Page last updated: 2024-11-07

alphaxalone

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Description

RU 5135: powerful antagonist of GABA stimulation of diazepam binding; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

alphaxalone: RN given refers to (3alpha,5alpha)-isomer; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID656742
CHEBI ID34944
MeSH IDM0049068
PubMed CID104845
CHEMBL ID190279
CHEBI ID34531
SCHEMBL ID57756
MeSH IDM0049068

Synonyms (114)

Synonym
gtpl2378
ru 5135
(3as,3bs,5ar,7s,9as,9bs,11as)-2-amino-7-hydroxy-9a,11a-dimethyl-3,3a,3b,4,5,5a,6,7,8,9,9b,11-dodecahydronaphtho[2,1-e]indol-10-one
CHEBI:34944
(7s)-ru5135
Q27088647
BIDD:PXR0037
5alpha-pregnane-3alpha-ol-11,20-dione
MLS001076262 ,
BRD-K41445866-001-03-0
alfaxalone
alphaxalone
23930-19-0
MLS000069684 ,
BPBIO1_001237
(3alpha,5alpha)-3-hydroxypregnane-11,20-dione
EU-0100929
5alpha-pregnan-3alpha-ol-11,20-dione, powder, >=98% (tlc)
cas-23930-19-0
LOPAC0_000929
D07282
alfaxalone (inn)
hydroxy-5 alpha-pregnane-11,20-dione
PRESTWICK3_001002
PRESTWICK2_001002
gr 2/234
delta(16)-alfaxalone
alfaxalonum [inn-latin]
alfadione
brn 3217240
5-alpha-pregnane-11,20-dione, 3-alpha-hydroxy-
(3-alpha,5-alpha)-3-hydroxypregnane-11,20-dione
3-hydroxypregnane-11,20-dione
alfaxalona [inn-spanish]
3alpha-hydroxy-5alpha-pregnane-11,20-dione
alfaxolone
pregnane-11,20-dione, 3-hydroxy-, (3-alpha,5-alpha)-
3alpha-hydroxy-5alpha-pregnan-11,20-dion
3-alpha-hydroxy-5-alpha-pregnane-11,20-dione
AB00384358
BSPBIO_001123
smr000058494
SPBIO_003004
PRESTWICK1_001002
PRESTWICK0_001002
NCGC00023100-04
5alpha-pregnan-3alpha-ol-11,20-dione
NCGC00023100-05
NCGC00023100-03
P 5052
NCGC00023100-06
(3r,5s,8s,9s,10s,13s,14s,17s)-17-acetyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-11-one
bdbm50164570
CHEMBL190279 ,
chebi:34531 ,
phaxan
HMS1571I05
(3r,5s,8s,9s,10s,13s,14s,17s)-17-acetyl-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-11-one
HMS3262J20
HMS2098I05
tox21_110884
dtxsid9022576 ,
dtxcid702576
CCG-205010
HMS2236N05
alfaxalona
alfaxalonum
unii-bd07m97b2a
4-08-00-02091 (beilstein handbook reference)
alfaxalone [inn:ban:dcf:jan]
bd07m97b2a ,
LP00929
alfaxalone [green book]
alfaxalone [who-dd]
alfaxalone [jan]
gr-2/234
alfaxalone [inn]
alfaxalone [mart.]
alfaxalone [mi]
3.alpha.-hydroxy-5.alpha.-pregnane-11,20-dione
gtpl5461
5alpha-alphaxalone
SCHEMBL57756
NCGC00023100-08
tox21_110884_1
NCGC00261614-01
tox21_500929
DUHUCHOQIDJXAT-OLVMNOGESA-N
alphaxolone
(3?,5?)-3-hydroxypregnane-11,20-dione
AKOS024457399
OPERA_ID_1629
sr-01000000168
SR-01000000168-3
J-015280
SR-01000000168-2
sr-01000076070
SR-01000076070-1
HMS3715I05
(3a,5a)-3-hydroxypregnane-11,20-dione
ey4 ,
pregnane-11,20-dione, 3-hydroxy-, (3a,5a)-
DB11371
(3beta,5alpha,8alpha,9beta,10alpha)-3-hydroxypregnane-11,20-dione
Q3611058
SDCCGSBI-0050903.P002
alfaxan multidose
n01ax05
alfaxalonum (inn-latin)
alfaxanmultidose idx
alfaxalone (mart.)
alfaxalona (inn-spanish)
alfaxan
alfaxanmultidose

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" No adverse effects were observed after recovery from anesthesia."( EFFICACY AND SAFETY OF A MEDETOMIDINE-AZAPERONE-ALFAXALONE COMBINATION IN CAPTIVE WHITE-TAILED DEER (ODOCOILEUS VIRGINIANUS).
Caulkett, N; Pon, K; Woodbury, M, 2016
)
0.43
"The combination of intranasal midazolam-butorphanol and intramuscular alfaxalone at the doses examined was a safe and effective method for sedating Quaker parrots."( Intranasal butorphanol and midazolam administered prior to intramuscular alfaxalone provides safe and effective sedation in Quaker parrots (Myiopsitta monachus).
