp study.
Bormann, J; Clapham, DE, 1985
)
1.71
"A study was conducted to assess the impact of single dosing and different dosing intervals of vigabatrin [gamma vinyl GABA (GVG)] in 11 patients with drug-resistant complex partial seizures."( Pharmacokinetic effects of vigabatrin on cerebrospinal fluid amino acids in humans.
Ben-Menachem, E, 1989
)
0.28
" Acute and long-term haloperidol administration induced significant leftward displacement of the control dose-response curves for picrotoxin but not those for strychnine or 3-mercaptopropionic acid (3-MPA)."( Behavioral aspects of GABAergic-dopaminergic interactions in the central nervous system.
Palermo-Neto, J; Sandoval, MR, 1989
)
0.28
" Dose-response curves of isoguvacine, a specific GABAA agonist, showed a shift to the right for the intrinsic bursting cells whatever the parameter measured (depolarization or conductance increase): the ED50 was 50-100 times higher for intrinsic bursting cells than for other non-intrinsic bursting cells, thus indicating that intrinsic bursting cells are tolerant to GABAA agonist."( Relationship between tolerance to GABAA agonist and bursting properties in neocortical neurons during GABA-withdrawal syndrome.
Brailowsky, S; Champagnat, J; Menini, C; Naquet, R; Silva-Barrat, C, 1989
)
0.28
" The overall pattern of decreased glucose use seen with progabide was different from that noted with previously studied GABA-mimetic drugs, such as muscimol, except for those changes observed in the extrapyramidal and sensory-motor areas for which similar dose-response relationships occurred."( Effects of the GABA receptor agonist, progabide, upon local cerebral glucose utilization.
Cudennec, A; Duverger, D; Lloyd, KG; MacKenzie, ET; McCulloch, J; Motohashi, N; Nishikawa, T; Scatton, B, 1987
)
0.27
" There was a sinistral shift of the GABA dose-response curve in the presence of 10 pM cortisol, with a significant potentiation of the GABA-induced contractions over the lower dose range of GABA (3-30 microM), whereas 100 nM cortisol caused a non-parallel dextral shift of the GABA dose-response curve, with a depression of the maximum GABA response indicative of non-competitive antagonism."( Cortisol: a potent biphasic modulator at GABAA-receptor complexes in the guinea pig isolated ileum.
Johnston, GA; Kerr, DI; Ong, J, 1987
)
0.27
" The characteristics of dose-response curves of GABA-induced Cl- currents (ICl) were mainly studied using the "concentration-clamp" technique, by which the external solution around isolated single neurons was rapidly changed within a few milliseconds."( Selective effects of enzyme treatment used for dissociating single cells on their GABA-receptor activities.
Akaike, N; Inoue, M, 1987
)
0.27
" The GABA antagonists 2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride (SR 95103) and 3-alpha-hydroxy-16-imino-5 beta-17-aza-androstan-11-one (R 5135) shifted and suppressed the dose-response curve of GABA on diazepam binding."( GABAA receptor populations bind agonists and antagonists differentially and with opposite affinities.
Maksay, G, 1988
)
0.27
" Dose-response curves were determined by administering cumulative doses IV during timeout periods that preceded sequential components of the fixed-interval schedule."( GABA-related drugs modulate the behavioral effects of lorazepam.
Spealman, RD; Wettstein, JG, 1988
)
0.27
" 3) The phenomenon was specific since the dose-response curve of the adenosine-inhibitory effect was comparable in preparations from tolerant animals and controls."( Decreased response to GABA-B agonists in longitudinal smooth muscle-myenteric plexus preparations from morphine-tolerant guinea-pigs.
Ciuffi, M; Franchi-Micheli, S; Gentilini, G; Gori, AM; Luzzi, S; Zilletti, L, 1988
)
0.27
" An analysis with dose-response curves revealed that 5-HT potentiated the maximum GABA current (Vmax), while it produced no significant change in the apparent dissociation constant (Km)."( 5-Hydroxytryptamine facilitates GABA-induced depolarization in bullfrog primary afferent neurons.
Akasu, T, 1988
)
0.27
" 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
)
0.27
" In this preparation, all these antagonists shifted the NMDA dose-response curve to the right in a parallel manner."( Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex.
Harrison, NL; Simmonds, MA, 1985
)
0.27
" Complete dose-response curves were carried out on individual neurons, reducing error introduced by cell-to-cell variability."( Modulation of neurotransmitter action: control of the gamma-aminobutyric acid response through the benzodiazepine receptor.
Chan, CY; Farb, DH, 1985
)
0.52
" An agonist of the GABAA receptor, muscimol, produces a dose-response curve similar to that of GABA, whereas the agonist of the GABAB receptor, baclofen, did not alter the membrane potential."( Pharmacological properties of gamma-aminobutyric acid-, glutamate-, and aspartate-induced depolarizations in cultured astrocytes.
Kettenmann, H; Schachner, M, 1985
)
0.56
" This dose-response curve of L-Glu was shifted to the left in the presence of D-Asp, although the maximal amount of release was unchanged."( Effects of D-aspartate on excitatory amino acid-induced release of [3H]GABA from goldfish retina.
Cha, JH; Dowling, JE; O'Brien, DR, 1986
)
0.27
" Addition of the acetylcholinesterase inhibitor, physostigmine, caused a leftward shift in the GABA dose-response curve and increased by 10-fold the sensitivity of the antral preparation to GABA stimulation."( Cholinergic mediation of gamma-aminobutyric acid-induced gastrin and somatostatin release from rat antrum.
Franklin, PA; Harty, RF, 1986
)
0.57
"Using a microperfusion technique for rapid application of agonists to single identified voltage-clamped neurons of the marine mollusc Aplysia, chloride conductances elicited by gamma-aminobutyric acid (GABA) and L-glutamate were found to differ in rates of activation and desensitization, voltage dependence and dose-response relations."( Distinct GABA and glutamate receptors may share a common channel in Aplysia neurons.
Carpenter, DO; King, WM, 1987
)
0.47
" In each case, the dose-response curve for the neurotoxin was extended, with about 50% of evoked release being inhibited at approximately 10 nM whereas 200 nM was required for the maximal blockade."( Characterization of the inhibitory action of botulinum neurotoxin type A on the release of several transmitters from rat cerebrocortical synaptosomes.
Ashton, AC; Dolly, JO, 1988
)
0.27
" Dose-response and time-course studies revealed that baclofen has little influence on neurotransmitter recognition site affinity, but rather enhances the synthesis or accumulation of second messenger that occurs in response to these agents."( Characterization of the relationship between gamma-aminobutyric acid B agonists and transmitter-coupled cyclic nucleotide-generating systems in rat brain.
Enna, SJ; Karbon, EW, 1985
)
0.53
" The dose-response relationships for GABA antagonism of [3H]alpha-dihydropicrotoxinin binding and for picrotoxinin antagonism of the GABA enhancement of [3H]flunitrazepam binding in cultured cortical neurons were also investigated."( The picrotoxinin binding site and its relationship to the GABA receptor complex.
Dichter, MA; Snodgrass, SR; White, WF, 1985
)
0.27
" 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
" Examination of the dose-response relation for GABA alone and in the presence of midazolam or flurazepam showed that the maximal response to GABA was increased by the benzodiazepine in some cells while it was unchanged in others."( Actions and interactions of GABA and benzodiazepines in the mouse hippocampal slice.
Biscoe, TJ; Duchen, MR, 1985
)
0.27
" The inhibitory effects of the selective GABAA-receptor agonists isoguvacine and muscimol were antagonized by bicuculline methochloride, which shifted the dose-response curves to the right in a parallel manner."( Quantitative evaluation of the potencies of GABA-receptor agonists and antagonists using the rat hippocampal slice preparation.
Kemp, JA; Marshall, GR; Woodruff, GN, 1986
)
0.27
"4,6,6-Trimethylcaprolactam antagonised GABAA receptor-mediated contractile responses in guinea-pig isolated ileum, displacing the GABA dose-response curve to the right in a non-parallel manner, and causing a depression of the maximum response."( Caprolactam-barbiturate interaction at the GABAA receptor complex in the guinea-pig intestine.
Kerr, DI; Ong, J; Prager, RH; Ward, DA, 1986
)
0.27
" Midazolam (greater than 10(-6) M) reliably potentiated GABA responses with a parallel shift to the left of the dose-response curve."( Electrophysiological studies in cultured mouse CNS neurones of the actions of an agonist and an inverse agonist at the benzodiazepine receptor.
Jensen, MS; Lambert, JD, 1986
)
0.27
" The dosage of MV-GABA which caused locomotor hypoactivity produced an impairment of the rotarod performance."( [Behavioral pharmacological action of Ca-4-(3,5-dihydroxy-3-methylpenthylamido) butyrate (mevalonic GABA, MV-GABA)].
Kameyama, T; Nabeshima, T; Noda, Y, 1987
)
0.27
"Safety and efficacy studies of new antiepileptic drugs require strict adherence to prescribed dosage regimens."( Compliant populations: variability in serum concentrations.
Graves, NM; Holmes, GB; Leppik, IE, 1988
)
0.27
"" Midazolam caused a shift to the left of the GABA log dose-response curve."( Modulation of GABA-gated chloride ion flux in rat brain by acute and chronic benzodiazepine administration.
Chiu, TH; Rosenberg, HC; Yu, O, 1988
)
0.27
" The dose-response curve of ifenprodil tartrate was shifted to the left by pre-incubation in calcium hopantenate."( A possible mechanism on the potentiating vascular effect of coadministration of ifenprodil tartrate and calcium hopantenate: a study in the internal carotid artery.
Honda, H; Irino, O; Iwata, T; Izumisawa, M; Matsuda, H; Shibuya, T; Shimura, H; Tsuji, H; Watanabe, Y, 1988
)
0.27
"0 mg/kg AOAA significantly potentiated the effects of diazepam, as indicated by a significant shift to the left in the diazepam dose-response curve relative to diazepam alone."( Potentiation of the anticonflict effects of diazepam, but not pentobarbital and phenobarbital, by aminooxyacetic acid (AOAA).
Beshears, JF; Commissaris, RL; Halas, NA; McCloskey, TC, 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
" The dose-response relationships of excitatory amino acids demonstrated the following rank order of potency: glutamate greater than aspartate = N-methyl-D-aspartate greater than kainate much greater than quisqualate."( Excitatory amino acid-evoked release of gamma-[3H]aminobutyric acid from striatal neurons in primary culture.
Weiss, S, 1988
)
0.27
" Values for the Hill coefficient derived from dose-response curves suggested that the binding of 2 molecules of GABA to the receptor is required for the activation of the chloride channel."( A patch clamp study of gamma-aminobutyric acid (GABA)-induced macroscopic currents in rat melanotrophs in cell culture.
Hughes, D; Kehl, SJ; McBurney, RN, 1987
)
0.58
" 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
)
0.54
" Replacement of [Na]o with Li+ completely removed the Na+ suppression, and GABA dose-response curve in Li+ external solution agreed well with that in Na+-free (Tris+) external solution."( Inhibition of Na+-dependent GABA uptake in isolated frog sensory nerve cell bodies by extra- and intracellular Li+.
Akaike, N; Ikemoto, Y; Nagasawa, K; Tokutomi, N, 1987
)
0.27
"gamma-Vinyl GABA (GVG), an irreversible inhibitor of GABA degradation, was administered to seizure-susceptible gerbils at different dosage regimens."( One to three day dose intervals during subchronic treatment of epileptic gerbils with gamma-vinyl GABA: anticonvulsant efficacy and alterations in regional brain GABA levels.
Frey, HH; Löscher, W, 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
" Bilateral nigral infusions of muscimol markedly facilitated the development of flurothyl seizures in a dose-response manner and differed significantly from the vehicle controls or rats infused with muscimol dorsally to the substantia nigra."( Age-related substantia nigra-mediated seizure facilitation.
Moshe, SL; Okada, R; Sperber, EF; Wong, BY; Zhao, DY, 1986
)
0.27
" A rigorous system of analysis was devised making use of the dose-response profiles in each of the 61 brain areas to construct a regional hierarchy of responsiveness to the three drugs and allowing comparison of their effects on the brain as a whole."( The effect of diazepam upon local cerebral glucose use in the conscious rat.
Ford, I; Kelly, PA; McCulloch, J, 1986
)
0.27
" Neurons in the thiamine-deficient animals were more sensitive to the inhibitory effects of 5-HT, as demonstrated by a significant parallel shift to the left of the dose-response curve."( Enhanced sensitivity of cerebellar Purkinje cells to iontophoretically-applied serotonin in thiamine deficiency.
Lee, RS; Strahlendorf, HK; Strahlendorf, JC, 1985
)
0.27
" Dosage and duration of drug treatment did not influence striatal or cortical GAD levels."( Brain glutamate decarboxylase in Parkinson's disease with particular reference to a premortem severity index.
Agid, Y; Dubois, B; Hauw, JJ; Javoy-Agid, F; Monfort, JC, 1985
)
0.27
" Observation of behaviour indicated that the novel GABA uptake blockers exerted no side-effects in anticonvulsant doses, whereas diazepam produced sedative effects at all active dosage levels."( Comparison of the anticonvulsant effects of two novel GABA uptake inhibitors and diazepam in amygdaloid kindled rats.
Löscher, W; Schwark, WS, 1985
)
0.27
" The log dose-response curve for depolarization was sigmoid with a mean ED(50) of 12."( Depolarizing actions of gamma-aminobutyric acid and related compounds on rat superior cervical ganglia in vitro.
Bowery, NG; Brown, DA, 1974
)
0.56
" Diazepam shifted GABA dose-response curves to the left by decreasing the apparent KD but without altering the apparent Vmax (Lineweaver-Burk analysis)."( Benzodiazepine receptor ligand actions on GABA responses. Benzodiazepines, CL 218872, zopiclone.
Macdonald, RL; Skerritt, JH, 1984
)
0.27
" Midazolam (10(-7)-10(-5) M) potentiated responses to all three agonists to a similar extent with a shift to the left of the dose-response curve."( Modulation of the responses to the GABA-mimetics, THIP and piperidine-4-sulphonic acid, by agents which interact with benzodiazepine receptors. An electrophysiological study on cultured mouse neurones.
Jensen, MS; Lambert, JD, 1984
)
0.27
" Dose-response data were obtained for barbiturate concentrations ranging from 1 microM to 3 mM."( Effects of barbiturates on inhibitory and excitatory responses to applied neurotransmitters in Aplysia.
Cote, IL; Wilson, WA, 1980
)
0.26
" Prevention is easy if treatment is gradually rather than abruptly withdrawn in all patients who receive the compound in high dosage for more than one month."( [Benzodiazepine physical dependence. 6 cases (author's transl)].
Bismuth, C; Dally, S; Lagier, G; Le Bellec, M, 1980
)
0.26
" Dose-response curves were constructed for amino-oxyacetic acid and gamma-acetylenic GABA."( Blockade of methamphetamine-induced depression of tyrosine hydroxylase by GABA transaminase inhibitors.
Gibb, JW; Hotchkiss, A, 1980
)
0.26
" 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
" In a dose-response study (2-26 nmol), 8 nmol caused a 46% decrease in striatal choline acetyltransferase (CAT) activity with minimal effects on the activities of glutamate decarboxylase (GAD) and tyrosine hydroxylase (TH) at 7 days."( Selective cholinergic neurotoxin: AF64A's effects in rat striatum.
Coyle, JT; Fisher, A; Hanin, I; Sandberg, K, 1984
)
0.27
" This dosage regimen produced a decrease in the forebrain concentrations of DA and NE at 7 and 20 days after injection."( Effect of 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP) on monoamine neurotransmitters in mouse brain & heart.
Boldry, R; Miller, D; Schmittgen, T; Uretsky, N; Wallace, RA, 1984
)
0.27
" Further, each dosing paradigm has been evaluated with a view to experimental error and interactive variables."( Effects of early lead exposure on neurotransmitter systems in the brain. A review with commentary.
Shellenberger, MK, 1984
)
0.27
" 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
" From an analysis of the dose-response curve of GABA with or without ibotenate, it is suggested that ibotenate acts on the GABA receptor in the crayfish neuromuscular junction."( Inhibitory action of ibotenic acid on the crayfish neuromuscular junction.
Ishida, M; Shinozaki, H, 1980
)
0.26
" Analysis of the effect of naloxone on GABA dose-response curves indicates that naloxone acts as a competitive antagonist at the neuronal GABA receptors."( Naloxone antagonism of GABA-evoked membrane polarizations in cultured mouse spinal cord neurons.
Barker, JL; Gruol, DL; Smith, TG, 1980
)
0.26
" The i--response counteracts the inhibitory effect of GABA at low GABA concentrations and can distort the dose-response curve."( Closing of membrane channels effected by gamma-amino-butyric acid (GABA) in crayfish muscle.
Dudel, J; Finger, W, 1980
)
0.26
" accommodation was enhanced) at the anesthetic dosage level."( A comparison of the effects of pentobarbital and diphenylhydantoin on the GABA sensitivity and excitability of adult sensory ganglion cells.
Connors, BW, 1981
)
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
" Step clamp data were used to construct dose-response curves."( Voltage clamp analysis of inhibitory synaptic action in crayfish stretch receptor neurons.
Adams, PR; Banks, FW; Constanti, A, 1981
)
0.26
" First, since two GABA-molecules are required to activate GABA-coupled chloride ion channels, the dose-response relationship for GABA is sigmoidal and steep."( Pharmacology of GABA-mediated inhibition of spinal cord neurons in vivo and in primary dissociated cell culture.
Macdonald, RL; Young, AB, 1981
)
0.26
" When washed P2 membranes were subjected to high-frequency homogenization, the biphasic dose-response relationship for pentobarbitone was markedly shifted to the right."( Dual action of pentobarbitone on GABA binding: role of binding site integrity.
Johnston, GA; Willow, M, 1981
)
0.26
" Picrotoxin, and agent which blocks the chloride ionophore of GABA-receptor complex, exhibited a parallel dose-response curve with respect to muscimol."( Acute and chronic effects of pentobarbital in relation to postsynaptic GABA receptors: a study with muscimol.
Ho, IK; Nabeshima, T; Sivam, SP, 1982
)
0.26
" The dose-response curve shifted to the right when the resting membrane was hyperpolarized, a fact suggesting an increase in apparent dissociation constant (Kapparent) of the receptor-GABA complex."( The voltage-dependent nature of the GABA-induced conductance change recorded from the ganglion cell of Aplysia.
Matsumoto, M, 1982
)
0.26
" Low concentrations (1 nM) of (+)-propranolol were observed to be equipotent with (+/-)-propranolol in shifting the dose-response curve of GABA-stimulated [3H]diazepam binding by approximately 1/2 log unit."( Nanomolar concentrations of propranolol inhibit GABA-stimulated benzodiazepine binding to rat cerebral cortex.
Morgan, PF; Stone, TW, 1982
)
0.26
" Bicuculline methobromide (13 microM) antagonized this action of SL75102 and shifted the log dose-response curve to the same extent as the GABA curve."( Evidence that SL75102 is an agonist at GABAb as well as GABAa receptors.
Bowery, NG; Hill, DR; Hudson, AL, 1982
)
0.26
" 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
)
0.26
" 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
" After chronic dosing the sedative effects of flunitrazepam showed tolerance and the increases in exploration remained while locomotion was less increased."( Effects of agents which enhance GABA-mediated neurotransmission on licking conflict in rats and exploration in mice.
Gardner, CR; Piper, DC, 1982
)
0.26
" We examined ionophoretic dose-response relations of the cells at stage 26, a couple of hours after the first acquisition of GABA sensitivity."( The appearance and development of chemosensitivity in Rohon-Beard neurones of the Xenopus spinal cord.
Bixby, JL; Spitzer, NC, 1982
)
0.26
" These actions of barbiturates were not accompanied by changes in the apparent dissociation constant of the GABA-current dose-response curve or the reversal potential for GABA currents."( Effect of barbiturates on the GABA receptor of cat primary afferent neurones.
Higashi, H; Nishi, S, 1982
)
0.26
" Dose-response curves were obtained for gamma-aminobutyric acid (GABA) in the presence and in the absence of glycine, and it was concluded that GABA and glycine are likely to activate the same receptors."( Effects of glycine on the crayfish neuromuscular junction. I. Glycine-operated inhibitory postsynaptic channels and a glycine-effected decrease in membrane conductance.
Finger, W, 1983
)
0.53
" A new technique was developed to permit the determination of complete electrophysiological dose-response curves on single neurons in cell culture, eliminating cell-to-cell variability as a problem that complicates the interpretation of pooled data."( Multiple embryonic benzodiazepine binding sites: evidence for functionality.
Borden, LA; Chan, CY; Farb, DH; Gibbs, TT, 1983
)
0.27
" Dose-response analysis of the action of ATP on the GABA-induced response suggests that the facilitatory action of ATP on the GABA response is effected on the GABA receptor channel complexes without changing the GABA affinity."( Actions of ATP on the soma of bullfrog primary afferent neurons and its modulating action on the GABA-induced response.
Akasu, T; Katayama, Y; Koketsu, K; Morita, K, 1984
)
0.27
" 2-week treatment periods were used; the median daily oral dosage of progabide was 24."( The effect of the GABA-agonist, progabide, on stretch and flexor reflexes and on voluntary power in spastic patients.
Mondrup, K; Pedersen, E, 1984
)
0.27
" The median daily dosage of progabide was 24."( The clinical effect of the GABA-agonist, progabide, on spasticity.
Mondrup, K; Pedersen, E, 1984
)
0.27
" Progabide was added to the concomitant antiepileptic treatment in a fixed dosage schedule."( Progabide: a controlled trial in partial epilepsy.
Angelo, HR; Christensen, JM; Dam, M; Gram, L; Hansen, BS; Lyon, BB; Philbert, A, 1983
)
0.27
" 4-hydroxybenzaldehyde, a potent SSADH inhibitor did not increase GABA level at a dosage which induces a 99% inhibition of SSADH."( [Mechanism of action of an anticonvulsant, sodium dipropylacetate].
Ciesielski, L; Gobaille, S; Klein, M; Mandel, P; Simler, S, 1981
)
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
" Protoveratrine A increased the uptake of 22Na+ into the slices with a similar dose-response curve to that found for gamma-aminobutyrate release."( The role of Ca2+ in the protoveratrine-induced release of gamma-aminobutyrate from rat brain slices.
Minchin, MC, 1980
)
0.26
" However, the effect on seizure threshold could not be enhanced by an increase in the daily dosage of the GABA-T inhibitors and, especially with higher doses, tolerance to the anticonvulsant effect developed."( Anticonvulsant and biochemical effects of inhibitors of GABA aminotransferase and valproic acid during subchronic treatment in mice.
Löscher, W, 1982
)
0.26
" Testicular weight was significantly lower in the group of rats treated with the low dosage of GAG (5 mg/kg), and serum prolactin was significantly lower in the rats treated with the high dosage of GAG (20 mg/kg) as compared with control rats."( Prolonged treatment with gamma-aminobutyric acid (GABA)-mimetic substances in prepubertal male rats.
Debeljuk, L; Díaz, MD; Maines, VM; Seilicovich, A, 1983
)
0.57
" 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
" Plasma prolactin levels, initially high, increased when the dosage was increased to 100 mg/day but did not increase further."( High doses of haloperidol in schizophrenia. A clinical, biochemical, and pharmacokinetic study.
Bianchetti, G; Cuche, H; Loo, H; Morselli, PL; Scatton, B; Zarifian, E, 1982
)
0.26
" In neither patient, the increase in haloperidol dosage affected paranoid symptoms."( [Use of haloperidol in high doses in schizophrenia. Clinical, biochemical and pharmacokinetic study].
Bianchetti, G; Cuche, H; Loo, H; Morselli, PL; Scatton, B; Zarifian, E, 1982
)
0.26
" In vitro ethanol dose-response curves (0-1."( Norepinephrine, gamma-aminobutyric acid, and choline reuptake kinetics and the effects of ethanol in long-sleep and short-sleep mice.
Collins, AC; Howerton, TC; Marks, MJ, 1982
)
0.61
"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
)
0.26
" 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
)
0.26
" These sites appear to be interdependent since analysis of the shift in the DPH dose-response curve by PTX and vice versa, showed neither truly non-competitive nor competitive interaction."( On the action of the anticonvulsant 5,5-diphenylhydantoin and the convulsant picrotoxin in crayfish stretch receptor.
Aickin, CC; Deisz, RA; Lux, HD, 1981
)
0.26
" Similar studies were conducted with rats treated at the highest lead dosage which did not result in weight loss (100 microgram lead as lead acetate/g body weight/day via intubation)."( Developmental studies of the uptake of choline, GABA and dopamine by crude synaptosomal preparations after in vivo or in vitro lead treatment.
Krigman, MR; Morell, P; Ramsay, PB, 1980
)
0.26
" The log dose-response relationship obtained from 6 preparations was sigmoidal and had an ED(50) of 13 muM."( The effect of gamma-aminobutyric acid on the input conductance and membrane potential of Ascaris muscle.
Martin, RJ, 1980
)
0.62
" The dose-response curves for GABA and glycine were sigmoidal with saturating concentrations of 100 and 300 microM, respectively."( GABA- and glycine-activated currents in the rod bipolar cell of the rabbit retina.
Dacheux, RF; Gillette, MA, 1995
)
0.29
" The EC50 obtained from the dose-response curves for GABA in eliciting a maximal response was comparable in neurons maintained in high K+ or in low K+ and treated with a single dose of NMDA, but that it increased significantly in cells maintained in low K+."( NMDA-mediated modulation of gamma-aminobutyric acid type A receptor function in cerebellar granule neurons.
Grayson, DR; Harris, BT; Vicini, S; Zhu, WJ, 1995
)
0.59
" The dose-response relationships for potentiation of 1 microM GABA-mediated chloride currents were studied for [3S-(3 alpha, 3a alpha, 5a beta, 7 beta, 9a alpha, 9b beta)]-1- [dodecahydro-7-(2-hydroxyethyl)-3a-methyl-1H-benz[e]inden-3- yl]ethanone (3), steroid 7, 3 alpha-hydroxy-5 alpha-pregnan-20-one (5), and the analogous 7 alpha-(2-hydroxyethyl)benz[e]indene analogue of steroid 5 (compound 1)."( Neurosteroid analogues. 3. The synthesis and electrophysiological evaluation of benz[e]indene congeners of neuroactive steroids having the 5 beta-configuration.
Covey, DF; Han, M; Hu, Y; Zorumski, CF, 1995
)
0.29
" Although there appears to be a clear dose-response relationship up to 3 g/day, it is not well documented if higher doses result in proportionately higher brain GABA levels."( Vigabatrin: effect on brain GABA levels measured by nuclear magnetic resonance spectroscopy.
Behar, K; Mattson, RH; Petroff, OA; Rothman, D, 1995
)
0.29
" The current dosage regime of anticonvulsants were maintained during the trial period."( Open label trial with vigabatrin in children with intractable epilepsy.
Wong, V,
)
0.13
" The EC50 of the GABA dose-response curve for the alpha 1 beta 2 combination was lower than that for the alpha 1 beta 2 gamma 2s combination."( Alcohol modulation of cloned GABAA receptor-channel complex expressed in human kidney cell lines.
Carter, DB; Hamilton, BJ; Kurata, Y; Marszalec, W; Narahashi, T, 1993
)
0.29
" Octanol produced a shift of the current dose-response curve toward lower concentrations of GABA."( Selective effects of alcohols on gamma-aminobutyric acid A receptor subunits expressed in human embryonic kidney cells.
Carter, DB; Hamilton, BJ; Kurata, Y; Marszalec, W; Narahashi, T, 1994
)
0.57
" In the flurothyl seizure model, SNR microinjection of the selective GABAA receptor agonist muscimol results in a biphasic dose-response curve in adults: Intermediate doses are anticonvulsant, but high doses have proconvulsant effects."( Age-related differences in the effects of GABAA agonists microinjected into rat substantia nigra: pro- and anticonvulsant actions.
Garant, DS; Moshé, SL; Sperber, EF; Xu, SG, 1995
)
0.29
" After 1-month observation, the patients entered a 7-month treatment period that involved administration of placebo for 1 month followed by VGB at the initial dosage of 40 mg/kg/day, to be increased to 60 and 80 mg/kg/day at 2-month intervals if seizures persisted."( Efficacy and tolerability of vigabatrin in children with refractory partial seizures: a single-blind dose-increasing study.
Buti, D; Cianchetti, C; Dalla Bernardina, B; Fontana, E; Fusco, L; Galeone, D; Gnanasakthy, A; Iudice, A; Torelli, D; Vigevano, F, 1995
)
0.29
" In the case of the wild type receptor, fipronil blocked GABA-induced currents inducing both a shift to the right in the GABA dose-response curve and depressing the maximum amplitude of responses to GABA."( Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila melanogaster.
Baylis, HA; Buckingham, SD; Hosie, AM; Sattelle, DB, 1995
)
0.29
" However, intravenous pharmacokinetics in rats were linear over the dosage range of 4-500 mg/kg."( Disposition of gabapentin (neurontin) in mice, rats, dogs, and monkeys.
Bockbrader, HN; Chang, T; DeHart, PD; Hanson, BJ; McNally, WP; Radulovic, LL; Türck, D; Vollmer, KO; von Hodenberg, A, 1995
)
0.29
" This effect which was quantified in terms of numbers of tongue protrusions, was dose-dependent: a bell-shaped dose-response was found (50-500 ng)."( Interactions of the subthalamic nucleus and the subpallidal area in oro-facial dyskinesia: role of GABA and glutamate.
Cools, AR; Helfrich, SE; Spooren, WP, 1995
)
0.29
" The plasma concentration ratio of the [R] to [S] enantiomers appears to remain constant across the vigabatrin dosage interval in adult volunteers, and in the present study this has also proved to be the case in 12 chronically treated adult epileptic patients."( Plasma vigabatrin enantiomer ratios in adults and children.
Appleton, DB; Burke, CJ; Eadie, MJ; Nagarajan, L; Schramm, T, 1993
)
0.29
" Oral dosing [3 mg/ml of drinking water, giving doses of GVG of 194 +/- 38 mg/kg/day and of EOS of 303 +/- 42 mg/kg/day (mean +/- SD)] was followed by microdialysis at 2, 8, and 21 days."( The effect of chronic treatment with the GABA transaminase inhibitors gamma-vinyl-GABA and ethanolamine-O-sulphate on the in vivo release of GABA from rat hippocampus.
Fowler, LJ; Qume, M; Whitton, PS, 1995
)
0.29
", significantly lowered the convulsive threshold of pentylenetetrazol (PTZ) in mice and shifted the dose-response curve of PTZ."( Correlation between in vitro and in vivo models of proconvulsive activity with the carbapenem antibiotics, biapenem, imipenem/cilastatin and meropenem.
Day, IP; Goudie, J; Nishiki, K; Williams, PD, 1995
)
0.29
" Co-expression of the mutants with beta 2 and gamma 2 subunits in human embryonic kidney cells produced functional receptors which are similar to the wild type in their sensitivity to a benzodiazepine agonist (U-92330), insensitivity to Zn, anion permeability, and GABA dose-response profiles as monitored with the whole cell patch clamp technique."( Acceleration of GABA-dependent desensitization by mutating threonine 266 to alanine of the alpha 6 subunit of rat GABAA receptors.
Altman, RA; Binder, JA; Dillon, GH; Im, HK; Im, WB; Pregenzer, JF, 1995
)
0.29
" We evaluated the cognitive and quality-of-life (QOL) effects of VGB in a double-blinded, add-on, placebo-controlled, parallel group dose-response study of patients with focal epilepsy whose complex partial seizures (CPS) were difficult to control."( Effects of differing dosages of vigabatrin (Sabril) on cognitive abilities and quality of life in epilepsy.
Arnett, JL; Dodrill, CB; Sommerville, KW; Sussman, NM, 1995
)
0.29
"4 the GABA dose-response curve indicates that the increases in the peak current are related to an augmented maximal current."( Modulation by extracellular pH of the activity of GABAA receptors on rat cerebellum granule cells.
Baldelli, P; Cupello, A; Robello, M, 1994
)
0.29
"Time- and dose-response analyses were undertaken to investigate the effects of the substituted hydrazine monoamine oxidase (MAO) inhibitors iproniazid and nialamide on the following: MAO-A and -B activity; levels of gamma-aminobutyric acid (GABA), alanine (ALA), and the neurotransmitter amines dopamine, noradrenaline, and 5-hydroxytryptamine (serotonin) and their acid metabolites; and the activity of GABA-transaminase and ALA-transaminase."( Effects of two substituted hydrazine monoamine oxidase (MAO) inhibitors on neurotransmitter amines, gamma-aminobutyric acid, and alanine in rat brain.
Baker, GB; Paetsch, PR; Takahashi, S; Todd, KG; Yamada, N, 1993
)
0.69
" In view of the evidence for the role of excitatory amino acids in destruction of CNS nerve cells, the optimal treatment must counteract the raised levels of CSF glutamate and the dosage of vitamin B6 must be adjusted accordingly."( Glutamate in pyridoxine-dependent epilepsy: neurotoxic glutamate concentration in the cerebrospinal fluid and its normalization by pyridoxine.
Baumeister, FA; Egger, J; Gsell, W; Shin, YS, 1994
)
0.29
"Data from published research were extracted and evaluated according to study design, sample size, dosing regimen, outcome measures, and treatment efficacy and safety."( Treatment of infantile spasms.
Casto, DT; Haines, ST, 1994
)
0.29
" In an attempt to image these changes in vivo, we performed high-field MRI on seven treated and four control dogs at baseline and after 15 weeks of dosing with vigabatrin (300 mg/kg/d)."( MRI monitoring of vigabatrin-induced intramyelinic edema in dogs.
Arezzo, JC; Gibson, JP; Heydorn, WE; Kastin, SJ; McBride, RG; Schroeder, CE; Sussman, NM; Weiss, KL; Yarrington, JT, 1994
)
0.29
" Propofol evoked current responses (EC50 = 61 microM) and shifted the dose-response curve of GABA-activated current to the left without altering the maximum of the GABA response."( Propofol modulates activation and desensitization of GABAA receptors in cultured murine hippocampal neurons.
MacDonald, JF; Orser, BA; Pennefather, PS; Wang, LY, 1994
)
0.29
" The dose-response profile of U-94863 in the alpha 1 beta 2 subtype was largely indistinguishable from that in the alpha 1 beta 2 gamma 2 subtype, suggesting no critical role for the gamma 2 subunit in potentiation of the GABA response by the pyrazinones."( Substituted pyrazinones, a new class of allosteric modulators for gamma-aminobutyric acidA receptors.
