Page last updated: 2024-11-04

tetraethylammonium

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5413
CHEMBL ID9324
CHEBI ID44296
SCHEMBL ID16267
MeSH IDM0029362

Synonyms (51)

Synonym
nsc-102778
tetraetilammonio [italian]
ammonium, tetraethyl-
tetramon
tetrylammonium
ethanaminium, n,n,n-triethyl-
brn 1738225
bdbm50149890
gtpl2343
lopac-t-2265
NCGC00016008-01
66-40-0
C07512
tetraethylammonium
tetraethylammonium ion
inchi=1/c8h20n/c1-5-9(6-2,7-3)8-4/h5-8h2,1-4h3/q+
[net4](+)
CHEBI:44296 ,
tetraethylazanium
net4(+)
n,n,n-triethylethanaminium
ethanaminium,n,n-triethyl-, dodeca-.mu.-chlorohexachlorohexatantalate(2-) octahedro (2:1)
ethanaminium,n,n-triethyl-, acetate
ammonium, dodeca-.mu.-chlorohexachlorohexatantalate(2-)(2:1), octahedro-
nsc156315
nsc-156315
nsc152122
NCGC00162361-01
NCGC00016008-03
CHEMBL9324 ,
tetraethylammonium cation
AKOS002264960
CCG-205259
5av7g7eiee ,
unii-5av7g7eiee
tetraetilammonio
4-04-00-00331 (beilstein handbook reference)
tetraethylamine
NCGC00016008-02
STL281844
tetraethylammonium ion(1+)
[14c]-tea
gtpl4575
[14c]tea
DB08837
SCHEMBL16267
tetraethyl ammonium
CBXCPBUEXACCNR-UHFFFAOYSA-N
DTXSID2045024
Q410728
NCGC00016008-06

Research Excerpts

Overview

Tetraethylammonium (TEA) is a potassium channel (KCh) blocker. It has been extensively used as a molecular probe to explore the structure of channels' ion pathway.

ExcerptReferenceRelevance
"Tetraethylammonium (TEA) is a potassium channel (KCh) blocker applied in the functional and pharmacological studies of the KChs. "( The evidence of HeLa cell apoptosis induced with tetraethylammonium using proteomics and various analytical methods.
Huang, HQ; Huang, L; Huang, QY, 2014
)
2.1
"Tetraethylammonium (TEA) is a potassium (K(+)) channel inhibitor that has been extensively used as a molecular probe to explore the structure of channels' ion pathway. "( Tuning the tetraethylammonium sensitivity of potassium channel Kcv by subunit combination.
Gu, LQ; Ritzo, B; Tan, Q; Tian, K, 2012
)
2.21
"Tetraethylammonium (TEA+) is an effective inhibitor of a variety of K+ channels, and has been widely used to reduce K+-sensitive background conductances in electrophysiological investigations of the Na+,K+-ATPase. "( Voltage-dependent inhibition of the Na+,K+ pump by tetraethylammonium.
Eckstein-Ludwig, U; Rettinger, J; Schwarz, W; Vasilets, LA, 1998
)
1.99

Effects

ExcerptReferenceRelevance
"Tetraethylammonium (TEA) has been used recently to probe natural and mutational variants of voltage-dependent K+ channels encoded by cDNA clones. "( Internal and external TEA block in single cloned K+ channels.
Brown, AM; Kirsch, GE; Taglialatela, M, 1991
)
1.72

Actions

Tetraethylammonium (TEA), increase twitch force of normal diaphragm. ions inhibit the hyperpolarizing response of cells to bradykinin or inositol 1,4,5-trisphosphate.

ExcerptReferenceRelevance
"Tetraethylammonium was added to enhance release."( Kinetic analysis of stimulation-evoked overflow of noradrenaline and dopamine beta-hydroxylase from the isolated rabbit heart. The effect of DOPA decarboxylase inhibition.
Muscholl, E; Spira, FJ, 1982
)
0.99
"A tetraethylammonium-induced increase of intracellular concentrations of calcium, [Ca2+]i, a response that depends on functional 113-picosiemen potassium channels, was also eliminated or markedly reduced by 10 nM beta-amyloid."( Soluble beta-amyloid induction of Alzheimer's phenotype for human fibroblast K+ channels.
Alkon, DL; Etcheberrigaray, R; Ito, E; Kim, CS, 1994
)
0.85
"tetraethylammonium (TEA), increase twitch force of normal diaphragm."( Inotrophic effects of the K(+) channel blocker TEA on dystrophic (mdx and dy/dy) mouse diaphragm.
Manubay, P; van Lunteren, E, 2001
)
1.03
"Tetraethylammonium ions inhibit the hyperpolarizing response of cells to bradykinin or inositol 1,4,5-trisphosphate."( Bradykinin-activated transmembrane signals are coupled via No or Ni to production of inositol 1,4,5-trisphosphate, a second messenger in NG108-15 neuroblastoma-glioma hybrid cells.
Higashida, H; Klee, W; Nirenberg, M; Streaty, RA, 1986
)
0.99

Treatment

Tetraethylammonium (TEA) broadened the action-potential and enhanced long-lasting hyperpolarizing after-potentials (AH) Treatment also resulted in excitatory postsynaptic potential/spike potentiation of N-methyl-D-aspartate receptor-mediated responses.