Conner, CM; Hoppes, SM; Simon, BT; Stevens, BJ, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" Due to its simplicity and sensitivity this method can be used on a routine basis for pharmacokinetic analysis of neuroactive steroids."( High-performance liquid chromatography of the neuroactive steroids alphaxalone and pregnanolone in plasma using dansyl hydrazine as fluorescent label: application to a pharmacokinetic-pharmacodynamic study in rats.
Danhof, M; Gladdines, WW; Irth, H; Smulders, CJ; van der Graaf, PH; Visser, SA, 2000
)
0.31
" The pharmacodynamic model consisted of a receptor model, featuring a monophasic saturable receptor activation model in combination with a biphasic stimulus-response model."( Mechanism-based pharmacokinetic-pharmacodynamic modeling of concentration-dependent hysteresis and biphasic electroencephalogram effects of alphaxalone in rats.
Danhof, M; Peletier, LA; Reijers, BP; Smulders, CJ; Van der Graaf, PH; Visser, SA, 2002
)
0.31
"The objective of the present investigation was to characterize the pharmacodynamic interaction between the synthetic neuroactive steroid alphaxalone and the benzodiazepine midazolam."( Mechanism-based modeling of the pharmacodynamic interaction of alphaxalone and midazolam in rats.
Danhof, M; Huntjens, DR; Peletier, LA; van der Graaf, PH; Visser, SA, 2003
)
0.32
"To determine the pharmacokinetic parameters of alfaxalone in dogs after the intravenous (IV) administration of clinical and supra-clinical doses of a 2-hydroxypropyl-beta-cyclodextrin (HPCD) alfaxalone formulation (Alfaxan-CD RTU)."( Plasma pharmacokinetics of alfaxalone in dogs after an intravenous bolus of Alfaxan-CD RTU.
Ferré, PJ; Lefebvre, HP; Li, Q; Pasloske, K; Ranasinghe, MG; Whittem, T, 2006
)
0.33
" Plasma concentrations of alfaxalone were assayed using a liquid chromatograph/mass selective detector technique and analyzed to estimate the main pharmacokinetic parameters by noncompartmental analysis."( Plasma pharmacokinetics of alfaxalone in dogs after an intravenous bolus of Alfaxan-CD RTU.
Ferré, PJ; Lefebvre, HP; Li, Q; Pasloske, K; Ranasinghe, MG; Whittem, T, 2006
)
0.33
" There was no clinically significant modification of the pharmacokinetic parameters between sexes and between the clinical (2 mg kg(-1)) and supra-clinical (10 mg kg(-1)) doses."( Plasma pharmacokinetics of alfaxalone in dogs after an intravenous bolus of Alfaxan-CD RTU.
Ferré, PJ; Lefebvre, HP; Li, Q; Pasloske, K; Ranasinghe, MG; Whittem, T, 2006
)
0.33
"This study aimed to determine the pharmacokinetic parameters and pharmacodynamics of alfaxalone in a 2-hydroxypropyl-beta-cyclodextrin alfaxalone formulation (Alfaxan), Jurox Pty Ltd, Rutherford, NSW, Australia) in cats after single administration at clinical and supraclinical dose rates and as multiple maintenance doses."( The pharmacokinetics and pharmacodynamics of alfaxalone in cats after single and multiple intravenous administration of Alfaxan at clinical and supraclinical doses.
Heit, MC; Pasloske, KS; Ranasinghe, MG; Whittem, T, 2008
)
0.35
" Venous blood samples were collected at strategic time points and plasma concentrations of alfaxalone were assayed using liquid chromatography-mass spectrometry (LC/MS) and analysed by noncompartmental pharmacokinetic analysis."( The pharmacokinetics and pharmacodynamics of the injectable anaesthetic alfaxalone in the horse.
Goodwin, WA; Keates, HL; Pasloske, K; Pearson, M; Ranasinghe, MG; Sauer, B, 2011
)
0.37
" Venous blood samples were collected at strategic time points and alfaxalone plasma concentrations were assayed using liquid chromatography-mass spectrometry (LC/MS) and analysed by noncompartmental pharmacokinetic analysis."( Plasma pharmacokinetics and pharmacodynamics of alfaxalone in neonatal foals after an intravenous bolus of alfaxalone following premedication with butorphanol tartrate.
Goodwin, W; Keates, H; Pasloske, K; Pearson, M; Ranasinghe, MG; Sauer, B, 2012
)
0.38
" The pharmacokinetic properties of alfaxalone administered intravenously and intraperitoneally in rats (n = 28) were investigated."( Plasma pharmacokinetics of alfaxalone after a single intraperitoneal or intravenous injection of Alfaxan(®) in rats.
Bellingham, MC; Keates, H; Lau, C; Pasloske, K; Ranasinghe, MG; Shiels, I, 2013
)
0.39
"0008), half-life (p=0."( A clinical evaluation of the pharmacokinetics and pharmacodynamics of intravenous alfaxalone in cyclodextrin in male and female rats following a loading dose and constant rate infusion.
