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muscimol

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Description

Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita. [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 CID4266
CHEMBL ID273481
CHEBI ID7035
SCHEMBL ID149693
MeSH IDM0014231

Synonyms (89)

Synonym
HMS3266G03
5-(aminomethyl)-isoxazol-3-ol
ccris 3720
rcra waste number p007
pantherin
rcra waste no. p007
5-(aminomethyl)isoxazol-3-ol hydrate
hsdb 6036
nsc 333569
einecs 220-430-4
3-hydroxy-5-aminomethylisoxazole-agarin
c4h6n2o2
5-(aminomethyl)-3(2h)-isoxazolone
5-(aminomethyl)-1,2-oxazol-3-ol
chembl273481 ,
bdbm23183
5-aminomethyl-3-hydroxyisoxazole
3(2h)-isoxazolone, 5-(aminomethyl)-
3-hydroxy-5-aminomethylisoxazole
3-isoxazolol, 5-(aminomethyl)-
5-(aminomethyl)-3-isoxazolol
wln: t5noj c1z eq
pantherine
nsc333569
nsc-333569
5-aminomethyl-3-isoxyzole
agarine
agarin
NCGC00015459-01
NCGC00024526-01
lopac-g-019
tocris-0289
BIOMOL-NT_000255
SMP1_000201
BPBIO1_000926
UPCMLD00X18174-72-6:001
muscimol
2763-96-4
C08311
muscimol, powder
LOPAC0_000591
NCGC00024526-03
NCGC00024526-02
ZINC22064260 ,
NCGC00015459-05
5-(aminomethyl)isoxazol-3(2h)-one
chebi:7035 ,
5-(aminomethyl)-1,2-oxazol-3-one
d5m179ty2e ,
unii-d5m179ty2e
AKOS006223439
CCG-204680
NCGC00015459-03
NCGC00015459-04
NCGC00015459-02
BCP9000968
BCPP000154
FT-0629033
3-hydroxy-5-aminomethyl-isoxazole
[3h]muscimol
5-(aminomethyl)-2,3-dihydro-1,2-oxazol-3-one
gtpl4090
gtpl4259
muscimol [hsdb]
muscimol [mi]
AKOS022719658
SCHEMBL149693
5-(aminomethyl)isoxazol-3-one
5(aminomethyl)-3(2h)-isooxazolone
5-(aminomethyl)-1,2-oxazol-3(2h)-one
HB0887
mfcd00057894
DTXSID5041069
bdbm50052792
J-016833
SR-01000075619-3
DB12458
BCP23771
Q412504
[3 h]-muscimol
[3h]-muscimol
HMS3678F05
HMS3414F05
A14005
SDCCGSBI-0050573.P002
5-(aminomethyl)-1,2-oxazol-3-one.
M-241
3-hydroxy-5-aminomethyl-isoxazole;5-aminomethyl-3-isoxazolol;5-aminomethyl-3-hydroxy-isoxazole
EN300-333440

Research Excerpts

Overview

Muscimol is a psychoactive isoxazole derived from the mushroom. It is thought to be an agonist of gamma-aminobutyric acid (GABA)

ExcerptReferenceRelevance
"Muscimol is a psychoactive isoxazole derived from the mushroom "( Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABA
Akk, G; Evers, AS; Germann, AL; Pierce, SR; Steinbach, JH; Sugasawa, Y, 2020
)
2.35
"Muscimol is a gamma-aminobutyric acid receptor agonist that selectively and temporarily inhibits neurons. "( Convection-Enhanced Delivery of Muscimol Into the Bilateral Subthalamic Nuclei of Nonhuman Primates.
Argersinger, DP; Elias, WJ; Heiss, JD; Hong, CS; Lonser, RR; Ray-Chaudhury, A; Walbridge, S; Zaghloul, KA, 2019
)
2.24
"Muscimol is a potent gamma-aminobutyric acid-A receptor agonist that temporarily and selectively suppresses neurons. "( Image-guided convection-enhanced delivery of muscimol to the primate brain.
Asthagiri, AR; Heiss, JD; Lonser, RR; Walbridge, S, 2010
)
2.06
"Muscimol is a GABA A-agonist that causes rapid and reversible suppression of neurophysiological activity. "( Imaging the spread of reversible brain inactivations using fluorescent muscimol.
Allen, TA; Brown, TH; Kholodar-Smith, DB; Laubach, M; Narayanan, NS; Zhao, Y, 2008
)
2.02
"(2) Muscimol is a selective agonist for the increase in resting conductance, while baclofen is a selective agonist for the decrease in action potential duration."( Functional and pharmacological differences between two types of GABA receptor on embryonic chick sensory neurons.
Dunlap, K, 1984
)
0.75
"Muscimol is a potent agonist at GABA-inhibitory synapses in mammalian brain. "( Anticonvulsant effects of muscimol.
Collins, RC, 1980
)
2
"Muscimol is a gamma-aminobutyric acid (GABA) agonist."( Effect of muscimol microinjections into the prepositus hypoglossi and the medial vestibular nuclei on cat eye movements.
Cheron, G; Galiana, HL; Godaux, E; Mettens, P, 1994
)
1.41
"Muscimol, thought to be a agonist of gamma-aminobutyric acid (GABA), was administered to eight neuroleptic-free subjects with tardive dyskinesia. "( Improvement in tardive dyskinesia after muscimol therapy.
Chase, TN; Crayton, JW; Tamminga, CA, 1979
)
1.97
"Muscimol is a direct-acting GABA agonist that presumably substituted for the absent GABA at the interface between the degenerating striatonigral GABAergic terminals and the GABAergic receptors located on SNr neurons."( Rescuing neurons from trans-synaptic degeneration after brain damage: helpful, harmful, or neutral in recovery of function?
Lindner, MD; Schallert, T, 1990
)
1
"Muscimol was found to be a more potent stimulator of 36Cl- flux in the LS cerebellum, as compared to the SS cerebellum, but a similar maximal level of uptake was achieved in the two lines."( Gamma-aminobutyric acid and alcohol actions: neurochemical studies of long sleep and short sleep mice.
Allan, AM; Harris, RA, 1986
)
0.99

Effects

Muscimol has been regarded as a universal agonist for all gamma-aminobutyric acid type A receptor (GABA(A)-R) subtypes. It has served as a backbone in the design of GABA agonists devoid of effects on the GABA-metabolizing enzyme, GABA transaminase, and GABA uptake systems.