ExcerptReferenceRelevance
"Tetraethylammonium pretreatment blunted the acetylcholine- and sodium nitroprusside-induced decrease in [K+]i by 82%, (n > 5, P < 0.001), respectively."( Nitric oxide relaxes rabbit corpus cavernosum smooth muscle via a potassium-conductive pathway.
Ganz, MB; Kasner, SE; Seftel, AD; Viola, KA, 1996
)
1.02
"Tetraethylammonium treatment also resulted in excitatory postsynaptic potential/spike potentiation of pharmacologically isolated N-methyl-D-aspartate receptor-mediated responses which could be reversed by subsequent low-frequency or tetanic stimuli."( Changes in neuronal excitability and synaptic function in a chronic model of temporal lobe epilepsy.
Bernard, C; Marsden, DP; Wheal, HV, 2001
)
1.03
"Pretreatment with tetraethylammonium inhibited this increase (0.2 +/- 0.1 microM)."( Noninvasive measurement of potassium efflux as an early indicator of cell death in mouse embryos.
Keefe, DL; Liu, L; Smith, PJ; Trimarchi, JR, 2000
)
0.63
"5. Treatment with tetraethylammonium (TEA) broadened the action-potential and enhanced long-lasting hyperpolarizing after-potentials (AH)."( Mechanism of action of galanin on myenteric neurons.
Palmer, JM; Tamura, K; Winkelmann, CK; Wood, JD, 1988
)
0.6

Toxicity

ExcerptReferenceRelevance
"The acute toxic effects of thiabendazole [2-(4'-thiazolyl)benzimidazole; TBZ] on the kidneys of ICR mice were investigated."( Acute renal toxicity of thiabendazole (TBZ) in ICR mice.
Fujitani, T; Tada, Y; Yoneyama, M, 1992
)
0.28
" In contrast apical treatment with PCBD-NAC was only toxic at high concentrations (greater than 850 microM), and this effect could hardly be inhibited by AOAA."( Differential toxicity as a result of apical and basolateral treatment of LLC-PK1 monolayers with S-(1,2,3,4,4-pentachlorobutadienyl)glutathione and N-acetyl-S-(1,2,3,4,4-pentachlorobutadienyl)-L-cysteine.
Mertens, JJ; Spenkelink, B; Temmink, JH; van Bladeren, PJ; van Doorn, WJ; Weijnen, JG, 1988
)
0.27
" The purpose of this study was to examine if an arene oxide intermediate is a toxic metabolite contributing to NDPS-induced nephropathy in rats."( Acute N-(3,4,5-trichlorophenyl)succinimide-induced nephrotoxicity in Sprague-Dawley and Fischer-344 rats.
Brown, PI; Lahoda, EP; Rankin, GO; Yang, DJ, 1986
)
0.27
" Pretreatment with phenobarbital enhanced the toxic response of renal cortical slices to CHCl3 in vitro as indicated by decreased p-aminohippurate and tetraethylammonium accumulation."( Mechanism of chloroform nephrotoxicity. IV. Phenobarbital potentiation of in vitro chloroform metabolism and toxicity in rabbit kidneys.
Bailie, MB; Hook, JB; Newton, JF; Smith, JH, 1984
)
0.47
"Whilst chemical cleavage of mismatch (CCM) detects all point mutations in DNA, its widespread use has been hampered by the complex multistage methodology and the need for toxic chemicals, in particular osmium tetroxide."( Potassium permanganate and tetraethylammonium chloride are a safe and effective substitute for osmium tetroxide in solid-phase fluorescent chemical cleavage of mismatch.
Deeble, VJ; Roberts, E; Taylor, GR; Woods, CG, 1997
)
0.59
" The exact toxic mechanism of PQ is still unclear but it is assumed to involve redox cycling and formation of reactive oxygen species."( The cytotoxic effect of paraquat to isolated renal proximal tubular segments from rabbits.
Friis, C; Mølck, AM, 1997
)
0.3
"Renal injury is a common side effect of the chemotherapeutic agent ifosfamide."( Ifosfamide toxicity in cultured proximal renal tubule cells.
Springate, J; Taub, M, 2007
)
0.34
"In addition to inhibiting the excitation conduction process in peripheral nerves, local anesthetics (LAs) cause toxic effects on the central nervous system, cardiovascular system, neuromuscular junction, and cell metabolism."( Cytotoxicity of local anesthetics in human neuronal cells.
Blanck, TJ; Garavito-Aguilar, ZV; Patel, S; Perez-Castro, R; Recio-Pinto, E; Rosenberg, A; Xu, F; Zhang, J, 2009
)
0.35
" Lidocaine, linked to the highest incidence of transient neurological symptoms, was not the most toxic LA, whereas bupivacaine, a drug causing a very low incidence of transient neurological symptoms, was the most toxic LA in our cell model."( Cytotoxicity of local anesthetics in human neuronal cells.
Blanck, TJ; Garavito-Aguilar, ZV; Patel, S; Perez-Castro, R; Recio-Pinto, E; Rosenberg, A; Xu, F; Zhang, J, 2009
)
0.35
" Sal significantly increased testicular P concentration compared with untreated controls and significantly elevated the testicular Ca and Fe concentrations compared with the toxic control group."( Ameliorative effects of deferiprone and tetraethylammonium salt of salinomycinic acid on lead-induced toxicity in mouse testes.
Dorkov, P; Gluhcheva, Y; Helbich, TH; Ivanova, J; Keppler, B; Koellensperger, G; Pashkunova-Martic, I; Pavlova, E; Petrova, E; Schaier, M, 2021
)
0.89

Pharmacokinetics

ExcerptReferenceRelevance
" Simulated release from a 20-vesicle point source produced DA concentrations sufficient for receptor activation up to 20 microm away with a DA half-life at this distance of several hundred milliseconds."( Dopamine-mediated volume transmission in midbrain is regulated by distinct extracellular geometry and uptake.
Cragg, SJ; Kume-Kick, J; Nicholson, C; Rice, ME; Tao, L, 2001
)
0.31
" Previous reports indicate that ELT is mainly eliminated in the liver, although its pharmacokinetic profile has not yet been clarified in detail."( Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent.
Horikawa, M; Ishiwata, N; Kato, Y; Matsubara, K; Nakamichi, N; Silver, DL; Sugiura, T; Takeuchi, K; Umeda, S, 2011
)
0.37
" Hence OCT can have a potential pharmacokinetic role in modulating the ocular bioavailability of their substrates administered topically, which are used as ocular therapeutics."( Potential pharmacokinetic role of organic cation transporters in modulating the transcorneal penetration of its substrates administered topically.
Azad, RV; Biswas, NR; Nirmal, J; Singh, SB; Thavaraj, V; Velpandian, T, 2013
)
0.39