Harris, J; Paine, S; White, KL, 2017
)
0.46
"The mean half-life and mean residence time of alfaxalone were longer after I/M (1."( Pharmacokinetics and effects of alfaxalone after intravenous and intramuscular administration to cats.
Belda, E; Escudero, E; Hernandis, V; Laredo, FG; Marín, P; Rodrigo-Mocholí, D, 2018
)
0.48
" Plasma alfaxalone concentrations were quantified by a liquid chromatography tandem-mass spectrometry method and analysed by non-compartmental pharmacokinetic analysis."( Clinical pharmacokinetics and pharmacodynamics of intravenous alfaxalone in young Thoroughbred horses premedicated with medetomidine and midazolam.
Aoki, M; Kushiro, A; Mae, N; Maeda, T; Minamijima, Y; Nagata, SI; Ohta, M; Wakuno, A; Yamazaki, Y, 2019
)
0.51
" This study assessed the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of alfaxalone given as a bolus intravenous injection of this formulation to human male volunteers."( Pharmacokinetic and Pharmacodynamic Analysis of Alfaxalone Administered as a Bolus Intravenous Injection of Phaxan in a Phase 1 Randomized Trial.
Anderson, BJ; Goodchild, CS; Sear, JW; Serrao, JM, 2020
)
0.56
"To evaluate the cardiovascular effects, pharmacokinetic (PK) data and recovery characteristics of an alfaxalone constant rate infusion (CRI) of different duration in dogs at manufacturer's recommended dose rate."( Alfaxalone total intravenous anaesthesia in dogs: pharmacokinetics, cardiovascular data and recovery characteristics.
Bosmans, T; Croubels, S; Dehuisser, V; Devreese, M; Duchateau, L; Gehring, R; Polis, I, 2019
)
0.51
"This study aimed to investigate the specific pharmacokinetic profile and effects of alfaxalone after intravenous (IV) and intramuscular (IM) administration to rabbits and evaluate the potential interaction with dexmedetomidine."( Pharmacokinetics and sedative effects of alfaxalone with or without dexmedetomidine in rabbits.
Belda, E; Escudero, E; Hernandis, V; Laredo, FG; Marín, P; Torres, CA, 2020
)
0.56
"This complete crossover study evaluated the pharmacodynamic effects of alfaxalone with preservatives administered to bearded dragons via intracoelomic (ICo; n = 10), SC (10), IM (9), and IV (9) injection at 15 mg/kg."( Use of alfaxalone in bearded dragons (Pogona vitticeps): optimizing pharmacodynamics and evaluating cardiogenic effects via echocardiography.
Allender, MC; Chinnadurai, SK; Fries, R; Kadotani, S; Keller, KA; Webb, JK, 2022
)
0.72
" There were significant differences between the sexes for plasma clearance, half-life and mean residence time in Lewis rats, and mean arterial blood pressure was significantly lower in the female rats at 120 min."( Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes.
Aldurdunji, M; Harris, J; Ortori, C; Paine, S; White, K, 2022
)
0.72
"To evaluate the pharmacodynamic effects and pharmacokinetics of a single intramuscular (IM) injection of alfaxalone in central bearded dragons (Pogona vitticeps) when injected at a cranial versus a caudal site."( Pharmacokinetics and pharmacodynamics of intramuscular alfaxalone in central bearded dragons (Pogona vitticeps): effect of injection site.
Alexander, AB; Allgood, H; Gatson, B; Hernandez, JA; Johnson, A; Martin de Bustamante, MG; Messenger, K; Shippy, S; Wellehan, JF, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
" Drug discrimination was used to examine the behavioral effects of L-838,417 and bretazenil, two low efficacy positive GABAA modulators that act at benzodiazepine sites, alone and in combination with benzodiazepines and a neuroactive steroid (alfaxolone)."( Differential behavioral effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys.
France, CP; McMahon, LR, 2006
)
0.33
"To describe the use of intramuscular (IM) premedication with alfaxalone alone or in combination with diazepam in pigs."( Effects of intramuscular alfaxalone alone or in combination with diazepam in swine.
Bertrán de Lis, BT; Santos González, M; Tendillo Cortijo, FJ, 2013
)
0.39
"IM administration of alfaxalone combined with diazepam resulted in a rapid onset of recumbency and deep sedation, with minimal side effects."( Effects of intramuscular alfaxalone alone or in combination with diazepam in swine.
Bertrán de Lis, BT; Santos González, M; Tendillo Cortijo, FJ, 2013
)
0.39
" Morphine at 1 or 2 mg/kg combined with medetomidine and alfaxalone in rabbits produced a suitable level of anaesthesia, although profound cardiorespiratory depression was found."( Cardiorespiratory, anaesthetic and recovery effects of morphine combined with medetomidine and alfaxalone in rabbits.
Del Mar Granados, M; Fernández-Sarmiento, A; Gómez-Villamandos, RJ; López Villalba, I; Manuel Domínguez, J; Morgaz, J; Muñoz-Rascón, P; Navarrete-Calvo, R, 2014
)
0.4
" Alfaxalone, alone or in combination with tramadol, did not produce satisfactory results for use as an anaesthetic for this species."( Anaesthetic effects in the ferret of alfaxalone alone and in combination with medetomidine or tramadol: a pilot study.