Carter, DB; Gammill, RB; Hamilton, BJ; Im, HK; Im, WB; Judge, TM; Pregenzer, JF, 1993
)
0.52
" Plasma concentrations are essentially proportional to dosages up to 1,800 mg daily, which is the highest dosage used in double-blind, placebo-controlled clinical trials."( Clinical pharmacokinetics of gabapentin.
McLean, MJ, 1994
)
0.29
" Based on pharmacokinetic considerations, it appears that the dosing regimen of gabapentin in subjects with renal impairment may be adjusted on the basis of creatinine clearance."( Pharmacokinetics of gabapentin in subjects with various degrees of renal function.
Blum, RA; Bockbrader, H; Busch, JA; Comstock, TJ; Keller, E; Reece, PA; Reetze, P; Schultz, RW; Sica, DA; Tuerck, D, 1994
)
0.29
" The primary analysis compared data for patients receiving GBP 900 mg/day with placebo; the GBP 1,200-mg/day group provided dose-response data."( Gabapentin (Neurontin) as add-on therapy in patients with partial seizures: a double-blind, placebo-controlled study. The International Gabapentin Study Group.
Anhut, H; Ashman, P; Feuerstein, TJ; Sauermann, W; Saunders, M; Schmidt, B,
)
0.13
" No dosage adjustment is necessary when GBP and CBZ or VPA are coadministered."( Lack of interaction of gabapentin with carbamazepine or valproate.
Bockbrader, HN; Chang, T; Erdman, GR; Leppik, IE; Posvar, EL; Radulovic, LL; Sedman, AJ; Uthman, BM; Wilder, BJ,
)
0.13
" Plasma [14C]GBP declined linearly after dosing while brain ISF [14C]GBP concentration peaked at approximately 1 h and then declined in parallel with plasma concentration."( Gabapentin anticonvulsant action in rats: disequilibrium with peak drug concentrations in plasma and brain microdialysate.
Schielke, GP; Taylor, CP; Vartanian, MG; Welty, DF, 1993
)
0.29
" The dose-response curve for GABA in the presence of 10(-3) M PC-G was shifted rightward and there was a decrease in maximum response."( Effect of penicillin on GABA-gated chloride ion influx.
Ito, M; Kishi, K; Mori, C; Shiraishi, H; Tsuda, A; Tsuda, H, 1994
)
0.29
" Dose-response showed that DL-(tetrazol-5-yl)glycine was about 100 and 500 times more potent than cis-methanoglutamate and NMDA, respectively."( The NMDA receptor agonist DL-(tetrazol-5-yl)glycine is a highly potent excitotoxin.
Lunn, WH; McDonald, JW; Salhoff, CR; Schoepp, DD, 1994
)
0.29
" ZNS daily dosage is 400-600 mg."( Antiepileptic drugs in development: prospects for the near future.
Leppik, IE, 1994
)
0.29
" None of the K+ channel blockers had an effect on the dose-response curve to NO, on the noradrenaline-induced contraction or on the relaxation to nitroglycerine (GTN)."( Prejunctional modulation of the nitrergic innervation of the canine ileocolonic junction via potassium channels.
Boeckxstaens, GE; De Man, JG; De Winter, BY; Herman, AG; Pelckmans, PP; Van Maercke, YM, 1993
)
0.29
" Cumulative dose-response curves for chlordiazepoxide were obtained before and during chronic chlordiazepoxide administration and during chronic saline administration."( Tolerance to the behavioral effects of chlordiazepoxide: pharmacological and biochemical selectivity.
Alastra, AJ; Cohen, C; Goldberg, SR; Marley, RJ; Sannerud, CA; Serdikoff, SL, 1993
)
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
)
0.29
" The dose-response curve was determined for GABA-stimulated 36Cl-accumulation into brain cortex microsacs."( Electric shock convulsions in the rabbit and brain cortex GABAA receptor function.
Cupello, A; Loeb, C; Patrone, A; Robello, M; Vignolo, L, 1993
)
0.29
" 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
" It is, however, obvious that both in rats and mice the severity of symptoms depends not only on dose and dosing schedule of TAA, but also on strain and body weight (age)."( Effects of inhibition of ornithine aminotransferase on thioacetamide-induced hepatogenic encephalopathy.
Grauffel, C; Knödgen, B; Sarhan, S; Seiler, N, 1993
)
0.29
" 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
" There was no abnormal locomotor activity in the L-CPA rats treated with MK-801 except for the first 4 hr following dosing when animals were severely sedated."( L-2-chloropropionic acid-induced neurotoxicity is prevented by MK-801: possible role of NMDA receptors in the neuropathology.
Gyte, A; Lock, EA; Simpson, MG; Widdowson, PS; Wyatt, I, 1996
)
0.29
"A 7-year-old boy with intractable epilepsy developed acute psychosis 3 days after initiating a rapid vigabatrin dosage escalation."( Vigabatrin-associated reversible acute psychosis in a child.
Beltrán Marqués, M; Cánovas Martínez, A; Delgado Cordón, F; Escrivá Aparisi, A; Ordovás Baines, JP, 1995
)
0.29
" The mean daily dosage for all 100 patients was 2107 mg, and the mean daily dosage for patients who continued gabapentin treatment was 2270 mg."( Efficacy and tolerability of gabapentin in clinical practice.
Morris, GL,
)
0.13
" A clear dose-response has been demonstrated, and the minimal effective dose level is 30 mg."( International experience with tiagabine add-on therapy.
Ben-Menachem, E, 1995
)
0.29
" GABA was applied in pulses to outside-out patches of muscle membrane, and, based on the dose-response of the peak currents and of their rise times, a linear model with five binding steps has been proposed."( A molecular scheme for the reaction between gamma-aminobutyric acid and the most abundant chloride channel on crayfish deep extensor abdominal muscle.
Adelsberger, H; Dudel, J; Parzefall, F; von Beckerath, N, 1996
)
0.56
" GBP is also active in this population, but only the 1,800 mg/day dosage was significantly better than placebo with respect to percent responders."( Clinical efficacy of new antiepileptic drugs in refractory partial epilepsy: experience in the United States with three novel drugs.
French, JA, 1996
)
0.29
" In a similarly designed United States trial, LTG was significantly superior to placebo at a 500-mg/day dosage but not at a 300-mg/day dosage."( Expanding antiepileptic drug options: clinical efficacy of new therapeutic agents.
Ben-Menachem, E, 1996
)
0.29
" Compared with control or mismatched ODN-treated cell cultures, treatment of granule neurons with alpha 6 antisense ODNs caused a decrease in GABA-induced maximal current density and increased the half-maximal concentration derived from GABA dose-response curves."( Alpha 6 and gamma 2 subunit antisense oligodeoxynucleotides alter gamma-aminobutyric acid receptor pharmacology in cerebellar granule neurons.
Grayson, DR; Vicini, S; Wang, JF; Zhu, WJ, 1996
)
0.53
" The apparent number of incorporated subunits for each class (alpha, beta, and gamma) could then be determined from the number of components comprising the compound GABA dose-response relationships."( Stoichiometry of a recombinant GABAA receptor.
Barot, S; Chang, Y; Wang, R; Weiss, DS, 1996
)
0.29
" The log dose-response curves for both antagonists for suppression of GABA effects were coincident, having a very shallow slope and covering the whole range of doses effective against the other agonists."( gamma-Aminobutyric acidA receptors and spinally mediated antinociception in rats.
Gent, JP; Goodchild, CS; Guo, Z; Nadeson, R; Porter, V, 1996
)
1.74
" We used in vivo microdialysis to determine a suitable dosing regimen for tiagabine (NNC328) to elevate extracellular levels of GABA within the hippocampus."( Postischemic inhibition of GABA reuptake by tiagabine slows neuronal death in the gerbil hippocampus.
Inglefield, JR; Perry, JM; Schwartz, RD, 1995
)
0.29
" In aged rats, the dose-response curve was shifted to the left, indicating an increase in the potency of GABA to inhibit [3H]t-butylbicycloorthobenzoate binding."( GABAA receptor binding in the aging rat inferior colliculus.
Albin, RL; Caspary, DM; Milbrandt, JC; Turgeon, SM, 1996
)
0.29
" Dose-response curves obtained for slow and fast desensitizing cells displayed similar degrees of cooperativity and antagonist affinity, but clearly greater GABA sensitivity for fast desensitizing cells."( Heterogeneous current responses to GABA and glycine are present in post-natally cultured hippocampal neurons.
Barry, PH; Fatima-Shad, K, 1995
)
0.29
" All the drugs can be conveniently given as a twice daily dosage apart from gabapentin, which has a short half-life and a midday dose is needed."( Clinical pharmacokinetics of newer antiepileptic drugs. Lamotrigine, vigabatrin, gabapentin and oxcarbazepine.
Binnie, CD; Elwes, RD, 1996
)
0.29
" We conclude that vigabatrin in SSADH deficiency should be administered in a gradually increasing dosage combined with frequent evaluation of the clinical condition and the EEG."( Seizures in a boy with succinic semialdehyde dehydrogenase deficiency treated with vigabatrin (gamma-vinyl-GABA).
Gibson, KM; Korinthenberg, R; Lehnert, W; Matern, D, 1996
)
0.29
" The optimized methods show good linearity, precision (RSD < 2%) and accuracy (bias < 2% for dosage forms)."( Validation of high-performance liquid chromatographic methods on two silica base-deactivated reversed phases for the determination of chloroprocaine and bupivacaine.
Brun, F; Veuthey, JL, 1996
)
0.29
" This may be related to dosage and speed of introduction."( Psychotic and severe behavioural reactions with vigabatrin: a review.
Ferrie, CD; Panayiotopoulos, CP; Robinson, RO, 1996
)
0.29
" SN606078 (10 microM) decreased the slope of the dose-response curve for GABA, suggesting a non-competitive mechanism of action."( Novel azole derivatives are antagonists at the inhibitory GABA receptor on the somatic muscle cells of the parasitic nematode Ascaris suum.
Bascal, Z; Holden-Dye, L; Smith, SW; Walker, RJ; Willis, RJ, 1996
)
0.29
" The highest dosage of 3 alpha-Diol (7."( Behavioral effects of 3 alpha-androstanediol. I: Modulation of sexual receptivity and promotion of GABA-stimulated chloride flux.
Erskine, MS; Frye, CA; Van Keuren, KR, 1996
)
0.29
" Once-a-day dosing should be as effective as divided doses."( Human brain GABA levels rise rapidly after initiation of vigabatrin therapy.
Behar, KL; Collins, TL; Mattson, RH; Petroff, OA; Rothman, DL, 1996
)
0.29
" Excitoxins when infused directly into the Nbm destroy non-specifically cell bodies but spare axons passing the injection site, whereas the specificity of AF64A to destroy cholinergic neurons depends on both the dosage applied and the site of injection."( Immunolesion by 192IgG-saporin of rat basal forebrain cholinergic system: a useful tool to produce cortical cholinergic dysfunction.
Bigl, V; Rossner, S; Schliebs, R, 1996
)
0.29
" The dose-response curve for GABA-induced currents was shifted by 16 microM to lower concentrations by 10 microM nefiracetam while the maximal response was reduced by 22."( Effects of the nootropic drug nefiracetam on the GABAA receptor-channel complex in dorsal root ganglion neurons.
Huang, CS; Ma, JY; Marszalec, W; Narahashi, T, 1996
)
0.29
" As compared to placebo, VAL, at the dosage of both 400 and 800 mg, significantly suppressed nocturnal blood melatonin levels, the higher dose being slightly more effective than the lower one."( Suppression of nocturnal plasma melatonin levels by evening administration of sodium valproate in healthy humans.
Borriello, R; Cassandro, P; Maj, M; Monteleone, P; Natale, M; Tortorella, A, 1997
)
0.3
" Dose-response curves showed a wide range of potencies, with (+/-)-exo-2-(6-chloro-3pyridinyl)-7-azabicyclo[2."( Pharmacology of directionally selective ganglion cells in the rabbit retina.
Kittila, CA; Massey, SC, 1997
)
0.3
" Specific indications and dosage schedules have been provided."( New antiepileptic drugs.
Brodie, MJ; Wilson, EA, 1996
)
0.29
" Group results during the controlled trial did not reach statistical significance at the dosage used."( Effectiveness of gabapentin in controlling spasticity: a quantitative study.
Graves, DE; Mueller, M; Olson, WH; Priebe, MM; Sherwood, AM, 1997
)
0.3
" According to the dose-response curves of GABA, TACA, isoguvacine and CACA, measured by the varied pressure duration method, the ED50 value of CACA was larger than those of the other compounds, and Emax of TACA was larger than that of GABA, whereas Emax values of isoguvacine and CACA were smaller."( Pharmacologic characteristics of excitatory gamma-amino-butyric acid (GABA) receptors in a snail neuron.
Han, XY; Takeuchi, H; Wong, SM; Zhang, W, 1997
)
0.3
" 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
)
0.3
" Generalized tonic-clonic seizures observed in EP mice were inhibited by valproate, administered 1 h prior to testing, in a dose-response fashion."( Effects of valproate on amino acid and monoamine concentrations in striatum of audiogenic seizure-prone Balb/c mice.
Alexiuk, NA; Vriend, JP, 1996
)
0.29
" In the present study, the effects of maternal cocaine dosage and of cocaine-elicited maternal seizures on the progeny were studied."( Cocaine administration in pregnant rabbits alters cortical structure and function in their progeny in the absence of maternal seizures.
Fischer, I; Friedman, E; Grayson, D; Jones, L; Levitt, P; Murphy, EH; O'Brien-Jenkins, A; Wang, HY; Wang, XH, 1997
)
0.3
" With a view to better defining the drug's dose-response relationships in the presence of concomitant alternative antiepileptic drugs."( Plasma concentrations of vigabatrin in epileptic patients.
López, E; Quintana, B; Rodriguez, I; Sánchez-Alcaraz, A, 1996
)
0.29
" It is important to realise, however, that the glia-specificity of these compounds depends both on the dosage and on the model used."( Use of fluorocitrate and fluoroacetate in the study of brain metabolism.
Fonnum, F; Hassel, B; Johnsen, A, 1997
)
0.3
" Gabapentin was well tolerated by patients in both dosage groups, and no patients exited the study due to adverse events, despite rapid initiation of full dose within 24 hours."( Gabapentin monotherapy: I. An 8-day, double-blind, dose-controlled, multicenter study in hospitalized patients with refractory complex partial or secondarily generalized seizures. The US Gabapentin Study Group 88/89.
Bergey, GK; Blume, WT; Crockatt, JG; Garofalo, E; LaMoreaux, L; Leiderman, DB; Morrell, MJ; Morris, HH; Penovich, PE; Pierce, M; Rosenfeld, W, 1997
)
0.3
" Results of outcome measures, including time to exit, completion rate, and mean time on monotherapy, showed no significant differences among dosage groups."( Gabapentin monotherapy: II. A 26-week, double-blind, dose-controlled, multicenter study of conversion from polytherapy in outpatients with refractory complex partial or secondarily generalized seizures. The US Gabapentin Study Group 82/83.
Abou-Khalil, B; Beydoun, A; Cantrell, D; Fischer, J; Garofalo, E; Greiner, M; Harden, C; Hayes, A; Labar, DR; Pierce, M; Ramsay, RE; Sackellares, JC; Uthman, BM, 1997
)
0.3
" Up to now, no single drug has been shown to be more effective at controlling seizures of a particular type than another, so other factors such as mechanism of action, pharmacokinetics, dosage regimens or the spectrum of adverse drug reactions and interactions are used when making a choice between one agent and another."( Newer anticonvulsant drugs: role of pharmacology, drug interactions and adverse reactions in drug choice.
Deckers, CL; Hekster, YA; Keyser, A; Meinardi, H; Natsch, S; Renier, WO, 1997
)
0.3
" 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
" In the presence of 10 mu M zinc, the dose-response curve for 4,5,6, 7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP; a GABAA agonist that suppresses GABAC-activated currents) was shifted to the left of the curve obtained in the absence of zinc, but without a significant change in the response maximum."( GABA receptors of bipolar cells from the skate retina: actions of zinc on GABA-mediated membrane currents.
Chappell, RL; Li, L; Qian, H; Ripps, H, 1997
)
0.3
"The relationship between the ratio of vigabatrin concentration to dosage (VGB C/D) and both patient age and the presence of other antiepileptic drugs (AEDs) was analyzed retrospectively by bivariate and multivariate methods in 179 patients with epilepsy (114 children and 65 adults)."( Vigabatrin serum concentration to dosage ratio: influence of age and associated antiepileptic drugs.
Armijo, JA; Arteaga, R; Bravo, J; Cuadrado, A, 1997
)
0.3
" In the test of physical dependence-producing potential with the drug-admixed food method in rats, vigabatrin and diazepam were given to rats mixed with food for 28 days in an increasing dosage schedule, followed by feeding a drug-free diet to observe withdrawal signs for 7 days."( Drug dependence study on vigabatrin in rhesus monkeys and rats.
Takada, K; Yanagita, T, 1997
)
0.3
" External H-7 shifted the dose-response curve of GABA-activated currents downward without changing the EC50 significantly (from 15."( Modulation of nicotinic ACh-, GABAA- and 5-HT3-receptor functions by external H-7, a protein kinase inhibitor, in rat sensory neurones.
Hu, HZ; Li, ZW, 1997
)
0.3
" Vigabatrin mean dosage during phase 3 was 63."( Vigabatrin in refractory childhood epilepsy. The Brazilian Multicenter Study.
Chisté, MA; da Costa, JC; Diament, A; Gherpelli, JL; Guerreiro, CA; Guerreiro, MM; Manreza, ML; Nunes, ML; Palmini, A; Pedroso, F; Reed, UC; Rotta, NT; Silva, EA; Vega-Gutiérrez, L; Vizioli, J, 1997
)
0.3
" Risk factors have included prior psychopathology, coexisting medical conditions, slow acetylator status, advanced age, concomitant medications, and increased permeability of the blood-brain barrier, as well as high antibiotic dosage and intrathecal or intravenous administration."( Antibiotics: neuropsychiatric effects and psychotropic interactions.
State, R; Sternbach, H,
)
0.13
" The dose-response relationship revealed an EC50 of 11."( Activation kinetics and single channel properties of recombinant alpha1beta2gamma2L GABA(A) receptor channels.
Adelsberger, H; Bufler, J; Dudel, J; Franke, C; Hertle, I; Jahn, K; Pestel, E; Zieglgänsberger, W, 1997
)
0.3
" Furosemide at a concentration of 1 mM depressed the maximal peak amplitude of the dose-response curve for either GABA or glycine to about 70% of control."( Action of furosemide on GABA- and glycine currents in rat septal cholinergic neurons in culture.
Kumamoto, E; Murata, Y, 1997
)
0.3
" In six patients, including three taking 6000 mg daily, GBP concentrations continued to rise linearly at each dosage increment."( High dose gabapentin in refractory partial epilepsy: clinical observations in 50 patients.
Brodie, MJ; Forrest, G; Sills, GJ; Wilson, EA, 1998
)
0.3
" 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
" Dose-response curves for the peak and the slow component yielded EC50 values of 139 and 24 microM, respectively."( Dentate gyrus basket cell GABAA receptors are blocked by Zn2+ via changes of their desensitization kinetics: an in situ patch-clamp and single-cell PCR study.
Berger, T; Kraushaar, U; Monyer, H; Schwarz, C, 1998
)
0.3
" A 6-month multicentre, open-label study, involved addition of gabapentin to pre-existing treatment at the initial dosage of 1200 mg and subsequent adjustment between 900 and 2400 mg/day according to efficacy and tolerability."( Gabapentin add-on therapy with adaptable dosages in 610 patients with partial epilepsy: an open, observational study. The French Gabapentin Collaborative Group.
Arzimanoglou, A; Baulac, M; Cavalcanti, D; Portal, JJ; Semah, F, 1998
)
0.3
" Both effects exhibited a tendency to a U-shaped dose-response curve."( Anticonvulsant action of gabapentin during postnatal development in rats.
Haugvicová, R; Mares, P, 1997
)
0.3
"When information became available on aplastic anemia and hepatotoxicity associated with felbamate, all patients were advised to taper their felbamate dosage over approximately 2 weeks."( Increased seizure frequency associated with felbamate withdrawal in adults.
Privitera, M; Shukla, R; Welty, TE, 1998
)
0.3
" Dosage and side effects were noted."( Clinical experience using gabapentin adjunctively in patients with a history of mania or hypomania.
Knoll, J; Stegman, K; Suppes, T, 1998
)
0.3
" There was a U-shaped dose-response curve and LHRH release was not inhibited at lower or higher cytokine concentrations."( Granulocyte-macrophage colony stimulating factor suppresses LHRH release by inhibition of nitric oxide synthase and stimulation of gamma-aminobutyric acid release.
Kimura, M; McCann, SM; Rettori, V; Yu, WH,
)
0.34
" A linear dose-response relationship was found on the glucose-induced insulin release in case of 3-min stimulation with 4 and 500 mM of glucose (lin-log graph)."( Dynamic insulin secretion from perifused rat pancreatic islets.
Csernus, VJ; Hammer, T; Peschke, D; Peschke, E, 1998
)
0.3
" dosing were 38."( Gabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsy.
Bockbrader, HN; DeCerce, J; Gidal, BE; Gonzalez, J; Kruger, S; Pitterle, ME; Ramsay, RE; Rutecki, P, 1998
)
0.3
" Awake mice were dosed with [1-(13)C]glucose, and brain extracts were analyzed by 13C NMR spectroscopy."( Quantification of the GABA shunt and the importance of the GABA shunt versus the 2-oxoglutarate dehydrogenase pathway in GABAergic neurons.
Fonnum, F; Hassel, B; Johannessen, CU; Sonnewald, U, 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
" From such recordings we constructed dose-response curves for peak and steady-state currents, for the rise times of the currents and for the time constants of desensitization."( Neuromuscular glutamatergic and GABAergic channels.
Adelsberger, H; Dudel, J; Heckmann, M,
)
0.13
"Based on the observations of other authors, we used this drug in dosage varying between 900 and 1,200 mg/day, in three patients with neuropathic pain, of both central and peripheral origin, and in whom the usual treatments had been unsatisfactory or could not be tolerated because of side-effects."( [Treatment of neuropathic pain with gabapentin ++].
Sánchez-Valiente, S, 1998
)
0.3
" For example, receptors formed by perch-rho 1B subunits were more sensitive to GABA than the receptors formed by other GABA-rho subunits, the dose-response curves for the various receptors revealed different Hill coefficients, and there were differences in the kinetics of the GABA-induced currents."( Molecular and pharmacological properties of GABA-rho subunits from white perch retina.
Dowling, JE; Qian, H; Ripps, H, 1998
)
0.3
" Neither bicuculline nor GABA altered the dose-response of steroids in the [3H]GHB assay, suggesting that there was no GABAA component involved in the steroid-inhibition of [3H]GHB binding."( Steroid-inhibition of [3H]gamma-hydroxybutyric acid (GHB) binding in thalamic relay nuclei increases during absence seizures.
Banerjee, PK; Liu, CC; Snead, OC, 1998
)
0.3
"A 4-week titration period to a maximum dosage of 3600 mg/d of gabapentin or matching placebo."( Gabapentin for the treatment of postherpetic neuralgia: a randomized controlled trial.
Bernstein, P; Harden, N; Magnus-Miller, L; Rowbotham, M; Stacey, B, 1998
)
0.3
" Gabapentin therapy proved to be very satisfactory in relieving muscular cramps with a relatively low dosage (600 mg/day) and without any remarkable side effects."( A case of myokymia-cramp syndrome successfully treated with gabapentin.
Cardinali, P; Parisi, L; Pierelli, F; Rossi, P; Serrao, M; Tramutoli, R, 1998
)
0.3
" The hyperpolarization was dose-dependent, and the GABA(B) receptor antagonist CGP 35,348 produced a rightward shift in the agonist dose-response curve."( A powerful GABA(B) receptor-mediated inhibition of GABAergic neurons in the arcuate nucleus.
Bosch, MA; Kelly, MJ; Rønnekleiv, K; Wagner, EJ, 1998
)
0.3
"This clinical study provides support for the pharmacological evidence that this preparation may be administered on a once or twice daily basis, depending on the individual patient's preference, total dosage and co-medication."( Once-daily versus twice-daily vigabatrin: is there a difference? The results of a double-blind pilot study.
Blankenhorn, V; Krämer, G; Mumford, JP; Richens, A; Stefan, H; Thümler, R; Zahner, B, 1999
)
0.3
" Four of the six partial clinical responders had deterioration of spasms with additional VGB dosage increases."( Vigabatrin in the treatment of infantile spasms.
Koo, B, 1999
)
0.3
" The results show that whether or not the introduction of vigabatrin results in an increase or a reduction in costs to the healthcare system depends largely on 3 factors: (i) the administered dosage of vigabatrin; (ii) the effect that vigabatrin has on hospital admissions; and (iii) the proportion of epileptic patients who take the drug."( The economic effects of introducing vigabatrin, a new antiepileptic medication.
Champagne, F; Contandriopoulos, AP; Kennedy, W; Reinharz, D; Tessier, G, 1995
)
0.29
" 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
"0 mg/kg dosage of 3 alpha,5 alpha-THP."( Prenatal stress reduces the effectiveness of the neurosteroid 3 alpha,5 alpha-THP to block kainic-acid-induced seizures.
Bayon, LE; Frye, CA, 1999
)
0.3
"Gabapentin is not available in a liquid dosage form for clinical use."( Development of two stable oral suspensions for gabapentin.
Nahata, MC, 1999
)
0.3
" Reduction of GBP dosage may be required in elderly patients with reduced renal function."( Effects of age and gender on single-dose pharmacokinetics of gabapentin.
Abel, RB; Bockbrader, HN; Boyd, RA; Sedman, AJ; Türck, D, 1999
)
0.3
"No significant relationship was seen between dosage and serum levels, nor between serum levels and efficacy or side-effect."( [In children with refractory epilepsy: vigabatrin or lamotrigine?].
Armijo, JA; Arteaga, R; Caviedes, BE; Herranz, JL,
)
0.13
" Once-a-day dosing is sufficient to increase GABA."( Acute effects of vigabatrin on brain GABA and homocarnosine in patients with complex partial seizures.
Collins, T; Hyder, F; Mattson, RH; Petroff, OA; Rothman, DL, 1999
)
0.3
" In electrophysiological experiments, the arginine 120 lysine (R120K) mutation in the alpha 1 subunit, when co-expressed with beta 2 and gamma 2 subunits in Sf-9 insect cells, induces a 180-fold rightward shift of the GABA dose-response curve compared with wild type alpha 1 beta 2 gamma 2s GABAA receptors."( Arginine residue 120 of the human GABAA receptor alpha 1, subunit is essential for GABA binding and chloride ion current gating.
Dekermendjian, K; Liljefors, T; Nielsen, M; Rasmussen, PB; Westh-Hansen, SE; Witt, MR, 1999
)
0.3
" Further studies are required to confirm this effect and to determine whether a dose-response relationship exists."( Treatment of social phobia with gabapentin: a placebo-controlled study.
Davidson, JR; Greist, JH; Janney, CA; Jefferson, JW; Katzelnick, DJ; Pande, AC; Sutherland, SM; Weisler, RH, 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
)
0.3
" Slow dosage escalation yields good tolerability."( Lamotrigine in the treatment of bipolar depression.
Bowden, CL; Mitchell, P; Suppes, T, 1999
)
0.3
" Because dosing is often modest, cost should rarely be the overriding factor in choosing a drug for a patient with newly diagnosed epilepsy in the developed world."( Monostars: an aid to choosing an antiepileptic drug as monotherapy.
Brodie, MJ, 1999
)
0.3
" Gabapentin was titrated up to a maximal dosage of 3600 mg/day to achieve seizure control or to tolerability."( Dosing to efficacy with neurontin: the STEPS trial. Study of Titration to Effect Profile of Safety.
Morrell, MJ, 1999
)
0.3
" The gabapentin dosage was titrated to effective tolerated dose up to 2400 mg/day."( Gabapentin as adjunctive therapy for partial seizures.
Bruni, J, 1999
)
0.3
" Therefore, gabapentin dosing must be optimized on an individual basis to achieve an adequate trial of the drug and obtain the best seizure control."( Gabapentin in the management of convulsive disorders.
McLean, MJ, 1999
)
0.3
" Conversion to TGB monotherapy can be achieved in patients with medically refractory epilepsy, although additional controlled studies are needed to confirm the efficacy of TGB as monotherapy and to establish the effective dosage range."( Tiagabine.
Schachter, SC, 1999
)
0.3
" Lamotrigine may offer a much-needed treatment alternative for bipolar depression and could be found effective for acute mania, but the need for slow dosage adjustment and the risk of rash may limit overall clinical utility."( Gabapentin and lamotrigine in bipolar disorder.
Botts, SR; Raskind, J, 1999
)
0.3
" The hyperpolarization was dose dependent, and the GABA(B) receptor antagonist CGP 35,348 produced a rightward shift in the agonist dose-response curve."( A powerful GABA(B) receptor-mediated inhibition of GABAergic neurons in arcuate nucleus.
Bosch, MA; Kelly, MJ; Rønnekleiv, OK; Wagner, EJ, 1999
)
0.3
"125 mg/kg) produced an apparent shift of the cocaine dose-response curve to the right."( The GABA(B) agonist CGP 44532 decreases cocaine self-administration in rats: demonstration using a progressive ratio and a discrete trials procedure.
Andrews, M; Brebner, K; Froestl, W; Phelan, R; Roberts, DC, 1999
)
0.3
" 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
)
0.59
" After lamotrigine was added for better seizure control and the dosage of gabapentin was tapered, anorgasmia improved."( Improved sexual function in three men taking lamotrigine for epilepsy.
Carwile, ST; Husain, AM; Miller, PP; Radtke, RA, 2000
)
0.31
"In the first series of experiments, three dose-response curves were generated that examined the effect of three doses of baclofen (1."( Effect of baclofen on cocaine self-administration in rats reinforced under fixed-ratio 1 and progressive-ratio schedules.
Brebner, K; Phelan, R; Roberts, DC, 2000
)
0.31
" We reported that daily dosing increased brain gamma-aminobutyric acid (GABA) in patients with epilepsy."( Effects of gabapentin on brain GABA, homocarnosine, and pyrrolidinone in epilepsy patients.
Hyder, F; Mattson, RH; Petroff, OA; Rothman, DL, 2000
)
0.56
" We report 11 MS patients with trigeminal neuralgia (TN): 6 intolerant to a therapeutic dosage of CBZ, showing serious adverse effects and subsequently treated with a combination of low-dose CBZ and gabapentin (GBP) (group 1); 5 treated with lamotrigine (LMT), showing adverse effects and subsequently treated with GBP (group 2)."( Low-dose gabapentin combined with either lamotrigine or carbamazepine can be useful therapies for trigeminal neuralgia in multiple sclerosis.
Leandri, M; Mancardi, GL; Messmer Uccelli, M; Solaro, C; Uccelli, A, 2000
)
0.31
" Furthermore, coexpression of wild-type rho1 and gamma2S subunits was found to shift the GABA dose-response curve."( Evidence for coassembly of mutant GABAC rho1 with GABAA gamma2S, glycine alpha1 and glycine alpha2 receptor subunits in vitro.
Lipton, SA; Pan, ZH; Zhang, D; Zhang, X, 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
" Pregnant Sprague-Dawley dams were dosed from gestational day (GD) 12 to postnatal day (PND) 7, whereupon the rat pups were dosed directly until PND 21 (group A) or PND 42 (group B)."( Neurotoxicological outcomes of perinatal heptachlor exposure in the rat.
Chapin, RE; Harris, MW; Meacham, CA; Moser, VC; Shafer, TJ; Ward, TR, 2001
)
0.31
" Study medication was to be given on a three-times-a-day dosing regimen."( Efficacy of gabapentin in migraine prophylaxis.
Klapper, J; Magnus, L; Mathew, NT; Ramadan, N; Rapoport, A; Saper, J; Stacey, B; Tepper, S, 2001
)
0.31
"Fourteen of the 18 (78%) treated for hypomania or mania had a positive response to a dosage range of 600-3,600 mg/day."( Gabapentin in the acute treatment of refractory bipolar disorder.
Altshuler, LL; Brown, ES; Denicoff, K; Frye, M; Gitlin, M; Goodman, R; Hwang, S; Keck, PE; Kupka, R; Leverich, G; McElroy, SL; Nolen, W; Post, R; Suppes, T, 1999
)
0.3
"Starting gabapentin therapy at an initial therapeutic dosage of 900 mg/day is well tolerated by patients with epilepsy and is as safe as initiating with a titration schedule over 3 days."( Rapid initiation of gabapentin: a randomized, controlled trial.
Bernstein, P; Fisher, RS; Magnus, L; Pellock, J; Penovich, PE; Sachdeo, RC, 2001
)
0.31
" Similarly, valproate combined with antipsychotics provided greater improvement in mania than antipsychotic medication alone and resulted in lower dosage of the antipsychotic medication."( Novel treatments for bipolar disorder.
Bowden, CL, 2001
)
0.31
" Optimal dosing remains unclear."( Gabapentin for treatment of behavioral and psychological symptoms of dementia.
Miller, LJ, 2001
)
0.31
" The designs and dosing regimens differed between studies."( Evidence for the use of gabapentin in the treatment of diabetic peripheral neuropathy.
Hemstreet, B; Lapointe, M, 2001
)
0.31
"A highly sensitive and specific method is proposed for the determination of vigabatrin (I) and gabapentin (II) in their dosage forms and spiked human plasma."( Spectrofluorimetric determination of vigabatrin and gabapentin in dosage forms and spiked plasma samples through derivatization with 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole.
Al-Deeb, OA; Belal, F; Hassan, EM; Khalil, NY,
)
0.13
" The combination PP and low-medium dosed VGB (1000-2000 mg/d) did not increase the GABA+/Cr signals."( Influence of pyridoxal 5'-phosphate alone and in combination with vigabatrin on brain GABA measured by 1H-NMR-spectroscopy.
Boesiger, P; Mueller, SG; Weber, OM; Wieser, HG, 2001
)
0.31
" Gabapentin was given at the daily dosage of 900 mg."( Drug-resistant cluster headache responding to gabapentin: a pilot study.
Cruccu, G; Gottlieb, A; Leandri, M; Luzzani, M, 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
" Also, the dosing of the drug in children has been complicated by negative behavioral adverse effects."( Gabapentin: a unique anti-epileptic agent.