ExcerptReferenceRelevance
"Muscimol sometimes has a comparable effect, but alpha-aminoisobutyric acid and glycine do not."( Intraneuronal effects of inhibitory amino acids.
Constanti, A; Krnjević, K; Nistri, A, 1980
)
0.98
"Muscimol has served as a backbone in the design of GABA agonists devoid of effects on the GABA-metabolizing enzyme, GABA transaminase, and GABA uptake systems."( Psychoactive Isoxazoles, Muscimol, and Isoxazole Derivatives from the Amanita (Agaricomycetes) Species: Review of New Trends in Synthesis, Dosage, and Biological Properties.
Cruces, W; Docampo-Palacios, ML; Okhovat, A; Ramirez, GA; Ray, KP, 2023
)
1.93
"Muscimol has no effect on sensory perception, odor generalization, and nonassociative learning, indicating a specific role of GABA during associative conditioning."( Focal uncaging of GABA reveals a temporally defined role for GABAergic inhibition during appetitive associative olfactory conditioning in honeybees.
Mueller, U; Raccuglia, D, 2013
)
1.11
"Muscimol has been regarded as a universal agonist for all gamma-aminobutyric acid type A receptor (GABA(A)-R) subtypes. "( Prototypic GABA(A) receptor agonist muscimol acts preferentially through forebrain high-affinity binding sites.
Chandra, D; Halonen, LM; Hellsten, K; Homanics, GE; Korpi, ER; Linden, AM; Procaccini, C, 2010
)
2.08
"Muscimol has potent antiepileptic efficacy after transmeningeal administration in animals. "( Transmeningeal muscimol can prevent focal EEG seizures in the rat neocortex without stopping multineuronal activity in the treated area.
Artan, NS; Baptiste, SL; Darisi, S; Devinsky, O; French, JA; Kuzniecky, RI; Ludvig, N; Medveczky, G; Mirowski, P; Tang, HM, 2011
)
2.16
"Muscimol has been used to increase our knowledge of central GABAergic systems, CNS physiology, and behavior. "( Physiological and behavioral studies with muscimol.
DeFeudis, FV, 1980
)
1.97
"Muscimol sometimes has a comparable effect, but alpha-aminoisobutyric acid and glycine do not."( Intraneuronal effects of inhibitory amino acids.
Constanti, A; Krnjević, K; Nistri, A, 1980
)
0.98
"Muscimol in the SNr has the same general effect as bicuculline in the SC."( Modification of saccadic eye movements by GABA-related substances. II. Effects of muscimol in monkey substantia nigra pars reticulata.
Hikosaka, O; Wurtz, RH, 1985
)
1.22
"Muscimol has been also demonstrated to competitively inhibit 3H-tetrodotoxin binding with the same drug."( [Tetrodotoxin competition with muscimol for the gamma-aminobutyric acid receptor].
Karanova, MV; Kuznetsov, VI; Sadykov, AA; Tonkikh, AK,
)
1.14

Actions

Muscimol was found to inhibit [3H]DA release from ME in a bicuculline-sensitive, strychnine-insensitive manner. The drug failed to produce hyperactivity, however, when injected into rats who had previously received an electrolytic median raphe lesion.

ExcerptReferenceRelevance
"Muscimol infusion to inactivate the mid-septotemporal hippocampus, as compared to saline infusion, significantly decreased the peak frequency of the PDs induced by GBL, decreased 30-120 Hz hippocampal gamma power, and hastened the transition of PDs to 1-2 Hz slow waves."( The hippocampus participates in a pharmacological rat model of absence seizures.
Arcaro, J; Chu, L; Kuo, M; Ma, J; Mirsattari, SM; Stan Leung, L, 2016
)
1.16
"Muscimol did not increase punished drinking."( Effects of agents which enhance GABA-mediated neurotransmission on licking conflict in rats and exploration in mice.
Gardner, CR; Piper, DC, 1982
)
0.99
"Muscimol produced an increase in RSA frequency with an inverted U-shaped dose response curve in the range 0.0001 to 1.0 mg/kg with maximal effect at 0.001 mg/kg."( Effects of GABAA and GABAB receptor agonists on reticular-elicited hippocampal rhythmical slow activity.
Coop, CF; Lambie, I; McNaughton, N, 1991
)
1
"Muscimol failed to produce hyperactivity, however, when injected into rats who had previously received an electrolytic median raphe lesion."( Evidence against serotonin involvement in the hyperactivity produced by injections of muscimol into the median raphe nucleus.
Asin, KE; Klitenick, MA; Wirtshafter, D, 1987
)
1.22
"Muscimol can inhibit electrically induced release of tritiated material by approximately 75% with half maximal effects at 2 microM."( Modulation of acetylcholine release from rat striatal slices by the GABA/benzodiazepine receptor complex.
Karobath, M; Supavilai, P, 1985
)
0.99
"Muscimol was found to inhibit [3H]DA release from ME in a bicuculline-sensitive, strychnine-insensitive manner, but had no effect in NI."( Effects of GABA receptor agonists on [3H]dopamine release from median eminence and pituitary neurointermediate lobe.
Anderson, R; Mitchell, R, 1985
)
0.99

Treatment

Muscimol (0.05 mg/kg) per se significantly increased the locomotor activity of stressed mice, exerted significant anti anxiety effect and significantly reduced the oxidative damage. Pretreatment did not change D-AP5-induced anxiolytic-like behaviors but potentiated avoidance memory impairment.