García-Olmo, DC; Giral, M; Gómez de Segura, IA; Gómez-Juárez, M, 2014
)
0.4
"This study evaluated the use of the injectable anesthetic, alphaxalone, as a single agent and in combination with ketamine, xylazine, and morphine in the Chilean rose tarantula, Grammostola rosea."( The use of injectable alphaxalone as a single agent and in combination with ketamine, xylazine, and morphine in the Chilean rose tarantula, Grammostola rosea.
Gjeltema, J; Posner, LP; Stoskopf, M, 2014
)
0.4
"To evaluate and compare the use of intramuscular (IM) premedication with dexmedetomidine in combination with ketamine or alfaxalone in pigs."( Effects of intramuscular dexmedetomidine in combination with ketamine or alfaxalone in swine.
Bertrán de Lis, BT; Santos, M; Tendillo, FJ, 2016
)
0.43
"IM dexmedetomidine in combination with ketamine in pigs induced moderate to deep sedation and fair to smooth induction of anaesthesia."( Effects of intramuscular dexmedetomidine in combination with ketamine or alfaxalone in swine.
Bertrán de Lis, BT; Santos, M; Tendillo, FJ, 2016
)
0.43
"To investigate the sedative, anaesthetic and cardiorespiratory effects of intramuscular (IM) administration of alfaxalone alone or in combination with dexmedetomidine in cats."( Clinical efficacy and cardiorespiratory effects of intramuscular administration of alfaxalone alone or in combination with dexmedetomidine in cats.
Belda, E; Bosmans, T; Laredo, FG; Rodrigo-Mocholí, D, 2016
)
0.43
"The pharmacological effects of intramuscular (IM) administration of alfaxalone combined with medetomidine and butorphanol were evaluated in 6 healthy beagle dogs."( The pharmacological effects of intramuscular administration of alfaxalone combined with medetomidine and butorphanol in dogs.
Fukui, S; Hatakeyama, N; Ishizuka, T; Itami, T; Miyoshi, K; Pasloske, K; Sano, T; Tamura, J; Yamashita, K, 2016
)
0.43
"Objectives Cardiorespiratory parameters and anaesthesia quality in cats anaesthetised with either intramuscular (IM) alfaxalone or ketamine both combined with dexmedetomidine and butorphanol for castration were evaluated."( Comparison of intramuscular alfaxalone and ketamine combined with dexmedetomidine and butorphanol for castration in cats.
Broussaud, S; Khenissi, L; Nikolayenkova-Topie, O; Touzot-Jourde, G, 2017
)
0.46
"To assess quality of sedation following intramuscular (IM) injection of two doses of alfaxalone in combination with butorphanol in cats."( Intramuscular injection of alfaxalone in combination with butorphanol for sedation in cats.
Archer, E; Deutsch, J; Jolliffe, C; Leece, EA, 2017
)
0.46
"To determine the intubation dose and select physiologic effects of alfaxalone alone or in combination with midazolam or ketamine in dogs."( Alfaxalone alone or combined with midazolam or ketamine in dogs: intubation dose and select physiologic effects.
Muñoz, KA; Robertson, SA; Wilson, DV, 2017
)
0.46
" Serum glucose and insulin concentrations were not influenced by administration of alfaxalone alone or when administered with midazolam or ketamine."( Alfaxalone alone or combined with midazolam or ketamine in dogs: intubation dose and select physiologic effects.
Muñoz, KA; Robertson, SA; Wilson, DV, 2017
)
0.46
" The objective of this study was to evaluate the anaesthetic effect of several doses of alfaxalone alone, considering differences between sexes, and alfaxalone combined with dexmedetomidine and fentanyl in the rat administered by the intraperitoneal route."( Anaesthetic effects of alfaxalone administered intraperitoneally alone or combined with dexmedetomidine and fentanyl in the rat.
Arenillas, M; Gomez de Segura, IA, 2018
)
0.48
"To characterize alfaxalone administered subcutaneously (SC) in guinea pigs, both alone and in combination with dexmedetomidine and buprenorphine."( Effects of subcutaneous alfaxalone alone and in combination with dexmedetomidine and buprenorphine in guinea pigs (Cavia porcellus).
Bradley, MP; Doerning, CM; Lester, PA; Nowland, MH, 2018
)
0.48
" Sevoflurane requirement, cardiovascular function, and induction/recovery quality were compared between horses maintained with sevoflurane in combination with medetomidine CRI (3 µg/kg/h) (Group M; n = 25) and those maintained with sevoflurane in combination with alfaxalone-medetomidine CRI (0."( Clinical evaluation of constant rate infusion of alfaxalone-medetomidine combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery.
Ito, H; Kushiro, A; Maeda, T; Nagata, SI; Ohta, M; Okano, A; Tokushige, H; Wakuno, A, 2018
)
0.48
" Sevoflurane in combination with alfaxalone-medetomidine CRI may be a clinically effective anesthetic technique for Thoroughbred racehorses."( Clinical evaluation of constant rate infusion of alfaxalone-medetomidine combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery.