Compound-Compound Interactions

ExcerptReferenceRelevance
"Alpha,alpha-disubstituted acetamides undergo oxidative dehomologation to give one-carbon-shorter ketones when reacted with a hypervalent iodine (lambda(5)) reagent in combination with tetraethylammonium bromide (TEAB) in various solvents."( Oxidative conversion of alpha,alpha-disubstituted acetamides to corresponding one-carbon-shorter ketones using hypervalent iodine (lambda5) reagents in combination with tetraethylammonium bromide.
Akamanchi, KG; Bellale, EV; Bhalerao, DS, 2008
)
0.73
" These results suggest that the inhibition of MATEs, but not OCT2, is a likely mechanism underlying the drug-drug interactions with cimetidine in renal elimination."( Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney.
Inoue, K; Ito, S; Kusuhara, H; Sugiyama, Y; Toyoshima, J; Yokochi, M; Yuasa, H, 2012
)
0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
" We hypothesized that endothelium-derived hyperpolarizing factors contribute to resting vascular tone by K(+)(Ca) channel activation and epoxyeicosatrienoic acid release and that endothelium-derived hyperpolarizing factors compensate for reduced nitric oxide bioavailability at rest and with endothelium-dependent vasodilators."( Endothelium-derived hyperpolarizing factor determines resting and stimulated forearm vasodilator tone in health and in disease.
Kavtaradze, N; Lin, J; Manatunga, A; Murrow, JR; Ozkor, MA; Quyyumi, AA; Rahman, AM, 2011
)
0.37
" Oral bioavailability was not affected (F = 64 ± 4 versus 59 ± 11; knockout versus wild type)."( Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
Bedwell, DW; Higgins, JW; Zamek-Gliszczynski, MJ, 2012
)
0.38
" Hence OCT can have a potential pharmacokinetic role in modulating the ocular bioavailability of their substrates administered topically, which are used as ocular therapeutics."( Potential pharmacokinetic role of organic cation transporters in modulating the transcorneal penetration of its substrates administered topically.
Azad, RV; Biswas, NR; Nirmal, J; Singh, SB; Thavaraj, V; Velpandian, T, 2013
)
0.39
"Through interference with free radicals, the nitroxide tempol potentially increases bioavailability of nitric oxide (NO) and along with modulation of potassium channels reduces blood pressure (BP)."( Negative inotropic and hypotensive effects of the superoxide dismutase mimetic tempol in pigs.
Buus, NH; Frederiksen, CA; Hyldebrandt, JA; Juhl-Olsen, P; Kristensen, MN; Simonsen, U; Sivén, E; Sloth, E, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" The concentration of TBZ in blood at 1 or 5 hr after dosing was lower in mice pretreated with microsomal monooxygenase system inducers and was higher in those pretreated with the inhibitors, than in those given TBZ alone."( Acute renal toxicity of thiabendazole (TBZ) in ICR mice.
Fujitani, T; Tada, Y; Yoneyama, M, 1992
)
0.28
"3 microM) shifted the dose-response curve to the right in a parallel manner."( Muscarinic receptor is coupled with a cation channel through a GTP-binding protein in guinea-pig chromaffin cells.
Inoue, M; Kuriyama, H, 1991
)
0.28
" A dose-response curve for the depolarizing shift of the activation and inactivation curves of IA, as a function of manganese concentration, could be fitted by a single binding site model with an apparent dissociation constant of approximately 17 mM."( A modulatory action of divalent cations on transient outward current in cultured rat sensory neurones.
Mayer, ML; Sugiyama, K, 1988
)
0.27
" Subsequent daily doses of gentamicin ranging from 0 to 120 mg/kg elicited a dose-response nephrotoxicity in both control and PVA-pretreated rats after 6 or 12 days of drug."( Dose-response studies of gentamicin nephrotoxicity in rats with experimental renal dysfunction. II. Polyvinyl alcohol glomerulopathy.
Brown, TT; Carver, MP; Monteiro-Riviere, NA; Riviere, JE, 1985
)
0.27
" The shapes of the dose-response curves for inhibition of the organic cation and organic anion transport are different, and the inhibition is competitive in each case."( Mechanisms for the renal secretion of cisplatin.
Herbert, BH; Nelson, JA; Santos, G, 1984
)
0.27
" The dose-response curve suggests a one-to-one stoichiometry for TEA-receptor binding with an apparent dissociation constant on 24 mM."( Inhibition of potassium conductance with external tetraethylammonium ion in Myxicola giant axons.
Binstock, L; Wong, BS, 1980
)
0.51
" Analysis of dose-response experimental results suggests that TEA binding resulted in a partial block of these channels with an equilibrium dissociation constant of approximately 12-15 mM."( Block of neuronal fast chloride channels by internal tetraethylammonium ions.
Blatz, AL; Sanchez, DY, 1994
)
0.54
" To this end, dose-response curves to phenylephrine and BaCl2 were studied in the renal vasculature under basal conditions and after the infusion of N(omega)-nitro-L-arginine methyl ester (L-NAME) and tetraethylammonium (TEA) in endothelium-intact and endothelium-denuded (CHAPS-treated) preparations."( Modulatory role of endothelium-derived relaxing factors on the response to vasoconstrictors and flow-pressure curve in the isolated perfused rat kidney.
Osuna, A; Vargas, F,
)
0.32
" Dose-response relations for TEA and 4-AP were obtained by exposing single cells to ten concentrations exponentially distributed over four orders of magnitude."( Variations in the ensemble of potassium currents underlying resonance in turtle hair cells.
Art, JJ; Goodman, MB, 1996
)
0.29
" The dose-response relation for IACh versus ACh concentration was fitted by the Hill equation with EC50 = approx."( Nicotinic acetylcholine sensitivity of rat petrosal sensory neurons in dissociated cell culture.
Nurse, CA; Zhong, H, 1997
)
0.3
" However, the inhibition of the combined CPA and CCh response was reduced and the dose-response curve of SIN-1 shifted to the right."( Involvement of intracellular Ca2+ stores in inhibitory effects of NO donor SIN-1 and cGMP.
Allescher, HD; Franck, H; Puschmann, A; Schusdziarra, V; Storr, M, 1998
)
0.3
" A dose-response relationship was established for the K+ channel blockers."( Differential effects of potassium channel blockers on the activity of the locomotor network in neonatal rat.
Cazalets, JR; Magoul, R; Sqalli-Houssaini, Y, 1999
)
0.3
" The model in which the occupancy of one of four binding sites by melatonin is sufficient to block the channels gives the best fit to the dose-response relationship, although all four binding sites can be occupied by the drug."( Multiple binding sites for melatonin on Kv1.3.
Csécsei, G; Damjanovich, S; Gáspár, R; Panyi, G; Péter, M; Pieri, C; Varga, Z, 2001
)
0.31