ExcerptReferenceRelevance
"Muscimol pretreatment did not change D-AP5-induced anxiolytic-like behaviors but potentiated avoidance memory impairment."( The role of CA3 GABAA receptors on anxiolytic-like behaviors and avoidance memory deficit induced by NMDA receptor antagonists.
Farahizadeh, M; Nasehi, M; Zarrabian, S; Zarrindast, MR, 2016
)
1.16
"The muscimol treated, hemisection-SCI rats also exhibited increased hindpaw withdrawal thresholds and latencies."( Suppressed GABAergic signaling in the zona incerta causes neuropathic pain in a thoracic hemisection spinal cord injury rat model.
Cho, CB; Lee, YJ; Moon, HC; Park, YS, 2016
)
0.92
"Muscimol treatment did not modify any of the parameters evaluated."( Aging impairs the control of prefrontal cortex on the release of corticosterone in response to stress and on memory consolidation.
De Blas, M; Garrido, P; Giné, E; Mora, F; Santos, Á, 2012
)
1.1
"Muscimol treatment in the saline-exposed group increased the mount and intromission latencies."( Maternal exposure to picrotoxin modifies the response of the GABAA receptor during sexual behavior of adult male rat offspring.
Baso, AC; Bernardi, MM; Felicio, LF; Kirsten, TB; Prosdocimi, FC; Teodorov, E, 2012
)
1.1
"Muscimol treatment also markedly increased Fos expression in the arcuate nucleus, which connects reciprocally to the lateral/perifornical hypothalamic area."( Activation of a subpopulation of orexin/hypocretin-containing hypothalamic neurons by GABAA receptor-mediated inhibition of the nucleus accumbens shell, but not by exposure to a novel environment.
Baldo, BA; Daniel, RA; Gual-Bonilla, L; Kelley, AE; Landry, CF; Sijapati, K, 2004
)
1.04
"In muscimol treated animals, significantly fewer neurons expressed PV in the inhibited hemicortex, but as many CTB labelled corticospinal neurons were present as in controls, along with an equally large corticospinal projection from contralateral to the implant, significantly greater than in controls."( Spinal cord plasticity in response to unilateral inhibition of the rat motor cortex during development: changes to gene expression, muscle afferents and the ipsilateral corticospinal projection.
Bradley, PM; Clowry, GJ; Davies, BM; Gibson, CL; Upile, NS, 2004
)
0.84
"Muscimol treatment increased the use of the response strategy in a dose-dependent manner without influencing learning speed, indicating that muscimol modulated strategy and not learning ability."( Intrahippocampal muscimol shifts learning strategy in gonadally intact young adult female rats.
Korol, DL; McElroy, MW,
)
1.19
"This muscimol treatment resulted in a total blockade of all stereotyped behaviors normally elicited by systemic apomorphine or by intranigral muscimol."( Evidence that the nigrotegmental GABAergic projection mediates stereotypy induced by apomorphine and intranigral muscimol.
Childs, JA; Gale, K, 1983
)
0.93
"Muscimol pretreatment inhibited release evoked by K+ depolarization or by receptor-mediated stimulation with glutamate."( Muscimol increases acetylcholine release by directly stimulating adult striatal cholinergic interneurons.
Adams, DT; Gold, PE; Login, IS; Pal, SN, 1998
)
2.46
"The muscimol treatment, however, did not mimic the effects of perinatal estrogen treatment."( GABAergic influence on the development of the sexually dimorphic nucleus of male and female rats.
Bach, F; Flügge, G; Wuttke, W, 1992
)
0.76
"Muscimol pretreatment (dosages ranging from 0.025 to 1.3 mg/kg) induced a clear-cut potentiation of gnawing elicited by methylphenidate (10 or 20 mg/kg) as early as 8 days of age (experiments 3 and 4)."( Ontogeny of GABA-ergic and dopaminergic mediation of gnawing behavior in the mouse.
Tirelli, E, 1987
)
0.99
"Pretreatment with muscimol (0.26 nmol) also prevented the antinociceptive effect caused by morphine (1.1 nmol) when administered alone at the same site, indicating an interaction between GABAergic and opioidergic interneurons."( Nociceptive vocalization response in guinea pigs modulated by opioidergic, GABAergic and serotonergic neurotransmission in the dorsal raphe nucleus.
Ferreira, MD; Menescal-de-Oliveira, L, 2014
)
0.73
"The treatment with muscimol, a gamma amino butyric acid receptor-A (GABA(A)) agonist, mitigates the AD syndrome and vascular dementia."( GABAA receptor agonist mitigates homocysteine-induced cerebrovascular remodeling in knockout mice.
Kumar, M; Lominadze, D; Moshal, KS; Pushpakumar, SB; Sen, U; Tyagi, N; Tyagi, SC; Vacek, T, 2008
)
0.66
"Rats treated with muscimol in CA1 explored all the objects equally well, irrespective of place or presentation time."( Differential roles of the dorsal hippocampal regions in the acquisition of spatial and temporal aspects of episodic-like memory.
Barbosa, FF; Pontes, IM; Ribeiro, AM; Ribeiro, S; Silva, RH, 2012
)
0.7
"Pretreatment with muscimol, a selective GABA(A) receptor agonist, significantly suppressed the ethanol-induced upregulation of IP(3) R-1 protein and its mRNA, which was significantly abolished by bicuculline, a selective GABA(A) receptor antagonist."( Activation of GABA(A) receptors suppresses ethanol-induced upregulation of type 1 IP(3) receptors.
Kurokawa, K; Mizuno, K; Ohkuma, S, 2013
)
0.71
"Pretreatment with muscimol, a GABAA receptor agonist, attenuated hippocampal neuronal injury elicited by TBT."( Allopregnanolone-mediated protective effects of progesterone on tributyltin-induced neuronal injury in rat hippocampal slices.
Ishida, A; Ishihara, Y; Kawami, T; Yamazaki, T, 2013
)
0.71
"Pretreatment with muscimol, a GABAA receptor agonist, over a concentration range of 0.1-10microM 24h before the treatment with 10microM Abeta (25-35) showed concentration-dependent inhibition on the Abeta (25-35)-induced neuronal apoptotic death."( Chronic stimulation of GABAA receptor with muscimol reduces amyloid beta protein (25-35)-induced neurotoxicity in cultured rat cortical cells.
Ban, JY; Lee, BY; Seong, YH, 2005
)
0.91
"Treatment with muscimol (0.05 mg/kg) per se significantly increased the locomotor activity of stressed mice, exerted significant anti anxiety effect and significantly reduced the oxidative damage."( Gabapentin attenuates acute hypoxic stress-induced behavioral alterations and oxidative damage in mice: possible involvement of GABAergic mechanism.
Goyal, R; Kumar, A, 2008
)
0.69
"Pretreatment with muscimol (100 ng i.c.v.) drastically reduced the drinking responses to i.c.v."( Gabaergic stimulation inhibits central actions of angiotensin II: pressor responses, drinking and release of vasopressin.
Bles, F; Ganten, D; Lang, RE; Rettig, R; Schwab, NA; Unger, T, 1983
)
0.59
"Pretreatment with muscimol into either the ventral posterior piriform cortex or perirhinal cortex, protected against the bilateral clonic seizures evoked from the ipsilateral AT."( Posterior piriform and perirhinal cortex relay seizures evoked from the area tempestas: role of excitatory and inhibitory amino acid receptors.
Gale, K; Halonen, T; Tortorella, A; Zrebeet, H, 1994
)
0.61
"Treatment with muscimol significantly increased the ED50 to 1.2 +/- 0.21 U, for a potency ratio of 1.55 +/- 0.34 (t = 1.7, P < .05)."( Medical therapy for intracerebral hematoma with the gamma-aminobutyric acid-A agonist muscimol.
Jackson-Friedman, C; Lonzo-Doktor, L; Lyden, PD, 1997
)
0.86
"Pretreatment with muscimol 10 min before administration of carbachol prevented the carbachol-evoked blood pressure changes."( Effect of muscimol on cholinomimetic-induced cardiovascular responses in rats.
Aker, R; Gören, Z; Iskender, E; Oktay, S; Onat, F; Tellioğlu, T, 1998
)
1.03
"Pretreatment with muscimol (1.7--3.5 micromol/kg, s.c.) or L-PIA (0.1--0.3 micromol/kg, s.c.) antagonized the increase of W and reduction of SWS and REMS induced by s.c."( Increase of waking and reduction of NREM and REM sleep after nitric oxide synthase inhibition: prevention with GABA(A) or adenosine A(1) receptor agonists.
Jantos, H; Monti, D; Monti, JM, 2001
)
0.63
"Treatment with muscimol, haloperidol, atropine or physostigmine all decreased the LA of both aldrin nontolerant and control rats."( Aldrin-induced locomotor activity: possible involvement of the central GABAergic-cholinergic-dopaminergic interaction.
Jamaluddin, S; Poddar, MK,
)
0.47
"Rats treated with muscimol or MK-801 exhibited significantly better visual-spatial learning compared with saline-treated subjects (p less than 0.001)."( Protective effect of synaptic inhibition during cerebral ischemia in rats and rabbits.
Hedges, B; Lyden, PD, 1992
)
0.61
"Treatment with muscimol (1 mg/kg, i.p.), a GABA agonist, produced hypothermia in normal rats and prevented an increase in BT of heat-exposed rats."( Does GABA act through dopaminergic/cholinergic interaction in the regulation of higher environmental temperature-induced change in body temperature?
Biswas, S; Poddar, MK, 1990
)
0.62
"Treatment with muscimol (1 mg/kg, i.p.), a GABA agonist, produced hypothermia at room temperature (28 +/- 1 degree C) and resistance to increase the body temperature when exposed to higher temperature (40 +/- 1 degree C)."( Involvement of GABA in environmental temperature-induced change in body temperature.
Biswas, S; Poddar, MK, 1988
)
0.61