Ito, H; Kushiro, A; Maeda, T; Nagata, SI; Ohta, M; Okano, A; Tokushige, H; Wakuno, A, 2018
)
0.48
"To evaluate the sedative and cardiorespiratory effects of IM administration of alfaxalone and butorphanol combined with acepromazine, midazolam, or dexmedetomidine in dogs."( Sedative and cardiorespiratory effects of intramuscular administration of alfaxalone and butorphanol combined with acepromazine, midazolam, or dexmedetomidine in dogs.
Aarnes, TK; Bednarski, RM; Cremer, J; Lerche, P; Murdock, MA; Riccó Pereira, CH, 2020
)
0.56
"4 mg/kg] combined with acepromazine [0."( Sedative and cardiorespiratory effects of intramuscular administration of alfaxalone and butorphanol combined with acepromazine, midazolam, or dexmedetomidine in dogs.
Aarnes, TK; Bednarski, RM; Cremer, J; Lerche, P; Murdock, MA; Riccó Pereira, CH, 2020
)
0.56
"To determine the dose of alfaxalone for IM administration combined with dexmedetomidine and hydromorphone that would allow endoscopic-guided orotracheal intubation in rabbits without causing a decrease in respiratory rate or apnea."( Assessment of intramuscular administration of three doses of alfaxalone combined with hydromorphone and dexmedetomidine for endoscopic-guided orotracheal intubation in domestic rabbits (Oryctolagus cuniculus).
Cremer, J; da Cunha, A; Hampton, CE; Liu, CC; Nevarez, JG; Queiroz-Williams, P; Reabel, SN, 2021
)
0.62
"Increasing doses of alfaxalone combined with hydromorphone and dexmedetomidine increased the success rate of endoscopic-guided orotracheal intubation."( Assessment of intramuscular administration of three doses of alfaxalone combined with hydromorphone and dexmedetomidine for endoscopic-guided orotracheal intubation in domestic rabbits (Oryctolagus cuniculus).
Cremer, J; da Cunha, A; Hampton, CE; Liu, CC; Nevarez, JG; Queiroz-Williams, P; Reabel, SN, 2021
)
0.62
"To evaluate the effects of IM and IV administration of alfaxalone alone and in combination with medetomidine, midazolam, or both on key stress-related neurohormonal and metabolic changes in isoflurane-anesthetized cats undergoing ovariohysterectomy or castration."( A randomized clinical trial on effects of alfaxalone combined with medetomidine and midazolam in preventing stress-related neurohormonal and metabolic responses of isoflurane-anesthetized cats undergoing surgery.
Hikasa, Y; Kamohara, H; Kamohara, T, 2022
)
0.72
"Compared with baseline concentrations, plasma adrenaline and noradrenaline concentrations decreased during anesthesia in cats premedicated with alfaxalone alone and in combination with medetomidine."( A randomized clinical trial on effects of alfaxalone combined with medetomidine and midazolam in preventing stress-related neurohormonal and metabolic responses of isoflurane-anesthetized cats undergoing surgery.
Hikasa, Y; Kamohara, H; Kamohara, T, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" Bioavailability after I/M injection of alfaxalone was 94."( Pharmacokinetics and effects of alfaxalone after intravenous and intramuscular administration to cats.
Belda, E; Escudero, E; Hernandis, V; Laredo, FG; Marín, P; Rodrigo-Mocholí, D, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Hill coefficients, determined from dose-response data, indicated that binding of at least two GABA molecules was required to activate the chloride channel."( GABA receptors on the cell-body membrane of an identified insect motor neuron.
David, JA; Pinnock, RD; Sattelle, DB; Wafford, KA, 1988
)
0.27
" 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
" 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
)
0.27
" Log-probit dose-response curves of the inhibitory effects of the anesthetics on the catecholamine releases induced by acetylcholine, nicotine, and muscarine were determined."( Selective actions of intravenous anesthetics on nicotinic- and muscarinic-receptor-mediated responses of the dog adrenal medulla.
Amakata, Y; Amenomori, Y; Hirano, H; Matsumoto, T; Sumikawa, K, 1983
)
0.27
") and at dosage sufficient to produce surgical anaesthesia and analgesia, we observed a sex difference in the efficacy of Althesin."( Sex difference in response to alphaxalone anaesthesia may be oestrogen dependent.
Borthwick, N; Dick, H; Dow, RC; Fink, G; Malnick, S; Sarkar, DK; Twine, M, 1982
)
0.26
" In a dose-response experiment, the ED50 of alfaxolone increased from 15."( Selective cyclodextrin inhibition of alfaxolone-induced ataxia.
Deutsch, SI; Koetzner, L; Mastropaolo, J; Riggs, RL, 1996
)
0.29
" Neither bicuculline nor GABA altered the dose-response of steroids in the [3H]GHB assay, suggesting that there was no GABAA component involved in the steroid-inhibition of [3H]GHB binding."( Steroid-inhibition of [3H]gamma-hydroxybutyric acid (GHB) binding in thalamic relay nuclei increases during absence seizures.