Dougherty, JA; Rhoney, DH, 2001
)
0.31
" With long-term dosing and once target doses were achieved at 4 weeks, significant elevations in GABA were observed compared with baseline for all three drugs (topiramate 46%, gabapentin 25%, lamotrigine 25%)."( Modulation of cerebral GABA by topiramate, lamotrigine, and gabapentin in healthy adults.
Faught, E; Gilliam, F; Hetherington, H; Ho, S; Kuzniecky, R; Martin, R; Pan, J, 2002
)
0.31
" There was no evidence to suggest dosing difficulties due to tolerance over the 3-year period."( Long-term use of gabapentin for treatment of pain after traumatic spinal cord injury.
Hicken, BL; Kezar, L; Ness, TJ; Putzke, JD; Richards, JS,
)
0.13
" Some of the point mutations caused shifts in the GABA dose-response curve, indicating that the mutations changed the apparent affinity of the receptor for GABA."( Volatile anesthetic actions on the GABAA receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations.
Harrison, NL; Jenkins, A; Nishikawa, K; Paraskevakis, I, 2002
)
0.31
" A slow upward dose titration is recommended to reduce the incidence of serious rash, but this may delay the attainment of adequate dosage for 6 weeks."( Lamotrigine update and its use in mood disorders.
Hurley, SC, 2002
)
0.31
" The selection and dosage of antiepileptic drugs requires proper attention to special pharmacokinetic and pharmacodynamic situations that are common in older individuals."( [Gabapentin in the treatment of epilepsy in the elderly].
Gil-Nagel, A,
)
0.13
" The classic AEDs had numerous problems, ranging from inconvenient dosing schedules to frequent side effects due to active metabolites and common drug interactions; newer agents have been developed to avoid some of these pitfalls."( Pharmacokinetics of new anticonvulsants in psychiatry.
Morris, HH, 1998
)
0.3
" No significant difference was found among other pain descriptors during the gabapentin and placebo treatment, although this may have been limited by the small sample size and low maximum dosage of gabapentin."( Gabapentin in the treatment of neuropathic pain after spinal cord injury: a prospective, randomized, double-blind, crossover trial.
Chen, B; DeLisa, JA; Johnston, M; Kirshblum, S; Millis, S; Tai, Q, 2002
)
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
)
0.31
" A sub-chronic dosing regimen of low cumulative manganese exposure (4."( Low cumulative manganese exposure affects striatal GABA but not dopamine.
Gwiazda, RH; Lee, D; Sheridan, J; Smith, DR, 2002
)
0.31
" During 2- and 6-week titration periods, respectively, GBP dosage reached 1,800 mg/day, and LTG, 150 mg/day."( Gabapentin versus lamotrigine monotherapy: a double-blind comparison in newly diagnosed epilepsy.
Anhut, H; Brodie, MJ; Chadwick, DW; Garofalo, EA; Maton, S; Messmer, SL; Murray, G; Otte, A; Sauermann, W, 2002
)
0.31
" Glycine dose-response curves were shifted to the right by GES (0."( Guanidinoethyl sulphonate is a glycine receptor antagonist in striatum.
Chepkova, AN; Haas, HL; Sergeeva, OA, 2002
)
0.31
" The mean effective dosage at the end of the 6-week treatment period was 1,855 mg, although therapeutic effects were already observed at the end of week 4 (1,391 mg)."( Treatment of restless legs syndrome with gabapentin: a double-blind, cross-over study.
de la Llave, Y; Garcia-Borreguero, D; Hernandez, G; Larrosa, O; Masramon, X; Verger, K, 2002
)
0.31
" Mean dosage +/- SD at week 8 was 1270 +/- 561."( Effectiveness of adjunctive gabapentin in resistant bipolar disorder: is it due to anxious-alcohol abuse comorbidity?
Akiskal, HS; Frare, F; Moretti, L; Perugi, G; Ruffolo, G; Toni, C; Torti, C, 2002
)
0.31
" BDNF action was mediated by TrkB-receptors and had no effects on: (i) the amplitude and dose-response of GABA-evoked IPSCs and (ii) the number of GABA(A) receptor clusters and the total functioning synapses, suggesting that the neurotrophin unlikely acted postsynaptically."( BDNF up-regulates evoked GABAergic transmission in developing hippocampus by potentiating presynaptic N- and P/Q-type Ca2+ channels signalling.
Baldelli, P; Carabelli, V; Carbone, E; Hernández-Guijo, JM; Novara, M, 2002
)
0.31
" After stabilising at each dosage, a sequence of serum and saliva samples were collected within the dosage interval; GBP and co-medication concentrations were determined and the results subjected to PK modelling."( The absorption of gabapentin following high dose escalation.
Beran, RG; Berry, DJ; Clarke, LA; Hung, WT; Plunkeft, MJ, 2003
)
0.32
" The high dosage of GABA needed to affect the light responses of HCs could be due to strong GABA uptake systems in the intact rabbit retina."( The effects of GABA and vigabatrin on horizontal cell responses to light and the effect of vigabatrin on the electroretinogram.
Hanitzsch, R; Küppers, L, 2002
)
0.31
"The influence of age and administered daily dosage on the plasma concentrations of gabapentin (GBP) at steady state was evaluated in a group of 41 children and young adults (aged 3-30 years) receiving long-term adjunctive treatment with GBP for the management of refractory partial-onset seizures."( Plasma gabapentin concentrations in children with epilepsy: influence of age, relationship with dosage, and preliminary observations on correlation with clinical response.
Bonanni, P; Bonomi, I; Ferrari, AR; Gatti, G; Guerrini, R; Perucca, E, 2003
)
0.32
" When neocortical slices were treated in vitro for 3 h with 10 microM SKF, ALLO was also reduced (25-30%) and in addition, the GABA dose-response curve was shifted to the right; however this shift was not as marked as the shift in the slices obtained from mice treated with SKF, in keeping with the smaller decrease of the ALLO content in these slices."( On the putative physiological role of allopregnanolone on GABA(A) receptor function.
Costa, E; Guidotti, A; Matsumoto, K; Mienville, JM; Puia, G; Takahata, H; Watanabe, H, 2003
)
0.32
" Higher, open-label gabapentin dosing was associated with 54% and 67% reductions in hot flash frequency and composite score from baseline, respectively."( Gabapentin's effects on hot flashes in postmenopausal women: a randomized controlled trial.
Guttuso, T; Kieburtz, K; Kurlan, R; McDermott, MP, 2003
)
0.32
" In this study, conventional analgesics were continued at a therapeutic level, and gabapentin was administrated for an 18-day titration period followed by a 5-week maintenance period at a dosage of 1800 mg/day or the maximum tolerable dosage."( Gabapentin effect on neuropathic pain compared among patients with spinal cord injury and different durations of symptoms.
Ahn, SH; Bae, JH; Jang, SH; Lee, BS; Moon, HW; Park, HW; Sakong, J, 2003
)
0.32
" In this report, we show that ATP elicits Ca(2+) responses producing a monophasic dose-response curve with an EC(50) value of 24."( GABAB receptor-mediated presynaptic potentiation of ATP ionotropic receptors in rat midbrain synaptosomes.
Gómez-Villafuertes, R; Gualix, J; Miras-Portugal, MT; Pintor, J, 2003
)
0.32
"The goals of this article were to review data on the efficacy and tolerability of gabapentin in the treatment of neuropathic pain in adults and to determine the optimal dosing schedule."( Gabapentin dosing for neuropathic pain: evidence from randomized, placebo-controlled clinical trials.
Backonja, M; Glanzman, RL, 2003
)
0.32
" Results form the basis of recommended pregabalin dosing regimens in patients with decreased renal function."( Pharmacokinetics of pregabalin in subjects with various degrees of renal function.
Alvey, CW; Bockbrader, HN; Cook, JA; Posvar, EL; Randinitis, EJ; Sedman, AJ, 2003
)
0.32
" In contrast, biochemical study (based on dosage of plasma levels of GABA and diazepam binding inhibitor, an endogenous ligand of GABAA and peripheral benzodiazepine receptors, showed contradictory results: patients with Angelman's syndrome showed significantly higher levels of GABA and diazepam binding inhibitor than patients without neurologic impairment but significantly lower levels than epileptic controls."( Peripheral markers of the gamma-aminobutyric acid (GABA)ergic system in Angelman's syndrome.
Borgatti, R; Cogliati, T; Elia, M; Ferrarese, C; Grasso, R; Musumeci, SA; Passoni, D; Piccinelli, P; Raggi, ME; Romeo, A; Valseriati, D; Viri, M, 2003
)
0.62
" To gain more insight into retinal excitotoxicity, we carried out a dose-response study in adult rats using alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), a glutamate analogue."( Low sensitivity of retina to AMPA-induced calcification.
Andrés, N; Mahy, N; Malpesa, Y; Rodríguez, MJ, 2003
)
0.32
" Given the maximal dosage studied, pregabalin had acceptable tolerability compared to placebo despite a greater incidence of side effects, which were generally mild to moderate in intensity."( Pregabalin for the treatment of postherpetic neuralgia: a randomized, placebo-controlled trial.
Bockbrader, H; Corbin, AE; Dworkin, RH; Garofalo, EA; LaMoreaux, L; Poole, RM; Sharma, U; Young, JP, 2003
)
0.32
"To establish the efficacy, safety, and tolerability of pregabalin administered twice-daily (BID) without dose titration as adjunctive treatment in patients with partial seizures and to confirm the dose-response relationship."( Dose-response trial of pregabalin adjunctive therapy in patients with partial seizures.
French, JA; Garofalo, EA; Knapp, LE; Kugler, AR; Robbins, JL, 2003
)
0.32
"Our objectives were to describe the exposure-response relationship of pregabalin add-on treatment for refractory partial seizures after multiple dosing in patients and to identify the factors that influence this relationship."( Exposure-response analysis of pregabalin add-on treatment of patients with refractory partial seizures.
Bockbrader, H; Burger, P; Corrigan, B; Frame, B; Garofalo, E; Lalonde, R; Miller, R, 2003
)
0.32
"Pregabalin add-on treatment demonstrates a dose-response relationship in 3 out of 4 patients with refractory partial seizures."( Exposure-response analysis of pregabalin add-on treatment of patients with refractory partial seizures.
Bockbrader, H; Burger, P; Corrigan, B; Frame, B; Garofalo, E; Lalonde, R; Miller, R, 2003
)
0.32
" More studies are needed to determine the best dosing regimen to optimize efficacy and tolerability."( A randomized, double-blind, placebo-controlled, fixed-dose, multicenter study of pregabalin in patients with generalized anxiety disorder.
Carter, CM; Cohn, CK; Crockatt, JG; Dubovsky, SJ; Feltner, DE; Liu-Dumaw, M; Pande, AC; Shrivastava, RK; Targum, SD, 2003
)
0.32
" The recommended dosage in adults is 300 mg at bedtime on day 1,300 mg BID on day 2, and 300 mg TID on day 3, titrating up as needed to 2400 to 3600 mg/d."( The use of gabapentin for the treatment of postherpetic neuralgia.
Kennedy, DH; Singh, D, 2003
)
0.32
"The purposes of this review were to assess the gabapentin titration and dosing regimens that have been published in peer-reviewed journals, to develop dosing recommendations to maximize antiseizure efficacy without compromising tolerability, and to formulate guidelines for an adequate therapeutic assessment of gabapentin dosage efficacy."( Gabapentin dosing in the treatment of epilepsy.
Gidal, BE; McLean, MJ, 2003
)
0.32
" These were reviewed to assess the range of dosing and titration schedules reported."( Gabapentin dosing in the treatment of epilepsy.
Gidal, BE; McLean, MJ, 2003
)
0.32
" Side effects occurred around the onset of dosing and were reported in some studies to be transient."( Gabapentin dosing in the treatment of epilepsy.
Gidal, BE; McLean, MJ, 2003
)
0.32
"Based in the literature here, in most adult patients, gabapentin may be initiated at a dosage of 900 mg/d and titrated to maintenance dosages > or = 3600 mg/d."( Gabapentin dosing in the treatment of epilepsy.
Gidal, BE; McLean, MJ, 2003
)
0.32
"35 ml) were added single dosing into this chamber with living physiological solution in concentration 10(-15)-10(-27) mol/l."( [Regulation of the neuronal functional state by ultra low doses of different biologically active substances. Nonspecific effect ].
Grechenko, TN; Terekhova, SF,
)
0.13
" Patients randomized to GBP started on 1800 mg/d and could have their dosage increased stepwise to 2400 and 3600 mg/d if seizures persisted."( Serum concentrations and effects of gabapentin and vigabatrin: observations from a dose titration study.
Johannessen, SI; Larsson, S; Lindberger, M; Luhr, O; Tomson, T, 2003
)
0.32
" Although its half-life is relatively short (6 to 8 hours), its duration of action is longer than anticipated from its pharmacokinetics in plasma, and a twice-daily dosing regimen is adequate to produce the desired response."( The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come?
Johannessen, SI; Perucca, E, 2003
)
0.32
" Hill slope coefficients for the tested anticonvulsants indicate that the dose-response curve was less steep for gabapentin than for phenytoin, carbamazepine and ethosuximide."( Potent analgesic effects of anticonvulsants on peripheral thermal nociception in rats.
Jevtovic-Todorovic, V; Rastogi, AJ; Todorovic, SM, 2003
)
0.32
" Corresponding dose-response relationships are close to single-site binding isotherms."( Structure-activity studies with Ginkgo biloba extract constituents as receptor-gated chloride channel blockers and modulators.
Chatterjee, SS; Kondratskaya, EL; Krishtal, OA, 2003
)
0.32
"Nicotine maintained stable self-administration under a progressive ratio schedule with a linear dose-response function ( r=0."( The GABAB receptor agonists baclofen and CGP44532 decreased nicotine self-administration in the rat.
Froestl, W; Markou, A; Paterson, NE, 2004
)
0.32
" After 1-d or 14-d withdrawal from Amph, they were challenged on day 8 (W1d) or on day 21 (W14d) with a single same dosage and then perfused."( Age- and region-dependent alterations in the GABAergic innervation in the brain of rats treated with amphetamine.
Chen, CT; Lin, TY; Yin, HS, 2004
)
0.32
" Dose-response (D-R) curves and kinetic measurements of GABA rho(1) currents were carried out in the presence or absence of antagonists."( Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor.
Calvo, DJ; Goutman, JD, 2004
)
0.32
" Most of these studies assayed changes in GABA dose-response curves, which are macroscopic measures that depend on the interplay of many processes and cannot resolve individual microscopic transitions."( An arginine involved in GABA binding and unbinding but not gating of the GABA(A) receptor.
Czajkowski, C; Jones, MV; Wagner, DA, 2004
)
0.32
" This dosage produced a substantial but non-significant decrease in the incidence of postherpetic pain-related responses."( Effects of the suppression of acute herpetic pain by gabapentin and amitriptyline on the incidence of delayed postherpetic pain in mice.
Kuraishi, Y; Nojima, H; Shiraki, K; Takahata, H; Takasaki, I, 2004
)
0.32
" This was followed by a 4-week stable dosing period when the patients continued to receive maximum tolerated doses, a 2-week washout period, then a crossover of 4 weeks of medication/placebo titration, and another 4 weeks of stable dosing period."( Gabapentin is a first line drug for the treatment of neuropathic pain in spinal cord injury.
Levendoglu, F; Ogün, CO; Ogün, TC; Ozerbil, O; Ugurlu, H, 2004
)
0.32
" 6-Methylflavone (60 microM) did not significantly affect the GABA dose-response curve at rho1 GABAC receptors."( Flumazenil-independent positive modulation of gamma-aminobutyric acid action by 6-methylflavone at human recombinant alpha1beta2gamma2L and alpha1beta2 GABAA receptors.
Chebib, M; Hall, BJ; Hanrahan, JR; Johnston, GA, 2004
)
0.58
" This was not seen following similar dosing of diazepam."( Sub-chronic administration of zolpidem affects modifications to rat sleep architecture.
Dunn, SL; Johnson, C; Koblan, KS; Motzel, SL; Renger, JJ, 2004
)
0.32
" Rapid clearance of the drug necessitates dosing three or more times per day to maintain therapeutic levels."( XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys.
Annamalai, T; Barrett, RW; Bu, L; Cundy, KC; De Vera, J; Estrela, J; Gallop, MA; Luo, W; Shirsat, P; Torneros, A; Yao, F; Zou, J, 2004
)
0.32
"5 mg/d, are reasonable initial dosages, and if symptoms do not improve within a week or two, the dosage can be doubled."( Management of hot flashes in breast cancer survivors and men with prostate cancer.
Stearns, V, 2004
)
0.32
" Caffeine shifted the GABA dose-response curve downward and decreased the maximum response to 57% without changing K(d) value."( [Inhibitory effect of caffeine on GABA-activated current in acutely isolated rat dorsal root ganglion neurons].
An, J; Li, S; Li, ZW; Sun, CK, 2004
)
0.32
" The norepinephrine dose-response curve was shifted to the left with dehydration, revealing an increase in norepinephrine sensitivity."( Dehydration-induced synaptic plasticity in magnocellular neurons of the hypothalamic supraoptic nucleus.
Di, S; Tasker, JG, 2004
)
0.32
"3 h, and dose-proportional maximal plasma concentrations and total exposures predict a dose-response relationship in clinical practice and allow an effective starting dose of 150 mg/day in clinical practice without need for titration."( Pregabalin pharmacology and its relevance to clinical practice.
Ben-Menachem, E, 2004
)
0.32
" Pregabalin, at 150, 300, and 600 mg/day, was significantly superior to placebo in reducing seizure frequency with a clear dose-response relationship."( Pregabalin as adjunctive therapy for partial seizures.
Brodie, MJ, 2004
)
0.32
" On Day 8, an antinociceptive dose-response curve was constructed and the 50% effective dose (ED(50)) values for morphine (given alone) were calculated for each study group."( The effects of intrathecal gabapentin on spinal morphine tolerance in the rat tail-flick and paw pressure tests.
Gilron, I; Hansen, C; Hong, M, 2004
)
0.32
" In all participants TMS procedures were carried out before and after administering GVG for three consecutive days at a daily dosage of 50 mg/kg."( Effect of Vigabatrin on motor responses to transcranial magnetic stimulation: an effective tool to investigate in vivo GABAergic cortical inhibition in humans.
Bernardi, G; Brusa, L; Caramia, MD; Galati, S; Marciani, MG; Palmieri, MG; Pierantozzi, M; Stanzione, P, 2004
)
0.32
" A dose-response curve revealed a bell-shaped effect of 3alpha,5alpha-THP on ePSA-NCAM+ progenitor proliferation, with greatest stimulation at nanomolar concentrations."( 3alpha,5alpha-Tetrahydroprogesterone (allopregnanolone) and gamma-aminobutyric acid: autocrine/paracrine interactions in the control of neonatal PSA-NCAM+ progenitor proliferation.
Avellana-Adalid, V; Baron-Van Evercooren, A; Cadepond, F; El-Etr, M; Gago, N; Samuel, D; Sananès, N; Schumacher, M, 2004
)
0.57
" This study examined the effects of gabapentin on signs of central sensitization (brush and pinprick hyperalgesia) in a human model of capsaicin-evoked pain, using a gabapentin dosing regimen similar to that used in the clinic."( Chronic oral gabapentin reduces elements of central sensitization in human experimental hyperalgesia.
Bach, FW; Brown, J; Chizh, BA; Gottrup, H; Jensen, TS; Juhl, G; Kristensen, AD; Lai, R, 2004
)
0.32
"01), but GBP daily dosage or concomitant AEDs had no significant influence on the ratio."( Association between patient age and gabapentin serum concentration-to-dose ratio: a preliminary multivariate analysis.
Adín, J; Armijo, JA; Pena, MA; Vega-Gil, N, 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
" Receptors desensitized and deactivated rapidly, and dose-response measurements estimated an EC(50) of approximately 30 microM."( GABAA receptor kinetics in the cerebellar nuclei: evidence for detection of transmitter from distant release sites.
Pugh, JR; Raman, IM, 2005
)
0.33
" Compared with the model group, the concentration of Glu in the middle and large dosage groups of TGF, during the 120 min of ischemia, reduced by 38."( [Effects of tianma gouteng fang on transmitter amino acids in the hippocampus extracellular liquids in freely moving rats subjected to brain ischemia].
Du, GY; Sun, XF; Wang, DQ; Wang, W; Ye, ZG; Zhang, CY; Zhao, DZ, 2004
)
0.32
"01) difference when the highest dosage of the drug was administered."( Oral treatment with PD-0200347, an alpha2delta ligand, reduces the development of experimental osteoarthritis by inhibiting metalloproteinases and inducible nitric oxide synthase gene expression and synthesis in cartilage chondrocytes.
Boileau, C; Boily, M; Brunet, J; El-Kattan, A; Flory, C; Martel-Pelletier, J; Pelletier, JP; Schrier, D; Tardif, G, 2005
)
0.33
" Initial studies examined the dose-response effects of injection of baclofen (0."( Injections of baclofen into the ventral medial prefrontal cortex block the initiation, but not the expression, of cocaine sensitization in rats.
Beyer, CE; Steketee, JD, 2005
)
0.33
" Further work is required to establish the optimal dosage and to validate the methods used to quantify the response to treatment."( Gabapentin can improve postural stability and quality of life in primary orthostatic tremor.
Byrnes, ML; Edwards, DJ; Mastaglia, FL; Rodrigues, JP; Stell, R; Thickbroom, G; Walters, SE, 2005
)
0.33
" 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
" The current study evaluated the anxiolytic efficacy of BID versus TID dosing of pregabalin in patients with generalized anxiety disorder."( Efficacy of pregabalin in the treatment of generalized anxiety disorder: double-blind, placebo-controlled comparison of BID versus TID dosing.
Feltner, DE; Fieve, RR; Pande, AC; Pohl, RB, 2005
)
0.33
"Gabapentin at a dosage of 1200 mg/d is safe and effective in treatment of epilepsy."( [Curative effect of gabapentin on refractory epilepsy].
Ding, MP; Hong, Z; Lü, CZ; Ma, GY; Pan, YF; Pan, YZ; Wang, DS; Wang, DX; Xiao, B; Zhao, QC; Zhu, GX, 2005
)
0.33
" These results present a novel interpretation of synergistic inhibition of certain epileptic discharges using vigabatrin and another drug, and that for successful synergistic treatment of epilepsies carefully designed timed dosage regimens are essential."( Antiepileptic action induced by a combination of vigabatrin and tiagabine.
Fueta, Y; Kunugita, N; Schwarz, W, 2005
)
0.33
" Following recovery, the phencyclidine dose-response curve was repeated in the fixed-interval paradigm."( Effects of phencyclidine on schedule-controlled responding following neurotoxic lesions of the striatum.
Carlson, KM; Wagner, GC, 2005
)
0.33
" Pregabalin dosing aimed at optimal balance of efficacy and tolerability provides significant pain relief and may reduce risks for AEs and therapy discontinuation."( Efficacy of pregabalin in neuropathic pain evaluated in a 12-week, randomised, double-blind, multicentre, placebo-controlled trial of flexible- and fixed-dose regimens.
Balkenohl, M; Freynhagen, R; Griesing, T; Strojek, K; Whalen, E, 2005
)
0.33
" Results of these studies showed efficacy at doses of 150 mg per day, and a dose-response relationship up to doses of 600 mg per day."( [Clinical experiences with pregabalin in the treatment of focal epilepsies].
Gil-Nagel Rein, A; Gómez-Alonso, J,
)
0.13
" Dose-response curves for current amplitudes, activation kinetics, and GABA-dependent desensitization parameters showed a parallel shift towards 30- to 40-fold higher GABA concentrations."( Molecular analysis of the A322D mutation in the GABA receptor alpha-subunit causing juvenile myoclonic epilepsy.
Bufler, J; Cossette, P; Krampfl, K; Lerche, H; Maljevic, S; Rouleau, GA; Ziegler, E, 2005
)
0.33
"6-fold shift in morphine's dose-response curve."( Attenuation of morphine tolerance by intrathecal gabapentin is associated with suppression of morphine-evoked excitatory amino acid release in the rat spinal cord.
Lee, MS; Lin, JA; Lin, SL; Wen, ZH; Wong, CS; Wu, CT; Yeh, CC, 2005
)
0.33
"Gabapentin has been shown to provide pain relief for post-herpetic neuralgia at dosage of 1200 to 2400 mg/day."( Starting dose of gabapentin for patients with post-herpetic neuralgia--a dose-response study.
Jean, WH; Mok, MS; Sun, WZ; Wu, CC, 2005
)
0.33
" H-89, per se, did not modify glutamate release but reduced extracellular GABA value at the higher dosage used (200 microM)."( Differential roles of mGlu8 receptors in the regulation of glutamate and gamma-aminobutyric acid release at periaqueductal grey level.
de Novellis, V; Maione, S; Marabese, I; Mariani, L; Palazzo, E; Rodella, L; Rossi, F; Siniscalco, D, 2005
)
0.56
" Responder rates across the effective doses (150-600 mg/day) ranged from 14% to 51% and demonstrated a significant dose-response relationship."( Defining success in clinical trials--profiling pregabalin, the newest AED.
Ryvlin, P, 2005
)
0.33
" In the presence of 300 microM Lu(3+), dose-response curves for GABA-evoked currents showed a significant enhancement of the maximum amplitude and an increase of the apparent affinity."( Analysis of macroscopic ionic currents mediated by GABArho1 receptors during lanthanide modulation predicts novel states controlling channel gating.
Calvo, DJ; Escobar, AL; Goutman, JD, 2005
)
0.33
"Patients were stabilised using phenobarbitone and/or potassium bromide to produce tolerable therapeutic serum concentrations and dosed additionally with gabapentin at 35 to 50 mg/kg/d (divided twice or three times daily) for 4 months."( Improving seizure control in dogs with refractory epilepsy using gabapentin as an adjunctive agent.
Govendir, M; Malik, R; Perkins, M, 2005
)
0.33
" At low concentration, bilobalide (3 microM) caused a parallel right shift and surmountable GABA maximal response of the GABA dose-response curve characteristic of a competitive antagonist."( Mixed antagonistic effects of bilobalide at rho1 GABAC receptor.
Chebib, M; Duke, RK; Huang, SH; Johnston, GA; Sasaki, K; Wada, K, 2006
)
0.33
"5-5 mg/kg) produced a rightward shift of a heroin dose-response curve, while vigabatrin (75-300 mg/kg), baclofen (0."( Role of opioidergic mechanisms and GABA uptake inhibition in the heroin-induced discriminative stimulus effects in rats.
Filip, M; Krówka, T; Przewłocki, R; Solecki, W,
)
0.13
" Dosage could be adjusted based on tolerability and maintained when a 4-week seizure-free period was achieved."( Pregabalin add-on treatment in patients with partial seizures: a novel evaluation of flexible-dose and fixed-dose treatment in a double-blind, placebo-controlled study.
Anhut, H; Barrett, JA; Brodie, MJ; Elger, CE; Lee, CM, 2005
)
0.33
" Lower incidence of adverse events and discontinuations were achieved in patients receiving pregabalin when dosing was individualized to optimize efficacy and tolerability."( Pregabalin add-on treatment in patients with partial seizures: a novel evaluation of flexible-dose and fixed-dose treatment in a double-blind, placebo-controlled study.
Anhut, H; Barrett, JA; Brodie, MJ; Elger, CE; Lee, CM, 2005
)
0.33
" Dose-response studies with 6-hydroxydopamine revealed that the application of 200 microg per animal caused hypokinetic signs (decreased ambulatory activity, increased inactivity, and reduced motor coordination), which paralleled several signs of degeneration of nigrostriatal dopaminergic neurons (dopamine depletion in the caudate-putamen, and decreased mRNA levels for tyrosine hydroxylase and superoxide dismutase-1 and -2 in the substantia nigra)."( Effects of rimonabant, a selective cannabinoid CB1 receptor antagonist, in a rat model of Parkinson's disease.
de Miguel, R; Fernández-Ruiz, J; García-Arencibia, M; González, S; Ramos, JA; Scorticati, C, 2006
)
0.33
" Tiagabine was initiated at 4 mg/day and then flexibly dosed twice a day to a maximum dose of 16 mg/day."( The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study.
Brown, C; Ondrasik, J; Pollack, MH; Rickels, K; Roy-Byrne, PP; Snyder, H; Van Ameringen, M, 2005
)
0.33
" The method was successfully applied to the analysis of gabapentin in plasma from dosed patients for therapeutic drug monitoring."( Simple and sensitive liquid chromatographic method with fluorimetric detection for the analysis of gabapentin in human plasma.
Chung, TC; Tai, CT; Wu, HL, 2006
)
0.33
"This trial evaluated the efficacy and safety of pregabalin dosed twice daily (BID) for relief of neuro-pathic pain associated with postherpetic neuralgia (PHN)."( Efficacy and tolerability of twice-daily pregabalin for treating pain and related sleep interference in postherpetic neuralgia: a 13-week, randomized trial.
Feister, HA; Rigaudy, L; Stoker, M; van Seventer, R; Versavel, M; Young, JP, 2006
)
0.33
"Pregabalin, dosed BID, reduced neuropathic pain associated with PHN and was well tolerated."( Efficacy and tolerability of twice-daily pregabalin for treating pain and related sleep interference in postherpetic neuralgia: a 13-week, randomized trial.
Feister, HA; Rigaudy, L; Stoker, M; van Seventer, R; Versavel, M; Young, JP, 2006
)
0.33
" The improved pharmacokinetic profile of pregabalin relative to gabapentin is manifested in linear and dose-independent absorption and a narrow therapeutic dosing range."( Pregabalin in neuropathic pain: a more "pharmaceutically elegant" gabapentin?
Guay, DR, 2005
)
0.33
" First, the maximally effective gabapentin dosage (600-2,700 mg/day) for each patient was determined during an initial dose-titration phase."( Blinded placebo crossover study of gabapentin in primary orthostatic tremor.
Byrnes, ML; Edwards, DJ; Mastaglia, FL; Rodrigues, JP; Stell, R; Thickbroom, GW; Walters, SE, 2006
)
0.33
" In contrast, CPCCOEt shifted the EtOH dose-response function downwards, enhanced the capacity of higher EtOH doses to elevate NAC levels of GABA and lowered extracellular dopamine and glutamate below baseline following EtOH injection."( Behavioral and neurochemical interactions between Group 1 mGluR antagonists and ethanol: potential insight into their anti-addictive properties.
Hannun, RA; Kapasova, Z; Lominac, KD; Middaugh, LD; Patterson, C; Szumlinski, KK, 2006
)
0.33
" In conclusion, single or repeated dosing of gabapentin reduced cutaneous but not muscle pain in healthy volunteers."( Multiple dose gabapentin attenuates cutaneous pain and central sensitisation but not muscle pain in healthy volunteers.
Segerdahl, M, 2006
)
0.33
" Pregabalin in both dosage treatment groups (400 mg/day, p < ."( Efficacy and safety of pregabalin in the treatment of generalized anxiety disorder: a 6-week, multicenter, randomized, double-blind, placebo-controlled comparison of pregabalin and venlafaxine.
Kasper, S; Montgomery, SA; Pande, AC; Tobias, K; Zornberg, GL, 2006
)
0.33
" Additionally, pregabalin (initial dosage 450 mg/day) was effective for the prevention of relapse of GAD over 34 weeks."( Pregabalin: in the treatment of generalised anxiety disorder.
Foster, RH; Frampton, JE, 2006
)
0.33
" Initial gabapentin dosage was 600 mg/day."( The effect of gabapentin in earlier stage of reflex sympathetic dystrophy.
Duman, I; Hazneci, B; Kalyon, TA; Tan, AK; Taşkaynatan, MA, 2007
)
0.34
" When dosed at 10mg/kg, beta-acids increased, in the elevated plus maze, open arm entries reducing in parallel those in closed arms."( Evidence that the beta-acids fraction of hops reduces central GABAergic neurotransmission.
Avallone, R; Baraldi, M; Brusiani, F; Losi, G; Puia, G; Rivasi, M; Zanoli, P; Zavatti, M, 2007
)
0.34
" Taking maximum relative contraction speed and minimal relative projected body area as a measure of the sponge's response, a comparison of the dose-response curves indicated a higher sensitivity of the contractile tissue for GABA than for L: -Glu."( GABA and glutamate specifically induce contractions in the sponge Tethya wilhelma.
Eich, A; Ellwanger, K; Nickel, M, 2007
)
0.34
" For these older drugs it has been common practice to adjust the dosage to achieve a serum drug concentration within a predefined 'therapeutic range', representing an interval where most patients are expected to show an optimal response."( Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed?
Johannessen, SI; Tomson, T, 2006
)
0.33
" We used a repeated dosing paradigm because there are precedents showing that repeated drug exposure may be necessary to demonstrate analgesia in neuropathic pain models."( Chemotherapy-evoked painful peripheral neuropathy: analgesic effects of gabapentin and effects on expression of the alpha-2-delta type-1 calcium channel subunit.
Bennett, GJ; Boroujerdi, A; Luo, ZD; Xiao, W, 2007
)
0.34
"We report the case of a woman with an apparent primary thunderclap headache which occurred frequently until she achieved a therapeutic dosage of gabapentin."( Persistent primary thunderclap headache responsive to gabapentin.
Black, DF; Garza, I, 2006
)
0.33
" There was no need to decrease of the dosage of GBP and the side effects were mild and of transitory nature."( [Efficacy, safety and effect on the quality of life of gabapentin in adult epilepsy--results of a prospective open-label quasi naturalistic Hungarian multicenter study (phase human-IV)].
Rajna, P; Szíjártó, E, 2006
)
0.33
" Thus, monitoring and dosage adjustment are required, without discontinuation of the drug."( Therapeutic management of chronic neuropathic pain: an examination of pharmacologic treatment.
Argyra, E; Moka, E; Siafaka, I; Vadalouca, A; Vrachnou, E, 2006
)
0.33
" Pregabalin was administered either intraperitoneally (IP) or intrathecally (IT) and dosed up incrementally until an antiallodynic effect without sedation or motor impairment was apparent."( Antiallodynic effect of pregabalin in rat models of sympathetically maintained and sympathetic independent neuropathic pain.
Han, DW; Kweon, TD; Lee, JS; Lee, YW, 2007
)
0.34
" The anticonvulsant and acute adverse effects of the combination of TPM with GBP at the fixed ratio of 1:1 were determined using the type I isobolographic analysis for nonparallel dose-response relationship curves (DRRCs)."( Isobolographic analysis of interaction between drugs with nonparallel dose-response relationship curves: a practical application.