Toxicity

ExcerptReferenceRelevance
" A better understanding of the mechanism underlying these adverse effects should allow for the safer use of these agents and might clarify mechanisms underlying certain clinical disorders."( Muscimol prevents NMDA antagonist neurotoxicity by activating GABAA receptors in several brain regions.
Dikranian, K; Farber, NB; Jiang, X; Nemmers, B, 2003
)
1.76
"Long-term, periodic, transmeningeal muscimol delivery with the SPD is essentially a safe procedure."( Long-term behavioral, electrophysiological, and neurochemical monitoring of the safety of an experimental antiepileptic implant, the muscimol-delivering Subdural Pharmacotherapy Device in monkeys.
Baptiste, SL; Carlson, C; Devinsky, O; French, JA; Kuzniecky, RI; Ludvig, N; Medveczky, G; Stefanov, DG; Tang, HM; Vaynberg, JK; Vazquez-DeRose, J, 2012
)
0.86

Pharmacokinetics

ExcerptReferenceRelevance
"To assess pharmacodynamic and neurochemical aspects of tolerance, lorazepam (2 mg/kg/day), or vehicle was administered chronically to male Crl: CD-1(ICR)BR mice via implantable osmotic pump."( Pharmacodynamic and receptor binding changes during chronic lorazepam administration.
Fahey, JM; Grassi, JM; Greenblatt, DJ; Pratt, JS; Pritchard, GA; Shader, RI,
)
0.13

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of enoxacin, a new quinolone antibacterial agent, and its combination with 4-biphenylacetate (BPA), an active metabolite of the non-steroidal antiinflammatory agent fenbufen, were examined on population spikes induced by electrical stimulation of the stratum radiatum in the CA1 pyramidal cell layer in rat hippocampal slices."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
" However, when levetiracetam (LEV; 50mg/kg) was combined with either procyclidine (PCD; 10mg/kg) or caramiphen (CMP; 10mg/kg) complete cessation of seizures was achieved, but the nicotinic antagonist mecamylamine was needed to induce full motor rest in some rats."( Enhanced efficacy of anticonvulsants when combined with levetiracetam in soman-exposed rats.
Aas, P; Enger, S; Jonassen, M; Myhrer, T, 2011
)
0.37

Bioavailability

ExcerptReferenceRelevance
" In an attempt to develop therapeutic agents which would maintain the pharmacological profiles of endogeneous neuroactive steroids but with increased oral bioavailability and reduced metabolic liability, we explored simple substitutions at the 3 beta-position of the endogenous neuroactive steroid, 3 alpha-hydroxy-5 alpha-pregnan-20-one (3 alpha, 5 alpha-P)."( Anxiolytic and anticonvulsant activity of a synthetic neuroactive steroid Co 3-0593.
Belluzzi, J; Gee, KW; Hawkinson, JE; Hogenkamp, D; Lan, NC; Stein, L; Upasani, R; Wieland, S; Wood, PL, 1997
)
0.3
" To provide proof of concept for the nomethiazole drug class, selected examples were assayed for restoration of synaptic function in hippocampal slices from AD-transgenic mice, reversal of cognitive deficits, and brain bioavailability of the prodrug and its neuroprotective MZ metabolite."( Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy.
Arancio, O; Fa', M; Luo, J; Qin, Z; Tavassoli, E; Teich, AF; Thatcher, GR; VandeVrede, L, 2012
)
0.38

Dosage Studied

Muscimol increased responsiveness to formalin and reduced the slope of the formalin dose-response relation. In slices prepared from UL animals, MVN cells in the rostral region of the ipsi-lesional nucleus showed a marked downregulation of their response to both muscicol and baclofen. Muscicolic acid (2 mg/kg) exerted the antiimmobility effect even after single dosing 1 h before the test.