Banerjee, PK; Liu, CC; Snead, OC, 1998
)
0.3
" Dose-response curves for antinociception were constructed using only nonsedative doses of these drugs."( Antinociceptive properties of neurosteroids: a comparison of alphadolone and alphaxalone in potentiation of opioid antinociception.
Goodchild, CS; Nadeson, R; Tucker, AP; Winter, L, 2003
)
0.32
" Nevertheless, for cats dosed with sequential maintenance doses, a regression line through their peak plasma concentrations indicated that there was no clinically relevant pharmacokinetic accumulation."( The pharmacokinetics and pharmacodynamics of alfaxalone in cats after single and multiple intravenous administration of Alfaxan at clinical and supraclinical doses.
Heit, MC; Pasloske, KS; Ranasinghe, MG; Whittem, T, 2008
)
0.35
" A dosage of 10 mg kg(-1) provides light sedation, appropriate for examination and venipuncture; 20 mg kg(-1) provides a level suitable for minor procedures or for endotracheal intubation and supplementation with inhalational anaesthesia; 30 mg kg(-1) produces an anaesthetic plane suitable for surgical procedures of limited duration (up to 40 minutes)."( Alfaxalone anaesthesia in the green iguana (Iguana iguana).
Bertelsen, MF; Sauer, CD, 2011
)
0.37
" At 35°C either dosage provided only short (5-10 minutes) and light sedation."( Intramuscular administration of alfaxalone in red-eared sliders (Trachemys scripta elegans)--effects of dose and body temperature.
Bertelsen, MF; Duse, A; Kischinovsky, M; Wang, T, 2013
)
0.39
" The results also demonstrate the presence of interactions between allosteric activators and potentiators, raising a possibility of effects on dosage requirements or changes in side effects."( The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists.
Akk, G; Eaton, MM; Li, P; Steinbach, JH, 2013
)
0.39
" Notably, an unacceptable long recovery period in both ketamine/medetomidine protocols (subsequently reversed with atipamezole) was observed, showing that α-2 adrenoreceptor agonists in the used dose and dosing regime is not the first choice for sedation in common marmosets in a standard research setting."( Comparison of three different sedative-anaesthetic protocols (ketamine, ketamine-medetomidine and alphaxalone) in common marmosets (Callithrix jacchus).
Bakker, J; Brok, HP; Langermans, JA; Pelt, ER; Remarque, EJ; Uilenreef, JJ, 2013
)
0.39
" None of the frogs dosed by immersion became anesthetized."( Alfaxalone anesthesia in bullfrogs (Lithobates catesbeiana) by injection or immersion.
Bailey, KM; Harms, CA; Motsinger-Reif, AA; Posner, LP; Richardson, EY, 2013
)
0.39
" A dosage of 10 mg/kg alfaxalone resulted in 33% mortality."( Alfaxalone as an intramuscular injectable anesthetic in koi carp (Cyprinus carpio).
Bailey, KM; Griffith, EH; Harms, CA; Lewbart, GA; Minter, LJ; Posner, LP, 2014
)
0.4
" A dose-response trial was conducted whereby 10, 30, and 50 mg/kg alfaxalone was administered subcutaneously (SC) to 10 Bengalese finches ( Lonchura domestica) in a randomized complete crossover study design."( ALFAXALONE ANESTHESIA IN THE BENGALESE FINCH ( LONCHURA DOMESTICA).
Bertelsen, MF; Nielsen, JB; Perrin, KL; Thomsen, AF, 2017
)
0.46
" The same dosage injected in the cranial site led to deeper anaesthesia than when injected caudally, suggesting that shunting to the liver and first-pass metabolism of alfaxalone occur when injected caudally, via the renal portal system."( Anaesthetic induction with alfaxalone in the ball python (Python regius): dose response and effect of injection site.
Bertelsen, MF; James, LE; Wang, T; Williams, CJ, 2018
)
0.48
" Response to noxious stimuli was absent in 2 of the rabbits given dexmedetomidine only, 4 of those given alfaxalone with dexmedetomidine, and all 6 of the animals dosed with alfaxalone, butorphanol, and dexmedetomidine; this last group displayed the longest absence of a toe-pinch response (57 ± 3 min)."( Intramuscular Administration of Alfaxalone Alone and in Combination for Sedation and Anesthesia of Rabbits (
Bradley, MP; Doerning, CM; Lester, PA; Nowland, MH, 2019
)
0.51
" Survival analysis was used to analyze the association between alfaxalone dosage and premedication with time-related variables."( Induction of General Anesthesia With Alfaxalone in the Domestic Chicken.
de Gier, R; Doneley, R; Henning, J; Mastakov, A, 2021
)
0.62
" Sedative depth, a composite score comprised of five assessment criteria, was observed every 5-min from dosing until arousal."( Differential effects of four intramuscular sedatives on cardiorespiratory stability in juvenile guinea pigs (Cavia porcellus).