Luszczki, JJ, 2007
)
0.34
" Here, a collection of subchronic to chronic rodent and nonhuman primate studies was evaluated to determine whether there is a consistent dose-response relationship among studies, whether there is a progression of effects with increasing dose, and whether these studies are adequate for evaluating the neurotoxicity of chronic low-level manganese exposures in humans."( Adequacy and consistency of animal studies to evaluate the neurotoxicity of chronic low-level manganese exposure in humans.
Gwiazda, R; Lucchini, R; Smith, D, 2007
)
0.34
" In contrast, the tmax and terminal half-life of gabapentin did not change after oral dosing for all treatments."( In vivo effects of glycyl-glutamate and glycyl-sarcosine on gabapentin oral absorption in rat.
Fleisher, D; Nguyen, TV; Smith, DE, 2007
)
0.34
" Individualization of dosage and avoidance of unnecessary polypharmacy are essential for safe utilization of anti-epileptic drugs."( [Epilepsy in the elderly].
Yoshino, A, 2007
)
0.34
" A single dose of 1 mug of VEGF, chosen from a dose-response study, highly disrupted the BBB in the ventral mesencephalon in a time-dependent manner."( Blood-brain barrier disruption induces in vivo degeneration of nigral dopaminergic neurons.
Cano, J; Machado, A; Rite, I; Venero, JL, 2007
)
0.34
"Gabapentin, at a maintenance dosage of 900 to 3600 mg/d for 8 weeks, or lactose placebo."( Relief of idiopathic subjective tinnitus: is gabapentin effective?
Chole, RA; Finnell, J; Piccirillo, JF; Spitznagel, E; Vlahiotis, A, 2007
)
0.34
"Adjuvants are compounds which by themselves have undesirable side-effects or low potency but in combination with opioids allow a reduction of narcotic dosing for postoperative pain control."( Useful adjuvants for postoperative pain management.
Buvanendran, A; Kroin, JS, 2007
)
0.34
" In addition the optimal time frame for cell grafting after ischemia and the optimal dosing of grafted cells were also studied."( Functional recovery in rats with ischemic paraplegia after spinal grafting of human spinal stem cells.
Cizkova, D; Hazel, T; Hefferan, MP; Johe, K; Kakinohana, O; Kucharova, K; Marsala, M; Marsala, S, 2007
)
0.34
" All fenamates tested (1-100 microM) dose-dependently potentiated GABA-evoked currents; mefenamic acid (MFA) was the most potent and efficacious and was found to shift the GABA dose-response curve to the left without effect on the maximum amplitude or the GABA Hill Slope."( Characterization of the interaction between fenamates and hippocampal neuron GABA(A) receptors.
Coyne, L; Halliwell, RF; Patten, D; Su, J,
)
0.13
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of pregabalin are reviewed."( Pregabalin: an antiepileptic agent useful for neuropathic pain.
Blommel, AL; Blommel, ML, 2007
)
0.34
" The starting dosage for patients with neuropathic pain associated with diabetic peripheral neuropathy is 50 mg three times daily and may be increased to 300 mg daily within one week based on efficacy and tolerability."( Pregabalin: an antiepileptic agent useful for neuropathic pain.
Blommel, AL; Blommel, ML, 2007
)
0.34
" Four of the available six placebo-controlled trials were found acceptable for a pooled analysis of dose-response relationship."( Dose-response relationship of pregabalin in patients with generalized anxiety disorder. A pooled analysis of four placebo-controlled trials.
Bech, P, 2007
)
0.34
" Treatment was continued for 6 days, during which the dosage was progressively decreased, and the mare was discharged."( Gabapentin for the treatment of neuropathic pain in a pregnant horse.
Davis, JL; Elce, Y; Posner, LP, 2007
)
0.34
" Sanjoinine A also increased sleeping rate and sleeping time when administered combined with pentobarbital at a sub-hypnotic dosage and showed synergistic effects with muscimol in potentiating sleeping onset and enhancing sleeping time induced by pentobarbital."( Sanjoinine A isolated from Zizyphi Spinosi Semen augments pentobarbital-induced sleeping behaviors through the modification of GABA-ergic systems.
Eun, JS; Han, H; Hong, JT; Kim, HC; Ma, Y; Oh, KW, 2007
)
0.34
" Better effects could be achieved with earlier use of high dosage GABA or Na-DMPS."( The antidotal effects of high-dosage gamma-aminobutyric acid on acute tetramine poisoning as compared with sodium dimercaptopropane sulfonate.
Han, J; Sun, P; Weng, Y, 2007
)
0.61
" In addition to reassurance, pregabalin was prescribed for these myotonic symptoms at a dosage of 50 mg by mouth three times daily."( Successful amelioration of oxaliplatin-induced hyperexcitability syndrome with the antiepileptic pregabalin in a patient with pancreatic cancer.
Hashmi, S; Saif, MW, 2008
)
0.35
" A flexible dosing approach appears appropriate to ensure patient compliance and treatment success."( Efficacy and safety of pregabalin in treatment refractory patients with various neuropathic pain entities in clinical routine.
Freynhagen, R; Grond, S; Hagebeuker, A; Junker, U; Konrad, C; Schmelz, M; Schüpfer, G; Von Giesen, HJ; Wagner, KJ; Ziegler, D, 2007
)
0.34
"A rapid, sensitive and accurate high performance liquid chromatography with UV detection method was developed and validated for the quantification of gabapentin in dosage forms."( Optimization of an HPLC method for determination of gabapentin in dosage forms through derivatization with 1-fluoro-2,4-dinitrobenzene.
Jalalizadeh, H; Shafiee, A; Souri, E, 2007
)
0.34
"Both gabapentin and pregabalin are approved for the management of postherpetic neuralgia (PHN), although dosing and pharmacokinetic differences between these medications may affect their use in actual practice."( A retrospective evaluation of the use of gabapentin and pregabalin in patients with postherpetic neuralgia in usual-care settings.
Gore, M; Sadosky, A; Stacey, B; Tai, KS, 2007
)
0.34
" However, the results should not be extrapolated to other gabapentin drug products and to other tablet dosage forms."( Comparison of the stability of split and intact gabapentin tablets.
Ciavarella, AB; Faustino, PJ; Gupta, A; Khan, MA; Sayeed, VA; Volpe, DA, 2008
)
0.35
" correlated with blood concentrations within 4 h after dosing, and maximal efficacy was obtained 2 h after dosing when the maximal blood concentration was achieved at either dose."( Effect of a new alpha 2 delta ligand PD-217014 on visceral hypersensitivity induced by 2,4,6-trinitrobenzene sulfonic acid in rats.
Kawai, M; Kurebayashi, Y; Ninomiya, N; Ohashi, K; Taylor, C, 2008
)
0.35
" However, patients on the same PGB dosage per body weight had rather different PGB trough concentrations, which could be explained only in part by age and comedication."( Serum concentrations of pregabalin in patients with epilepsy: the influence of dose, age, and comedication.
Jürgens, U; May, TW; Neb, R; Rambeck, B, 2007
)
0.34
"We introduce a system for temperature control of a commercial microfluidic superfusion device that, in combination with patch-clamp, enables rapid acquisition of dose-response data at different temperatures."( Ligand-specific temperature-dependent shifts in EC50 values for the GABAA receptor.
Bridle, H; Jesorka, A; Lincoln, P; Millingen, M; Orwar, O, 2008
)
0.35
" The most frequently used dosing regimen involved a starting dose of 150mg/d and dose escalation to 300mg/d after one week (mean: 301mg/d, administered in two doses)."( Efficacy and safety of pregabalin in patients with diabetic peripheral neuropathy or postherpetic neuralgia: Open-label, non-comparative, flexible-dose study.
Baron, R; Binder, A; Brasser, M; Brunnmüller, U; May, M, 2008
)
0.35
" Withdrawal of female rats from prolonged systemic dosing with progesterone leads to increased numbers of alpha4, beta1 and delta GABA(A) receptor subunit-immunoreactive neurones in the PAG."( GABA in the female brain -- oestrous cycle-related changes in GABAergic function in the periaqueductal grey matter.
Lovick, TA, 2008
)
0.35
" Redox modulation of GABArho(1) receptors was strongly dependent on the GABA concentration; dose-response curves for GABA were shifted to the left in the presence of reducing agents, whereas oxidizing agents produced the opposite effect, without changes in the maximal response to GABA and in the Hill coefficient."( Redox modulation of homomeric rho1 GABA receptors.
Calero, CI; Calvo, DJ, 2008
)
0.35
" It also significantly increased the falling asleep rate and duration of sleeping time at a sub-hypnotic dosage of pentobarbital (28 mg/kg)."( Cyclopeptide alkaloid fraction from Zizyphi Spinosi Semen enhances pentobarbital-induced sleeping behaviors.
Han, H; Hong, JT; Kim, YB; Ma, Y; Nam, SY; Oh, KW; Yun, YP, 2008
)
0.35
"To evaluate the efficacy, safety, and tolerability of pregabalin across the effective dosing range, to determine differences in the efficacy of three times daily (TID) versus twice daily (BID) dosage schedules, and to use time-to-event analysis to determine the time to onset of a sustained therapeutic effect using data from seven trials of pregabalin in painful diabetic peripheral neuropathy (DPN)."( Efficacy, safety, and tolerability of pregabalin treatment for painful diabetic peripheral neuropathy: findings from seven randomized, controlled trials across a range of doses.
Durso-Decruz, E; Emir, B; Freeman, R, 2008
)
0.35
" Only one trial included all three of these dosages, and TID dosing was used in four."( Efficacy, safety, and tolerability of pregabalin treatment for painful diabetic peripheral neuropathy: findings from seven randomized, controlled trials across a range of doses.
Durso-Decruz, E; Emir, B; Freeman, R, 2008
)
0.35
"Treatment with pregabalin across its effective dosing range is associated with significant, dose-related improvement in pain in patients with DPN."( Efficacy, safety, and tolerability of pregabalin treatment for painful diabetic peripheral neuropathy: findings from seven randomized, controlled trials across a range of doses.
Durso-Decruz, E; Emir, B; Freeman, R, 2008
)
0.35
" This was seen in the 150 mg/day, 300-450 mg/day and 600 mg/day dosing groups."( Efficacy of pregabalin in depressive symptoms associated with generalized anxiety disorder: a pooled analysis of 6 studies.
Baldinetti, F; Baldwin, DS; Mandel, F; Stein, DJ, 2008
)
0.35
" Double-blind treatment was with placebo or the patient's optimal fixed dosage of pregabalin."( Fibromyalgia relapse evaluation and efficacy for durability of meaningful relief (FREEDOM): a 6-month, double-blind, placebo-controlled trial with pregabalin.
Crofford, LJ; Haig, GM; Martin, SA; Mease, PJ; Sharma, U; Simpson, SL; Young, JP, 2008
)
0.35
" Pantogam was administered in dosage 750-3000 mg per day along with traditional and atypical neuroleptics."( [Pantogam in daily psychiatric practice].
Bogdan, MN; Kontsevoĭ, VA; Riakhovskiĭ, VV; Rotshteĭn, VG, 2007
)
0.34
" Further well-designed trials are warranted to establish the most appropriate dosing regimen in patients on HD."( Role of gabapentin in the treatment of uremic pruritus.
Gommer, J; Scates, AC; Vila, T, 2008
)
0.35
" Therefore, conventional sustained formulations would likely result in decreased bioavailability, as the dosage form would pass through the window of absorption before the drug could be completely released."( Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive- extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in hea
Berner, B; Gordi, T; Hou, E; Kasichayanula, S, 2008
)
0.35
" Gabapentin plasma concentrations were measured in serial plasma samples collected >or=48 hours following dosing on days 1 and 8 using a validated high performance liquid chromatography/tandem mass spectrometry system with a lowest limit of quantitation of 75 ng/mL."( Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive- extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in hea
Berner, B; Gordi, T; Hou, E; Kasichayanula, S, 2008
)
0.35
" However, BID dosing resulted in apparently lower C(max) (mean ratio: 81%; CI 90%, 76%-86%) and greater C(min) values (mean ratio: 118%; CI 90%, 107%-130%), while G-ER QD dosing was associated with numerically greater C(max) (mean ratio: 116%; CI 90%, 109%-123%), and lower C(min) values (mean ratio: 52%; CI 90%, 48%-56%) compared with G-IR TID during a 24-hour dosing period."( Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive- extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in hea
Berner, B; Gordi, T; Hou, E; Kasichayanula, S, 2008
)
0.35
"This exploratory study found that in these healthy subjects, the daily exposure provided by less frequent G-ER dosing was not significantly different from same daily dose with G-IR, administered more frequently."( Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive- extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in hea
Berner, B; Gordi, T; Hou, E; Kasichayanula, S, 2008
)
0.35
" Recommendations for future research to inform clinical practice should include cost-effectiveness studies and dose-response analysis in order to determine the schema employed and the duration of treatment."( Efficacy of pregabalin and gabapentin for neuropathic pain in spinal-cord injury: an evidence-based evaluation of the literature.
Amaniti, E; Kouvelas, D; Papazisis, G; Tzellos, TG, 2008
)
0.35
"Time to onset of pain relief and improvement in allodynia in 269 patients with postherpetic neuralgia was examined in a 4-week randomized trial comparing flexibly dosed pregabalin (150-600 mg/d), fixed-dose pregabalin (300 mg/d), and placebo."( Pregabalin for postherpetic neuralgia: placebo-controlled trial of fixed and flexible dosing regimens on allodynia and time to onset of pain relief.
Barrett, JA; Phillips, KF; Rowbotham, MC; Stacey, BR; Whalen, E, 2008
)
0.35
" Gabapentin and R-PIA were administered to obtain the dose-response curve and the 50% effective dose (ED(50))."( The interaction of gabapentin and N6-(2-phenylisopropyl)-adenosine R-(-)isomer (R-PIA) on mechanical allodynia in rats with a spinal nerve ligation.
Jun, IG; Park, JY, 2008
)
0.35
" It is effective with two or three-times daily dosing in a dose range of 150 to 600 mg daily."( Pregabalin for neuropathic pain based on recent clinical trials.
Stacey, BR; Swift, JN, 2006
)
0.33
"In this study, a straightforward and automated pulsed flow-based procedure was developed for the chemiluminometric determination of gabapentin [1-(aminomethyl)cyclo-hexaneacetic acid], a new generation antiepileptic drug, in different formulated dosage forms."( Rapid chemiluminometric determination of gabapentin in pharmaceutical formulations exploiting pulsed-flow analysis.
Cerdà, V; Estela, JM; Lima, JL; Manera, M; Miró, M; Ribeiro, MF; Santos, JL,
)
0.13
" We evaluated the efficacy of pregabalin 600 mg/d (300 mg dosed BID) versus placebo for relieving DPN-associated neuropathic pain, and assessed its safety using objective measures of nerve conduction (NC)."( Efficacy and safety of pregabalin 600 mg/d for treating painful diabetic peripheral neuropathy: a double-blind placebo-controlled trial.
Arezzo, JC; Lamoreaux, L; Pauer, L; Rosenstock, J, 2008
)
0.35
" After 1-weeks' dosage escalation, pregabalin-treated patients received 300 mg BID for 12 weeks."( Efficacy and safety of pregabalin 600 mg/d for treating painful diabetic peripheral neuropathy: a double-blind placebo-controlled trial.
Arezzo, JC; Lamoreaux, L; Pauer, L; Rosenstock, J, 2008
)
0.35
" Log-probit analysis was used to evaluate dose-response effects and calculate the ED(50) values for gabapentin, tiagabine, and their combination at the fixed-ratio of 1:1 in the phases I and II of the formalin test in mice."( Synergistic interaction of gabapentin with tiagabine in the formalin test in mice: an isobolographic analysis.
Czuczwar, M; Czuczwar, SJ; Kolacz, A; Luszczki, JJ; Przesmycki, K, 2009
)
0.35
" XP13512 may therefore provide more predictable gabapentin exposure and decreased dosing frequency."( Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin.
Canafax, DM; Cundy, KC; Luo, W; Moors, TL; Sastry, S; Zou, J, 2008
)
0.35
" The method was applied successfully to the determination of this drug in pharmaceutical dosage form."( Spectrophotometric and spectrofluorimetric methods for the determination of pregabalin in bulk and pharmaceutical preparation.
Onal, A; Sagirli, O, 2009
)
0.35
" The most commonly reported AEs were dizziness and somnolence, however, they were most pronounced during the first week of treatment, followed by a sharp fall in incidences across all dosing groups to <5% from Week 2 and onwards."( Add-on treatment with pregabalin for partial seizures with or without generalisation: pooled data analysis of four randomised placebo-controlled trials.
Baldinetti, F; Gil-Nagel, A; Leon, T; Zaccara, G, 2009
)
0.35
" However, the dose-response curve significantly shifted toward lower concentration values in G93A motor neurons and the extent of desensitization also increased in these neurons."( GAB(A) receptors present higher affinity and modified subunit composition in spinal motor neurons from a genetic model of amyotrophic lateral sclerosis.
Carunchio, I; Merlo, D; Mollinari, C; Pieri, M; Zona, C, 2008
)
0.35
" Daily median dosage was 300 mg."( Pregabalin in patients with primary brain tumors and seizures: a preliminary observation.
Novy, J; Rossetti, AO; Stupp, R, 2009
)
0.35
" Nine patients meeting Diagnostic and Statistical Manual, fourth edition criteria for PTSD who were on stable doses of antidepressants were treated open label with flexibly dosed pregabalin for 6 weeks."( Pregabalin augmentation of antidepressants in patients with accident-related posttraumatic stress disorder: an open label pilot study.
Han, C; Marks, DM; Masand, PS; Pae, CU; Patkar, AA, 2009
)
0.35
" Steady-state serum concentrations of gabapentin, distributed over a dosage interval, were obtained from 16 adult patients."( A population pharmacokinetic model of gabapentin developed in nonparametric adaptive grid and nonlinear mixed effects modeling.
Carlsson, KC; Eriksen, HO; Hoem, NO; Karlsson, MO; Moberg, ER; van de Schootbrugge, M, 2009
)
0.35
" injection of aggregated Abeta25-35 in dosage 30nmol/rat resulted in impairment in spatial alternation behavior."( Effects of beta-amyloid on behavioral and amino acids spectrum in rats' brain and their modulation by embryonic proteins.
Aghajanov, M; Mkrtchyan, L; Navasardyan, G; Safaryan, K; Yenkoyan, K,
)
0.13
" The GABA dose-response properties of alpha(1)-beta(3)-alpha(1)/beta(3)-delta and beta(3)-alpha(1)-delta/alpha(1)-beta(3) match most closely the properties of non-concatenated alpha(1)beta(3)delta receptors."( Unanticipated structural and functional properties of delta-subunit-containing GABAA receptors.
Baur, R; Kaur, KH; Sigel, E, 2009
)
0.35
"Our findings show that, contrary to what would be expected on the basis of gene dosage criteria, the striatal regions in which rl/rl mice exhibited decreased density of PV+ interneurons were either unaltered (rostral striatum) or equally altered (dorsomedial and ventromedial intermediate striatum, caudal striatum) in rl/+ mice."( Reelin haploinsufficiency reduces the density of PV+ neurons in circumscribed regions of the striatum and selectively alters striatal-based behaviors.
Ammassari-Teule, M; Biamonte, F; Keller, F; Marrone, C; Mercuri, NB; Sgobio, C, 2009
)
0.35
" However, the whole-cell GABA dose-response and the single-channel effective opening rate curves were shifted to higher GABA concentrations, suggesting that the concatemeric receptors have a lower affinity to GABA."( Activation and modulation of concatemeric GABA-A receptors expressed in human embryonic kidney cells.
Akk, G; Bracamontes, J; Li, P; Steinbach, JH, 2009
)
0.35
" To be included in the meta-analysis, RCTs had to compare gabapentin with placebo in the treatment of hot flashes in women with natural or tamoxifen-induced menopause, regardless of the sample size, dosage used, duration of treatment, or frequency of the episodes."( Gabapentin for the treatment of hot flashes in women with natural or tamoxifen-induced menopause: a systematic review and meta-analysis.
Goulis, DG; Kouvelas, D; Toulis, KA; Tzellos, T, 2009
)
0.35
" The dose-response curve was bell-shaped."( Interactions between the anxiogenic effects of CB1 gene disruption and 5-HT3 neurotransmission.
Aliczki, M; Halasz, J; Haller, J; Mikics, E; Vas, J, 2009
)
0.35
" Patients in group B who were receiving gabapentin continued this treatment up to a maximum daily dosage of 2400 mg during the observation period."( Adequacy assessment of oxycodone/paracetamol (acetaminophen) in multimodal chronic pain : a prospective observational study.
Bertini, L; Carucci, A; Gatti, A; Mammucari, M; Occhioni, R; Sabato, AF, 2009
)
0.35
" In several pregabalin dosage groups the dosage was escalated during days 1-7, whereas in others pregabalin was initiated at a fixed dosage without escalation."( Rapid onset of seizure suppression with pregabalin adjunctive treatment in patients with partial seizures.
Barrett, JA; Perucca, E; Ramsay, RE; Robbins, J; Spiegel, K, 2009
)
0.35
" At the dosing schemes most commonly used in placebo-controlled trials, significant seizure-suppressing activity was observed after only 2 days of treatment."( Rapid onset of seizure suppression with pregabalin adjunctive treatment in patients with partial seizures.
Barrett, JA; Perucca, E; Ramsay, RE; Robbins, J; Spiegel, K, 2009
)
0.35
" The introduction of the compound in dosage according to the scheme of antioxidant therapy, inhibited the tumor growth by ca."( Synthesis, characterization, in vivo antitumor properties of the cluster rhenium compound with GABA ligands and its synergism with cisplatin.
Collery, P; Domasevitch, KV; Golichenko, AA; Shtemenko, AV; Shtemenko, NI; Zabitskaya, ED, 2009
)
0.35
"The median dosage of gabapentin was 1800 mg/daily."( The efficacy and safety of gabapentin in carpal tunnel patients: open label trial.
Erdemoglu, AK,
)
0.13
" Linear regression analysis was used to evaluate the dose-response relationships between logarithms of antiepileptic drug doses and their resultant maximum possible antinociceptive effects in the mouse hot-plate test."( Synergistic interaction of gabapentin with tiagabine in the hot-plate test in mice: an isobolographic analysis.
Czuczwar, M; Czuczwar, SJ; Kołacz, A; Luszczki, JJ; Przesmycki, K; Wojda, E,
)
0.13
" The infant continued to receive gabapentin; the dosage was increased to 10 mg/kg at bedtime after 6 days, then to 5 mg/kg in the morning and 10 mg/kg at bedtime 10 days later."( Gabapentin therapy for pain and irritability in a neurologically impaired infant.
Cox, TH; Garner, SS; Haney, AL, 2009
)
0.35
" Up to estimated 336 patients (interim analyses) with acute herpes zoster pain (VAS > 30 mm) will be randomised to one of three groups (a) semi-standardised acupuncture (168 patients); (b) gabapentine with individualised dosage between 900-3600 mg/d (84 patients); (c) sham laser acupuncture."( Acupuncture in acute herpes zoster pain therapy (ACUZoster) - design and protocol of a randomised controlled trial.
Fleckenstein, J; Hoffrogge, P; Irnich, D; Kramer, S; Lang, PM; Lehmeyer, L; Mansmann, U; Pfab, F; Ring, J; Schober, GM; Schotten, KJ; Thoma, S; Weisenseel, P, 2009
)
0.35
" The 32 mg dose of BL-1020 resulted in an average D(2) RO of 44% at 4-6 h post dosing (pd), which declined to 33% at 24 h pd."( BL-1020, a novel antipsychotic candidate with GABA-enhancing effects: D2 receptor occupancy study in humans.
Antoni, G; Appel, L; Eriksson, C; Geffen, Y; Heurling, K; Kapur, S, 2009
)
0.35
" A dose-response effect was evident for PGB that reached a plateau at a dose of 300 mg/d."( Comparative efficacy of pregabalin and benzodiazepines in treating the psychic and somatic symptoms of generalized anxiety disorder.
Feltner, DE; Herman, B; Lydiard, RB; Rickels, K, 2010
)
0.36
" In the present retrospective study we evaluated the impact of these vendor changes on ketamine dosing to establish anaesthesia, on pilocarpine-induced seizure susceptibility, and on basal extracellular hippocampal noradrenaline, dopamine, serotonin, gamma-amino butyric acid, and glutamate levels of all pilocarpine-treated rats included in our studies."( Intrastrain differences in seizure susceptibility, pharmacological response and basal neurochemistry of Wistar rats.
Aourz, N; Clinckers, R; De Bundel, D; Meurs, A; Michotte, Y; Portelli, J; Smolders, I, 2009
)
0.35
"Pregabalin 4 mg kg(-1) PO produces plasma concentrations within the extrapolated therapeutic range from humans for sufficient time to suggest that a twice daily dosing regime would be adequate."( Pharmacokinetics of single-dose oral pregabalin administration in normal dogs.
Badgley, BL; Dewey, CW; Gleed, RD; Horne, W; Ludders, JW; Salazar, V; Schwark, W, 2009
)
0.35
" Gabapentin was rapidly absorbed and eliminated in dogs, indicating that frequent dosing is needed to maintain minimum targeted plasma concentrations."( Pharmacokinetics of oral gabapentin in greyhound dogs.
Cohen, RL; Kukanich, B, 2011
)
0.37
" Its normal plasma half-life is 2 - 3 hours; dosage modifications are obligatory in renal insufficiency."( Drug-induced encephalopathy secondary to non renal dosing of common medications in Two dialysis patients.
Iloanya, PC; Nye, D; Onuigbo, MA, 2009
)
0.35
" Analysis of the log dose-response curves for oxcarbazepine or gabapentin in a presence of amitriptyline and oxcarbazepine or gabapentin applied alone, revealed a synergism in oxcarbazepine-amitriptyline and additivity in gabapentin-amitriptyline combination."( Analysis of the antinociceptive interactions in two-drug combinations of gabapentin, oxcarbazepine and amitriptyline in streptozotocin-induced diabetic mice.
Bosković, B; Micov, AM; Prostran, MS; Stepanović-Petrović, RM; Tomić, MA; Ugresić, ND; Vucković, SM, 2010
)
0.36
" The initial daily dosage was 75 mg, subsequently adjusted according to the drug's efficacy and the individual patients' tolerability at 2-week intervals."( Pregabalin in the treatment of chronic migraine: an open-label study.
Calandre, EP; Garcia-Leiva, JM; Rico-Villademoros, F; Rodriguez-Lopez, CM; Vilchez, JS,
)
0.13
" Patients were then started on open-label pregabalin (75, 150, 300 and 600 mg/day) according to a forced titration dosing regimen, while continuing the same dosage of oxycodone or placebo for 4 weeks."( A randomized, controlled trial of oxycodone versus placebo in patients with postherpetic neuralgia and painful diabetic neuropathy treated with pregabalin.
Duffull, SB; Moore, BJ; Nissen, LM; O'Callaghan, JP; Smith, MT; Zin, CS, 2010
)
0.36
" A dose-response relationship was apparent for at least 50% pain relief and for adverse event outcomes."( Pregabalin in fibromyalgia: meta-analysis of efficacy and safety from company clinical trial reports.
Derry, S; McQuay, HJ; Moore, RA; Straube, S, 2010
)
0.36
" In both conditions, PGB was found efficacious with significant improvement in withdrawal symptoms at the dosage ranges of 150-450 mg/day (AD) and 225-900 mg/day (BD)."( Pregabalin in the treatment of alcohol and benzodiazepines dependence.
Konstantakopoulos, G; Oulis, P, 2010
)
0.36
"Although not definitive, our findings suggest that gabapentin administered at these doses with this dosing regimen holds little promise for the treatment of tobacco dependence in a population of smokers seeking treatment."( Gabapentin for smoking cessation.
Croghan, IT; Ebbert, JO; Hays, JT; Schroeder, DR; Sood, A; Sood, R; Wyatt, KD, 2010
)
0.36
"The aim of this study was to characterize the anticonvulsant effects of 1-methyl-1,2,3,4-tetrahydroisoquinoline (MeTHIQ--an endogenous parkinsonism-preventing substance) in combination with four second-generation antiepileptic drugs (AEDs: lamotrigine [LTG], oxcarbazepine [OXC], pregabalin [PGB], and topiramate [TPM]) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for parallel and non-parallel dose-response relationship curves (DRRCs)."( Interactions of 1-methyl-1,2,3,4-tetrahydroisoquinoline with lamotrigine, oxcarbazepine, pregabalin, and topiramate in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis.
Antkiewicz-Michaluk, L; Czuczwar, SJ; Luszczki, JJ; Raszewski, G, 2010
)
0.36
" Pregabalin average daily dosage (SD) was 385."( Pregabalin for painful HIV neuropathy: a randomized, double-blind, placebo-controlled trial.
Clifford, DB; Durso-De Cruz, E; Emir, B; Freeman, R; Glue, P; Murphy, TK; Schifitto, G; Scott, GN; Simpson, DM; Whalen, E, 2010
)
0.36
" Pregabalin however, required a dosage adjustment in case of renal insufficiency."( [Therapeutic drug monitoring of pregabaline].
Bentué-Ferrer, D; Tribut, O; Verdier, MC,
)
0.13
" To further test the hypothesis that IL15 directly modulates GABA turnover by reuptake mechanisms, the dose-response relationship of IL15 on (3)H-GABA uptake was determined in two neuronal cell lines."( Interleukin-15 receptor is essential to facilitate GABA transmission and hippocampal-dependent memory.
Feng, J; Guo, X; He, Y; Hsuchou, H; Kastin, AJ; Khan, RS; Li, Z; Pan, W; Pistell, PJ; Wang, WH; Wu, X, 2010
)
0.36
" Time to achieve effective dosing is relatively quick and there is a range of dosing available."( Treatment of post-burn neuropathic pain: evaluation of pregablin.
Turner, L; Wong, L, 2010
)
0.36
" Patients with chronic kidney disease often receive inappropriately high gabapentin dosage for their kidney function, occasioning overt toxicity; advanced age and comorbidity predispose these patients for toxicity."( Gabapentin toxicity in patients with chronic kidney disease: a preventable cause of morbidity.
McKian, KP; Qian, Q; Zand, L, 2010
)
0.36
" Other gabapentin doses or dosing regimens warrant further study."( Clinical evaluation of perioperative administration of gabapentin as an adjunct for postoperative analgesia in dogs undergoing amputation of a forelimb.
Hellyer, PW; Mich, PM; Uhrig, SR; Wagner, AE, 2010
)
0.36
"To characterize the anticonvulsant effects of pregabalin (PGB - a third-generation antiepileptic drug) in combination with carbamazepine (CBZ - a classical antiepileptic drug) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for non-parallel dose-response relationship curves (DRRCs)."( Interaction of pregabalin with carbamazepine in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis for non-parallel dose-response relationship curves.
Luszczki, JJ, 2010
)
0.36
" We argue that contradictions to these patterns are the result of variations in (a) the location of drug infusion, (b) the dosage of the drug and/or (c) the time point of drug administration."( Behavioral and neural analysis of GABA in the acquisition, consolidation, reconsolidation, and extinction of fear memory.
Cranney, J; Makkar, SR; Zhang, SQ, 2010
)
0.36
"4%) with gabapentin at a dosage of 900 mg/d and in 9 patients (20."( Gabapentin in the treatment of hiccups in patients with advanced cancer: a 5-year experience.
Aielli, F; Aloisi, P; Ficorella, C; Galletti, B; Porzio, G; Verna, L, 2010
)
0.36
"This six-arm, double-blind, placebo-controlled, dose-response study randomized patients (N=137) with moderate-to-severe idiopathic RLS in an equal ratio to placebo or pregabalin 50, 100, 150, 300, or 450 mg/day."( A randomized, double-blind, 6-week, dose-ranging study of pregabalin in patients with restless legs syndrome.
Allen, R; Chen, C; García-Borreguero, D; Knapp, L; Miceli, J; Peterson, BT; Soaita, A; Wohlberg, C, 2010
)
0.36
" Pregabalin was safe and well tolerated across the entire dosing range."( A randomized, double-blind, 6-week, dose-ranging study of pregabalin in patients with restless legs syndrome.
Allen, R; Chen, C; García-Borreguero, D; Knapp, L; Miceli, J; Peterson, BT; Soaita, A; Wohlberg, C, 2010
)
0.36
"The objectives of the 3 phase I studies described herein were (1) to compare the pharmacokinetics of gabapentin delivered from a novel gastric-retentive dosage form vs an immediate-release formulation, (2) to assess the dose proportionality of the gastric-retentive extended-release formulation, and (3) to determine the effect of food on the pharmacokinetics of gabapentin delivered from this formulation."( Pharmacokinetics of gabapentin in a novel gastric-retentive extended-release formulation: comparison with an immediate-release formulation and effect of dose escalation and food.
Chen, C; Cowles, VE; Hou, E, 2011
)
0.37
" These findings indicate that preoperative use of gabapentin followed by postoperative dosing for two days did not significantly affect the postoperative pain, sleep, opioid consumption or patient-perceived quality of recovery for patients undergoing cardiac surgery."( Effect of gabapentin on pain after cardiac surgery: a randomised, double-blind, placebo-controlled trial.
Cornelissen, HR; Fraser, JF; Liessmann, CD; O'Connell, L; Rapchuk, IL, 2010
)
0.36
" Dropout is an important treatment failure endpoint, which can be analyzed using time-to-event models that incorporate daily dosing or other time-varying information."( Modeling dropout from adverse event data: impact of dosing regimens across pregabalin trials in the treatment of generalized anxiety disorder.
Frame, B; Hutmacher, M; Lalovic, B; Miller, R, 2011
)
0.37
" These results offer an explanation for the steep dose-response curve of GHB seen in vivo, and suggest potential target receptors for further investigation."( γ-Hydroxybutyrate and the GABAergic footprint: a metabolomic approach to unpicking the actions of GHB.
Balcar, VJ; Hanrahan, JR; Maher, AD; Nasrallah, FA; Rae, CD, 2010
)
0.36
", lamotrigine [LTG], oxcarbazepine [OXC] and topiramate [TPM]) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for non-parallel dose-response relationship curves (DRRCs)."( Additive interactions of pregabalin with lamotrigine, oxcarbazepine and topiramate in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis for non-parallel dose-response relationship curves.
Czuczwar, SJ; Filip, D; Luszczki, JJ, 2010
)
0.36
" The maximum response of the GABA dose-response curve decreased to 71."( Prokineticin 2 suppresses GABA-activated current in rat primary sensory neurons.