ExcerptRelevanceReference
"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
)
0.83
" There was a dose-response effect seen in muscimol-treated rabbits."( Protective effect of synaptic inhibition during cerebral ischemia in rats and rabbits.
Hedges, B; Lyden, PD, 1992
)
0.55
" 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
" In the present study, we determined, in rat pups, the effect of nigral infusions of gamma-vinyl-GABA (GVG) on clonic-tonic seizures induced by flurothyl, generated a dose-response curve of the GVG effect and investigated the possible role of the nigral GABAA receptor in mediating the GVG effect."( Is the anticonvulsant effect of substantia nigra infusion of gamma-vinyl-GABA (GVG) mediated by the GABAA receptor in rat pups?
Moshé, SL; Sperber, EF; Xu, SG, 1991
)
0.28
" 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
" The dose-response relationships showed that the effect of enoxacin was 100 times potentiated in the presence of BPA (10(-5) M)."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
" The dose-response curve 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 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
)
0.83
" The inhibitory effect of GABA was mimicked by the type B GABA agonist baclofen, displaying a similar dose-response relationship as GABA."( Presynaptic effects of gamma-aminobutyric acid on norepinephrine release and uptake in rat pineal gland.
Cardinali, DP; Chuluyan, HE; Rosenstein, RE, 1990
)
0.28
", dose-response curves for induction of behaviors by SP (i."( Baclofen, gamma-aminobutyric acidB receptors and substance P in the mouse spinal cord.
Hwang, AS; Wilcox, GL, 1989
)
0.28
" To determine the effects of chronic dosage in mice, alprazolam (2 mg/kg/day) was administered via osmotic pumps for 1-14 days, and open-field activity, plasma and brain concentrations, benzodiazepine receptor binding in vivo and in vitro, [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding, and muscimol-stimulated chloride uptake were determined."( Chronic benzodiazepine administration. IV. Rapid development of tolerance and receptor downregulation associated with alprazolam administration.
Greenblatt, DJ; Lopez, F; Miller, LG; Roy, RB; Shader, RI; Woolverton, S, 1989
)
0.45
" 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
" Time- and dose-response relationships were region specific suggesting that estradiol might influence GABAA-receptor binding through multiple mechanisms."( Regional specificity of gamma-aminobutyric acid receptor regulation by estradiol.
McEwen, BS; Nock, B; O'Connor, LH, 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
" Chlorpromazine caused a slight shift in the dose-response curves as did chlordiazepoxide when used with phencyclidine."( Quantitative electrocortical changes in the rat induced by phencyclidine and other stimulants.
Bond, A; Neal, H, 1985
)
0.27
" 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
)
0.55
" 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
)
0.5
" The shape of the muscimol dose-response curve was shallow, suggestive of negative cooperativity or heterogeneous receptors, but tissue uptake of agonist, possible diffusion barriers and apparent functional desensitization complicated these results."( gamma-Aminobutyric acid receptor-regulated 36Cl- flux in mouse cortical slices.
Olsen, RW; Yang, JS, 1987
)
0.61
"A rabbit tooth pulp antinociceptive model was used to investigate the effect of prior administration of diazepam or muscimol on the potency and duration of fentanyl and meperidine Potency experiments compared ED(50) values in all-or-none dose-response assays between both muscimol (0."( Diazepam enhances fentanyl and diminishes meperidine antinociception.
Bergman, SA; Williams, G; Wyn, RL,
)
0.34
"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
" 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
)
1.18
" 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
)
0.56
" 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
" 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
)
0.94
" 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
)
0.68
" 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
" In animals implanted with chronically indwelling cannulae, a muscimol (25-400 ng) dose-response analysis confirmed the greater sensitivity of the MR site."( Intra-raphe muscimol induced hyperactivity depends on ascending serotonin projections.
Lorens, SA; Sainati, SM, 1982
)
0.88
" 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
)
0.49
" The selectivity of this antagonism is discussed since TAG also shifted to the right the blood pressure dose-response curve obtained with muscimol."( TAG antagonises the central cardiovascular effects of taurine.
Bloch, R; Bousquet, P; Feldman, J; Schwartz, J, 1984
)
0.47
" Their ED50 values were determined from their dose-response curves."( A new method for the evaluation of benzodiazepines based on their ability to block muscimol-induced myoclonic jerks in mice.
Haddox, VG; Menon, MK; Vivonia, CA, 1981
)
0.49
" When applied topically to cortex, muscimol blocks focal penicillin, bicuculline, and picrotoxin discharges in a dose-response relationship."( Anticonvulsant effects of muscimol.
Collins, RC, 1980
)
0.84
"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
)
0.44
" 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
)
0.51
", 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
" No clear dose-response relationships were noted in the analgesic response to the combination of the progestins and MUSC."( Perispinal progestins enhance the antinociceptive effects of muscimol in the rat.
Beyer, C; Caba, M; González-Mariscal, G, 1994
)
0.53
" Diazepam shifted the dose-response curve for muscimol-stimulated flux to about 4-fold lower concentrations without affecting the maximum response."( Reconstitution of purified GABAA receptors: ligand binding and chloride transporting properties.
Dunn, SM; Thuynsma, RP, 1994
)
0.55
" 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
)
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
" Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating development of tolerance."( Development of tolerance in mice to the sedative effects of the neuroactive steroid minaxolone following chronic exposure.
Ford, E; Hagan, RM; Marshall, FH; Mullings, J; Oakley, NR; Stratton, SC; Worton, SP, 1997
)
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
" Within each of the three dosage periods, the duration of sleep and extent of reduction in body temperature of the rats decreased with time."( Effects of pentobarbital on the expression of GABAA receptor beta 1 mRNA in the hippocampus: differential responses of CA1 and CA3.
Lee, YP; Yin, HS, 1998
)
0.3