Berry, MJ; Dyson, RM; Gray, CL; Pacharinsak, C; Sixtus, RP, 2021
)
0.62
" The consistency of respiratory parameters during the entire exposure time is paramount to ensuring dosing accuracy."( Comparison of Alfaxalone-Midazolam, Tiletamine-Zolazepam, and KetamineAcepromazine Anesthesia during Plethysmography in Cynomolgus Macaques (
Astleford, SM; Bowling, PA; Casselman, AM; Dixon, BC; Ghering, JM; Marion, BM; White, CE, 2022
)
0.72
" This approach can be used to propose bespoke dosing regimens for optimal use of alfaxalone."( Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes.
Aldurdunji, M; Harris, J; Ortori, C; Paine, S; White, K, 2022
)
0.72
"9 correlated positively with the dosage of rocuronium, indicating that recovery time of rocuronium was also dose-dependent in dogs anesthetized with alfaxalone."( ED
Chen, IY; Daimaruya, N; Itami, T; Sano, T; Sugita, C; Wei, Y; Yamashita, K, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
11-oxo steroidAny oxo steroid that has an oxo substituent at position 11.
corticosteroid hormoneAny of a class of steroid hormones that are produced in the adrenal cortex.
[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 (55)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
endonuclease IVEscherichia coliPotency28.18380.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.63100.100020.879379.4328AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.49150.006038.004119,952.5996AID1159521; AID1159523
TDP1 proteinHomo sapiens (human)Potency19.24710.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency13.85470.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743063
progesterone receptorHomo sapiens (human)Potency29.84930.000417.946075.1148AID1346795
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency3.98110.28189.721235.4813AID2326
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.06270.001530.607315,848.9004AID1224820; AID1224821; AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
GVesicular stomatitis virusPotency8.70900.01238.964839.8107AID1645842
alpha-galactosidaseHomo sapiens (human)Potency6.30964.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02240.035520.977089.1251AID504332
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency11.22020.10009.191631.6228AID1346983
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency23.70830.000627.21521,122.0200AID743202
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency6.42410.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency1.77830.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.01190.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.01630.00106.000935.4813AID943; AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency8.70900.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.70900.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Alpha-synucleinHomo sapiens (human)Potency25.92900.56239.398525.1189AID652106
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.70900.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.70900.01238.964839.8107AID1645842
[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 piRattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.505710.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.497310.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.498810.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.504610.0000AID71982; AID71999
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)0.53800.00132.22068.3000AID71999
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)0.53800.00321.79008.3000AID71999
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)0.53800.00321.54318.3000AID71999
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.53800.00321.54318.3000AID71999
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.506510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.505710.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.48050.00010.507510.0000AID71982; AID71999
[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)1.05000.00112.000910.0000AID1507385; AID1507386; AID1507388
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC50 (µMol)1.28750.00141.957810.0000AID1507385; AID1507386; AID1507388; AID240319
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC50 (µMol)0.45000.00301.65329.8000AID1507388
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC50 (µMol)2.00000.01201.17515.2000AID240319
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC50 (µMol)1.56670.00141.776810.0000AID1507385; AID1507386; AID240319
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)POT0.70000.10500.64402.0000AID52291
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (138)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
monoatomic ion transportGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
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)
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)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
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)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo 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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (52)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
ligand-gated monoatomic ion channel activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
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-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-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
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)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (49)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
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)
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)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
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)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo 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-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (116)

Assay IDTitleYearJournalArticle
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1525556Inhibition of human TASK3 expressed in Xenopus oocytes at 100 uM by whole cell patch clamp assay relative to control2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
TASK Channels Pharmacology: New Challenges in Drug Design.
AID427876Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABA receptor from rat cortical membrane by scintillation counting in absence of GABA2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
AID601362Anesthetic effect in mouse assessed as duration of loss of righting reflex at 16 mg/kg, iv2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity.
AID1507386Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced current by measuring GABA EC50 at 2.5 uM incubated for 15 to 25 secs by two-electrode voltage clamp assa2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID427877Ratio of IC50 for rat cortical membrane GABA receptor in absence of GABA to IC50 for rat cortical membrane GABA receptor in presence of GABA2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
AID729041Stimulation of [3H]flunitrazepam binding to GABA type A receptor in mouse primary cortical neurons at 100 uM after 30 mins by liquid scintillation counting analysis relative to allopregnanolone2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity.
AID427875Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABAA receptor from rat cortical membrane by scintillation counting in presence of 1 uM GABA2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
AID1507385Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expressed in Xenopus laevis oocytes assessed as potentiation of GABA chloride current incubated for 15 to 25 secs by two-electrode voltage clamp assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID240319Effective concentration against GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
AID1507392Induction of [3H]azietomidate photoincorporation at human GABAA receptor alpha1beta3gamma2 expressed in HEK293 TetR cells at 30 uM after 30 mins by liquid scintillation counting method2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID1507388Displacement of [3H]muscimol from human GABAA receptor alpha1beta3gamma2 expressed in HEK293 TetR cell membranes after 1 hr by liquid scintillation counting method2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID1066193Anesthetic effect in mouse assessed as onset of loss of righting reflex at 8 to 16 mg/kg, iv2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.