" These results suggest that MET is endowed with peculiar hypophagic effects at dosage levels that are not able to affect gross behaviour in mice."( Methylamine and benzylamine induced hypophagia in mice: modulation by semicarbazide-sensitive benzylamine oxidase inhibitors and aODN towards Kv1.1 channels.
Banchelli, G; Galeotti, N; Ghelardini, C; Pirisino, R; Raimondi, L, 2001
)
0.31
" Kinase assays demonstrated dose-response relationships between dietary salt intake and the activities of p38 MAP kinase and p42/44 MAP kinase."( Increased dietary salt activates rat aortic endothelium.
Sanders, PW; Ying, WZ, 2002
)
0.31
" The biphasic dose-response for D-diltiazem confirmed the low sensitivity of Ca2+ channels for the molecule."( Voltage-gated channels and calcium homeostasis in mammalian rod photoreceptors.
Bordais, A; Cia, D; Forster, V; Picaud, S; Rendon, A; Sahel, JA; Varela, C, 2005
)
0.33
" Dose-response curves for transport and the ratio of dye concentration in the secreted fluid to that in the bathing medium (S/M) were determined for Texas Red as well as for P-gp substrates (rhodamine 123, daunorubicin), the organic anion fluorescein and the organic cation quinacrine."( Transepithelial transport of fluorescent p-glycoprotein and MRP2 substrates by insect Malpighian tubules: confocal microscopic analysis of secreted fluid droplets.
Leader, JP; O'Donnell, MJ, 2005
)
0.33
"1 ion channel blocker (TEA) dosage response is characterized and the binding activity is examined."( Open-access microfluidic patch-clamp array with raised lateral cell trapping sites.
Hung, PJ; Lau, AY; Lee, LP; Wu, AR, 2006
)
0.33
" The dose-response curves could be modeled by a competition model that reduces the pool of free PIP(2)."( Electrostatic interaction of internal Mg2+ with membrane PIP2 Seen with KCNQ K+ channels.
Hille, B; Suh, BC, 2007
)
0.34
" Dose-response curves of donepezil effect both on I (C) and I (K) were shifted right along horizontal axis when donepezil was applied in combination with TEA."( The binding of donepezil with external mouth of K+-channels of molluscan neurons.
Bukanova, JV; Marchenko, EV; Rossokhin, AV; Skrebitsky, VG; Solntseva, EI, 2009
)
0.35
"We derive equations for the effective concentration giving 10% inhibition (EC10) with 95% confidence limits for probit (log-normal), Weibull, and logistic dose-response models on the basis of experimentally derived median effective concentrations (EC50s) and the curve slope at the central point (50% inhibition)."( Dose-response regressions for algal growth and similar continuous endpoints: calculation of effective concentrations.
Christensen, ER; Kusk, KO; Nyholm, N, 2009
)
0.35
"3 x 10(-3) mol/L) produced a significant rightward shift in the phenylephrine dose-response curve, but had no effects on the potassium chloride-induced contraction."( Relaxant effects of matrine on aortic smooth muscles of guinea pigs.
Dai, GD; Fu, XY; Yan, L; Zheng, J; Zheng, P; Zhou, R; Zhou, X, 2009
)
0.35
" Levcromakalim produced concentration-dependent inhibitory effect on myometrial spontaneity and relaxant effect and the dose-response curve (DRC) was shifted towards right in the presence of glybenclamaide."( Cellular coupling of potassium channels with beta2 adrenoceptors in mediating myometrial relaxation in buffaloes (Bubalus bubalis).
Choudhury, S; Garg, SK; Mishra, SK; Singh, TU, 2010
)
0.36
" NE dose-response curves were studied before and after BK(Ca) blockade or after combined blockade of BK(Ca) and NO synthase (NOS) in femoral arteries with intact endothelium from normotensive Wistar (WIS), hypertensive hereditary hypertriglyceridemic (HTG), or spontaneously hypertensive rats (SHR)."( Influence of calcium-dependent potassium channel blockade and nitric oxide inhibition on norepinephrine-induced contractions in two forms of genetic hypertension.
Karen, P; Kunes, J; Lísková, S; Petrová, M; Zicha, J,
)
0.13
" The temporal logarithmic concentration generator was also integrated with planar patch-clamp chips for dose-response assays on ion channels."( A microfluidic concentration generator for dose-response assays on ion channel pharmacology.
Chen, CY; Jong, DS; Wo, AM, 2012
)
0.38
" IC50 values of the WT and mutants for the mercury compounds were derived from dose-response analyses."( Functional and molecular effects of mercury compounds on the human OCTN1 cation transporter: C50 and C136 are the targets for potent inhibition.
Galluccio, M; Iannì, M; Indiveri, C; Peta, V; Pochini, L; Scalise, M, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quaternary ammonium ionA derivative of ammonium, NH4(+), in which all four of the hydrogens bonded to nitrogen have been replaced with univalent (usually organyl) groups.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency37.68580.100020.879379.4328AID488773; AID588453
NFKB1 protein, partialHomo sapiens (human)Potency11.22020.02827.055915.8489AID895; AID928
thyroid stimulating hormone receptorHomo sapiens (human)Potency3.98110.001318.074339.8107AID926; AID938
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency3.16230.00106.000935.4813AID943
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency33.80780.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1Mus musculus (house mouse)IC50 (µMol)0.54000.28001.32753.9000AID678794
Solute carrier family 22 member 1Mus musculus (house mouse)Ki128.00003.60005.45007.3000AID682044
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)156.00000.40003.10009.7000AID679160
Solute carrier family 22 member 1 Homo sapiens (human)Ki160.66670.55004.26507.4600AID679156; AID679498; AID681146
Solute carrier family 22 member 2Mus musculus (house mouse)IC50 (µMol)3.50002.80004.76678.0000AID678785
Solute carrier family 22 member 3Homo sapiens (human)IC50 (µMol)10,300.00000.09003.72779.5000AID679482
Solute carrier family 22 member 3Homo sapiens (human)Ki1,372.00000.12000.12000.1200AID681584
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki144.20000.13002.37856.9000AID678997; AID679199; AID681574
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)Ki52.20000.39002.32959.4000AID681637
[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)
Solute carrier family 22 member 1Mus musculus (house mouse)Km38.000010.000010.000010.0000AID680370
Solute carrier family 22 member 2Homo sapiens (human)Km150.25000.02891.04072.6000AID678793; AID678957; AID679158; AID679159
Solute carrier family 22 member 1 Homo sapiens (human)Activity168.00000.71005.30179.7000AID681117
Solute carrier family 22 member 1 Homo sapiens (human)Km115.66000.47704.03089.0000AID386626; AID680362
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)Km2.32002.32002.32002.3200AID386626