" In the mouse pentylenetetrazole (PTZ) convulsive model, intravenous pretreatment with cefazolin (800 mg/kg) or imipenem (200 mg/kg) shifted the dose-response curve of PTZ (i."( Low convulsive activity of a new carbapenem antibiotic, DK-35C, as compared with existing congeners.
Cho, JH; Jin, C; Jung, I; Kim, DH; Kim, M; Ku, HJ; Oh, CH; Yook, J, 1999
)
0.3
" increased the percentage of loss of the righting reflex in a dose-dependent manner with an ED50 value of 140 (95% confidence limits 123-160) mg kg-1 (n = 40; eight animals per dose, five doses per dose-response curve)."( Propofol anaesthesia in mice is potentiated by muscimol and reversed by bicuculline.
Dohi, T; Irifune, M; Kawahara, M; Maeoka, K; Nishikawa, T; Shimizu, Y; Sugimura, M; Takarada, T, 1999
)
0.56
"1-1 microM) of muscimol, and the muscimol dose-response (0."( Brain allopregnanolone regulates the potency of the GABA(A) receptor agonist muscimol.
Costa, E; Guidotti, A; Matsumoto, K; Mienville, JM; Pinna, G; Puia, G; Uzunova, V, 2000
)
0.89
" In slices prepared from UL animals, MVN cells in the rostral region of the ipsi-lesional nucleus showed a marked downregulation of their response to both muscimol and baclofen, seen as a rightward shift and a decrease in slope of the dose-response relationships for the two agonists."( Rapid compensatory changes in GABA receptor efficacy in rat vestibular neurones after unilateral labyrinthectomy.
Cameron, SA; Dutia, MB; Him, A; Yamanaka, T, 2000
)
0.5
" Dose-response determinations of ethanol, pentobarbital, midazolam, muscimol and morphine were made under the training condition of 30 min pretreatment interval."( Characterization of the discriminative stimulus effects of GABA(A) receptor ligands in Macaca fascicularis monkeys under different ethanol training conditions.
Azarov, A; Grant, KA; Green-Jordan, K; Szeliga, KT; Waters, CA, 2000
)
0.54
" 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
)
1.22
" Administration of a 1 mM solution of muscimol (based on dose-response data) into this well abolished the reflex pressor response to contraction (change in mean arterial blood pressure before was 47 +/- 7 mmHg and after muscimol was 3 +/- 2 mmHg)."( Dorsal horn administration of muscimol abolishes the muscle pressor reflex.
Wilson, LB, 2001
)
0.87
" The improving effects of huperzine A exhibited a bell-shaped dose-response curve."( Huperzine A reverses scopolamine- and muscimol-induced memory deficits in chick.
Gao, Y; Guan, LC; Kuang, PZ; Tang, XC, 2000
)
0.58
"0 microg) were administered to obtain the dose-response curve and the 50% effective dose (ED(50))."( The interaction between intrathecal neostigmine and GABA receptor agonists in rats with nerve ligation Injury.
Choi, IC; Han, SM; Hwang, JH; Hwang, KS; Kim, JU; Park, PH, 2001
)
0.31
" VS-3 neuron GABA receptors were activated by muscimol and inhibited by picrotoxin but not bicuculline, and their dose-response relationship had an EC(50) of 103."( Peripheral GABAergic inhibition of spider mechanosensory afferents.
French, AS; Panek, I; Sekizawa, S; Seyfarth, EA; Torkkeli, PH, 2002
)
0.57
" Analysis of the dose-response relation for morphine after inactivation of descending fibers revealed that, except for the tail immersion test, high doses of morphine could not overcome the block induced by muscimol."( The role of descending fibers from the rostral ventromedial medulla in opioid analgesia in rats.
Franklin, KB; Gilbert, AK, 2002
)
0.5
" 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
" Dose-response curves for muscimol in the presence of 3,3', 5-L-triiodothyronine (L-T3) indicated a noncompetitive inhibition of muscimol-stimulated (36)Cl(-) uptake by the thyroid hormone."( Inhibition of the activity of the native gamma-aminobutyric acid A receptor by metabolites of thyroid hormones: correlations with molecular modeling studies.
Burke, LA; Chapell, R; Leidenheimer, NJ; Martin, JV; Newman, MA; Padron, JM, 2004
)
0.62
" First of all, the effect of muscimol on EEG power of infusion area was observed for confirmation of the dosage of muscimol to inhibit the function of infusion area."( Disconnection of the hippocampal-prefrontal cortical circuits impairs spatial working memory performance in rats.
Cai, JX; Wang, GW, 2006
)
0.63
" 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
)
0.53
" Separate groups of rats received bilateral intra-VTA injections of the GABA-A antagonist picrotoxin (34 ng/side, n = 7; 68 ng/side, n = 8), GABA-A agonist muscimol (14 ng/side, n = 8), GABA-B agonist baclofen (56 ng/side, n = 7; 100 ng/side, n = 6), picrotoxin (68 ng/side) co-injected with the GABA-B antagonist 2-hydroxysaclofen (100 ng/side, n = 7; 2 microg/side, n = 8) or artificial cerebrospinal fluid (aCSF, n = 6) to assess the effects of the various compounds on the cocaine self-administration dose-response curve."( Contribution of ventral tegmental GABA receptors to cocaine self-administration in rats.
Backes, EN; Hemby, SE, 2008
)
0.54
" 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
" MELA also increased sleep rate and sleep time in the combined administration with pentobarbital at the sub-hypnotic dosage and showed synergic effects with muscimol in potentiating sleep onset and enhancing sleep time induced by pentobarbital."( Methanol extract of Longanae Arillus augments pentobarbital-induced sleep behaviors through the modification of GABAergic systems.
Eun, JS; Hong, JT; Kim, YB; Lee, MK; Ma, H; Ma, Y; Nam, SY; Oh, KW, 2009
)
0.55
" The results showed that muscimol injections into BLA/BMA, at dosage levels between 100 and 200 ng/side, produced major deficits in retrieval behavior and minor deficits in nursing behavior."( The importance of the basolateral/basomedial amygdala for goal-directed maternal responses in postpartum rats.
Bettis, JK; Bress, JA; Denicola, AL; Gary, AJ; Knapp, SE; Numan, M; Ranker, LR, 2010
)
0.66
"The EtOH dose-response curve was not altered by pretreatment with pBBG or by transgenic overexpression of Glo1."( Glyoxalase 1 (GLO1) Inhibition or Genetic Overexpression Does Not Alter Ethanol's Locomotor Effects: Implications for GLO1 as a Therapeutic Target in Alcohol Use Disorders.
Barkley-Levenson, AM; Lagarda, FA; Palmer, AA, 2018
)
0.48
" However, neither manipulation altered the dose-response curve for EtOH's locomotor effects, whereas muscimol appeared to enhance the locomotor sedative effects of EtOH."( Glyoxalase 1 (GLO1) Inhibition or Genetic Overexpression Does Not Alter Ethanol's Locomotor Effects: Implications for GLO1 as a Therapeutic Target in Alcohol Use Disorders.
Barkley-Levenson, AM; Lagarda, FA; Palmer, AA, 2018
)
0.7
" Importantly, the dose-response curve for this action was right-shifted relative to working memory, as seen with systemic administration."( Receptor and circuit mechanisms underlying differential procognitive actions of psychostimulants.
Berridge, CW; Spencer, RC, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Occurs in Manufacturing (4 Items)