Gan, YB; Hu, WP; Li, XM; Liu, YQ; Qiu, F; Wang, BH; Wang, XJ; Wu, D; Xiong, YC, 2010
)
0.36
" The absolute bioavailability of gabapentin drops from 60% to 33% as the dosage increases from 900 to 3600 mg/day, while the absolute bioavailability of pregabalin remains at > or = 90% irrespective of the dosage."( A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin.
Bockbrader, HN; Burger, P; Chapel, S; Janiczek, N; Miller, R; Wesche, D, 2010
)
0.36
" After confirmation of the established allodynia, gabapentin at 10, 30, 60 and 100μg or clonidine at 5, 15, 30 and 50μg was injected as a monotherapy in conscious rats through the intrathecal catheter to obtain the dose-response curve of %MPE (maximum possible effect) of the antiallodynic effect and its ED(50)."( Intrathecal gabapentin and clonidine synergistically inhibit allodynia in spinal nerve-ligated rats.
Asada, A; Funao, T; Mori, T; Nishikawa, K; Yamama, Y, 2010
)
0.36
" Pregabalin dosage was increased from 150 to 600 mg/d during the first 4 weeks."( Pregabalin for the treatment of men with chronic prostatitis/chronic pelvic pain syndrome: a randomized controlled trial.
Alexander, RB; Anderson, RU; Cen, L; Chuai, S; Krieger, JN; Kusek, JW; Landis, JR; Litwin, MS; McNaughton-Collins, M; Nickel, JC; Nyberg, LM; O'Leary, M; Pontari, MA; Propert, KJ; Schaeffer, AJ; Shoskes, DA; White, PC; Zeitlin, S, 2010
)
0.36
" Dosing started at 20 mg/d and increased over 7 days to 40 mg/d."( An open-label tolerability study of BL-1020 antipsychotic: a novel gamma aminobutyric acid ester of perphenazine.
Anand, R; Dan, I; Geffen, Y; Vasile, D,
)
0.13
"A simple, fast, and sensitive HPLC method was developed and validated for the evaluation of pregabalin in a pharmaceutical dosage form using fluorescamine as a derivatization agent for the first time."( Rapid high-performance liquid chromatography method for determination of pregabalin in a pharmaceutical dosage form following derivatization with fluorescamine.
Grabnar, I; Martinc, B; Mrhar, A; Vovk, T,
)
0.13
"0009), except for the lowest dosage (150 mg/day) in the youngest age group."( Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 clinical studies.
Cheung, R; Emir, B; Murphy, TK; Semel, D; Zlateva, G, 2010
)
0.36
" Reassessment and modulation of dosing and/or medications occurred at 3- and 6-month intervals."( An open-label comparison of nabilone and gabapentin as adjuvant therapy or monotherapy in the management of neuropathic pain in patients with peripheral neuropathy.
Bestard, JA; Toth, CC,
)
0.13
" Linear regression analysis was used to evaluate a dose-response relationship between logarithms of pregabalin doses and their resultant maximum possible antinociceptive effects (MPAE) using the hot-plate test in mice."( Dose-response relationship analysis of pregabalin doses and their antinociceptive effects in hot-plate test in mice.
Łuszczki, JJ,
)
0.13
" The PWT in PSL mice was dose-dependently increased by intraperitoneal injection of gabapentin, but the anti-allodynic effects varied according to its dosing time."( Molecular basis for the dosing time-dependency of anti-allodynic effects of gabapentin in a mouse model of neuropathic pain.
Hamamura, K; Inoue, K; Koyanagi, S; Kusunose, N; Matsunaga, N; Ohdo, S; Tsuda, M; Uchida, T; Yoshida, M, 2010
)
0.36
"These findings suggest that the dosing time-dependent difference in the anti-allodynic effects of gabapentin is attributable to the circadian oscillation of α2δ-1 subunit expression in the DRG and indicate that the optimizing its dosing schedule helps to achieve rational pharmacotherapy for neuropathic pain."( Molecular basis for the dosing time-dependency of anti-allodynic effects of gabapentin in a mouse model of neuropathic pain.
Hamamura, K; Inoue, K; Koyanagi, S; Kusunose, N; Matsunaga, N; Ohdo, S; Tsuda, M; Uchida, T; Yoshida, M, 2010
)
0.36
"This pharmacostatistical model showed that: (1) pregabalin oral clearance (CL/F) was directly proportional to creatinine clearance (CLcr), but was independent of gender, race, age, female hormonal status, daily dose, and dosing regimen; (2) apparent volume of distribution was dependent on body weight and gender; (3) absorption rate was decreased when given with food; and (4) coadministration with marketed antiepileptic drugs (AEDs) had no significant effect on pregabalin CL/F."( Population pharmacokinetics of pregabalin in healthy subjects and patients with chronic pain or partial seizures.
Bockbrader, HN; Burger, P; Corrigan, BW; Knapp, L, 2011
)
0.37
" The most commonly used dosage was 450 mg/d."( [Lyrica (pregabalin) in the treatment of focal refractory epilepsy in adults].
Andreeva, OV; Iakunina, AV; Kalinin, VA; Vlasov, PN, 2010
)
0.36
" We also assessed the association between serious AEs and pregabalin, and investigated whether pregabalin AEs display a dose-response relationship."( The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials.
Gangemi, P; Perucca, P; Specchio, L; Zaccara, G, 2011
)
0.37
" We used relative risks (RRs) to assess the association of any [99% confidence intervals (CIs)] or serious AEs (95% CIs) with pregabalin, and risk differences (RDs, 95% CIs) to investigate dose-response relationships of pregabalin AEs."( The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials.
Gangemi, P; Perucca, P; Specchio, L; Zaccara, G, 2011
)
0.37
" There was a selective dose-response pattern in the onset of pregabalin AEs, with certain AEs appearing at lower doses than others."( The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials.
Gangemi, P; Perucca, P; Specchio, L; Zaccara, G, 2011
)
0.37
" Pregabalin AEs appear according to a selective dose-response pattern, possibly reflecting the severity of dysfunction of distinct anatomic structures."( The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials.
Gangemi, P; Perucca, P; Specchio, L; Zaccara, G, 2011
)
0.37
" There were no statistically significant differences found regarding sex, age or daily dosage between this latter group compared with the patients who registered for the study but did not fill in a questionnaire."( Intensive monitoring of pregabalin: results from an observational, Web-based, prospective cohort study in the Netherlands using patients as a source of information.
Härmark, L; Straus, S; van Grootheest, K; van Puijenbroek, E, 2011
)
0.37
" No comprehensive data exist regarding the optimal dosage of pregabalin on reducing postoperative pain and opioid consumption in spinal surgery."( Effective dose of peri-operative oral pregabalin as an adjunct to multimodal analgesic regimen in lumbar spinal fusion surgery.
Choi, YS; Kim, JC; Kim, KN; Kwak, YL; Lee, JY; Shim, JK, 2011
)
0.37
" In a long-term test, the antidepressant-like effect of MFP was better than that of GABA at the same dosage (2."( Antidepressant effect of GABA-rich monascus-fermented product on forced swimming rat model.
Chuang, CY; Lo, YH; Pan, TM; Shi, YC; You, HP, 2011
)
0.37
" A greater frequency reduction was observed in those patients who increased the dosage within the first month of therapy."( Efficacy and tolerability of pregabalin as preventive treatment for migraine: a 3-month follow-up study.
Ciuffoli, A; Pizzolato, R; Prosperini, L; Sette, G; Villani, V, 2011
)
0.37
" Trazodone, flexibly dosed (50-300 mg/day), was administered to 66 fibromyalgia patients during 12 weeks; 41 patients who completed the treatment accepted to receive pregabalin, also flexibly dosed (75-450 mg/day), added to trazodone treatment for an additional 12-week period."( Trazodone plus pregabalin combination in the treatment of fibromyalgia: a two-phase, 24-week, open-label uncontrolled study.
Calandre, EP; Molina-Barea, R; Morillas-Arques, P; Rico-Villademoros, F; Rodriguez-Lopez, CM, 2011
)
0.37
" A therapeutic strategy and optimal dosage of medications including gabapentin should be established for the treatment of SUNCT."( [Japanese SUNCT patient responsive to gabapentin].
Imai, K; Ito, Y; Kato, T; Nishida, S; Suzuki, J; Yasuda, T, 2011
)
0.37
" This study assessed the efficacy of GEn vs placebo and compared the pharmacokinetics of gabapentin after oral dosing of GEn or gabapentin in patients with PHN."( Efficacy of gabapentin enacarbil vs placebo in patients with postherpetic neuralgia and a pharmacokinetic comparison with oral gabapentin.
Backonja, MM; Canafax, DM; Cundy, KC, 2011
)
0.37
" Gabapentin was restarted at the original dosage and the symptoms resolved within 8 hours."( Akathisia induced by gabapentin withdrawal.
Hendriks, E; Hsiung, L; See, S, 2011
)
0.37
" The low pregabalin dosage and the short time to elevation of liver enzyme levels suggest an idiosyncratic reaction."( Pregabalin-induced hepatotoxicity.
Junyent, TT; Pellicer, MJ; Sendra, JM, 2011
)
0.37
"In 32 PHN patients being administered gabapentin, without changing the frequency of dosing, the drug was substituted with pregabalin at one-sixth dosage of gabapentin."( Replacement of gabapentin with pregabalin in postherpetic neuralgia therapy.
Hidaka, I; Ifuku, M; Inada, E; Iseki, M; Komatus, S; Morita, Y, 2011
)
0.37
"It was suggested that the analgesic action of pregabalin in PHN was six times that of gabapentin in terms of effectiveness in dosage conversion."( Replacement of gabapentin with pregabalin in postherpetic neuralgia therapy.
Hidaka, I; Ifuku, M; Inada, E; Iseki, M; Komatus, S; Morita, Y, 2011
)
0.37
" The results indicate that pretreatment with Parawixin 10 prevents the onset of seizures induced with kainic acid, N-methyl-D-aspartate, and pentylenetetrazole in a dose-response manner."( Neurobiological activity of Parawixin 10, a novel anticonvulsant compound isolated from Parawixia bistriata spider venom (Araneidae: Araneae).
Beleboni, RO; Coutinho-Netto, J; Cunha, AO; dos Santos, WF; Fachim, HA; Gobbo-Neto, L; Lopes, NP; Pereira, AC, 2011
)
0.37
"Pregabalin was increased to ≤600 mg/day during a 9-week dose optimization period with dosage maintained for 12 additional weeks."( An open-label, add-on study of pregabalin in patients with partial seizures: a multicenter trial in Greece.
Emir, B; Garganis, K; Giannakodimos, S; Gkiatas, K; Karageorgiou, K; Kazis, D; Kimiskidis, VK; Lyras, L; Papadimitriou, A; Papathanasopoulos, P; Plaitakis, A; Tsounis, S, 2011
)
0.37
"To examine medication dosing patterns of duloxetine and pregabalin among patients with fibromyalgia."( Medication dosing patterns associated with duloxetine and pregabalin among patients with fibromyalgia.
Sun, P; Watson, P; Zhao, Y; Zhao, Z, 2011
)
0.37
"Among patients with fibromyalgia, duloxetine and pregabalin initiators had different dosing patterns."( Medication dosing patterns associated with duloxetine and pregabalin among patients with fibromyalgia.
Sun, P; Watson, P; Zhao, Y; Zhao, Z, 2011
)
0.37
" The new drug combines generic gabapentin with a polymeric delivery system allowing for extended release and is licensed to be given only as a once-daily dosing regimen."( Extended-release gabapentin in post-herpetic neuralgia.
Farquhar-Smith, P; Thomas, B, 2011
)
0.37
"Although GpER has been approved by the FDA for once-daily use in PHN, there is a relative paucity of data for both its efficacy and the optimum dosing schedule (once or twice a day)."( Extended-release gabapentin in post-herpetic neuralgia.
Farquhar-Smith, P; Thomas, B, 2011
)
0.37
" This allows for once-daily dosing and less variability in serum levels."( Gabapentin enacarbil for the treatment of restless legs syndrome (RLS).
Burke, RA; Faulkner, MA, 2011
)
0.37
"Study limitations include a short timeframe and using data from different dosage schemes for GBP and PGB."( Economic evaluation of duloxetine as a first-line treatment for painful diabetic peripheral neuropathy in Mexico.
Carlos, F; Dueñas, H; Galindo-Suárez, RM; Ramírez-Gámez, J; Ramos, E, 2012
)
0.38
" The objective of the current study was to examine the dose-response relationship for treatment of GAD with pregabalin."( Pregabalin: dose-response relationship in generalized anxiety disorder.
Boschen, MJ, 2012
)
0.38
"The current study pools results from previous fixed-dose treatment trials of GAD with pregabalin and uses curve-fitting statistical procedures to generate curvilinear regression lines as a synthesis of previous dose-response information."( Pregabalin: dose-response relationship in generalized anxiety disorder.
Boschen, MJ, 2012
)
0.38
" The dosage was adjusted according to the level of pain control and side-effects."( Use of single- and multi-drug regimens in the management of classic (idiopathic) trigeminal neuralgia: an 11-year experience at a single Sri Lankan institution.
Ariyawardana, A; Pallegama, R; Ranasinghe, A; Sitheeque, M, 2012
)
0.38
" protocol XP066), to determine whether dosage adjustments are necessary in patients with renal impairment."( Clinical pharmacokinetics of gabapentin after administration of gabapentin enacarbil extended-release tablets in patients with varying degrees of renal function using data from an open-label, single-dose pharmacokinetic study.
Blumenthal, R; Chen, D; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J, 2012
)
0.38
"The data suggest that dosage adjustment for gabapentin enacarbil is necessary in patients with impaired renal function."( Clinical pharmacokinetics of gabapentin after administration of gabapentin enacarbil extended-release tablets in patients with varying degrees of renal function using data from an open-label, single-dose pharmacokinetic study.
Blumenthal, R; Chen, D; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J, 2012
)
0.38
"To review the pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, precautions, dosing recommendations, and patient counseling for gabapentin enacarbil for the treatment of restless legs syndrome (RLS) in adults."( Gabapentin enacarbil for treatment of restless legs syndrome in adults.
Farver, DK; Hayes, WJ; Lemon, MD, 2012
)
0.38
" They have been shown to help in reaching the desired effect when administered at drug-specific modes and at proven effective dosing throughout the perioperative period."( Non-opioid IV adjuvants in the perioperative period: pharmacological and clinical aspects of ketamine and gabapentinoids.
Weinbroum, AA, 2012
)
0.38
"To compare medication dosing patterns of duloxetine and pregabalin among patients with diabetic peripheral neuropathic pain (DPNP)."( Dosing pattern comparison between duloxetine and pregabalin among patients with diabetic peripheral neuropathic pain.
Bernauer, M; Sun, P; Watson, P; Zhao, Y; Zhao, Z, 2012
)
0.38
" healthcare claims database, we examined the dosing patterns of duloxetine and pregabalin among commercially insured patients with DPNP aged 18 to 64 who initiated (a 90-day medication gap) duloxetine or pregabalin therapy in 2006."( Dosing pattern comparison between duloxetine and pregabalin among patients with diabetic peripheral neuropathic pain.
Bernauer, M; Sun, P; Watson, P; Zhao, Y; Zhao, Z, 2012
)
0.38
"The commercially insured patients with DPNP who initiated duloxetine or pregabalin therapy had different dosing patterns."( Dosing pattern comparison between duloxetine and pregabalin among patients with diabetic peripheral neuropathic pain.
Bernauer, M; Sun, P; Watson, P; Zhao, Y; Zhao, Z, 2012
)
0.38
" These results suggest this dosing regimen of gabapentin is not efficacious in improving outcomes in patients undergoing shoulder arthroscopy under general anesthesia with an interscalene block."( Perioperative administration of gabapentin for shoulder arthroscopy: a prospective, randomized, double-blind, placebo-controlled study.
Bowen, K; Goff, J; Maye, J; Mohan, E; Osborne, L; Spence, D, 2011
)
0.37
" Sixty-nine healthy subjects (21-30 years) underwent a laboratory-based within-session cumulative oral alcohol dosing procedure, achieving a mean peak blood alcohol level of 100."( GABRA2 markers moderate the subjective effects of alcohol.
Guo, X; Kranzler, HR; Li, N; McCaul, ME; Uhart, M; Wand, GS; Weerts, EM; Yan, X, 2013
)
0.39
" In APP/PS1 mice, a murine model of AD, at 8 months of age the cerebellum is devoid of fibrillar Aβ, but dosage of soluble Aβ(1-42), the form which is more prone to aggregation, showed higher levels in this structure than in the forebrain."( Excitability and synaptic alterations in the cerebellum of APP/PS1 mice.
Boda, E; Hoxha, E; Montarolo, F; Parolisi, R; Tempia, F, 2012
)
0.38
" Study treatments were dosed incrementally over a three week period, to reach daily doses of 150 mg venlafaxine and 200mg pregabalin by the CO(2) challenge test day."( Evaluation of the effects of venlafaxine and pregabalin on the carbon dioxide inhalation models of Generalised Anxiety Disorder and panic.
Bailey, JE; Craig, K; Dawson, GR; Diaper, A; Dourish, CT; Nutt, DJ; Osman-Hicks, V; Rich, AS, 2013
)
0.39
"Available evidence suggests that monotherapy with pregabalin, within the dosage range of 150 - 600 mg/d, is a promising "novel" option for the safe and efficacious relapse prevention of both AD and BD."( Efficacy and safety of pregabalin in the treatment of alcohol and benzodiazepine dependence.
Konstantakopoulos, G; Oulis, P, 2012
)
0.38
" After confirming hyperalgesia, pregabalin or saline (for control mice) in a volume of 10 mL/kg was administered orally at a dosage of 30 mg/kg, twice daily from day 2 after surgery."( The immunomodulatory effect of pregabalin on spleen cells in neuropathic mice.
Jang, Y; Jeong, DC; Song, HK; Yeom, MY, 2012
)
0.38
" The objective of this paper is to report the steady-state pharmacokinetics and safety of gabapentin with different dosing regimens of gabapentin-ER in postmenopausal women with hot flashes."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
" C(max) generally increased with increasing dose as did C(min) and C(avg) for the various treatments in a manner that was consistent with the dosing regimen."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
"The pharmacokinetic profile of gabapentin-ER may allow for once- or twice-daily dosing while maintaining bioavailability and thus efficacy."( Steady-state pharmacokinetics of gabapentin after administration of a novel gastroretentive extended-release formulation in postmenopausal women with vasomotor symptoms.
Cowles, VE; Gordi, T; Hou, SY, 2012
)
0.38
" The gastroretentive once-daily formulation of gabapentin (G-GR) allows for less frequent dosing while maintaining efficacy and may also reduce adverse events (AEs) associated with high plasma concentration of gabapentin occurring during the waking hours."( Clinical development of a once-daily gastroretentive formulation of gabapentin for treatment of postherpetic neuralgia: an overview.
Argoff, CE; Chen, C; Cowles, VE, 2012
)
0.38
" The GR technology used in G-GR resulted in a decreased dosing frequency from three times per day for the IR product to once daily in the treatment of PHN, while maintaining the same efficacy with an apparent reduced incidence of AEs common to G-IR therapy."( Clinical development of a once-daily gastroretentive formulation of gabapentin for treatment of postherpetic neuralgia: an overview.
Argoff, CE; Chen, C; Cowles, VE, 2012
)
0.38
"Linear regression analysis was used to evaluate the dose-response relationships between logarithms of drug doses and their resultant maximum possible antinociceptive effects in the mouse hot-plate test."( Synergistic interaction of pregabalin with the synthetic cannabinoid WIN 55,212-2 mesylate in the hot-plate test in mice: an isobolographic analysis.
Florek-Łuszczki, M; Luszczki, JJ, 2012
)
0.38
" The AEs reported most frequently were somnolence and dizziness; there was a dose-response relationship to these AEs."( Dose response of Gabapentin Enacarbil versus placebo in subjects with moderate-to-severe primary restless legs syndrome: an integrated analysis of three 12-week studies.
Barrett, RW; Kavanagh, ST; VanMeter, SA; Warren, S, 2012
)
0.38
" Once-daily dosing has been shown to provide comparable drug exposure with an identical daily dose of the immediate-release formulation when administered three times daily."( Gabapentin for once-daily treatment of post-herpetic neuralgia: a review.
Beal, B; Moeller-Bertram, T; Schilling, JM; Wallace, MS, 2012
)
0.38
" This review focuses on the ADME properties of gabapentin and illustrates how GR delivery enhances its absorption compared with IR formulations and allows once-daily dosing with the evening meal for the treatment of PHN."( The intestinal absorption mechanism of gabapentin makes it appropriate for gastroretentive delivery.
Chen, C; Cowles, VE; Sweeney, M, 2013
)
0.39
"For full compatibility groups (age, ASA status and anthropometric data, equal operation duration and the equipotential drug dosage adjustment is revealed, that in group of propofol-fentanyl TIVA in the early postoperative period in school age children postoperative cognitive dysfunction (POCD) is developing, which in case of absence of the corresponding correction is maintained after 1 month after operation (at least) in 80% of cases."( [Correction of early cognitive disorders in school-age children operated under total intravenous anaesthesia].
Gus'kov, IE; Lobov, MA; Lugovoĭ, AV; Miatchin, PS; Ovezov, AM; Panteleeva, MV,
)
0.13
"The objective of this modeling study was to assess different dosage regimens that might be used to guide clinicians in transitioning patients from gabapentin to pregabalin therapy when such a transition is clinically warranted."( Gabapentin to pregabalin therapy transition: a pharmacokinetic simulation.
Bockbrader, HN; Budhwani, MN; Wesche, DL, 2013
)
0.39
" Based on initial dose-response experiment, DBAN (60 mg/kg) was administrated orally for 7 days."( Potential protective effect of taurine against dibromoacetonitrile-induced neurotoxicity in rats.
El-Sayeh, BM; Salem, HA; Sayed, RH, 2012
)
0.38
" Urine was collected from three male Wistar rats for 24 h after dosing with (14)C-labelled lesogaberan (170 mg/kg, 10 MBq/kg); plasma samples were taken 2 and 24 h after dosing."( Identification of the metabolites of lesogaberan using linear trap quadrupole orbitrap mass spectrometry and hydrophilic interaction liquid chromatography.
Aurell-Holmberg, A; Castagnoli, N; Ekdahl, A, 2013
)
0.39
" Drug dosage was determined by initial VAS (visual analog scale) scores."( A four arm, double blind, randomized and placebo controlled study of pregabalin in the management of post-burn pruritus.
Ahuja, RB; Gupta, GK, 2013
)
0.39
" The effective doses, for 20%, 50%, and 80% response (ED(20), ED(50), and ED(80), respectively), of each drug were calculated using least squares linear regression analysis, and then dose-response curves were compared."( Relative potency of pregabalin, gabapentin, and morphine in a mouse model of visceral pain.
Keyhanfar, F; Shamsi Meymandi, M, 2013
)
0.39
" No difference was observed between slopes of dose-response curves."( Relative potency of pregabalin, gabapentin, and morphine in a mouse model of visceral pain.
Keyhanfar, F; Shamsi Meymandi, M, 2013
)
0.39
"In this animal model of visceral pain, all three drugs exhibited parallel dose-response curves."( Relative potency of pregabalin, gabapentin, and morphine in a mouse model of visceral pain.
Keyhanfar, F; Shamsi Meymandi, M, 2013
)
0.39
"Pregabalin, within a dosage of 150-450 mg/day, showed beneficial effects for alcohol relapse prevention and contrasting results for the treatment of the withdrawal syndrome."( Pregabalin for alcohol dependence: a critical review of the literature.
Clerici, M; Guglielmo, R; Janiri, L; Martinotti, G, 2012
)
0.38
"PHN pain reduction after G-GR treatment can be observed as early as the second day of dosing and continues for at least 10 weeks."( Once-daily gastroretentive gabapentin for postherpetic neuralgia: integrated efficacy, time to onset of pain relief and safety analyses of data from two phase 3, multicenter, randomized, double-blind, placebo-controlled studies.
Irving, GA; Rauck, RL; Sweeney, M; Vanhove, GF; Wallace, MS, 2013
)
0.39
" It has also been reported that pregabalin used with oxycodine reveals analgesic effect with smaller dosage than pregabalin alone."( [Case of acute exacerbation of neuropathic cancer pain rapidly relieved by simultaneous oral intake of immediate release oxycodone and pregabalin].
Baba, M; Gomwo, I, 2012
)
0.38
" This study examines dosing patterns, therapy outcomes, healthcare utilization and costs of patients with PHN who initiate treatment with gabapentin or pregabalin."( Real-world treatment of post-herpetic neuralgia with gabapentin or pregabalin.
Becker, L; Halpern, R; Johnson, P; Sweeney, M, 2013
)
0.39
" The mean daily dosage was 826 mg for gabapentin and 187 mg for pregabalin."( Real-world treatment of post-herpetic neuralgia with gabapentin or pregabalin.
Becker, L; Halpern, R; Johnson, P; Sweeney, M, 2013
)
0.39
" Suboptimal dosing and discontinuation may be associated with supplementary use of other analgesics, especially opioids."( Real-world treatment of post-herpetic neuralgia with gabapentin or pregabalin.
Becker, L; Halpern, R; Johnson, P; Sweeney, M, 2013
)
0.39
" Three dosage levels (1, 2 and 4 mg/kg body weight) and non-administration were tested by an increase and decrease method."( Calming effect of orally administered γ-aminobutyric acid in Shih Tzu dogs.
Goto, A; Okumoto, A; Tanaka, T; Tani, N; Uetake, K, 2012
)
0.38
" Mean PGB dosage was 279 mg/day."( Effect of pregabalin add-on treatment on seizure control, quality of life, and anxiety in patients with brain tumour-related epilepsy: a pilot study.
Carapella, CM; Dinapoli, L; Fabi, A; Maschio, M; Pace, A; Pompili, A; Sperati, F; Vidiri, A, 2012
)
0.38
"Mean pre-withdrawal pregabalin dosage was 386 mg/day, decreasing to 70 mg/day at mean lowest dosage."( Spasticity increases during pregabalin withdrawal.
Baguley, IJ; Braid, JJ; Kirker, SG, 2013
)
0.39
" Mean daily PRG dosage was 1424 mg."( Pregabalin abuse and dependence in Germany: results from a database query.
Freudenmann, RW; Gahr, M; Hiemke, C; Kölle, MA; Schönfeldt-Lecuona, C, 2013
)
0.39
" Analyses were performed on safety data from patients who received G-GR for 10 weeks in the randomized controlled study and who then received an additional 14 weeks of G-GR, asymmetrically dosed in the current study."( Long-term safety of gastroretentive gabapentin in postherpetic neuralgia patients.
Irving, G; Jensen, MP; Rauck, R; Sweeney, M; Vanhove, GF; Wallace, M, 2013
)
0.39
" The effective dosing regimen of gabapentin IR (G-IR) for PHN is 1800 mg/day in three divided doses."( Pharmacokinetics, efficacy, and tolerability of a once-daily gastroretentive dosage form of gabapentin for the treatment of postherpetic neuralgia.
Chen, C; Cowles, VE; Han, CH; Sweeney, M, 2013
)
0.39
" The results also demonstrate the presence of interactions between allosteric activators and potentiators, raising a possibility of effects on dosage requirements or changes in side effects."( The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists.
Akk, G; Eaton, MM; Li, P; Steinbach, JH, 2013
)
0.39
"67 days of study drug, with eight patients receiving a dosage of 300 mg thrice daily (TID), 24 receiving 600 mg TID, 14 receiving 800 mg TID, and seven receiving 1200 mg TID."( Gabapentin is ineffective as an analgesic adjunct in the immediate postburn period.
Eid, A; Heard, J; Horsfield, A; Kealey, P; Kral, L; Liao, J; Rosenquist, R; Wibbenmeyer, L,
)
0.13
" In the further course, she increased the daily PRG dosage and consulted other physicians to receive additional PRG prescriptions."( Concerns about pregabalin: further experience with its potential of causing addictive behaviors.
Franke, B; Freudenmann, RW; Gahr, M; Kölle, MA; Schönfeldt-Lecuona, C,
)
0.13
"To demonstrate the premise of individualized dosing charts (IDCs) as a clinical-bedside decision-support tool to individualize dosage regimens for drugs in which the interpatient variability is controlled by the pharmacokinetic (PK) behavior of the patient, to calculate the optimal sampling schedule (OSS), which minimizes the number of blood samples per patient."( Validation of a novel approach for dose individualization in pharmacotherapy using gabapentin in a proof of principles study.
Anaissie, EJ; Blau, GE; Fausel, C; Laínez, JM; Orcun, S; Reklaitis, GV; Suvannasankha, A, 2013
)
0.39
" The dose amount and dosing interval must be adjusted to maximize the probability of staying within the target concentration range."( Validation of a novel approach for dose individualization in pharmacotherapy using gabapentin in a proof of principles study.
Anaissie, EJ; Blau, GE; Fausel, C; Laínez, JM; Orcun, S; Reklaitis, GV; Suvannasankha, A, 2013
)
0.39
"IDCs display the risk of a patient violating the target concentration range for any dosage regimen."( Validation of a novel approach for dose individualization in pharmacotherapy using gabapentin in a proof of principles study.
Anaissie, EJ; Blau, GE; Fausel, C; Laínez, JM; Orcun, S; Reklaitis, GV; Suvannasankha, A, 2013
)
0.39
"A dosage of 600 mg of gabapentin plus 4 mg of dexamethasone significantly reduced the 24-hour incidence of nausea and PONV."( The effect of gabapentin premedication on postoperative nausea, vomiting, and pain in patients on preoperative dexamethasone undergoing craniotomy for intracranial tumors.
Misra, S; Parthasarathi, G; Vilanilam, GC, 2013
)
0.39
" In contrast to previous publications where exorbitant high concentrations were used, the effects of lavender oil in behavioral, biochemical, and electrophysiological experiments were investigated in physiological concentrations in the nanomolar range, which correlate to a single dosage of 80 mg/d in humans that was used in clinical trials."( Lavender oil-potent anxiolytic properties via modulating voltage dependent calcium channels.
Klugbauer, N; Leuner, K; Müller, WE; Nöldner, M; Schuwald, AM; Wilmes, T, 2013
)
0.39
" Pathology did not indicate a difference in occurrence and types of lesions between control and dosed birds."( Methylmercury egg injections: part 2--pathology, neurochemistry, and behavior in the avian embryo and hatchling.
Basu, N; Bradley, M; Mittal, K; Rutkiewicz, J, 2013
)
0.39
" Range of dosage may fluctuate considerably, from 75 mg to 600 mg per day."( The potential of pregabalin in neurology, psychiatry and addiction: a qualitative overview.
Aguglia, E; Cavuto, M; De Berardis, D; Di Giannantonio, M; Iasevoli, F; Lupi, M; Martinotti, G; Salone, A; Santacroce, R; Sarchione, F; Serroni, N; Signorelli, M; Valchera, A, 2013
)
0.39
" We also summarised data on adverse events from all single dosage studies and calculated risk differences (RDs) and numbers needed to harm (NNHs)."( Gabapentin or pregabalin for the prophylaxis of episodic migraine in adults.
Chronicle, EP; Linde, M; McCrory, DC; Mulleners, WM, 2013
)
0.39
" One trial of gabapentin enacarbil (523 participants) failed to demonstrate a significant difference versus placebo or between doses for gabapentin enacarbil titrated to between 1200 mg and 3000 mg with regard to proportion of responders; there was also no evidence of a dose-response trend."( Gabapentin or pregabalin for the prophylaxis of episodic migraine in adults.
Chronicle, EP; Linde, M; McCrory, DC; Mulleners, WM, 2013
)
0.39
"At a simulated intragastric dosage of approximately 4 mg/kg every 8 hours, median pregabalin steady-state plasma concentration in healthy horses was within the therapeutic range reported for humans."( Pharmacokinetics of single-dose intragastric and intravenous pregabalin administration in clinically normal horses.
Divers, TJ; Mullen, KR; Schwark, W, 2013
)
0.39
" Multiple dosing regimens may be beneficial in reducing acute and chronic pain; however, more robust randomized control studies are needed."( Is there a role for gabapentin in preventing or treating pain following thoracic surgery?
Frazer, S; Hunt, I; Zakkar, M, 2013
)
0.39
" The medicine dosage will be titrated up to the participant's optimal dose, to a maximum 600 mg per day."( PRECISE - pregabalin in addition to usual care for sciatica: study protocol for a randomised controlled trial.
Billot, L; Day, RO; Hancock, MJ; Harris, I; Jan, S; Koes, BW; Latimer, J; Lin, CW; Maher, CG; Mathieson, S; McLachlan, AJ; Pik, J, 2013
)
0.39
" Several derivatization methods have been developed and used for their determination in bulk or pharmaceutical dosage forms."( A simple high-throughput method for determination of antiepileptic analogues of γ-aminobutyric acid in pharmaceutical dosage forms using microplate fluorescence reader.
Martinc, B; Vovk, T, 2013
)
0.39
" We estimated summary risk ratios for each outcome and evaluated dose-response in regression models."( Gabapentin add-on for drug-resistant partial epilepsy.
Al-Bachari, S; Hutton, JL; Marson, AG; Pulman, J, 2013
)
0.39
" When NBI was administered prior to dosing with carb, the increase in DA, decrease in GABA, and biphasic effect on GLu was similar to that seen after dosing with carb only."( S-(N, N-diethylcarbamoyl)glutathione (carbamathione), a disulfiram metabolite and its effect on nucleus accumbens and prefrontal cortex dopamine, GABA, and glutamate: a microdialysis study.
Faiman, MD; Kaul, S; Latif, SA; Lunte, CE; Williams, TD, 2013
)
0.39
" A dose-response curve was established for pregabalin at a fixed morphine dose and revealed that, at low doses, pregabalin dose-dependently enhanced the antinociceptive effects, while the opposite was true at high doses (17 and 25 mg/kg)."( Assessment of the antinociceptive effects of pregabalin alone or in combination with morphine during acetic acid-induced writhing in mice.
Keyhanfar, F; Shamsi Meymandi, M, 2013
)
0.39
" The aim of this study was to evaluate the cardiovascular (CV) effects of 3 weeks of dosing with venlafaxine, pregabalin and placebo on young healthy adults."( Changes in cardiovascular function after venlafaxine but not pregabalin in healthy volunteers: a double-blind, placebo-controlled study of orthostatic challenge, blood pressure and heart rate.
Bailey, JE; Craig, K; Dawson, GR; Diaper, A; Dourish, CT; Nutt, DJ; Rich, AS; Wilson, SJ, 2013
)
0.39
"To compare the efficacy, discontinuation rates, and safety of once nightly versus twice daily dosing of pregabalin in a community-based trial."( Twice daily versus once nightly dosing of pregabalin for fibromyalgia: a double-blind randomized clinical trial of efficacy and safety.