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Km98.33330.27005.695010.0000AID678993; AID678994; AID679189; AID679190; AID679196; AID679825
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)Km130.25719.40009.40009.4000AID679292; AID679635; AID681589; AID681622; AID681625; AID681626; AID681631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
histamine metabolic processSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 3Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin transportSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
organic anion transportSolute carrier family 22 member 3Homo sapiens (human)
monocarboxylic acid transportSolute carrier family 22 member 3Homo sapiens (human)
monoamine transportSolute carrier family 22 member 3Homo sapiens (human)
spermidine transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine transportSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
regulation of appetiteSolute carrier family 22 member 3Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 3Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
histamine transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 3Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
epinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 3Homo sapiens (human)
startle responsePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
regulation of muscle contractionPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuroblast proliferationPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
protein localizationPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cell communication by electrical couplingPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
magnesium ion homeostasisPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuronal action potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
optic nerve developmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
hippocampus developmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cerebral cortex developmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
corpus callosum developmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuronal signal transductionPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuromuscular processPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of touchPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
protein homooligomerizationPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
regulation of postsynaptic membrane potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
axon developmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cellular response to magnesium ionPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
regulation of presynaptic membrane potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
carnitine transportSolute carrier family 22 member 4Homo sapiens (human)
triglyceride metabolic processSolute carrier family 22 member 4Homo sapiens (human)
sodium ion transportSolute carrier family 22 member 4Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 4Homo sapiens (human)
carnitine metabolic processSolute carrier family 22 member 4Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 4Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 4Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 4Homo sapiens (human)
acetate ester transportSolute carrier family 22 member 4Homo sapiens (human)
carnitine transmembrane transportSolute carrier family 22 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
protein bindingSolute carrier family 22 member 3Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
disordered domain specific bindingPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
protein bindingSolute carrier family 22 member 4Homo sapiens (human)
ATP bindingSolute carrier family 22 member 4Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
amino acid transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
amino-acid betaine transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
carnitine transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
symporter activitySolute carrier family 22 member 4Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 4Homo sapiens (human)
PDZ domain bindingSolute carrier family 22 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
nuclear outer membraneSolute carrier family 22 member 3Homo sapiens (human)
plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
endomembrane systemSolute carrier family 22 member 3Homo sapiens (human)
membraneSolute carrier family 22 member 3Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
mitochondrial membraneSolute carrier family 22 member 3Homo sapiens (human)
neuronal cell bodySolute carrier family 22 member 3Homo sapiens (human)
presynapseSolute carrier family 22 member 3Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cytosolPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cell junctionPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
dendritePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
cytoplasmic vesiclePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
paranode region of axonPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
presynaptic membranePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuronal cell bodyPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
axon initial segmentPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
perikaryonPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
axon terminusPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
juxtaparanode region of axonPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
calyx of HeldPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
synapsePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
postsynaptic membranePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
anchoring junctionPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
glutamatergic synapsePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
dendritePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
paranode region of axonPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
synapsePotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
juxtaparanode region of axonPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
neuronal cell bodyPotassium voltage-gated channel subfamily A member 1Homo sapiens (human)
mitochondrionSolute carrier family 22 member 4Homo sapiens (human)
plasma membraneSolute carrier family 22 member 4Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 4Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 4Homo sapiens (human)
mitochondrial membraneSolute carrier family 22 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (159)