ItemProcessFrequency
Candiescore-ingredient1
Confectioneriescore-ingredient1
Sweet snackscore-ingredient1
Snackscore-ingredient1

Roles (4)

RoleDescription
fungal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in fungi, the kingdom that includes microorganisms such as the yeasts and moulds.
GABA agonistA drug that binds to and activates gamma-aminobutyric acid receptors.
psychotropic drugA loosely defined grouping of drugs that have effects on psychological function.
oneirogenAny substance that produces or enhances dream-like states of consciousness.
[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
isoxazolesOxazoles in which the N and O atoms are adjacent.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
alkaloidAny of the naturally occurring, basic nitrogen compounds (mostly heterocyclic) occurring mostly in the plant kingdom, but also found in bacteria, fungi, and animals. By extension, certain neutral compounds biogenetically related to basic alkaloids are also classed as alkaloids. Amino acids, peptides, proteins, nucleotides, nucleic acids, amino sugars and antibiotics are not normally regarded as alkaloids. Compounds in which the nitrogen is exocyclic (dopamine, mescaline, serotonin, etc.) are usually classed as amines rather than alkaloids.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.66840.003245.467312,589.2998AID2517
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency22.38720.177814.390939.8107AID2147
GLS proteinHomo sapiens (human)Potency22.38720.35487.935539.8107AID624146
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency2.39341.069113.955137.9330AID720538
cytochrome P450 2C19 precursorHomo sapiens (human)Potency39.81070.00255.840031.6228AID899
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency28.18380.00106.000935.4813AID943
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
D-amino-acid oxidaseSus scrofa (pig)IC50 (µMol)100.00000.18802.047810.0000AID1798301; AID404688
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)0.01600.00011.14948.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.00850.00000.21085.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50 (µMol)0.01600.00011.03936.0000AID255278
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.00850.00090.83985.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)0.01600.00011.29158.0000AID255278
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.00850.00000.18819.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.505710.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.00400.00020.561410.0000AID71568
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.497310.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.00400.00020.635210.0000AID71568
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.00400.00020.621710.0000AID71568
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00550.00010.498810.0000AID71429; AID71435; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.00400.00020.675810.0000AID71568
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.504610.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00400.00020.646910.0000AID71568
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00320.00132.22068.3000AID71429
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50 (µMol)0.01600.00011.30188.0000AID255278
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.00850.00010.20769.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.00400.00020.671210.0000AID71568
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50 (µMol)0.01600.00010.98006.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.00850.00010.24425.6234AID1184359; AID71287
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)0.00320.00321.79008.3000AID71429
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)0.00320.00321.54318.3000AID71429
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)0.01600.00011.19936.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.00850.00010.25155.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.00850.00010.24015.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)0.01600.00010.93746.0000AID255278
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.00850.00000.28325.6234AID1184359; AID71287
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.00320.00321.54318.3000AID71429
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)0.01600.00011.01936.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.00850.00020.37095.6234AID1184359; AID71287
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)IC50 (µMol)100.00000.00060.09430.1880AID404688
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.506510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.00400.00020.557710.0000AID71568
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.505710.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.00400.00020.640310.0000AID71568
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.00400.00020.570810.0000AID71568
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.00850.00020.41199.0000AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
GABA theta subunitRattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.00540.00010.507510.0000AID71429; AID71436; AID71447; AID71830; AID71831
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.00400.00020.656110.0000AID71568
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50 (µMol)0.01600.00011.02016.0000AID255278
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.00850.00090.89545.6234AID1184359; AID71287
[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 receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)5.83080.00112.000910.0000AID1184360; AID724586; AID733887
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)EC50 (µMol)27.00000.07552.12458.0000AID733887
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC50 (µMol)0.38640.00141.957810.0000AID1184360; AID1184366; AID1184368; AID724586; AID724594; AID724595
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)EC50 (µMol)1.08060.26911.09214.6000AID1184362; AID406570; AID724585; AID733884
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)Kd2.30000.60001.53332.3000AID71415
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC50 (µMol)27.00000.00301.65329.8000AID733887
Gamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)Kd1.40000.60001.23331.7000AID71414
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC50 (µMol)27.00000.00301.58219.8000AID733887
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC50 (µMol)5.56950.01001.20095.6234AID1184368; AID724595; AID733887
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC50 (µMol)5.72700.01201.17515.2000AID1184366; AID724594; AID733887
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC50 (µMol)2.43360.00141.776810.0000AID1184360; AID1184366; AID1184368; AID724586; AID724594; AID724595; AID733887
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)EC50 (µMol)27.00000.07551.59585.2000AID733887
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)EC50 (µMol)27.00000.07551.19595.2000AID733887
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