Kivitz, AJ; Maricic, MJ; Nasser, K; Silver, DS; Silverman, SL, 2014
)
0.4
"While a nightly dosing schedule of pregabalin has been used by clinicians hoping to improve treatment, this study showed no significant difference (either beneficial or detrimental) between either treatment option."( Twice daily versus once nightly dosing of pregabalin for fibromyalgia: a double-blind randomized clinical trial of efficacy and safety.
Kivitz, AJ; Maricic, MJ; Nasser, K; Silver, DS; Silverman, SL, 2014
)
0.4
" Advantage was taken of this to screen for genetic modifiers; Adar overexpression lethality is rescued by reduced dosage of the Rdl (Resistant to dieldrin), gene encoding a subunit of inhibitory GABA receptors."( The ADAR RNA editing enzyme controls neuronal excitability in Drosophila melanogaster.
Baines, RA; Keegan, LP; Li, X; O'Connell, MA; Overton, IM, 2014
)
0.4
" GABA dose-response curves of cells co-expressing WT subunits with their respective L9'S mutants exhibited multiple components, with the number of discernible components enabling a subunit stoichiometry of 2α, 2β and 1δ to be deduced for α4β3δ receptors."( Stoichiometry of δ subunit containing GABA(A) receptors.
Mortensen, M; Patel, B; Smart, TG, 2014
)
0.4
" Dosing was set by the Dixon sequential up-down method; that is, a greater or less than 30% reduction in capsaicin pain decreased or increased the dose, respectively, by a fixed interval for the next subject."( Determination of the effective dose of pregabalin on human experimental pain using the sequential up-down method.
Wallace, MS; Wong, W, 2014
)
0.4
"Mean median daily dosage over 6 months was 53."( Effectiveness of duloxetine compared with pregabalin and gabapentin in diabetic peripheral neuropathic pain: results from a German observational study.
Birklein, F; Boess, FG; Happich, M; Schacht, A; Schneider, E; Wilhelm, S; Ziegler, D, 2014
)
0.4
" Here we describe a patient who displayed perverted head-shaking and positional downbeat nystagmus after prescription of a high dosage of pregabalin."( Perverted head-shaking and positional downbeat nystagmus in pregabalin intoxication.
Choi, JY; Jung, JM; Kim, SU; Kwon, DY; Park, YM; Woo, YS, 2014
)
0.4
" The extent of liver damage at different dosage and long term treatment with GPN is not yet clear."( Chronic effect of gabapentin on liver function in adult male rats.
Abdollahi, A; Meshkibaf, MH; Miladpoor, B; Shole Var, F, 2013
)
0.39
"Women in the study group received 75 mg pregabalin 2 hours before surgery and then every 12 hours for 2 doses, and women in the control group received an identical capsule and the same dosage of placebo."( A randomized, double-blind, placebo-controlled trial of oral pregabalin for relief of shoulder pain after laparoscopic gynecologic surgery.
Charuluxananan, S; Nutthachote, P; Sirayapiwat, P; Wisawasukmongchol, W,
)
0.13
" Time-course data for the dose-response effects were analyzed using two-way analysis of variance and the posthoc Tukey-Kramer multiple-comparison test."( Antinociceptive effects of mirtazapine, pregabalin, and gabapentin after chronic constriction injury of the infraorbital nerve in rats.
Hashimoto, R; Hosokawa, K; Mashimo, T; Nakae, A; Nakai, K, 2014
)
0.4
" Dosage and side effects were recorded at each visit."( Long-term efficacy of OROS® hydromorphone combined with pregabalin for chronic non-cancer neuropathic pain.
Casali, M; Dauri, M; Lazzari, M; Sabato, AF; Sabato, E; Tufaro, G, 2014
)
0.4
" A dose-response analysis suggested increasing effect with increasing dose."( Pregabalin add-on for drug-resistant partial epilepsy.
Hemming, K; Marson, AG; Pulman, J, 2014
)
0.4
" We tested phenotypic homogeneity and gene dosage effects in the mouse null alleles muted (Bloc1s5(mu/mu)) and dysbindin (Bloc1s8(sdy/sdy))."( Mutations in the BLOC-1 subunits dysbindin and muted generate divergent and dosage-dependent phenotypes.
Faundez, V; Gokhale, A; Larimore, J; Mullin, AP; Singleton, KS; Talbot, K; Tang, J; Tornieri, K; Zlatic, SA, 2014
)
0.4
" The starting dosage of pregabalin was 75 mg/day and was increased up to as much as 300 mg/day, depending on the individual patient's condition, while tapering off hypnotics."( Effects of pregabalin in patients with hypnotic-dependent insomnia.
Cho, YW; Song, ML, 2014
)
0.4
" However, cost-analysis is only part of the equation when treating chronic pain patients and undervalues the relationships of enhanced compliance due to single-daily dosing and stable and reliable pharmacokinetics associated with extended-duration preparations using either retentive technologies or delayed absorption strategies."( Can Chronic Pain Patients Be Adequately Treated Using Generic Pain Medications to the Exclusion of Brand-Name Ones?
Anantamongkol, U; Candido, KD; Chiweshe, J; Knezevic, NN,
)
0.13
"4 mg/kg) produced a downward shift in the cocaine dose-response curve under a fixed ratio schedule of reinforcement and decreased the cocaine breaking point."( On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats.
Filip, M; Fuxe, K; Gołembiowska, K; Kamińska, K; Suder, A; Wydra, K, 2015
)
0.42
" After surgical treatment, sham and ischemic hypoxia group were treat with normal saline; conventional treatment group was received TPM solution 100 mg/kg, 2 times/d; degradation therapy group received TPM solution 150 mg/kg, 2 times/d, per 3 d treatment each dosage was reduced 50 mg/kg, the lowest reduced to 50 mg/kg."( Protective effect of topiramate on hypoxic-ischemic brain injury in neonatal rat.
Jiang, H; Lei, JJ; Zhang, YH, 2014
)
0.4
" All patients were titrated to 1800 mg G-GR/d over 2 weeks and maintained at that dosage for 6 weeks, for 8 weeks total treatment."( Real-world experience with once-daily gabapentin for the treatment of postherpetic neuralgia (PHN).
Dunteman, ED; Kareht, S; Markley, HG; Sweeney, M, 2015
)
0.42
" Once daily (QD) dosing may be appropriate for ease of clinical use and patient convenience."( Pregabalin controlled-release pharmacokinetics in healthy volunteers: analysis of four multiple-dose randomized clinical pharmacology studies.
Alebic-Kolbah, T; Alvey, CW; Bockbrader, HN; Chew, ML; Pitman, VW; Plotka, A; Scavone, JM, 2014
)
0.4
" It may be related with using a similar dosage of dopaminergic drugs."( Augmentation in restless legs syndrome patients in Korea.
Cho, YW; Jeon, JY; Lee, HB; Moon, HJ; Song, ML, 2015
)
0.42
" There were no significant differences in acute pain outcomes with pregabalin 100-300 mg between single preoperative dosing regimens and those including additional doses repeated after surgery."( Impact of pregabalin on acute and persistent postoperative pain: a systematic review and meta-analysis.
Habib, AS; Mishriky, BM; Waldron, NH, 2015
)
0.42
" We compared dosing and side effects in 34 CKD/ESKD patients with similar patients receiving HD (n = 15)."( Efficacy and safety of gabapentin for uremic pruritus and restless legs syndrome in conservatively managed patients with chronic kidney disease.
Brennan, F; Brown, MA; Cheikh Hassan, HI; Collett, G; Josland, EA, 2015
)
0.42
" We conclude that endogenous N/OFQ functionally opposes DOP transmission in substantia nigra reticulata and that NOP receptor antagonists might be used in combination with DOP receptor agonists to reduce their dosage while maintaining their full therapeutic efficacy."( Stimulation of δ opioid receptor and blockade of nociceptin/orphanin FQ receptor synergistically attenuate parkinsonism.
Ledonne, A; Mabrouk, OS; Mercuri, N; Morari, M; Viaro, R; Volta, M, 2014
)
0.4
" The result showed that: visual analogue scale (VAS) and quality of sleep (QS) of three groups of patients after treatment all decreased obviously; group A had slow work, large amount of dosage and many adverse effects; group B had quick work, but the improvement on pain and sleep was not satisfactory; the curative effect of group C was higher than group A and B (p<0."( Curative effect research on curing intercostal neuralgia through paravertebral nerve block combined with pregabalin.
Wu, X; Xiao, P; Zhu, X, 2014
)
0.4
" GBP dosing was rapidly escalated within days of SAH up to a median of 1,200 mg/day, with a range of 300 mg three times a day to 900 mg three times a day."( Safety and tolerability of gabapentin for aneurysmal subarachnoid hemorrhage (sah) headache and meningismus.
Dhakal, LP; Freeman, WD; Hodge, DO; Mayes, M; Nagal, J; Nagel, J; Ng, LK; Richie, A, 2015
)
0.42
" Systemic nicotine given before the sample phase of the CMOR task reversed the ketamine-induced impairment, but this effect was blocked by co-administration of the GABAA receptor antagonist bicuculline at a dosage that itself did not cause impairment."( α₄β₂ Nicotinic receptor stimulation of the GABAergic system within the orbitofrontal cortex ameliorates the severe crossmodal object recognition impairment in ketamine-treated rats: implications for cognitive dysfunction in schizophrenia.
Cloke, JM; Winters, BD, 2015
)
0.42
" Indeed, we and others have previously reported that treatment of adolescent rats with olanzapine (OLA; a widely prescribed AAPD) on postnatal days 28-49, under dosing conditions that approximate those employed therapeutically in humans, causes long-term behavioral and neurobiological perturbations."( Olanzapine antipsychotic treatment of adolescent rats causes long term changes in glutamate and GABA levels in the nucleus accumbens.
Frost, DO; Gullapalli, RP; Xu, S, 2015
)
0.42
" We compared the overall rate of CSEs and intolerable CSEs (ICSEs-CSEs that led to dosage reduction or discontinuation) between different AEDs in both monotherapy and polytherapy."( Cosmetic side effects of antiepileptic drugs in adults with epilepsy.
Buchsbaum, R; Chen, B; Choi, H; Detyniecki, K; Hirsch, LJ; Javed, A; Kato, K; Legge, A; Moeller, J, 2015
)
0.42
" Cosmetic side effects leading to dosage change or discontinuation occurred most frequently with pregabalin and valproic acid compared with all other AEDs (13."( Cosmetic side effects of antiepileptic drugs in adults with epilepsy.
Buchsbaum, R; Chen, B; Choi, H; Detyniecki, K; Hirsch, LJ; Javed, A; Kato, K; Legge, A; Moeller, J, 2015
)
0.42
"Weight gain and alopecia were the most common patient-reported CSEs in this study, and weight gain was the most likely cosmetic side effect to result in dosage adjustment or medication discontinuation."( Cosmetic side effects of antiepileptic drugs in adults with epilepsy.
Buchsbaum, R; Chen, B; Choi, H; Detyniecki, K; Hirsch, LJ; Javed, A; Kato, K; Legge, A; Moeller, J, 2015
)
0.42
" Participants were dosed with gabapentin alone (n = 39), zolpidem tartrate alone (n = 38), and the combination (gabapentin + zolpidem) (n = 38) over three treatment periods, which were separated by ≥7 days."( Pharmacokinetic effects of simultaneous administration of single-dose gabapentin 500 mg and zolpidem tartrate 10 mg in healthy volunteers: a randomized, open-label, crossover trial.
Furey, SA; Galitz, LA; Jayawardena, S, 2015
)
0.42
" Before dosing and at 30, 60, 120, 240 min, general behaviors within 5 min were recorded."( [Mechanism of Bailemian capsules in the treatment of insomnia in mice].
Bian, Y; Tang, X, 2014
)
0.4
" Dosing information can guide treatment trials and future prospective studies."( Gabapentin for management of recurrent pain in 22 nonverbal children with severe neurological impairment: a retrospective analysis.
Hauer, JM; Solodiuk, JC, 2015
)
0.42
" Patients of the first group received adaptol in dosage 1000 mg daily and patients of the second group received noofen in dosage 500 mg daily."( [Asthenic disorders in children and their differentiated treatment].
Anisimova, TI; Bondarchuk, IL; Chutko, LS; Iakovenko, EA; Nikishena, IS; Sergeev, AV; Surushkina, SI, 2014
)
0.4
" Effects of orally dosed standard analgesics on CRANE were examined 48 h following bilateral CFA injection."( Complete Freund's adjuvant-induced reduction of exploratory activity in a novel environment as an objective nociceptive endpoint for sub-acute inflammatory pain model in rats.
Bannon, AW; Joshi, SK; Zhu, CZ, 2015
)
0.42
" The physician must determine the best dosing strategy, consider the use of combination therapy, and decide how best to treat patients who have responded poorly to other treatment options in the past."( Pregabalin for painful diabetic peripheral neuropathy: strategies for dosing, monotherapy vs. combination therapy, treatment-refractory patients, and adverse events.
Juhn, MS; Parsons, B; Sadosky, A; Varvara, R, 2015
)
0.42
" A discussion of pregabalin dosing and adverse events is also presented."( Pregabalin for painful diabetic peripheral neuropathy: strategies for dosing, monotherapy vs. combination therapy, treatment-refractory patients, and adverse events.
Juhn, MS; Parsons, B; Sadosky, A; Varvara, R, 2015
)
0.42
" GBP has a favorable adverse effect profile in therapeutic dosing with the most common reported effects being dizziness, fatigue, drowsiness, weight gain, and peripheral edema."( An acute gabapentin fatality: a case report with postmortem concentrations.
Cantrell, FL; Gary, RD; McIntyre, IM; Mena, O, 2015
)
0.42
" Compounded dosage forms of gabapentin are commonly used for pain management, however, the penetration and efficacy of gabapentin in these compounded topical formulations has not been fully studied."( Skin permeation and antinociception of topical gabapentin formulations.
Asbill, S; Bryson, E; Sweitzer, S,
)
0.13
" The intensity of tactile allodynia in STZ-induced diabetic mice was alleviated by the oral administration of PGN; however, the antiallodynic effect varied according to its dosing time."( Dosing time-dependent changes in the analgesic effect of pregabalin on diabetic neuropathy in mice.
Akamine, T; Hashimoto, H; Koyanagi, S; Kusunose, N; Matsunaga, N; Ohdo, S; Taniguchi, M, 2015
)
0.42
"Gabapentin may have a role in the treatment of mild alcohol withdrawal, but future studies should focus on adequate dosing strategies."( The role of gabapentin in the management of alcohol withdrawal and dependence.
Hall-Flavin, D; Leung, JG; Nelson, S; Schak, KM; Schmidt, KA, 2015
)
0.42
" We demonstrated that histaminergic activity was regulated by group II metabotropic glutamate receptors (mGluR 2 and 3) using systemic dosing with mGluR 2/3 agonist and antagonists and an mGluR 2 positive allosteric modulator."( Glutamatergic regulation of brain histamine neurons: In vivo microdialysis and electrophysiology studies in the rat.
Dijkman, U; Fell, MJ; Flik, G; Folgering, JH; Johnson, BJ; Perry, KW; Svensson, KA; Westerink, BH, 2015
)
0.42
" The best compartmental, oral model was used to simulate the concentration-time profiles resulting from different dosing scenarios."( Pharmacokinetics of Compounded Intravenous and Oral Gabapentin in Hispaniolan Amazon Parrots ( Amazona ventralis ).
Baine, K; Cox, S; Jones, MP; Martín-Jiménez, T, 2015
)
0.42
" Since, 5-HT6 antagonists improved the effectiveness of gabapentinoids, reduction in the dosage and frequency of gabapentinoids treatment may reduce the side effects."( 5-HT6 receptor antagonist attenuates the memory deficits associated with neuropathic pain and improves the efficacy of gabapentinoids.
Babu, VA; Bhyrapuneni, G; Goura, V; Jayarajan, P; Nirogi, R; Shinde, A; Yathavakilla, S, 2015
)
0.42
" A different sensitivity of these neurons to MCH may explain the dose-response effect on 5-HT release."( Melanin-concentrating hormone projections to the dorsal raphe nucleus: An immunofluorescence and in vivo microdialysis study.
Abin-Carriquiry, JA; Lagos, P; Scorza, C; Torterolo, P; Urbanavicius, J, 2016
)
0.43
" Most of the studies evaluating the efficacy of GHB in the treatment of AWS use a dosage of 50 mg/kg divided in three or four administrations per day."( Clinical applications of sodium oxybate (GHB): from narcolepsy to alcohol withdrawal syndrome.
Busardò, FP; Kyriakou, C; Marinelli, E; Napoletano, S; Zaami, S, 2015
)
0.42
"Gabapentin displays non-linear drug disposition, which complicates dosing for optimal therapeutic effect."( Pharmacokinetic/Pharmacodynamic Relationship of Gabapentin in a CFA-induced Inflammatory Hyperalgesia Rat Model.
Holm, R; Keizer, R; Kreilgaard, M; Larsen, MS; Munro, G; Mørk, A; Savic, R, 2016
)
0.43
" Antipsychotic dosage was negatively correlated with GABA+ levels, but the on-off medication studies indicated no difference in GABA+ levels on antipsychotics compared with off antipsychotics."( Prefrontal GABA Levels Measured With Magnetic Resonance Spectroscopy in Patients With Psychosis and Unaffected Siblings.
Apud, JA; Barnett, AS; Berman, KF; DeJong, K; Dickinson, D; Kuo, S; Marenco, S; Meyer, C; Shen, J; van der Veen, JW; Weinberger, DR, 2016
)
0.43
" Gabapentin has a favorable adverse effect profile in therapeutic dosing with the most common reported effects being dizziness, fatigue, drowsiness, weight gain, and peripheral edema."( Gabapentin concentrations and postmortem distribution.
Gary, RD; Hamm, CE; McIntyre, IM, 2016
)
0.43
"To evaluate efficacy, appropriate dosing regimen and safety of gabapentin on UP in hemodialysis (HD) patients."( Gabapentin: A promising therapy for uremic pruritus in hemodialysis patients: A randomized-controlled trial and review of literature.
Abdelkhalik, Z; Alkot, R; Eldesouky, F; Farag, F; Nofal, A; Nofal, E, 2016
)
0.43
" Our data demonstrate that the timing and dosing of antiandrogens are critical to maximizing the antitumor effects of combination therapy."( Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse.
Fu, YX; Guo, Y; Liang, Y; Pu, Y; Xu, M; Yang, K; Yang, X, 2016
)
0.43
" Rodent models of CIPN have been developed using a range of dosing regimens to reproduce pain-like behaviours akin to patient-reported symptoms."( Chemotherapy-induced painful neuropathy: pain-like behaviours in rodent models and their response to commonly used analgesics.
Duggett, NA; Flatters, SJL; Hopkins, HL, 2016
)
0.43
" We present an overview of dosing regimens to produce CIPN models and their phenotype of pain-like behaviours."( Chemotherapy-induced painful neuropathy: pain-like behaviours in rodent models and their response to commonly used analgesics.
Duggett, NA; Flatters, SJL; Hopkins, HL, 2016
)
0.43
"The review outlines the latest description of the most-relevant rodent models of CIPN enabling comparison between chemotherapeutics, dosing regimen, rodent strain, and sex."( Chemotherapy-induced painful neuropathy: pain-like behaviours in rodent models and their response to commonly used analgesics.
Duggett, NA; Flatters, SJL; Hopkins, HL, 2016
)
0.43
" One month later, she reported that she had self-reduced the gabapentin dosage to 300 mg once daily, after which she noticed improvement in her daytime sleepiness and fatigue and experienced one hallucination approximately one week after the dosage reduction."( Visual hallucinations associated with gabapentin use.
Derkits, ME; Parsons, KA, 2016
)
0.43
" Intriguingly, this receptor is lacking canonical GABA binding sites but it can be activated by GABA and dose-response relationships for α1β2γ2L and α1γ2L receptors overlap."( Comparison of kinetic and pharmacological profiles of recombinant α1γ2L and α1β2γ2L GABAA receptors - A clue to the role of intersubunit interactions.
Brodzki, M; Czyzewska, MM; Jatczak, M; Kisiel, M; Mozrzymas, JW; Rutkowski, R, 2016
)
0.43
"Databases were searched for peer-reviewed papers demonstrating gabapentin misuse, characterized by taking a larger dosage than prescribed or taking gabapentin without a prescription, and diversion."( Gabapentin misuse, abuse and diversion: a systematic review.
Havens, JR; Smith, RV; Walsh, SL, 2016
)
0.43
" Dose-response curves (DRC) and isobolographic analysis were used to confirm their synergistic antihyperalgesic and anti-allodynic responses in a rat neuropathic pain model involving chronic constriction injury of the sciatic nerve and in von Frey and acetone tests."( The Antinociceptive Effects of Tramadol and/or Gabapentin on Rat Neuropathic Pain Induced by a Chronic Constriction Injury.
Corona-Ramos, JN; De la O-Arciniega, M; Déciga-Campos, M; Domínguez-Ramírez, AM; Espinosa-Juárez, JV; Jaramillo-Morales, OA; López-Muñoz, FJ; Medina-López, JR, 2016
)
0.43
"The aim of this review was to evaluate current literature for dosing recommendations for the use of antiepileptic medications in patients receiving renal replacement therapy (RRT)."( Antiepileptic dosing for critically ill adult patients receiving renal replacement therapy.
Bastin, ML; Cook, AM; Oyler, DR; Smetana, KS, 2016
)
0.43
" Micromedex® DRUGDEX as well as package inserts were used to obtain known pharmacokinetic properties and dosage adjustment recommendations in RRT if known."( Antiepileptic dosing for critically ill adult patients receiving renal replacement therapy.
Bastin, ML; Cook, AM; Oyler, DR; Smetana, KS, 2016
)
0.43
"Data regarding antiepileptic drug use in RRT are limited and mostly consist of case reports limiting our proposed dosing recommendations."( Antiepileptic dosing for critically ill adult patients receiving renal replacement therapy.
Bastin, ML; Cook, AM; Oyler, DR; Smetana, KS, 2016
)
0.43
"Additional studies are necessary before specific dosing recommendations can be made for most antiepileptic drugs in critically ill patients receiving RRT, specifically with newer agents."( Antiepileptic dosing for critically ill adult patients receiving renal replacement therapy.
Bastin, ML; Cook, AM; Oyler, DR; Smetana, KS, 2016
)
0.43
" The animal model, using a sub-chronic dosing regimen (sc) with the non-competitive NMDA receptor antagonist PCP (phencyclidine), evolved from previous work in rats (for PCP) and primates (for cognition)."( Modelling the cognitive and neuropathological features of schizophrenia with phencyclidine.
Neill, JC; Reynolds, GP, 2016
)
0.43
" Previous studies showed that opioids combined with gabapentin for management of cancer pain reduced the dosage of opioids."( The research on long-term clinical effects and patients' satisfaction of gabapentin combined with oxycontin in treatment of severe cancer pain.
Chen, DL; Li, YH; Wang, ZJ; Zhu, YK, 2016
)
0.43
" Therefore, in women with a uterus, it is recommended that physicians prescribe combination therapy only to treat menopausal symptoms such as vasomotor symptoms (hot flashes) and vaginal atrophy, using the smallest effective dosage for the shortest possible duration."( Hormone Therapy and Other Treatments for Symptoms of Menopause.
Crider, M; Hill, DA; Hill, SR, 2016
)
0.43
" Although there was no difference in kainate dosing or seizure count between them, the metabolic pattern of injury was different."( Metabolic injury in a variable rat model of post-status epilepticus.
de Lanerolle, N; Kelly, KM; Pan, JW; Pearce, PS; Rapuano, A; Wu, Y, 2016
)
0.43
"To study impulsivity in adolescents with attention deficit hyperactivity disorder (ADHD) and evaluate the efficacy of noophen in dosage 500 mg daily for 45 days in the treatment of this disorder."( [Impulsivity in adolescents with attention deficit hyperactivity disorder].
Anisimova, TI; Chutko, LS; Kropotov, YD; Sergeev, AV; Surushkina, EY; Yakovenko, EA,
)
0.13
" Cyclobenzaprine specimens were equally likely to be positive whether the dose was oral or topical, although mean levels after topical dosing were approximately 13-21% those after oral dosing."( Urinary Concentrations of Topically Administered Pain Medications.
Bell, P; Glinn, MA; Harvey, A; Lickteig, AJ; Rappold, B; Recer, S; Salske, M; Stensland, J; Weber, L, 2017
)
0.46
"In this study, we evaluated the dose-response efficacy of levetiracetam (12."( Combination therapy of levetiracetam and gabapentin against nonconvulsive seizures induced by penetrating traumatic brain injury.
Cao, Y; Liao, Z; Lu, XM; Mountney, A; Shear, DA; Tortella, FC, 2017
)
0.46
" However, the two drugs manifested different dose-response profiles."( Combination therapy of levetiracetam and gabapentin against nonconvulsive seizures induced by penetrating traumatic brain injury.
Cao, Y; Liao, Z; Lu, XM; Mountney, A; Shear, DA; Tortella, FC, 2017
)
0.46
" We report on a case of a 31 year old female who presented to the emergency department with unilateral leg pain, weakness, and swelling after increasingly titrating her Gabapentin dosage over three weeks."( Radiologic Findings in Gabapentin-Induced Myositis.
Chang, DR; Coupal, TM; Munk, PL; Ouellette, HA; Pennycooke, K, 2017
)
0.46
" In addition, there was a negative correlation between the gabapentin dosage and the occurrence of nausea and vomiting."( The efficacy of gabapentin in reducing pain intensity and postoperative nausea and vomiting following laparoscopic cholecystectomy: A meta-analysis.
Dong, Y; Tan, H; Wang, L; Zhang, J, 2017
)
0.46
"The present work aims to investigate the anxiolytic activity of 6-styryl-2-pyrone (STY), obtained from Aniba panurensis, in behavioral tests and amino acids dosage on male Swiss mice."( The anxiolytic-like effect of 6-styryl-2-pyrone in mice involves GABAergic mechanism of action.
Barbosa-Filho, JM; Chaves, EMC; Dantas, LP; Honório-Júnior, JER; Lúcio, ASSC; Monteiro, VS; Nonato, DTT; Patrocínio, MCA; Sousa, CNS; Vasconcelos, SMM; Viana, GSB, 2018
)
0.48
" However, 50% of these oocytes were usable for full dose-response experiments."( Evaluating the longevity of surgically extracted Xenopus laevis oocytes for the study of nematode ligand-gated ion channels.
Abdelmassih, SA; Cochrane, E; Forrester, SG, 2017
)
0.46
" The goal of this study was to assess the association between gabapentin dosing and adverse outcomes by obtaining estimates of the 30-day risk of hospitalization with altered mental status and mortality in older adults (mean age 76 years) in Ontario, Canada initiated on high dose (>600 mg/day; n = 34,159) compared to low dose (≤600 mg/day; n = 76,025) oral gabapentin in routine outpatient care."( Gabapentin dose and the 30-day risk of altered mental status in older adults: A retrospective population-based study.
Burneo, J; Dev, VK; Dixon, SN; Fleet, JL; Garg, AX; Kuwornu, PJ; Montero-Odasso, M, 2018
)
0.48
"GEn requires less frequent dosing compared with GBP-IR and fluctuates less with sustained gabapentin exposure throughout the day."( Pharmacokinetics of immediate release, extended release, and gastric retentive gabapentin formulations in healthy adults
.
Aronoff, GM; Ciric, S; Lal, R; Swearingen, D, 2018
)
0.48
" No information is available on dose-response effects of Mn on putrescine abundance and related polyamine metabolism."( Putrescine as indicator of manganese neurotoxicity: Dose-response study in human SH-SY5Y cells.
Chandler, JD; Fernandes, J; Go, YM; Jones, DP; Liu, KH; Uppal, K, 2018
)
0.48
" Moreover, GBP is a freely water-soluble drug, thus it is considered a challenging candidate to be formulated as extended release dosage form."( Gastroretentive raft liquid delivery system as a new approach to release extension for carrier-mediated drug.
Aboelwafa, AA; Abouelatta, SM; El-Gazayerly, ON, 2018
)
0.48
" We estimated summary risk ratios (RR) for each outcome and evaluated dose-response in regression models."( Gabapentin add-on treatment for drug-resistant focal epilepsy.
Al-Bachari, S; Hutton, JL; Marson, AG; Panebianco, M; Weston, J, 2018
)
0.48
" We develop a system in human pluripotent stem cells (hPSCs) using CRISPR/Cas9 and SMASh technology, with which we can target endogenous proteins for precise dosage control in hPSCs and at multiple stages of neural differentiation."( Precisely controlling endogenous protein dosage in hPSCs and derivatives to model FOXG1 syndrome.
Hu, B; Li, M; Li, W; Mi, T; Mo, F; Teng, Z; Wu, Y; Zhang, B; Zhou, Q; Zhu, W, 2019
)
0.51
" Vinpocetine was administered as a dietary supplement over 6 months, reaching a dosage of 20 mg three times per day, and resulted in a sustained, dose-dependent reduction in spike-wave discharge frequency on electroencephalograms."( Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation.
Andresen, JM; Billakota, S; Devinsky, O; Fedorov, NB; Gay, BC; Gerlach, AC; Stewart, GR, 2019
)
0.51
" Pantogam (syrup 100 mg/ml) or placebo were prescribed orally 15-30 minutes after feeding, twice a day, in a daily dosage of 30-50 mg/kg body weight."( [Pharmacotherapy of psychomotor developmental delay in 6-12 months preterm infants with hypoxic-ischemic encephalopathy (the double-blind comparative multicenter placebo-controlled study)].
Davydova, LA; Gaynetdinova, DD; Guzeva, VI; Romanova, TA; Zavadenko, AN; Zavadenko, NN, 2019
)
0.51
" In addition, BGT-1 deficiency or dosing with NNC 05-2090 stimulated the expression of the anti-apoptotic gene, c-Met in the liver, suggesting the involvement of c-Met in the function on hepatocytes of BGT-1 apoptosis."( Betaine/GABA transporter-1 (BGT-1) deficiency in mouse prevents acute liver failure in vivo and hepatocytes apoptosis in vitro.
Ci, L; Fei, J; Huang, F; Huang, Q; Li, Q; Liu, Z; Lu, T; Shen, R; Shi, J; Sun, R; Wan, Z; Wang, Z; Yang, H; Yang, X; Zhang, M, 2020
)
0.56
" Finally, in vitro results demonstrated that GABA (ranging from 10 to 50 μg/μL) markedly inhibited preimplantation embryo development in a dose-response manner."( GABA consumption during early pregnancy impairs endometrial receptivity and embryo development in mice.
Cao, K; Liang, H; Luo, W; Tan, D; Tan, Y; Tian, N; Wang, X; Zhang, Q, 2020
)
0.56
" The highest dosage of GABA yogurt had a greater beneficial effect with respect to insulin resistance than the lower dosages."( Effect of γ-aminobutyric acid-rich yogurt on insulin sensitivity in a mouse model of type 2 diabetes mellitus.
Chen, L; Li, X; Lu, Y; Lu, Z; Zhu, X, 2020
)
0.56
" Consistent with this observation, VU0360172 could also enhance thalamic GAT-1 protein expression, depending on the dosing regimen."( Pharmacological activation of mGlu5 receptors with the positive allosteric modulator VU0360172, modulates thalamic GABAergic transmission.
Bruno, V; Cannella, M; Celli, R; Ciruela, F; Di Menna, L; Mascio, G; Ngomba, RT; Nicoletti, F; Pittaluga, A; Santolini, I; van Luijtelaar, G; Vergassola, M; Wall, MJ, 2020
)
0.56
" We estimated summary risk ratios (RR) for each outcome and evaluated dose-response in regression models."( Gabapentin add-on treatment for drug-resistant focal epilepsy.
Al-Bachari, S; Hutton, JL; Marson, AG; Panebianco, M, 2021
)
0.62
" This dosage of CPF does not inhibit brain cholinesterase activity but inhibits FAAH activity."( Persistent proteomic changes in glutamatergic and GABAergic signaling in the amygdala of adolescent rats exposed to chlorpyrifos as juveniles.
Alugubelly, N; Carr, RL; Mohammed, AN, 2021
)
0.62
" This specialized assessment may require dosing neonatal rats at postnatal day 7 at the peak of the brain growth spurt and evaluating brain tissue 24 to 48 hours following dosing."( Use of Both Fluoro-Jade B and Hematoxylin and Eosin to Detect Cell Death in the Juvenile Rat Brain Exposed to NMDA-Receptor Antagonists or GABA-Receptor Agonists in Safety Assessment.
Davis, S; Mendes, OR; Picut, CA; Swanson, C; Weil, DS, 2021
)
0.62
" Pregnant C57BL/6 J mice were intraperitoneally injected with a dosage of 500 mg/kg valproic acid (VPA) on embryonic day 10."( Size anomaly and alteration of GABAergic enzymes expressions in cerebellum of a valproic acid mouse model of autism.
Kwan, KM; Ma, SY, 2022
)
0.72
"1 nM at equilibrium with this diazepam dosing schedule."( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points.
Burkat, PM, 2022
)
0.72
" Gabapentenoid dosing varied among studies."( Gabapentinoids and Acetaminophen as Adjuvants for Managing Postoperative Pain.
Gill, C; Giuliano, K, 2022
)
0.72
" Moreover, the voluntary oral administration is suitable for repeated dosing of DREADDs ligands."( Validation of DREADD agonists and administration route in a murine model of sleep enhancement.
Anaclet, C; Ferrari, LL; Gompf, HS; Ogbeide-Latario, OE, 2022
)
0.72
" These findings strongly support individualised dosing of tDCS, at least in M1."( tDCS induced GABA change is associated with the simulated electric field in M1, an effect mediated by grey matter volume in the MRS voxel.
Bachtiar, V; Barron, HC; Berrington, A; Clarke, WT; Hanayik, T; Hinson, EL; Johansen-Berg, H; Johnstone, A; Kolasinski, J; Nandi, T; Nettekoven, C; Puonti, O; Stagg, CJ; Thielscher, A; Winkler, AM,
)
0.13
" Besides pregabalin (150 mg/day), the patients, upon their group assignment, received CoQ10 at a dosage of 100 mg every 8 h or matched placebo for 8 consecutive weeks."( Coenzyme Q10 as a potential add-on treatment for patients suffering from painful diabetic neuropathy: results of a placebo-controlled randomized trial.