Assay IDTitleYearJournalArticle
AID1346635Mouse TRPV2 (Transient Receptor Potential channels)2007Molecular pharmacology, Nov, Volume: 72, Issue:5
Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
AID1346666Human Kv1.7 (Voltage-gated potassium channels)2002European journal of human genetics : EJHG, Jan, Volume: 10, Issue:1
Characterisation of the human voltage-gated potassium channel gene, KCNA7, a candidate gene for inherited cardiac disorders, and its exclusion as cause of progressive familial heart block I (PFHBI).
AID1346657Human Kv1.6 (Voltage-gated potassium channels)1990The EMBO journal, Jun, Volume: 9, Issue:6
Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family.
AID1346713Human Kv7.3 (Voltage-gated potassium channels)2000British journal of pharmacology, Feb, Volume: 129, Issue:3
Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels.
AID1346458Human KNa1.2 (Calcium- and sodium-activated potassium channels)2006The Journal of neuroscience : the official journal of the Society for Neuroscience, May-10, Volume: 26, Issue:19
Opposite regulation of Slick and Slack K+ channels by neuromodulators.
AID1346699Human Kv7.4 (Voltage-gated potassium channels)2008The Journal of biological chemistry, Nov-07, Volume: 283, Issue:45
Homomeric and heteromeric assembly of KCNQ (Kv7) K+ channels assayed by total internal reflection fluorescence/fluorescence resonance energy transfer and patch clamp analysis.
AID1346670Human Kv4.1 (Voltage-gated potassium channels)2002Molecular and cellular biochemistry, Sep, Volume: 238, Issue:1-2
Endogenous Kv channels in human embryonic kidney (HEK-293) cells.
AID1346442Human KCa2.2 (Calcium- and sodium-activated potassium channels)2010Progress in neurobiology, Jul, Volume: 91, Issue:3
Small conductance calcium-activated potassium channels: from structure to function.
AID1346465Rat KNa1.1 (Calcium- and sodium-activated potassium channels)2005Trends in neurosciences, Aug, Volume: 28, Issue:8
For K+ channels, Na+ is the new Ca2+.
AID1346705Rat Kv3.4 (Voltage-gated potassium channels)1992The EMBO journal, Jul, Volume: 11, Issue:7
Characterization of a Shaw-related potassium channel family in rat brain.
AID1346466Rat KNa1.2 (Calcium- and sodium-activated potassium channels)2006The Journal of neuroscience : the official journal of the Society for Neuroscience, May-10, Volume: 26, Issue:19
Opposite regulation of Slick and Slack K+ channels by neuromodulators.
AID1346689Human Kv7.5 (Voltage-gated potassium channels)2000The Journal of biological chemistry, Aug-04, Volume: 275, Issue:31
KCNQ5, a novel potassium channel broadly expressed in brain, mediates M-type currents.
AID1346695Rat Kv3.3 (Voltage-gated potassium channels)1992Proceedings. Biological sciences, Apr-22, Volume: 248, Issue:1321
Cloning of ShIII (Shaw-like) cDNAs encoding a novel high-voltage-activating, TEA-sensitive, type-A K+ channel.
AID1346690Mouse Kv1.1 (Voltage-gated potassium channels)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346449Human KCa2.1 (Calcium- and sodium-activated potassium channels)2010Progress in neurobiology, Jul, Volume: 91, Issue:3
Small conductance calcium-activated potassium channels: from structure to function.
AID1346655Human Kv2.2 (Voltage-gated potassium channels)1998The American journal of physiology, 05, Volume: 274, Issue:5
Molecular identification of a component of delayed rectifier current in gastrointestinal smooth muscles.
AID1346689Human Kv7.5 (Voltage-gated potassium channels)2000The Journal of biological chemistry, Jul-21, Volume: 275, Issue:29
Molecular cloning and functional expression of KCNQ5, a potassium channel subunit that may contribute to neuronal M-current diversity.
AID1346696Human Kv7.2 (Voltage-gated potassium channels)2000British journal of pharmacology, Feb, Volume: 129, Issue:3
Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels.
AID1346681Mouse Kv3.1 (Voltage-gated potassium channels)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346707Mouse Kv1.3 (Voltage-gated potassium channels)1994Molecular pharmacology, Jun, Volume: 45, Issue:6
Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346705Rat Kv3.4 (Voltage-gated potassium channels)1991FEBS letters, Jan-28, Volume: 278, Issue:2
Cloning and functional expression of a TEA-sensitive A-type potassium channel from rat brain.
AID1346668Rat Kv2.1 (Voltage-gated potassium channels)2006The Biochemical journal, Jun-01, Volume: 396, Issue:2
Modulation of Kv2.1 channel gating and TEA sensitivity by distinct domains of SNAP-25.
AID1346696Human Kv7.2 (Voltage-gated potassium channels)2000Molecular pharmacology, Sep, Volume: 58, Issue:3
Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.
AID1346703Rat Kv3.2 (Voltage-gated potassium channels)2002The Journal of physiology, Jan-15, Volume: 538, Issue:Pt 2
Gating, modulation and subunit composition of voltage-gated K(+) channels in dendritic inhibitory interneurones of rat hippocampus.
AID1346452Human KCa2.3 (Calcium- and sodium-activated potassium channels)2010Progress in neurobiology, Jul, Volume: 91, Issue:3
Small conductance calcium-activated potassium channels: from structure to function.
AID1346477Human Kir2.3 (Inwardly rectifying potassium channels)1994The Journal of biological chemistry, Aug-12, Volume: 269, Issue:32
Cloning and expression of a novel human brain inward rectifier potassium channel.
AID1346659Mouse Kv1.7 (Voltage-gated potassium channels)1998The Journal of biological chemistry, Mar-06, Volume: 273, Issue:10
Genomic organization, chromosomal localization, tissue distribution, and biophysical characterization of a novel mammalian Shaker-related voltage-gated potassium channel, Kv1.7.
AID1346671Human Kv1.8 (Voltage-gated potassium channels)2000American journal of physiology. Renal physiology, Jun, Volume: 278, Issue:6
KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
AID1210304Induction of human PMAT activity expressed in Xenopus laevis oocytes assessed as induction of inward current at 2.5 mM in NaCl buffer at pH 7.5 by two-microelectrode voltage-clamp method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Electrophysiological characterization of the polyspecific organic cation transporter plasma membrane monoamine transporter.
AID681117TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells2003Molecular pharmacology, Mar, Volume: 63, Issue:3
Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1.
AID681584TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID679158TP_TRANSPORTER: uptake in OCT2-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID678793TP_TRANSPORTER: uptake in OCT2A-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID680186TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, TEA: 500 uM) in Xenopus laevis oocytes2000The Journal of biological chemistry, Feb-11, Volume: 275, Issue:6
Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta.
AID680954TP_TRANSPORTER: uptake in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID681149TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
AID1210863AUC (0 to t) in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID682273TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.025 uM, TEA: 2000 uM) in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID679292TP_TRANSPORTER: uptake (apical to cell) in OCT2-expressing NIH3T3 cells1999Toxicological sciences : an official journal of the Society of Toxicology, Feb, Volume: 47, Issue:2