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

Molecular Functions (18)

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

Ceullar Components (32)

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

Bioassays (96)

Assay IDTitleYearJournalArticle
AID1137319Skeletal muscle relaxant activity in iv dosed chronic spinal Sprague-Dawley rat assessed as reduction of flexor spasm administered every 15 mins interval1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
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.
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.
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.
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.
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.
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.
AID703698Activation of Gamma-aminobutyric acid type-A receptor in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced cytotoxicity at 50 uM incubated for 1 hr prior to glutamate-challenge measured after 24 hrs by MTT assay in pr2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy.
AID1137326Dissociation constant, pKa of the compound1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
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.
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.
AID1137320Toxicity in iv dosed chronic spinal Sprague-Dawley rat assessed as lethality at cumulative dose of 16 mg/kg, iv1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
AID225347Activity to antagonise mercaptopropionic acid (MPA) induced convulsions in mouse after subcutaneous administration1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles.
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.
AID72454Affinity for GGABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID1184372Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay relative to GABA2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID71415Partial agonist activity against human rho-1 subunit GABA-C receptor expressed in Xenopus oocytes2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.
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.
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.
AID117219Lethal dose which causes death in 50% of the mice within 48 hr of ip administration1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
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.
AID1137318Anticonvulsant activity in po dosed Swiss mouse assessed as reduction of 3-mercaptopropionic acid-induced tonic extensor-seizures within 3 to 7 mins1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
AID71831Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
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.
AID212017Toxicity measured in mouse by subcutaneous administration1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles.
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.
AID338215Displacement of [3H]GABA from GABAA receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
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.
AID404688Inhibition of pig D-amino acid oxidase2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
AID764968Binding affinity to mouse brain GABAA receptor by Scatchard analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID1137322Skeletal muscle relaxant activity in chronic spinal mongrel cat assessed as reduction of flexor spasm up to 7.5 mg/kg, iv administered every 15 mins interval1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
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.
AID112310Effective dose which decreases the 50% of the lethality induced by bicuculline in mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
AID73511Percent 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.
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.
AID71447Displacement of [3H]- muscimol in cerebral tissue of male rats1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis and pharmacological evaluation of cis-2,3,3a,4,5,6,7,7a-octahydro-3-oxoisoxazolo[5,4-c]pyridine: a structural analogue of the GABA agonist THIP.
AID338216Displacement of [3H]GABA from GABAA receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID1184371Agonist activity at human GABAAalpha5beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay relative to GABA2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(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.
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.
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.
AID703699Activation of Gamma-aminobutyric acid type-A receptor in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced cytotoxicity at 50 uM incubated for 1 hr prior to glutamate-challenge measured after 24 hrs by MTT assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy.
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.
AID255278Percent inhibition against GABAA receptor alpha at a compound concentration of 1 uM2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID109841Ability to displace [3H]flunitrazepam ([3H]-FNP) binding to mouse brain after intraperitoneal administration at a dose 320 umol/kg1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles.
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.
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.
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.
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.
AID1184369Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay relative to GABA2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID128167Activity tested to antagonise cyclic GMP after administration of isoniazid in mouse brain1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles.
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.
AID74656Percent 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.
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.
AID212014Toxicity was measured in mouse by intraperitoneal administration; value ranges from 3.2-101989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles.
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.
AID112309Effective dose which decreases the 50% of the convulsions induced by bicuculline in mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
AID48905BMC-sensitive inhibitory effect on cat spinal neurons relative to that of GABA was expressed in vivo as relative potency; Greater activity1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
AID1184367Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay relative to GABA2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
AID733884Partial agonist 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.
AID71449Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane at 0.003-0.006 uM1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1137325Toxicity in Swiss mouse at 8 mg/kg, po1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Kojic amine--a novel gamma-aminobutyric acid analogue.
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.
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.
AID71414Partial agonist activity against human rho-2 subunit GABA-C receptor expressed in Xenopus oocytes2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.
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.
AID130609Tested for the antagonism of bicuculline -induced convulsions in female mice intraperitoneally1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis and pharmacological evaluation of cis-2,3,3a,4,5,6,7,7a-octahydro-3-oxoisoxazolo[5,4-c]pyridine: a structural analogue of the GABA agonist THIP.
AID724587Displacement of [3H]muscimol from GABAA receptor in rat synaptic membrane after 60 mins by scintillation counting analysis2013Journal 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.
AID174405Tested for its GABA agonistic activity against spontaneous firing in explants from cerebellum of 2-4 day old rats1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis and pharmacological evaluation of cis-2,3,3a,4,5,6,7,7a-octahydro-3-oxoisoxazolo[5,4-c]pyridine: a structural analogue of the GABA agonist THIP.
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.
AID733882Agonist activity at GABAC receptor (unknown origin) expressed in Xenopus laevis oocytes2013ACS medicinal chemistry letters, Apr-11, Volume: 4, Issue:4
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
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.
AID1798301In vitro D-Amino Acid Oxidase Assay from Article 10.1021/jm800200u: \\Synthesis and Biological Evaluation of d-Amino Acid Oxidase Inhibitors.\\2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,556)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901265 (27.77)18.7374
1990's1194 (26.21)18.2507
2000's1104 (24.23)29.6817
2010's871 (19.12)24.3611
2020's122 (2.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 72.88

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 Index72.88 (24.57)
Research Supply Index8.46 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index133.77 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (72.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (0.19%)5.53%
Reviews97 (2.06%)6.00%
Case Studies7 (0.15%)4.05%
Observational0 (0.00%)0.25%
Other4,586 (97.60%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Convection Enhanced Delivery of Muscimol to Study the Pathophysiology Underlying the Clinical Features of Parkinson's Disease [NCT00921128]Phase 10 participants (Actual)Interventional2009-06-02Withdrawn
Trial of Intracerebral Infusion in Patients With Medically Intractable Epilepsy [NCT00005925]Phase 13 participants (Actual)Interventional2000-06-23Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]