AID604802Modulation of rat GABA-A alpha1beta2gamma2L receptor expressed in Xenopus oocytes assessed as increase of GABA-induced chloride current at 1 uM by two electrode voltage-clamp method relative to control2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID114282Hypnotic dose was determined by observing loss of righting reflex for a minimum period of 30 sec in 50% of treated mice after i.v. administration.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID604805Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as loss of righting reflex2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID1066190Anesthetic effect in mouse assessed as recovery of righting reflex at 1 to 8 mg/kg, iv2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.
AID604801Modulation of rat GABA-A alpha1beta2gamma2L receptor expressed in Xenopus oocytes assessed as increase of GABA-induced chloride current at 0.1 uM by two electrode voltage-clamp method relative to control2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID604804Modulation of rat GABA-A alpha1beta2gamma2L receptor expressed in Xenopus oocytes assessed as increase of chloride current at 10 uM by two electrode voltage-clamp method relative to GABA2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID601364Anesthetic effect in mouse assessed as immediate loss of righting reflex at 16 mg/kg, iv2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity.
AID227352Compound was evaluated for anesthetic activity (lowest dose producing loss of righting reflex)1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Anesthetic steroid mobility in model membrane preparations as examined by high-resolution 1H and 2H NMR spectroscopy.
AID604803Modulation of rat GABA-A alpha1beta2gamma2L receptor expressed in Xenopus oocytes assessed as increase of GABA-induced chloride current at 10 uM by two electrode voltage-clamp method relative to control2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID1507402Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expressed in Xenopus laevis oocytes assessed as potentiation of GABA chloride current up to 100 uM incubated for 15 to 25 secs by two-electrode voltage clamp assay relative to contr2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID604806Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as loss of swimming reflex2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID71999The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID71848Inhibition of [35S]TBPS binding to GABA-A receptor in rat cerebral cortex.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.
AID1507393Induction of [3H]R-mTFD-MPAB photoincorporation at human GABAA receptor alpha1beta3gamma2 expressed in HEK293 TetR cells at 30 uM after 30 mins by liquid scintillation counting method2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID604810Modulation of rat GABA-A alpha1beta2gamma2L receptor expressed in Xenopus oocytes assessed as increase of GABA-induced chloride current by two electrode voltage-clamp method relative to control2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID604809Displacement of [35S]TBPS from GABA-A receptor picrotoxin binding site in rat brain cortical membranes after 2 hrs by scintillation counting2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID604807Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as loss of swimming reflex at 3 uM2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID1507389Displacement of [3H]muscimol from human GABAA receptor alpha1beta3gamma2 expressed in HEK293 TetR cell membranes up to 100 uM after 1 hr by liquid scintillation counting method relative to control2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID1507399Anesthetic activity in tadpole assessed as loss of righting reflexes2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID1507398Anesthetic activity in tadpole assessed as loss of righting reflexes at 0.03 to 10 uM pretreated with tadpole followed by compound washout and transfer to fresh water measured up to 1 hr2017European journal of medicinal chemistry, Aug-18, Volume: 136Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
AID71982Inhibition of binding of tert-butyl bicyclophosphorothionate ([35 S]TBPS) at Gamma-aminobutyric acid A receptor from rat whole brain membranes2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Conformationally constrained anesthetic steroids that modulate GABA(A) receptors.
AID601361Anesthetic effect in mouse assessed as time taken for recovery of righting effect and walking at 16 mg/kg, iv2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID210604Therapeutic index by the ratio between LD50 to HD501997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID729040Stimulation of [3H]flunitrazepam binding to GABA type A receptor in mouse primary cortical neurons after 30 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity.
AID604808Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as loss of swimming reflex at 10 uM2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues.
AID52291Concentration required to potentiate GABA-evoked currents in voltage-clamped bovine chromaffin cells by 300%1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID1066192Anesthetic effect in mouse assessed as onset of loss of righting reflex at 1 to 8 mg/kg, iv2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.
AID1066198Anesthetic effect in mouse assessed as duration of loss of righting reflex at 16 mg/kg, iv2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.
AID1066191Anesthetic effect in mouse assessed as recovery of righting reflex at 8 to 16 mg/kg, iv2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.
AID244328Maximal efficacy for GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expressed in Xenopus oocytes2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
AID601360Anesthetic effect in mouse assessed as loss of righting reflex at 8 mg/kg, iv2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity.
AID221372Hypnotic dose required to cause a loss of righting reflex for a minimum period of 30 s in 50 percent of treated mice after intravenous administration.2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Conformationally constrained anesthetic steroids that modulate GABA(A) receptors.
AID119225Effect on interval between loss of righting reflex and return to righting reflex (sleep duration) was measured at a dose twice that of hypnotic dose.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (586)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990105 (17.92)18.7374
1990's95 (16.21)18.2507
2000's62 (10.58)29.6817
2010's242 (41.30)24.3611
2020's82 (13.99)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials157 (28.09%)5.53%
Reviews0 (0.00%)6.00%
Reviews12 (2.15%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies9 (1.61%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other36 (100.00%)84.16%
Other381 (68.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]