Amini, P; Mehrpooya, M; Mirjalili, M; Mohammadi, Y; Sajedi, F, 2022
)
0.72
" Male offsprings were injected with EPO and NEPO in a clinically proper postnatal dosing regimen on postnatal days (PND) 1-5, and autistic-like behaviors were tested at the end of the first month."( The effects of postnatal erythropoietin and nano-erythropoietin on behavioral alterations by mediating K-Cl co-transporter 2 in the valproic acid-induced rat model of autism.
Basiri, M; Darvishzadeh-Mahani, F; Haratizadeh, S; Nozari, M; Ranjbar, M, 2023
)
0.91
"Participants were randomly assigned (2:1) to daily dosing with ASP8062 25 mg or placebo on days 1-10."( A phase 1 randomized, placebo-controlled study to investigate potential interactions between ASP8062, a positive allosteric modulator of the GABA
Alsharif, MN; Blahunka, P; Blauwet, MB; Erdman, J; Heo, N; Ito, M; Kelsh, D; Marek, GJ; Spence, A; Walzer, M, 2023
)
0.91
" They were also excluded if they lacked sufficient information about how long or at what dosage they had been using the drug."( Abuse and addiction in gabapentinoid drug users for neuropathic pain.
Aydin Özaslan, E; Kiliç, Z, 2023
)
0.91
" We are most familiar with the incremental dosing strategy where a ceiling dose is eventually attained guided by efficacy and patient tolerance, after which a fixed dosing regimen is prescribed."( Comparative Descriptive Analysis of Physician Versus Patient-Directed Gabapentin Usage In Chronic Pain - A Preliminary Report.
Burns, JC; Gill, JS; Madabhushi, SV; Robinson, CL; Ruan, QZ; Simopoulos, TT, 2023
)
0.91
" Of the patients still taking gabapentin, 73% were on a fixed schedule, while 27% were on a variable dosing schedule."( Comparative Descriptive Analysis of Physician Versus Patient-Directed Gabapentin Usage In Chronic Pain - A Preliminary Report.
Burns, JC; Gill, JS; Madabhushi, SV; Robinson, CL; Ruan, QZ; Simopoulos, TT, 2023
)
0.91
" None of the patients we surveyed had been given the autonomy to adjust gabapentin doses by their providers and this could significantly reduce the proportion of patients who would be encouraged to run a variable dosing regimen."( Comparative Descriptive Analysis of Physician Versus Patient-Directed Gabapentin Usage In Chronic Pain - A Preliminary Report.
Burns, JC; Gill, JS; Madabhushi, SV; Robinson, CL; Ruan, QZ; Simopoulos, TT, 2023
)
0.91
" Based upon this pilot study, the variable dosing option may be an option for improved therapeutic efficacy or as an alternative to those whose lifestyles do not allow for fixed dosing regimens."( Comparative Descriptive Analysis of Physician Versus Patient-Directed Gabapentin Usage In Chronic Pain - A Preliminary Report.
Burns, JC; Gill, JS; Madabhushi, SV; Robinson, CL; Ruan, QZ; Simopoulos, TT, 2023
)
0.91
" The ameliorative effect of FDH-GABA on premature aging showed a clear dose-response relationship, and at the same time, the changes of intestinal microorganisms showed a certain correlation with the relevant indexes of nervous system."( Beneficial effect of GABA-rich fermented milk whey on nervous system and intestinal microenvironment of aging mice induced by D-galactose.
He, W; Jiang, Y; Min, J; Song, H; Yang, Z; Zhao, S, 2024
)
1.44
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Occurs in Manufacturing (56 Product(s))

Product Categories

Product CategoryProducts
Professional Supplements9
Active Lifestyle & Fitness6
Vitamins & Supplements32
Herbs, Botanicals & Homeopathy5
Pet Supplies1
Weight Management2
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Products

ProductBrandCategoryCompounds Matched from IngredientsDate Retrieved
Allergy Research Group 200 Mg of Zen -- 120 Vegetarian CapsulesAllergy Research GroupProfessional SupplementsGABA2024-11-29 10:47:42
Allergy Research Group Zen -- 200 mg - 60 Vegetarian CapsulesAllergy Research GroupProfessional SupplementsGABA2024-11-29 10:47:42
Amy Myers MD Rest and Restore -- 60 CapsulesAmy Myers MDProfessional SupplementsGamma-Aminobutyric Acid2024-11-29 10:47:42
Amy Myers MD Rest and Restore Max -- 60 CapsulesAmy Myers MDProfessional Supplements5-Hydroxytryptophan, Gamma-Aminobutyric Acid, Melatonin2024-11-29 10:47:42
Animal PM Sleep & Nighttime Recovery Pill Pack -- 30 PacksAnimalActive Lifestyle & FitnessGamma-Aminobutyric Acid, Arginine Alpha-Ketoglutarate, Phosphorus, Vitamin B6, Vitamin B62024-11-29 10:47:42
Aurora NutraScience Ultra Liposomal Sleep Support -- 10 fl ozAurora NutraScienceVitamins & SupplementsVitamin C, Gamma-Aminobutyric Acid, Melatonin2024-11-29 10:47:42
Aurora NutraScience Ultra-Liposomal Sleep Support -- 30 PacketsAurora NutraScienceVitamins & SupplementsVitamin C, Gamma-Aminobutyric Acid, Melatonin2024-11-29 10:47:42
Bach Rescue Plus Mood & Stress Support Gummies Orange -- 60 GummiesBachHerbs, Botanicals & HomeopathyVitamin D3, GABA, Saffron2024-11-29 10:47:42
Bark & Whiskers Stress Support Powder for Dogs & Cats -- 1.29 ozBark & WhiskersPet Supplies5-HTP, GABA, Vitamin B6, Vitamin B62024-11-29 10:47:42
Bio Nutrition Sleep Wellness with Wild Lettuce Extract -- 60 Vegetarian CapsulesBio NutritionVitamins & Supplements5-HTP, GABA, Melatonin2024-11-29 10:47:42
Designs for Sport Sleep Complex - NSF Certified for Sport -- 60 Vegetarian CapsulesDesigns for SportProfessional Supplements5-HTP, Chamomile, Gamma-Aminobutyric Acid, Melatonin, Vitamin B6, Vitamin B62024-11-29 10:47:42
Douglas Laboratories GABA -- 500 mg - 60 CapsulesDouglas LaboratoriesProfessional SupplementsGABA2024-11-29 10:47:42
Evlution Nutrition NiteLean - Nighttime Weight Loss Support -- 30 Veggie CapsulesEvlution NutritionWeight Management5-HTP, Chromium, Gamma-Aminobutyric Acid, Melatonin2024-11-29 10:47:42
Evlution Nutrition SleepMode -- 60 Veggie CapsulesEvlution NutritionVitamins & SupplementsGABA2024-11-29 10:47:42
Force Factor Ultimate Magnesium Orange Creamsicle -- 330 mg - 60 Soft ChewsForce FactorVitamins & SupplementsGamma-Aminobutyric Acid2024-11-29 10:47:42
Irwin Naturals Power to Sleep PM 6 mg Melatonin -- 60 Liquid SoftgelsIrwin NaturalsVitamins & Supplementsannatto, GABA, glycerin, maltodextrin, Melatonin, titanium dioxide2024-11-29 10:47:42
Irwin Naturals Power to Sleep PM® -- 120 Liquid SoftgelsIrwin NaturalsVitamins & SupplementsGABA, glycerin, Melatonin2024-11-29 10:47:42
Irwin Naturals Power to Sleep PM® Melatonin-Free -- 50 Liquid SoftgelsIrwin NaturalsVitamins & Supplements5-HTP, leaf, GABA, glycerin, maltodextrin, Vitamin B6, titanium dioxide, Vitamin B62024-11-29 10:47:42
Irwin Naturals Stress-Defy™ -- 84 Liquid SoftgelsIrwin NaturalsVitamins & SupplementsGABA, glycerin, maltodextrin, Vitamin B6, Riboflavin, Thiamin, titanium dioxide, Vitamin B62024-11-29 10:47:42
Kal GABA L-Thenine Stress B Lozenge Natural Mango Tangerine -- 100 LozengesKALVitamins & SupplementsVitamin C, cellulose, fructose, Folate, GABA, Inositol, Niacin, Pantothenic Acid, Vitamin B6, stearic acid, Thiamine, Cyanocobalamin, Vitamin B6, Xylitol2024-11-29 10:47:42
Kyolic Aged Garlic Extract Stress and Fatigue Relief Formula 101 -- 300 CapsulesKyolicHerbs, Botanicals & HomeopathyGABA, Microcrystalline cellulose, Vitamin B6, Thiamine, Vitamin B12, Vitamin B62024-11-29 10:47:42
Kyolic Aged Garlic Extract™ Stress and Fatigue Relief Formula 101 -- 200 CapsulesKyolicHerbs, Botanicals & HomeopathyCellulose, GABA, Vitamin B6, Vitamin B1, Vitamin B12, Vitamin B62024-11-29 10:47:42
Luminite Natural Sleep Support -- 30 CapsulesLuminiteVitamins & SupplementsGABA, L-Glycine, Melatonin2024-11-29 10:47:42
MenoLabs Well Rested™ Sleep Support For Women -- 60 CapsulesMenoLabsVitamins & Supplements5-HTP, GABA, L-Glycine, Microcrystalline cellulose, Melatonin2024-11-29 10:47:42
Natural Factors Stress-Relax Pharma GABA -- 100 mg - 60 Vegetarian CapsulesNatural FactorsVitamins & SupplementsGamma-Amino butyric Acid2024-11-29 10:47:42
Natural Vitality Calm Sleep Capsules -- 60 CapsulesNatural VitalityVitamins & SupplementsGamma-Aminobutyric Acid, microcrystalline cellulose, Melatonin2024-11-29 10:47:42
Natural Vitality Calm Sleep Drink Mix Mixed Berry -- 6 ozNatural VitalityVitamins & Supplements Citric acid, Citric acid, leaf, Gamma-Aminobutyric Acid, magnesium carbonate, Melatonin2024-11-29 10:47:42
Natural Vitality Calm Sleep Supplement Drink Mixed Berry -- 4 ozNatural VitalityVitamins & Supplements Citric acid, Citric acid, leaf, GABA, Magnesium Carbonate, Melatonin2024-11-29 10:47:42
Nature Made Wellblends Sleep Longer Melatonin (10mg) L Theanine GABA -- 35 Tri-Layer TabletsNature MadeVitamins & SupplementsGABA, Melatonin2024-11-29 10:47:42
NutriBiotic Ultra-Hydrating Peptide Face Creme -- 2 fl ozNutriBioticBeauty & Personal Careallantoin, cetearyl alcohol, panthenol, ethylhexylglycerin, gamma-aminobutyric acid, glyceryl stearate, dimethicone, phenoxyethanol2024-11-29 10:47:42
NutriCology ZenMind -- 120 Vegetarian CapsulesNutriCologyVitamins & SupplementsGABA2024-11-29 10:47:42
Olly Goodbye Stress Berry Verbena -- 42 GummiesOllyVitamins & Supplementscitric acid, citric acid, GABA, beet sugar2024-11-29 10:47:42
Olly Goodbye Stress® -- 60 SoftgelsOllyHerbs, Botanicals & HomeopathyGABA, glycerin, titanium dioxide, Withania somnifera2024-11-29 10:47:42
Olly Mellow Menopause Relief For Hot Flashes with EstroG-100 & Gaba -- 30 CapsulesOllyHerbs, Botanicals & HomeopathyGABA, microcrystalline cellulose2024-11-29 10:47:42
Orgain SleepDeep Supplement - 3mg Melatonin - L-Theanine & Magnesium -- 60 Capsules (30-Day Supply)OrgainVitamins & SupplementsChamomile, GABA, Melatonin2024-11-29 10:47:42
Orgain StressLess Supplement - Vegan Ashwagandha GABA Magnesium -- 90 CapsulesOrgainVitamins & Supplements5-HTP, Chamomile, GABA2024-11-29 10:47:42
SFI Health Sleep Support Complex -- 180 CapsulesSFI HealthProfessional SupplementsGABA2024-11-29 10:47:42
Snap Supplements Sleep Complex with Melatonin -- 60 CapsulesSnap SupplementsVitamins & Supplements5-HTP, GABA, Melatonin2024-11-29 10:47:42
Source Naturals HGH Surge -- 150 TabletsSource NaturalsActive Lifestyle & Fitness5-HTP, Acetyl L-Carnitine, Chromium, DMAE, GABA, L-Glutamine, Glycine, Huperzine A, microcrystalline cellulose, Niacin, Ornithine Ketoglutarate, stearic acid2024-11-29 10:47:42
Source Naturals NightRest with Melatonin -- 100 TabletsSource NaturalsVitamins & Supplementsdibasic calcium phosphate, GABA, Glycine, Melatonin, Stearic acid, Taurine2024-11-29 10:47:42
Source Naturals Serene Science™ GABA Calm™ Orange -- 120 LozengesSource NaturalsVitamins & SupplementsGABA, Glycine, mannitol, N-Acetyl L-Tyrosine, Sorbitol, stearic acid, Taurine2024-11-29 10:47:42
Source Naturals Serene Science™ Theanine Serene™ with Relora® -- 120 TabletsSource NaturalsVitamins & SupplementsGABA, Sorbitol, stearic acid, Taurine2024-11-29 10:47:42
SUKU Vitamins Buh Bye Stress™ Gummy Vitamins -- 50 GummiesSUKU VitaminsVitamins & Supplementscitric acid, citric acid, GABA, sodium citrate2024-11-29 10:47:42
SUKU Vitamins Restful Sleep Gummy Vitamins Blackberry Hibiscus -- 50 GummiesSUKU VitaminsVitamins & Supplementscitric acid, agar, citric acid, GABA, Melatonin, sodium citrate2024-11-29 10:47:42
Thorne Research PharmaGABA-100 -- 60 CapsulesThorne ResearchProfessional SupplementsGamma-Aminobutyric Acid, Microcrystalline cellulose, magnesium citrate2024-11-29 10:47:42
Thorne Research PharmaGABA-250 -- 60 CapsulesThorne ResearchProfessional SupplementsGamma-Aminobutyric Acid, Microcrystalline cellulose, magnesium citrate2024-11-29 10:47:42
TransformHQ Nighttime Shake - 28 Servings Chocolate Mousse -- 1.65 lbsTransformHQActive Lifestyle & FitnessGABA2024-11-29 10:47:42
TransformHQ Nighttime Shake - 28 Servings Pineapple Upside Down Cake -- 1.4 lbsTransformHQActive Lifestyle & FitnessGABA2024-11-29 10:47:42
Tropical Oasis Sleep-A-Weigh Plus -- 32 fl ozTropical OasisWeight Managementcitric acid, 5-Hydroxytryptophan, Vitamin C, citric acid, GABA, L-Lysine, Melatonin, Vitamin B6, Vitamin B6, xylitol2024-11-29 10:47:42
TruLabs Sleep Nighttime Drink Mix Honey Lemon -- 6 PacketsTruLabsVitamins & Supplements5-HTP, health, Chloride, Folate, GABA, Melatonin, Niacin, Vitamin B6, stevia, sucralose, Vitamin B6, Ashwagandha2024-11-29 10:47:42
Type Zero Clean Pre Workout Cherry Limeade -- 21 ServingsType ZeroActive Lifestyle & Fitnesscitric acid, Vitamin C, Beta-Alanine, Betaine Anhydrous, Chromium, citric acid, GABA, N-Acetyl L-Tyrosine, Vitamin B122024-11-29 10:47:42
Type Zero Clean Pre Workout Fruit Punch -- 21 ServingsType ZeroActive Lifestyle & Fitnesscitric acid, Vitamin C, Beta-Alanine, Betaine Anhydrous, Chromium, citric acid, GABA, N-Acetyl L-Tyrosine, Vitamin B122024-11-29 10:47:42
Vena Spa Water Radiance Renewal Drink Powder Strawberry Kiwi -- 20 Stick PacketsVenaVitamins & Supplements Citric acid, Vitamin C, Citric acid, Gamma-Aminobutyric Acid, L-Glycine, L-Lysine, Nicotinamide Adenine Dinucleotide2024-11-29 10:47:42
Vitanica GABA Ease™ -- 60 Vegetarian CapsulesVitanicaVitamins & SupplementsGABA, Vitamin B6, Vitamin B62024-11-29 10:47:42
Youtheory Relax Magnesium Powder Stress Formula + L-Theanine Berry -- 4.4 ozYoutheoryVitamins & Supplementsleaf, GABA, L-glycine, stevia, xylitol2024-11-29 10:47:42
Zhou Driftoff™ -- 60 Veggie CapsulesZhouVitamins & SupplementsGABA, Melatonin, Tryptophan2024-11-29 10:47:42

Roles (4)

RoleDescription
neurotransmitterAn endogenous compound that is used to transmit information across the synapse between a neuron and another cell.
signalling moleculeA molecular messenger in which the molecule is specifically involved in transmitting information between cells. Such molecules are released from the cell sending the signal, cross over the gap between cells by diffusion, and interact with specific receptors in another cell, triggering a response in that cell by activating a series of enzyme controlled reactions which lead to changes inside the cell.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
Saccharomyces cerevisiae metaboliteAny fungal metabolite produced during a metabolic reaction in Baker's yeast (Saccharomyces cerevisiae).
[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
gamma-amino acidA non-proteinogenic amino-acid in which the amino group is located on the carbon atom at the position gamma to the carboxy group.
monocarboxylic acidAn oxoacid containing a single carboxy group.
amino acid zwitterionThe zwitterionic form of an amino acid having a negatively charged carboxyl group and a positively charged amino group.
[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]

Pathways (32)

PathwayProteinsCompounds
Glutamate Metabolism2244
4-Hydroxybutyric Aciduria/Succinic Semialdehyde Dehydrogenase Deficiency2244
Homocarnosinosis2244
Hyperinsulinism-Hyperammonemia Syndrome2244
2-Hydroxyglutric Aciduria (D and L Form)2244
Succinic Semialdehyde Dehydrogenase Deficiency2244
Arginine Metabolism2848
Ornithine Metabolism1631
Putrescine Degradation II815
4-Aminobutanoate Degradation I39
4-Aminobutanoate Degradation29
Glutamic Acid Metabolism1317
Butanoate Metabolism922
2-Oxo-glutaric acid + 4-Amino-butanoic acid = L-Glutamic acid + Succinate semialdehyde ( Glutamic acid and Glutamine metabolism )14
Arginine and Proline metabolism ( Arginine and Proline metabolism )4255
Glutamic acid and Glutamine metabolism ( Glutamic acid and Glutamine metabolism )1926
Fragile X syndrome23
7q11.23 copy number variation syndrome213
Dravet syndrome284
Dravet syndrome: Scn1a-A1783V point mutation model789
polyamine degradation (N-acetyl pathway)012
GABA degradation09
AtMetExpress overview0109
Biosynthesis of gamma-aminobutyric acid (GABA) by polyamine oxidation05
Neurotransmitter release in cholinergic motor neurons04
Iron uptake and transport030
MECP2 and associated Rett syndrome011
Biochemical pathways: part I0466
Cannabinoid receptor signaling020
Valproic acid pathway022
Biogenic amine synthesis03
Sudden infant death syndrome (SIDS) susceptibility pathways07

Protein Targets (102)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency0.31625.623417.292931.6228AID485281
thioredoxin reductaseRattus norvegicus (Norway rat)Potency19.95260.100020.879379.4328AID588453
ATAD5 protein, partialHomo sapiens (human)Potency1.45750.004110.890331.5287AID493106
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency0.19160.531815.435837.6858AID504845
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.63100.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.12670.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00350.540617.639296.1227AID2364; AID2528
D(1A) dopamine receptorHomo sapiens (human)Potency4.10920.02245.944922.3872AID488982
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency19.95260.010039.53711,122.0200AID1479
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency1.12200.794321.275750.1187AID624246
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency0.07940.010323.856763.0957AID2662
gemininHomo sapiens (human)Potency1.12200.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.05730.005612.367736.1254AID624032
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency2.81570.891312.067628.1838AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency31.62280.015812.3113615.5000AID1461
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
[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)Ki0.11650.00090.89545.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.11650.00090.89545.6234AID1184359; AID71287
Histone deacetylase 3Homo sapiens (human)Ki8.19000.00020.42378.1900AID447579
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)0.02920.00001.01016.8100AID71390; AID71392; AID71399; AID71401
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.11650.00000.21085.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.11650.00090.83985.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.11650.00000.18819.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.505710.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki700.02470.00020.561410.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.497310.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki700.02470.00020.635210.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki700.02470.00020.621710.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.03320.00010.498810.0000AID270052; AID71429; AID71431; AID71435; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki700.02470.00020.675810.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.03230.00010.504610.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki700.02470.00020.646910.0000AID1638732; AID1638733; AID71568
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)2.15200.00132.22068.3000AID242571; AID242581; AID242582; AID242583; AID71429
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.11650.00010.20769.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki700.02470.00020.671210.0000AID1638732; AID1638733; AID71568
Sodium- and chloride-dependent GABA transporter 1Homo sapiens (human)IC50 (µMol)5.26230.01013.090310.0000AID1476513; AID1599050; AID1602654; AID205303
Sodium- and chloride-dependent taurine transporterHomo sapiens (human)IC50 (µMol)354.000010.0000182.0000354.0000AID1794824
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.11650.00010.24425.6234AID1184359; AID71287
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)2.51000.00321.79008.3000AID205447; AID71429
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)0.02000.00321.54318.3000AID71429
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)IC50 (µMol)10.32410.03712.19228.5114AID1544944; AID1736174; AID595473; AID722623; AID749115
Sodium- and chloride-dependent GABA transporter 2Mus musculus (house mouse)IC50 (µMol)20.72141.41255.26838.1283AID1736176; AID595474; AID749114
Sodium- and chloride-dependent GABA transporter 3Mus musculus (house mouse)IC50 (µMol)17.57431.54883.67618.1283AID1736177; AID595475; AID749113
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.11650.00010.25155.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.11650.00010.24015.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.11650.00000.28325.6234AID1184359; AID71287
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.02000.00321.54318.3000AID71429
Sodium- and chloride-dependent betaine transporterHomo sapiens (human)IC50 (µMol)15.87710.85116.052136.0000AID1476514; AID1476529; AID1476530; AID1476531; AID1476532; AID1476533; AID1476534; AID1476535; AID1476536; AID1476537; AID1476538; AID1476539; AID1476540; AID1476541; AID1476542; AID1476543; AID1476544; AID1476545; AID1476546; AID1476547; AID1476548; AID1476549; AID1476550; AID1476551; AID1476553; AID1476554; AID1476555; AID1599053; AID1794822; AID205304
Sodium- and chloride-dependent GABA transporter 3Homo sapiens (human)IC50 (µMol)5.39621.00004.13318.9200AID1476507; AID1476552; AID1599052; AID72446
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.11650.00020.37095.6234AID1184359; AID71287
Histone deacetylase 4Homo sapiens (human)Ki8.19000.00021.62559.1242AID447579
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.506510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki700.02470.00020.557710.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.505710.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki700.02470.00020.640310.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki700.02470.00020.570810.0000AID1638732; AID1638733; AID71568
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.11650.00090.89545.6234AID1184359; AID71287
Histone deacetylase 1Homo sapiens (human)Ki8.19000.00000.49888.1900AID447579
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.11650.00020.41199.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.11650.00090.89545.6234AID1184359; AID71287
Histone deacetylase 7Homo sapiens (human)Ki8.19000.00022.00059.5000AID447579
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
GABA theta subunitRattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Histone deacetylase 2Homo sapiens (human)Ki8.19000.00000.47098.1900AID447579
Polyamine deacetylase HDAC10Homo sapiens (human)Ki8.19000.00000.76878.1900AID447579
Histone deacetylase 11 Homo sapiens (human)Ki8.19000.00011.21478.1900AID447579
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.11650.00090.89545.6234AID1184359; AID71287
Histone deacetylase 8Homo sapiens (human)Ki8.19000.00020.75258.1900AID447579
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.03330.00010.507510.0000AID270052; AID71429; AID71431; AID71436; AID71443; AID71448; AID71830; AID71837; AID72296
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki700.02470.00020.656110.0000AID1638732; AID1638733; AID71568
Sodium- and chloride-dependent GABA transporter 2Homo sapiens (human)IC50 (µMol)26.00006.20006.20006.2000AID1599051
Histone deacetylase 6Homo sapiens (human)Ki8.19000.00010.41568.1900AID447579
Histone deacetylase 9Homo sapiens (human)Ki8.19000.00021.85209.0000AID447579
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.11650.00090.89545.6234AID1184359; AID71287
Histone deacetylase 5Homo sapiens (human)Ki8.19000.00021.29939.5000AID447579
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC50 (µMol)0.02920.00001.05326.8100AID71390; AID71392; AID71399; AID71401
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)Kd1.70000.60001.15001.7000AID71408
Hsf1 proteinMus musculus (house mouse)EC50 (µMol)195.00000.160024.4900236.5000AID2382
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)EC50 (µMol)0.53000.53001.87365.3700AID729173
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)20.76200.00112.000910.0000AID1184360; AID1248432; AID1599027; AID296924; AID406576; AID697071; AID724586; AID72923; AID733887
Gamma-aminobutyric acid receptor subunit alpha-6Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)EC50 (µMol)24.84960.07552.12458.0000AID296924; AID406576; AID697071; AID733887
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC50 (µMol)13.62890.00141.957810.0000AID1184360; AID1184366; AID1184368; AID1248432; AID1599027; AID1599031; AID1599033; AID296924; AID724586; AID724594; AID724595; AID72923; AID73084; AID73239; AID73365; AID73519; AID73542
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC50 (µMol)2.30000.01901.73677.0000AID729172
Gamma-aminobutyric acid receptor subunit gamma-2Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit deltaMus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)EC50 (µMol)0.52750.26911.09214.6000AID1184362; AID1599026; AID321738; AID406570; AID724585; AID733885
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)Kd1.70000.60001.53332.3000AID71408
Gamma-aminobutyric acid receptor subunit alpha-2Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit alpha-3Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit gamma-3Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC50 (µMol)26.78780.00301.65329.8000AID406576; AID697071; AID72923; AID73084; AID73239; AID73365; AID733887; AID73519; AID73542
Gamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)Kd1.70000.60001.23331.7000AID71408
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC50 (µMol)7.00910.00301.58219.8000AID1599033; AID406576; AID697071; AID733887; AID73519
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC50 (µMol)8.78180.01001.20095.6234AID1184368; AID406576; AID697071; AID724595; AID73239; AID733887
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC50 (µMol)10.15140.01201.17515.2000AID1184366; AID406576; AID697071; AID724594; AID73084; AID733887
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC50 (µMol)5.38240.00141.776810.0000AID1184360; AID1184366; AID1184368; AID1248432; AID1599027; AID1599031; AID1599033; AID406576; AID697071; AID724586; AID724594; AID724595; AID733887
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)EC50 (µMol)16.00090.07551.59585.2000AID1599031; AID406576; AID697071; AID73365; AID733887
Gamma-aminobutyric acid receptor subunit beta-1Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit alpha-1Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC50 (µMol)6.15000.01902.149910.0000AID366055; AID729172
Gamma-aminobutyric acid receptor subunit beta-3Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC50 (µMol)2.30000.01901.73677.0000AID729172
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)EC50 (µMol)10.02250.07551.19595.2000AID406576; AID697071; AID733887; AID73542
Gamma-aminobutyric acid receptor subunit alpha-5Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit piMus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit alpha-4Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Platelet glycoprotein VIHomo sapiens (human)Kd0.04110.04110.04110.0411AID1692270
Gamma-aminobutyric acid receptor subunit thetaMus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid receptor subunit gamma-1Mus musculus (house mouse)EC50 (µMol)14.30000.87101.02291.1749AID127636
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)EC50 (µMol)1.11500.07941.62765.3700AID406573; AID729173
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (294)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
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)
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
negative regulation of adenylate cyclase activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
neuron-glial cell signalingGamma-aminobutyric acid type B receptor subunit 2Homo 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)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
modulation of chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-1Homo 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)
signal transductionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
visual perceptionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
memorySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
associative learningSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
synapse organizationSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chemical synaptic transmissionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to toxic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to sucroseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to inorganic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to lead ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to purine-containing compoundSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to estradiolSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to cocaineSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to calcium ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
inorganic anion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chloride transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
positive regulation of cell differentiationSodium- and chloride-dependent taurine transporterHomo sapiens (human)
nitrogen compound transportSodium- and chloride-dependent taurine transporterHomo sapiens (human)
neurotransmitter transportSodium- and chloride-dependent taurine transporterHomo sapiens (human)
amino acid transportSodium- and chloride-dependent taurine transporterHomo sapiens (human)
taurine transmembrane transportSodium- and chloride-dependent taurine transporterHomo sapiens (human)
alanine transportSodium- and chloride-dependent taurine transporterHomo sapiens (human)
modulation of chemical synaptic transmissionSodium- and chloride-dependent taurine transporterHomo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent taurine transporterHomo sapiens (human)
amino acid import across plasma membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
import across plasma membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent taurine transporterHomo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent taurine transporterHomo 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)
amino acid transmembrane transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
glycine betaine transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent betaine transporterHomo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
response to xenobiotic stimulusSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
taurine transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 3Homo 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 transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 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)
response to hypoxia4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
copulation4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
locomotory behavior4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
response to xenobiotic stimulus4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
gamma-aminobutyric acid metabolic process4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
gamma-aminobutyric acid biosynthetic process4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
response to iron ion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
cerebellum development4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of heat generation4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of insulin secretion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
negative regulation of dopamine secretion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
response to nicotine4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
exploration behavior4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
response to ethanol4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
negative regulation of blood pressure4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of dopamine metabolic process4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
behavioral response to cocaine4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of uterine smooth muscle contraction4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of inhibitory postsynaptic potential4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of prolactin secretion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
positive regulation of aspartate secretion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
gamma-aminobutyric acid catabolic process4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo 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)
monoatomic ion transportProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid transportProton-coupled amino acid transporter 1Homo sapiens (human)
taurine transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
proline transportProton-coupled amino acid transporter 1Homo sapiens (human)
alanine transportProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid import across plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
glycine transportProton-coupled amino acid transporter 1Homo sapiens (human)
proline transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
proton transmembrane transportProton-coupled amino acid transporter 1Homo sapiens (human)
L-alanine transportProton-coupled amino acid transporter 1Homo 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)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo 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)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
positive regulation of platelet aggregationPlatelet glycoprotein VIHomo sapiens (human)
enzyme-linked receptor protein signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
platelet activationPlatelet glycoprotein VIHomo sapiens (human)
collagen-activated tyrosine kinase receptor signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
collagen-activated signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
platelet aggregationPlatelet glycoprotein VIHomo sapiens (human)
immune response-regulating signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
nitrogen compound transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
creatine transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
nitrogen compound transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid import across plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
osteoblast differentiationGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of cell population proliferationGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
positive regulation of glutamate secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of gamma-aminobutyric acid secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of epinephrine secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of dopamine secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
response to nicotineGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
response to ethanolGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of synaptic transmissionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
positive regulation of growth hormone secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
neuron-glial cell signalingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo 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)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (109)

Processvia Protein(s)Taxonomy
GABA-A receptor activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
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)
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
protein bindingGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
protein heterodimerization activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
transmembrane signaling receptor activityGamma-aminobutyric acid type B receptor subunit 2Homo 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 rho-1Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
protein-containing complex bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-1Homo 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 rho-2Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
identical protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
metal ion bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid:sodium symporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
taurine transmembrane transporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
taurine:sodium symporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
amino acid transmembrane transporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent taurine transporterHomo sapiens (human)
alanine transmembrane transporter activitySodium- and chloride-dependent taurine transporterHomo 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)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
protein bindingSodium- and chloride-dependent betaine transporterHomo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transmembrane transporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
taurine:sodium symporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
amino acid bindingSodium- and chloride-dependent GABA transporter 3Homo 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)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 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)
4-aminobutyrate transaminase activity4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
pyridoxal phosphate binding4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
succinate-semialdehyde dehydrogenase binding4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
4-aminobutyrate:2-oxoglutarate transaminase activity4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
identical protein binding4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
metal ion binding4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
(S)-3-amino-2-methylpropionate transaminase activity4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
iron-sulfur cluster binding4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo 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)
amino acid:proton symporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
proline:proton symporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
taurine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
protein bindingProton-coupled amino acid transporter 1Homo sapiens (human)
amino acid transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
alanine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
L-alanine transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
L-proline transmembrane transporter activityProton-coupled amino acid transporter 1Homo sapiens (human)
glycine transmembrane transporter activityProton-coupled amino acid transporter 1Homo 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)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo 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)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
transmembrane signaling receptor activityPlatelet glycoprotein VIHomo sapiens (human)
protein bindingPlatelet glycoprotein VIHomo sapiens (human)
collagen bindingPlatelet glycoprotein VIHomo sapiens (human)
signaling receptor activityPlatelet glycoprotein VIHomo sapiens (human)
collagen receptor activityPlatelet glycoprotein VIHomo sapiens (human)
protein tyrosine kinase bindingPlatelet glycoprotein VIHomo sapiens (human)
amino acid:sodium symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
creatine transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine:sodium symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
protein bindingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
protein heterodimerization activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
extracellular matrix protein bindingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo 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)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (91)

Processvia Protein(s)Taxonomy
cellular_componentGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
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)
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
cytoplasmGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
G protein-coupled GABA receptor complexGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
G protein-coupled receptor heterodimeric complexGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid type B receptor subunit 2Homo 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 gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
glutamatergic synapseGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-1Homo 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)
plasma membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
neuronal cell bodySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
cell surfaceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membrane protein complexSodium- and chloride-dependent taurine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
apical plasma membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
dendriteSodium- and chloride-dependent taurine transporterHomo sapiens (human)
microvillus membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
neuronal cell bodySodium- and chloride-dependent taurine transporterHomo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent taurine transporterHomo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent taurine transporterHomo sapiens (human)
cell projectionSodium- and chloride-dependent taurine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent taurine transporterHomo 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 membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
presynapseSodium- and chloride-dependent betaine transporterHomo sapiens (human)
cell projectionSodium- and chloride-dependent betaine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
cell projectionSodium- and chloride-dependent GABA transporter 3Homo 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)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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)
mitochondrion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
mitochondrial matrix4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
4-aminobutyrate transaminase complex4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
mitochondrion4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo 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)
lysosomal membraneProton-coupled amino acid transporter 1Homo sapiens (human)
endoplasmic reticulumProton-coupled amino acid transporter 1Homo sapiens (human)
plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
apical plasma membraneProton-coupled amino acid transporter 1Homo sapiens (human)
vacuolar membraneProton-coupled amino acid transporter 1Homo 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)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo 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)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
membrane raftPlatelet glycoprotein VIHomo sapiens (human)
plasma membranePlatelet glycoprotein VIHomo sapiens (human)
cell surfacePlatelet glycoprotein VIHomo sapiens (human)
extracellular exosomePlatelet glycoprotein VIHomo sapiens (human)
tetraspanin-enriched microdomainPlatelet glycoprotein VIHomo sapiens (human)
plasma membranePlatelet glycoprotein VIHomo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
extracellular exosomeSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
presynapseSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
cell projectionSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
extracellular spaceGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
endoplasmic reticulum membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
synaptic vesicleGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
axolemmaGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
mitochondrial membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
dendritic spineGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
dendritic shaftGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
Schaffer collateral - CA1 synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
glutamatergic synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled GABA receptor complexGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled receptor heterodimeric complexGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo 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)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (383)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
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.
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
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID366056Activity at rat GABAA alpha-1F64C-beta-2 receptor mutant expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID1599052Inhibition of human GAT3 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID1164681Displacement of [3H]flunitrazepam form benzodiazepine receptor in rat cerebral cortex assessed as specific radio-ligand binding level at 1 uM incubated for 20 mins by liquid scintillation counting method2014European journal of medicinal chemistry, Oct-30, Volume: 86Studies on the anticonvulsant activity of 4-alkyl-1,2,4-triazole-3-thiones and their effect on GABAergic system.
AID71720Binding affinity towards [3H]GHB binding site at 10 uM1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of gamma-hydroxybutyric acid. Synthesis and binding studies.
AID497827Protection against fragile X syndrome phenotypes in Fmr1 null mutant Drosophila Fmr1'3/TM6C assessed as embryo viability at 40 uM at 25 degC by flow cytometry relative to untreated homozygous embryos2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID296921Agonist activity at human GABAC rho 1 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID1736176Inhibition of mouse GTA 3 receptor2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
AID724596Agonist activity at human GABAA alpha5beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
AID739648Cytotoxicity against triple-negative human Hs578T cells assessed as growth inhibition after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
A novel metformin derivative, HL010183, inhibits proliferation and invasion of triple-negative breast cancer cells.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1476550Inhibition of human BGT1 Y453A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID366040Agonist activity at rat recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID297971Antagonist activity at human glycine alpha-1 receptor in HEK293 cells by FMP assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID1476544Inhibition of human BGT1 Q378P mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID134937Evaluation of General motor activity in mouse at dose 200 mg/kg1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID711587Lipophilicity, log P of the compound2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID595509Selectivity ratio of pIC50 for mouse GAT3 topIC50 for mouse GAT12011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID447579Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.
AID71435In vitro inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID1476536Inhibition of human BGT1 A328G mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID179766In vitro inhibition of GABA uptake in rat brain synaptic membranes1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID296916Agonist activity at GABAC rho 1 receptor expressed in tsA-201 cells by FMP assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID1137326Dissociation constant, pKa of the compound1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
AID21243Partition coefficient of the compound1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor gamma-vinyl-GABA.
AID366360Agonist activity at rat GABAA alpha-1R66C-beta-2 receptor mutant expressed in Xenopus laevis oocytes assessed as inhibition of induction of current at -60 mV at 35 mM by Two-Electrode voltage clamp method in presence of 2 mM 2-sulfonatoethyl methanethiosu2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID1476513Inhibition of human GAT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID681145TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Genomics, Jan, Volume: 79, Issue:1
The human T-type amino acid transporter-1: characterization, gene organization, and chromosomal location.
AID139780Onset for sleeping time after administration in mice induced by sodium pentobarbital1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID338176Displacement of [3H]GABA from GABAB receptor in presence of isoguvacine assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID1184366Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID111648Percentage decrease in general motor activity with respect to vehicle-injected control in mice at a dose of 30 mg/kg after ip administration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID724585Agonist activity at human GABAA rho1 receptor expressed in TSA201 cells after 1 min by FLIPR assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
AID296914Agonist activity at human GABAC rho 1 receptor expressed in HEK293 cells by FMP assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID73068Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID128118Uptake of the [14C]-compound in mouse liver 5 minutes after ip administration of 160 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1476537Inhibition of human BGT1 V336A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID296925Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID1476543Inhibition of human BGT1 F367Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID722623Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.
AID1476514Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID366038Agonist activity at rat recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID71399Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
AID128121Uptake of the [14C]-compound in mouse liver 5 minutes after iv administration of 30 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID71448Inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptosomal membranes1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
AID1476535Inhibition of human BGT1 F324C mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476552Inhibition of human GAT3 S468Y mutant expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID128111Uptake of the [14C]-compound in mouse brain 5 minutes after ip administration of 160 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID71391In vitro binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptic membranes at pH 7.41990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline.
AID1638732Displacement of [3H]muscimol from orthosteric binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID1638733Displacement of [3H]NCS-382 from high-affinity GHB binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID462613Permeability across artificial membrane assessed as membrane retention at 200 uM by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID752245Binding affinity to GABA receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID136515Latency to the onset of generalized clonic epileptic seizures by picrotoxin was measured and evaluated as a percent of the control in mice.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID129381Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after ip administration of 210 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1599026Agonist activity at recombinant human GABA-A rho-1 receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID724594Agonist activity at human GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
AID296915Agonist activity at human GABAC rho 1 receptor expressed in HEK293 cells by FMP assay relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID72446Inhibitory activity against human sodium and chloride dependent GABA transporter 31994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
AID1476548Inhibition of human BGT1 I386F mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID366359Agonist activity at rat GABAA alpha-1S68C-beta-2 receptor mutant expressed in Xenopus laevis oocytes assessed as reduction of induction of current at -60 mV at 65 uM by Two-Electrode voltage clamp method in presence of 450 uM 2-sulfonatoethyl methanethios2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID129380Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after ip administration of 160 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1599050Inhibition of human GAT1 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID71433In vitro effect on GABA uptake in a crude preparation of synaptosomes from rat brain.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
AID71443Inhibitory effect was measured for [3H]GABA-uptake from rat synaptosomal membrane1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Synthesis of alkyl-substituted arecoline derivatives as gamma-aminobutyric acid uptake inhibitors.
AID1476533Inhibition of human BGT1 K317R mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID242571H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
AID227716Brain-uptake index (BUI) was determined for the compound in rat1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID366041Agonist activity at rat recombinant GABAA alpha-4-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID205303Inhibitory activity against human GABA transporter-1 (hGAT1)1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
AID1184368Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID1599028Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells assessed as GABA-induced maximum response incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue 2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID73502Compound was tested for the inhibitory effect against Gamma-amino-N-butyrate transaminase from pig brain, activity expressed as Km1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
4-Amino-2-(substituted methyl)-2-butenoic acids: substrates and potent inhibitors of gamma-aminobutyric acid aminotransferase.
AID205304Inhibition of human GABA transporter (hBGT-1) activity.1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
AID71442Inhibition of 2 nM [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor in rat brain crude synaptic membranes1982Journal of medicinal chemistry, Feb, Volume: 25, Issue:2
Aminomethyl-1,2,4-benzothiadiazines as potential analogues of gamma-aminobutyric acid. Unexpected discovery of a taurine antagonist.
AID296923Agonist activity at rat GABA alpha-1-T129S-beta-2-gamma-2 receptor mutant expressed in HEK293 cells by Whole-cell patch-clamp technique relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID71421Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane at 0.022-0.039 uM1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1599053Inhibition of human BGT1 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID296918Agonist activity at GABAC rho 1 receptor S168T mutant expressed in tsA-201 cells by FMP assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID20536Solubility in pH 5.0 phosphate buffer (0.1 M) at 37 degrees Centigrade.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID729172Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Evaluation of difluoromethyl ketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor.
AID129382Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after ip administration of 60 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID72923Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID733885Agonist activity at GABAC rho1 receptor (unknown origin)2013ACS medicinal chemistry letters, Apr-11, Volume: 4, Issue:4
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.
AID724595Agonist activity at human GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
AID595482Selectivity ratio of pIC50 for mouse GAT3 to pIC50 for mouse GAT22011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID296917Agonist activity at GABAC rho 1 receptor expressed in tsA-201 cells by FMP assay relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID73084Agonist activity on human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID25082pKA value was determined; Experiment 21982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
AID71436In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID227711Brain penetration index calculated as ([Brain]/[Liver])x100 @ 5 min after sc administration in mice at 3-39 mg/kg1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor gamma-vinyl-GABA.
AID1476541Inhibition of human BGT1 Q346Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID366058Activity at rat GABAA alpha-1S68C-beta-2 receptor mutant expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID40838Percent inhibition of [3H]- Diazepam binding to GABA-A Benzodiazepine receptor of rat frontal cortex membranes (ND = no data)1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1184359Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID497836Suppression of glutamate-induced Futsch protein overexpression in head lysates of laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model at 40 uM by Western blot2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID181196In vivo pentobarbital (30 mg/kg ip)-induced hypnosis in rats after intracerebroventricular administration at a dose of 3.90 uL2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
Synthesis and biological evaluation of GABA derivatives able to cross the blood-brain barrier in rats.
AID128117Uptake of the [14C]-compound in mouse liver 5 minutes after ip administration of 120 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID111695BPI index was determined at 5 min after subcutaneous administration1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
gamma-Aminobutyric acid esters. 2. Synthesis, brain uptake, and pharmacological properties of lipid esters of gamma-aminobutyric acid.
AID1476538Inhibition of human BGT1 V337I mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476549Inhibition of human BGT1 Y453S mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID751884Binding affinity to GABA receptor (unknown origin) by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID595473Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID267284Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
AID111523Tested for the quanitity of [14C]-labeled (radioactivity) compound taken up into the brain following subcutaneous injection1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID296924Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID1476534Inhibition of human BGT1 A321M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1599031Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID1476555Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID191876Vmax was measured for [3H]GABA-uptake from rat synaptosomal membrane.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Synthesis of alkyl-substituted arecoline derivatives as gamma-aminobutyric acid uptake inhibitors.
AID366055Activity at rat wild type GABAA alpha-1-beta-2 receptor expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID366358Agonist activity at rat GABAA alpha-1F64C-beta-2 receptor mutant expressed in Xenopus laevis oocytes assessed as reduction of induction of current at -60 mV at 3.6 mM by Two-Electrode voltage clamp method in presence of 10 uM 2-sulfonatoethyl methanethios2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID71408Agonist activity against Gamma-aminobutyric acid type C (GABA-C) receptor derived from bovine retinal RNA expressed in Xenopus oocytes2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.
AID196024Concentration inhibiting GABA uptake rat brain synaptosomes.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID286351Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat cerebral cortex membranes2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
AID366039Agonist activity at rat recombinant GABA alpha-2-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID129390Evaluation of Brain Penetration Index in mouse1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1544944Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1).
AID733887Agonist activity at GABAA receptor (unknown origin)2013ACS medicinal chemistry letters, Apr-11, Volume: 4, Issue:4
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.
AID129383Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after iv administration of 30 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1602654Inhibition of human GAT1 expressed in COS cells assessed as decrease in [3H]GABA uptake after 10 mins by scintillation counting analysis2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.
AID595483Selectivity ratio of pIC50 for mouse GAT3 to pIC50 for mouse GAT42011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID26352Dissociation constant (pKa)1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
AID406576Agonist activity at human alpha-1-beta-2-gamma-2L GABAA receptor expressed in Xenopus oocytes assessed as inhibition of current production by two electrode voltage clamp method2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
AID16862Partition coefficient in 1-octanol/water system measured using radio active compounds1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID385594Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A,S343A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method2007The 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.
AID25820PKa values of the compound1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID346419Displacement of radiolabeled GABA from GABA receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID73490Compound was tested for the inhibition of Gamma-amino-N-butyrate transaminase (GABA-AT)1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.
AID73519Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID297970Antagonist activity at human rho1 GABAc receptor in HEK293 cells by FMP assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID73362Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID1476553Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1285631Displacement of [3H]GABA from rat cerebral cortex GABA receptor2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID71396Displacement of [3H]-GABA from Gamma-aminobutyric acid type B receptor in rat brain membranes1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Stereoselective syntheses of the trans-decahydroquinoline-5-carboxylic acid epimers. Diastereomeric zwitterionic probes of gamma-aminobutyric acid related biological properties in vitro and in vivo.
AID630741Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Three-dimensional quantitative structure-activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1).
AID749115Inhibition of mouse GAT1 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
AID1476530Inhibition of human BGT1 Q299L mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID749112Inhibition of mouse GAT4 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
AID198301Cleavage rate against hairpin ribozyme at 2 mM, in presence of 0.5 uM magnesium ions2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Novel spermine-amino acid conjugates and basic tripeptides enhance cleavage of the hairpin ribozyme at low magnesium ion concentration.
AID1476507Inhibition of human GAT3 L314Q mutant expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID52376Ability to inhibit potassium induced transmitter release in cerebellar granule cells expressing high affinity GABA receptors at 55 mM KCl1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
AID71275In vitro effect on Gamma-aminobutyric acid agonism on single neurons of cat spinal cord (--- is similar activity to GABA)1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
AID71431In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
AID242581H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
AID406570Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
AID1184725Displacement of [3H]CGP54626 from recombinant HA-tagged GB1 subunit/Flag-tagged GB2 subunit receptor (unknown origin) expressed in CHO cells by scintillation proximity assay2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Discovery of a Negative Allosteric Modulator of GABAB Receptors.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID180670Inhibition of high affinity neuronal GABA uptake by synaptosomes of rat brain membrane1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
AID242583H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1638747Displacement of [3H]NCS382 from high-affinity GHB binding site of alpha4betadelta receptor in mouse brain membranes2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID140740Sleeping time in mice after administration in mice induced by sodium pentobarbital1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID71437In vitro inhibition of [3H]THIP binding to Gamma-aminobutyric acid receptor in rat brain synaptic membranes1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID71549Agonistic activity Gamma-aminobutyric acid A receptor chloride uptake, full agonist2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist.
AID1476554Inhibition of human BGT1/human GAT3 chimera C expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476547Inhibition of human BGT1 I386M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID296919Agonist activity at GABAC rho 1 receptor S168T mutant expressed in tsA-201 cells by FMP assay relative to GABA2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID205447Inhibitory activity against rat GABA transporter-2 (rGAT2)1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
AID72156In vitro binding affinity against Gamma-aminobutyric acid A receptor in rat brain synaptic membranes at pH 7.11990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline.
AID1476542Inhibition of human BGT1 S353A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID16864Partition coefficient in octanol/water system was determined using [14C]-labeled compounds.1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID724586Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
AID71998Inhibition of [3H]muscimol binding to GABA-A receptor from rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID73512Percent of enzyme inhibition by Gamma-amino-N-butyrate transaminase assay method; ND means no data1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1476551Inhibition of human BGT1 Y453S/Y454A double mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID179593In vitro inhibition of [3H]GABA uptake in rat Hippocampal slices.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake.
AID739647Cytotoxicity against triple-negative human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
A novel metformin derivative, HL010183, inhibits proliferation and invasion of triple-negative breast cancer cells.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID689059Activity of pig GABA aminotransferase using alpha-ketoglutarate as substrate after 16 hrs by Hanes-Woolf plot analysis2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase.
AID128119Uptake of the [14C]-compound in mouse liver 5 minutes after ip administration of 210 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID71401Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID1476532Inhibition of human BGT1 H312N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID227951Compound was evaluated for kinetic constant Kcat/Km1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.
AID52378Ability to inhibit potassium induced transmitter release in cerebellar granule cells expressing high and low affinity GABA receptors at 55 mM KCl1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
AID73474Compound was tested for the inhibitory effect against Gamma-amino-N-butyrate transaminase from bacteria, activity expressed as Km1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
4-Amino-2-(substituted methyl)-2-butenoic acids: substrates and potent inhibitors of gamma-aminobutyric acid aminotransferase.
AID48904BMC-sensitive inhibitory effect on cat spinal neurons relative to that of GABA was expressed in vivo as relative potency; Equal activity1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID1476545Inhibition of human BGT1 S381A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID297969Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID1692270Binding affinity to human platelet lysate GP6 at 0.1 uM by surface plasmon resonance analysis2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1476539Inhibition of human BGT1 I340V mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
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.
AID128114Uptake of the [14C]-compound in mouse brain 5 minutes after iv administration of 30 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1476546Inhibition of human BGT1 C382T mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID229945I/U ratio for neutral amino acids.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
AID184436Km was measured for [3H]GABA-uptake from rat synaptosomal membrane.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Synthesis of alkyl-substituted arecoline derivatives as gamma-aminobutyric acid uptake inhibitors.
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.
AID73542Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-22001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID1476531Inhibition of human BGT1 K310N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID447578Inhibition of HDAC in human Hela cells nuclear extracts assessed as residual activity at 500 uM by fluorimetric assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.
AID198302Cleavage rate against hairpin ribozyme at 5 mM with 0.5 uM magnesium ions2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Novel spermine-amino acid conjugates and basic tripeptides enhance cleavage of the hairpin ribozyme at low magnesium ion concentration.
AID497839Suppression of glutamate-induced beta-lobe midline crossing deffect in mushroom bodies of laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model at 40 uM by Fas2 staining based confocal microscopy2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID751744Displacement of [3H]Muscimol from central-type GABAA receptor muscimol binding site in Wistar rat brain at 10 uM after 10 mins relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID270052Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat spinal cord2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
AID1736175Inhibition of mouse GTA 2 receptor2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
AID497840Suppression of glutamate-induced beta-lobe midline crossing deffect in mushroom bodies of laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model assessed as incidence of severe deffects at 40 uM by Fas2 staining b2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID1476529Inhibition of human BGT1 F295Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID72296Inhibition of [3H]GABA binding to gamma-aminobutyric-acid A (GABA-A) receptor1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and biochemical evaluation of baclofen analogues locked in the baclofen solid-state conformation.
AID25081pKA value was determined; Experiment 11982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
AID689060Ratio of Kcat to Km for pig GABA aminotransferase2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase.
AID733886Agonist activity at GABAB receptor (unknown origin)2013ACS medicinal chemistry letters, Apr-11, Volume: 4, Issue:4
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.
AID711528Activity of GABA aminotransferase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1184370Agonist activity at human GABAAalpha5beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID234828Survival ratio was calculated for determination of dose dependency.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID71562Displacement of [3H]-GABA from Gamma-aminobutyric acid A receptor in rat brain membranes1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Stereoselective syntheses of the trans-decahydroquinoline-5-carboxylic acid epimers. Diastereomeric zwitterionic probes of gamma-aminobutyric acid related biological properties in vitro and in vivo.
AID1184362Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID144355In vitro inhibition of N8-Acetylspermidine deacetylase from rat liver cytosol(apparent Ki)1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Inhibition of N8-acetylspermidine deacetylase by active-site-directed metal coordinating inhibitors.
AID1599029Agonist activity at recombinant human GABA-A alpha3beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID242582H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
AID71837Inhibition of [3H]muscimol binding to gamma-aminobutyric-acid A (GABA-A) receptor1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
AID385593Activity at human GABAA alpha1beta2 S410A-gamma-2-LS327A,S343A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method2007The 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.
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.
AID73365Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-4-beta-3-gamma-22001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID406573Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
AID296922Agonist activity at rat GABA alpha-1-T129S-beta-2-gamma-2 receptor mutant expressed in HEK293 cells by Whole-cell patch-clamp technique2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID128120Uptake of the [14C]-compound in mouse liver 5 minutes after ip administration of 60 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID22614Maximal rate constant was determined1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Inactivation of gamma-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acid.
AID233587Ratio of IC50 for GABA-B and GABA-A receptors1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID128122Uptake of the [14C]-compound in mouse liver 5 minutes after sc administration of 270 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID385592Activity at human GABAA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method2007The 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.
AID286350Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat spinal cord brainstem membranes2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
AID751679Displacement of [3H]Muscimol from central-type GABAA receptor muscimol binding site in Wistar rat brain after 10 mins2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID71297Percent displacement of [3H]GABA at Gamma-aminobutyric acid receptor of rat brain membranes at 0.01 uM1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
Epimeric cis-decahydroquinoline-5-carboxylic acids: effects on gamma-aminobutyric acid uptake and receptor binding in vitro.
AID181332In vivo pentobarbital (30 mg/kg ip)-induced hypnosis in rats after iv administration at a dose of 92 umol2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
Synthesis and biological evaluation of GABA derivatives able to cross the blood-brain barrier in rats.
AID337892Displacement of [3H]GABA from GABAB receptor in presence of isoguvacine1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID366060Ratio of EC50 for rat wild type GABAA alpha-1-beta-2 receptor over EC50 for rat GABAA alpha-1F64C-beta-2 receptor mutant by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID180320Inhibitory concentration that suppress the CA1 population spike in rat hippocampus slices1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor gamma-vinyl-GABA.
AID74657Percent of enzyme inhibition by Glutamate decarboxylase assay method; ND means no data1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID52375Ability to inhibit potassium induced transmitter release in cerebellar granule cells expressing high affinity GABA receptors at 30 mM KCl1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
AID16860Octanol:water partition coefficient is evaluated1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
gamma-Aminobutyric acid esters. 2. Synthesis, brain uptake, and pharmacological properties of lipid esters of gamma-aminobutyric acid.
AID73483Compound was tested for the inhibition of Gamma-amino-N-butyrate transaminase (GABA-AT)1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.
AID1687096Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to depolarizing pulse at 10 uM by whole cell patch clamp assay relative to contr2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Targeting of N-Type Calcium Channels via GABA
AID73492Michaelis-Menten constant of the compound.1999Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
2,6-Difluorophenol as a bioisostere of a carboxylic acid: bioisosteric analogues of gamma-aminobutyric acid.
AID340244Inhibition of GABA receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID1336324Displacement of [3H]GABA from rat cerebral cortex GABA receptor at 100 uM2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID23728Apparent partition coefficient between 1-octanol and pH 5.0 phosphate buffer (0.1 M) at 37 degrees Centigrade.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID383684Effect on D-amphetamine-induced hyperactivity in Wistar rat at 1 mg/kg, po2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID1736174Inhibition of mouse GTA 1 receptor2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
AID296920Agonist activity at human GABAC rho 1 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
AID366043Agonist activity at rat recombinant GABAA alpha-6-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID595476Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID73368Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-4-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID71392Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID184167Percent inhibition of high affinity [3H]GABA uptake into rat brain synaptosomes at 10 uM1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
Epimeric cis-decahydroquinoline-5-carboxylic acids: effects on gamma-aminobutyric acid uptake and receptor binding in vitro.
AID128113Uptake of the [14C]-compound in mouse brain 5 minutes after ip administration of 60 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1736177Inhibition of mouse GTA4 receptor2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
AID462611Effective permeability across artificial membrane at 200 uM by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID73218Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID366062Ratio of EC50 for rat wild type GABAA alpha-1-beta-2 receptor over EC50 for rat GABAA alpha-1S68C-beta-2 receptor mutant by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID179937Inhibition of GABA uptake from rat diencephalon-midbrain,1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID595475Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID52377Ability to inhibit potassium induced transmitter release in cerebellar granule cells expressing high and low affinity GABA receptors at 30 mM KCl1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
AID128112Uptake of the [14C]-compound in mouse brain 5 minutes after ip administration of 210 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID1476540Inhibition of human BGT1 S345A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID72436In vitro GABA uptake was determined in synaptosome suspensions1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline.
AID497833Cytoprotection against glutamate-induced toxicity in laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model assessed as genetic segregation ratio at 40 uM by flow cytometry relative to untreated embryos2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID497828Protection against fragile X syndrome phenotypes in laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C assessed as homozygous Fmr1-/- embryo viability at 40 uM at 25 degC by flow cytometry relative to untreated homozygous embryos fed 2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID697071Agonist activity at human alpha1beta2gamma2L GABAA receptor expressed in Xenopus oocytes assessed as potentiation of channel current response by two-electrode voltage clamp electrophysiology assay2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID136516Latency to the protection against lethality by picrotoxin was measured and evaluated as a percent of the control in mice.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives.
AID595474Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
AID1599033Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID497835Cytoprotection against glutamate-induced toxicity in laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model assessed as embryo viability at 40 uM in presence of GABAB receptor antagonist CGP-54626 by flow cytometr2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID128110Uptake of the [14C]-compound in mouse brain 5 minutes after ip administration of 120 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID462612Permeability across artificial membrane assessed as compound transport at 200 uM after 4 hrs by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID128116Uptake of the [14C]-compound in mouse brain 5 minutes after sc administration of 380 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID73239Agonist activity on human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
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.
AID72002Inhibition of [3H]GABA uptake in rat brain membranes1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Stereoselective syntheses of the trans-decahydroquinoline-5-carboxylic acid epimers. Diastereomeric zwitterionic probes of gamma-aminobutyric acid related biological properties in vitro and in vivo.
AID129385Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after sc administration of 270 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID124607Ability to penetrate the blood-brain barrier of mice was evaluated by measuring the brain penetration index (BPI) at dose 3-39 mg/Kg, administered subcutaneously; range is 0.04-1.811985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
gamma-Aminobutyric acid esters. 2. Synthesis, brain uptake, and pharmacological properties of lipid esters of gamma-aminobutyric acid.
AID1184360Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID366042Agonist activity at rat recombinant GABAA alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells assessed as induction of current by whole cell patch-clamp technique2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID181328In vivo pentobarbital (30 mg/kg ip)-induced hypnosis in rats after iv administration at a dose of 184 umol2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
Synthesis and biological evaluation of GABA derivatives able to cross the blood-brain barrier in rats.
AID1599027Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID124612Percent amount of compound was determined in liver per gram of tissue after 5 min of administration at a dose of 3-39 mg/Kg; range is 4.2-1651985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
gamma-Aminobutyric acid esters. 2. Synthesis, brain uptake, and pharmacological properties of lipid esters of gamma-aminobutyric acid.
AID71429Displacement of [3H]gamma-aminobutyric acid from sodium-independent Gamma-aminobutyric acid (GABA-A) receptor synaptic membrane binding sites from rat brain tissue1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
(+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid.
AID127636Activation of chloride ion uptake into mouse brain synaptoneurosomes2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist.
AID71822Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID71830Displacement of [3H]GABA from Gamma-aminobutyric acid A receptor ofrat brain membranes1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
AID1248432Partial agonist activity at GABAAalpha1beta2gamma2s receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as induction of chloride current by two-microelectrode voltage-clamp method2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Nitrogenated honokiol derivatives allosterically modulate GABAA receptors and act as strong partial agonists.
AID1164680Displacement of [3H]muscimol form GABAA receptor in rat cerebral cortex assessed as specific radio-ligand binding level at 1 uM incubated for 10 mins by liquid scintillation counting method2014European journal of medicinal chemistry, Oct-30, Volume: 86Studies on the anticonvulsant activity of 4-alkyl-1,2,4-triazole-3-thiones and their effect on GABAergic system.
AID127923Concentration of liver in mice after sc administration at 3-39 mg/kg; 4.17-65.05 nM/g1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor gamma-vinyl-GABA.
AID127921Concentration of brain in mice after sc administration at 3-39 mg/kg; 0.04-0.17 nM/g1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor gamma-vinyl-GABA.
AID18280Michaelis-Menten constant was determined1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Inactivation of gamma-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acid.
AID366061Ratio of EC50 for rat wild type GABAA alpha-1-beta-2 receptor over EC50 for rat GABAAalpha1F66Cbeta2 receptor mutant by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID297967Antagonist activity at human alpha-7 nAChR in tsA201 cells coexpressed with Ric3 by FMP assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID566253Inhibition of rat GABA receptor2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID128115Uptake of the [14C]-compound in mouse brain 5 minutes after sc administration of 270 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID71287Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of human cerebellar cortex preparation1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
AID71258Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID1599051Inhibition of human GAT2 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
AID749113Inhibition of mouse GAT3 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
AID497843Suppression of glutamate-induced courtship behavior deffect in laboratory prepared food feeded male Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model assessed as courtship behavior towards female flies at 40 uM for 10 mins by courtship inde2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID497834Cytoprotection against glutamate-induced toxicity in laboratory prepared food feeded Fmr1 null mutant Drosophila Fmr1'3/TM6C fragile X syndrome model assessed as embryo viability at 40 uM by flow cytometry relative to untreated embryos2008Nature chemical biology, Apr, Volume: 4, Issue:4
Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila.
AID729173Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Evaluation of difluoromethyl ketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor.
AID111657Tested for the quanitity of [14C]-labeled (radioactivity) compound taken up into the liver following subcutaneous injection1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID129379Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after ip administration of 120 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID71390Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor.1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
AID227713Ratio of the amount in brain as a percent of that present in liver at 5 min is expressed as Brain penetration index (BPI)1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
gamma-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation.
AID366057Activity at rat GABAA alpha-1R66C-beta-2 receptor mutant expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID749114Inhibition of mouse GAT2 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
AID366059Activity at rat GABAA alpha-1T129C-beta-2 receptor mutant expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID733540Displacement of [125I]-N-(p-I-Bn)-THAZ from 5HT2C in rat cerebral cortex membrane at 300 uM after 1 hr by scintillation counting analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.
AID71270Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-6-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID781327pKa (acid-base dissociation constant) as determined by Morgenthaler ref: ChemMedChem 20072014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID129386Brain penetration index is the ratio of the uptake in brain/liver X 100, 5 min after sc administration of 380 umol/kg of the [14C]-compound.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID179951Inhibition of [3H]GABA Binding to synaptic membranes from rat cerebellum in receptor binding assay1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID385595Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method2007The 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.
AID366063Ratio of EC50 for rat wild type GABAA alpha-1-beta-2 receptor over EC50 for rat GABAA alpha-1T129C-beta-2 receptor mutant by Two-Electrode voltage clamp method2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
AID71554Displacement of GABA activated [3H]diazepam binding in rat brain membranes1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Stereoselective syntheses of the trans-decahydroquinoline-5-carboxylic acid epimers. Diastereomeric zwitterionic probes of gamma-aminobutyric acid related biological properties in vitro and in vivo.
AID297968Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells by FMP assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID73533Maximal response relative to Gamma-aminobutyric acid A against human Gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 expressed in Xenopus oocytes2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
AID385596Activity at human GABAA alpha-1-beta-2-S410A-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method2007The 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.
AID128123Uptake of the [14C]-compound in mouse liver 5 minutes after sc administration of 380 umol/kg.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Gamma-aminobutyric acid esters. 1. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of gamma-aminobutyric acid.
AID321738Agonist activity at human recombinant GABAc rho1 receptor expressed in Xenopus laevis oocytes at -60mV by two-electrode voltage clamp method2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors.
AID267285Inhibition of [3H]GABA binding in GABAA receptor in rat brain synaptic membranes2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
AID71568Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of rat ganglion neurons1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
AID773896Displacement of [3H]-3-hydroxycyclopent-1-enecarboxylic acid from GHB binding site in Sprague-Dawley rat cerebral cortex at 1 mM after 1 hr by scintillation counting analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.
AID24201Partition coefficient (logD)1999Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21
Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.
AID270053Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat cerebral cortex2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
AID1347151Optimization of GU AMC 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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
AID1347154Primary screen GU AMC 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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1346001Rat GABAB1 (GABAB receptors)1997Nature, Mar-20, Volume: 386, Issue:6622
Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38,268)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909524 (24.89)18.7374
1990's8075 (21.10)18.2507
2000's9916 (25.91)29.6817
2010's8508 (22.23)24.3611
2020's2245 (5.87)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 61.78

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 Index61.78 (24.57)
Research Supply Index10.64 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index228.20 (26.88)
Search Engine Supply Index3.99 (0.95)

This Compound (61.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,423 (3.54%)5.53%
Reviews4,199 (10.44%)6.00%
Case Studies1,128 (2.80%)4.05%
Observational28 (0.07%)0.25%
Other33,437 (83.15%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Use of Gabapentin as Preanesthetic Medication in Oncologic Children Undergoing in Fast Procedures With Sevofluran [NCT03681574]Phase 4135 participants (Actual)Interventional2017-07-01Completed
Double Blind Evaluation of Gamma-aminobutyric Acid Tartarate 100 mg, Glutamic Acid 100 mg, Dibasic Calcium Phosphate 50 mg, Thiamine Nitrate 25 mg, Pyridoxine Chloride 10 mg and Cyanocobalamin 5 mcg Versus Ginger for Vertigo-kinetosis [NCT05221892]Phase 4334 participants (Actual)Interventional2021-11-22Completed
Plasmakinetics of GABA From Tomatoes as Compared to GABA From a Supplement, After a Single Oral Administration in Healthy Young Men [NCT04086108]12 participants (Actual)Interventional2019-11-04Completed
Vurdering af Perifere GABAA-receptorer Med Henblik på Lokal Smertelindring [NCT02928328]90 participants (Anticipated)Interventional2016-10-31Recruiting
A Phase I/II, 3-Arm, Open Label, Single Centre Study to Investigate the Safety and Effect of Oral GABA Therapy on Beta-Cell Regeneration in Type 1-diabetes Patients [NCT03635437]Phase 1/Phase 235 participants (Actual)Interventional2018-09-05Completed
An Open-label, Multi-center, 6-week, Sequential Cohort Study Designed to Determine the Safety and Tolerability of Two Dose Ranges of BL-1020 in Hospitalized Subjects With Chronic Schizophrenia or Schizo-affective Disorder [NCT00480571]Phase 290 participants (Anticipated)Interventional2007-06-30Completed
Effects Of Gamma Aminobutyric Acid On The Progression Of New Onset Juvenile [NCT01781884]60 participants (Anticipated)Interventional2013-01-31Recruiting
The Use of Glutamic Acid Decarboxylase (GAD)and Gamma-Amino Butyric Acid(GABA)in the Treatment of Type I Diabetes. [NCT02002130]Phase 1101 participants (Actual)Interventional2015-01-31Completed
Sleep, Pain and Aging: Potential Underlying Mechanisms [NCT04683640]Phase 2254 participants (Anticipated)Interventional2021-04-02Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]