A transfected cell model for the renal toxin transporter, rOCT2.
AID1210857Volume of distribution at steady state in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID678806TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells2000Biochimica et biophysica acta, Jun-01, Volume: 1466, Issue:1-2
Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.
AID681622TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999Biochimica et biophysica acta, Mar-04, Volume: 1417, Issue:2
Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes.
AID679635TP_TRANSPORTER: uptake (electrogenesis) in Xenopus laevis oocytes2000The Journal of biological chemistry, Sep-22, Volume: 275, Issue:38
Mechanism of electrogenic cation transport by the cloned organic cation transporter 2 from rat.
AID1210832Drug recovery in Oct1/Oct2-knockout FVB mouse urine assessed as corrected compound recovery by measuring nominal to observerd glomerular filtration rate ratio at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID678986TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999Biochemical and biophysical research communications, Feb-16, Volume: 255, Issue:2
Molecular cloning and characterization of two novel human renal organic anion transporters (hOAT1 and hOAT3).
AID682222TP_TRANSPORTER: inhibition of Guanidine uptake (Guanidine: 35 uM, TEA: 5000 uM) in OCT3-expressing HeLa cells1998The Journal of biological chemistry, Jun-26, Volume: 273, Issue:26
Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta.
AID1210303Induction of human PMAT activity expressed in Xenopus laevis oocytes assessed as induction of inward current at 2.5 mM in NaCl buffer at pH 6 by two-microelectrode voltage-clamp method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Electrophysiological characterization of the polyspecific organic cation transporter plasma membrane monoamine transporter.
AID680332TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Biochemical and biophysical research communications, Aug-23, Volume: 296, Issue:3
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.
AID588966Substrates of transporters of clinical importance in the absorption and disposition of drugs, OCT22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID386627Activity of human OCT1 expressed in HEK293 cells assessed per mg of protein2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID679825TP_TRANSPORTER: uptake (electrogenesis,-50mV) in Xenopus laevis oocytes1996The Journal of biological chemistry, Dec-20, Volume: 271, Issue:51
Electrogenic properties and substrate specificity of the polyspecific rat cation transporter rOCT1.
AID681575TP_TRANSPORTER: uptake in Xenopus laevis oocytes1998FEBS letters, Jun-12, Volume: 429, Issue:2
Identification of multispecific organic anion transporter 2 expressed predominantly in the liver.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1210827Volume of distribution at steady state in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID679482TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.2 uM) in OCT3-expressing HEK293 cells2001Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 363, Issue:1
Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID679196TP_TRANSPORTER: uptake (basolateral to cell) in OCT1-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID682060TP_TRANSPORTER: uptake in Octn2-HEK cells2000The Journal of biological chemistry, Dec-22, Volume: 275, Issue:51
Molecular and functional characterization of organic cation/carnitine transporter family in mice.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1210825Initial plasma concentration in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID682291TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, TEA: 500 uM) in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID1209585Drug uptake in Sprague-Dawley rat brain slices in presence of 50 nM of monensin2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1210858Terminal half life life in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID1210826Clearance in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID678994TP_TRANSPORTER: uptake in Xenopus laevis oocytes2000Biochemical pharmacology, Jul-15, Volume: 60, Issue:2
Role of organic cation transporters in the renal secretion of nucleosides.
AID1210828Terminal half life in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID386626Activity of human OCT1 expressed in HEK293 cells2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID678785TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes2002Biochemical and biophysical research communications, Aug-23, Volume: 296, Issue:3
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.
AID681637TP_TRANSPORTER: inhibition of TEA uptake (apical to cell) in OCT2-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID680388TP_TRANSPORTER: uptake in OCTN1-expressing HEK 293 cells1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID681631TP_TRANSPORTER: uptake (basolateral to cell) in OCT2-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID681150TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
AID588972Substrates of transporters of clinical importance in the absorption and disposition of drugs, MATE12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID678997TP_TRANSPORTER: inhibition of MPP+ uptake in Xenopus laevis oocytes2000The Journal of pharmacology and experimental therapeutics, Mar, Volume: 292, Issue:3
Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).
AID680325TP_TRANSPORTER: uptake in OCT3-expressing HeLa cells1998The Journal of biological chemistry, Jun-26, Volume: 273, Issue:26
Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta.
AID681574TP_TRANSPORTER: inhibition of TEA uptake (basolateral to cell) in OCT1-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID1210853AUC (0 to t) in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID681589TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001American journal of physiology. Renal physiology, Sep, Volume: 281, Issue:3
Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1.
AID1210861Inulin renal clearance in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID681750TP_TRANSPORTER: inhibition of PAH uptake (PAH: 50 uM, TEA; 5000 uM) in Xenopus laevis oocytes1997The Journal of biological chemistry, Nov-28, Volume: 272, Issue:48
Expression cloning and characterization of ROAT1. The basolateral organic anion transporter in rat kidney.
AID678794TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes2002Biochemical and biophysical research communications, Aug-23, Volume: 296, Issue:3
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.
AID678807TP_TRANSPORTER: uptake in OCT2-expressing HEK293 cells1999Molecular pharmacology, Jul, Volume: 56, Issue:1
Selective substrates for non-neuronal monoamine transporters.
AID1210830Creatinine renal clearance in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID679144TP_TRANSPORTER: uptake in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID681625TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The American journal of physiology, 12, Volume: 277, Issue:6
rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger.
AID1210829Drug excretion in Oct1/Oct2-knockout FVB mouse urine at 10 mg/kg, iv after 2 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID494749Inhibition of [3H]choline uptake at choline transporter 1 in mouse brain synaptosome2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
3-D-QSAR and docking studies on the neuronal choline transporter.
AID1210860Creatinine renal clearance in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID1209586Drug uptake in Sprague-Dawley rat brain slices in presence of 1 uM of decynium-222011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1210859Drug excretion in wild type FVB mouse urine at 10 mg/kg, iv after 2 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID1210862Drug recovery in wild type FVB mouse urine assessed as corrected compound recovery by measuring nominal to observerd glomerular filtration rate ratio at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID679190TP_TRANSPORTER: uptake in OCT1A expressing Xenopus laevis oocytes1997The Journal of biological chemistry, Jun-27, Volume: 272, Issue:26
Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A).
AID680344TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
AID1210831Inulin renal clearance in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID681146TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID680529TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.01 uM, TEA: 500 uM) in OCTN2-expressing HEK293 cells2001Molecular pharmacology, Feb, Volume: 59, Issue:2
Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2.
AID682044TP_TRANSPORTER: inhibition of MPP+ uptake in Xenopus laevis oocytes2000The Journal of pharmacology and experimental therapeutics, Mar, Volume: 292, Issue:3
Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).
AID681169TP_TRANSPORTER: uptake in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID588969Substrates of transporters of clinical importance in the absorption and disposition of drugs, OCT12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1210854AUC (0 to infinity) in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID682220TP_TRANSPORTER: uptake (electrogenesis, -50mV) in Xenopus laevis oocytes1998The Journal of biological chemistry, Jun-26, Volume: 273, Issue:26
Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta.
AID682002TP_TRANSPORTER: inhibition of Choline uptake (Choline: 10 uM, TEA: 1000 uM) in Xenopus laevis oocytes2001The Journal of biological chemistry, Nov-09, Volume: 276, Issue:45
Ventricular choline transport: a role for organic cation transporter 2 expressed in choroid plexus.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID678993TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999Molecular pharmacology, Dec, Volume: 56, Issue:6
Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate.
AID680362TP_TRANSPORTER: uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID679497TP_TRANSPORTER: uptake in Xenopus laevis oocytes1997DNA and cell biology, Jul, Volume: 16, Issue:7
Cloning and characterization of two human polyspecific organic cation transporters.
AID679159TP_TRANSPORTER: uptake (electrogenesis) in Xenopus laevis oocytes1997DNA and cell biology, Jul, Volume: 16, Issue:7
Cloning and characterization of two human polyspecific organic cation transporters.
AID681709TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.025 uM, TEA: 2000 uM) in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID1210855Initial plasma concentration in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID679169TP_TRANSPORTER: uptake in Xenopus laevis oocytes2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID588973Substrates of transporters of clinical importance in the absorption and disposition of drugs, MATE2-K2010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID680480TP_TRANSPORTER: inhibition of Levofloxacin transepithelial transport (basal to apical) (Levofloxacin: 100 uM, TEA: 2500 uM) in MDR1-expressing LLC-PK1 cells1997The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2
Transport of quinolone antibacterial drugs by human P-glycoprotein expressed in a kidney epithelial cell line, LLC-PK1.
AID681362TP_TRANSPORTER: uptake in Xenopus laevis oocytes1997The Journal of biological chemistry, Jul-25, Volume: 272, Issue:30
Expression cloning and characterization of a novel multispecific organic anion transporter.
AID679160TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes2002Pharmaceutical research, Aug, Volume: 19, Issue:8
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).
AID679502TP_TRANSPORTER: uptake in Octn1-HEK cells2000The Journal of biological chemistry, Dec-22, Volume: 275, Issue:51
Molecular and functional characterization of organic cation/carnitine transporter family in mice.
AID682130TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, TEA: 5 uM) in Xenopus laevis oocytes2001Molecular pharmacology, May, Volume: 59, Issue:5
Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney.
AID680329TP_TRANSPORTER: uptake in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID679329TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
AID679397TP_TRANSPORTER: inhibition of PAH uptake (PAH: 50 uM, TEA: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, Sep, Volume: 56, Issue:3
The antiviral nucleotide analogs cidofovir and adefovir are novel substrates for human and rat renal organic anion transporter 1.
AID682015TP_TRANSPORTER: decrease in excretion via small intestine in Oct1 -/- mouse2001Molecular and cellular biology, Aug, Volume: 21, Issue:16
Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene.
AID678957TP_TRANSPORTER: uptake in Xenopus laevis oocytes1997DNA and cell biology, Jul, Volume: 16, Issue:7
Cloning and characterization of two human polyspecific organic cation transporters.
AID1525573Inhibition of human TASK3 expressed in Xenopus oocytes at 1 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.
AID1217063Inhibition of OCT1-mediated [14C]tetraethylammonium uptake in human OCT1 expressing HEK293/PDZK1 cells by scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent.
AID1210856Clearance in wild type FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID680370TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999Hepatology (Baltimore, Md.), May, Volume: 29, Issue:5
Cloning and functional expression of a mouse liver organic cation transporter.
AID681601TP_TRANSPORTER: uptake in OCT1-expressing HEK293 cells1998British journal of pharmacology, Sep, Volume: 125, Issue:1
Catecholamine transport by the organic cation transporter type 1 (OCT1).
AID681626TP_TRANSPORTER: uptake in OCT2-expressing MDCK cells1999The American journal of physiology, 12, Volume: 277, Issue:6
rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger.
AID681440TP_TRANSPORTER: uptake in Octn1-HRPE cells2000Biochimica et biophysica acta, Jun-01, Volume: 1466, Issue:1-2
Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.
AID679501TP_TRANSPORTER: decrease in liver concentration in Oct1 -/- mouse2001Molecular and cellular biology, Aug, Volume: 21, Issue:16
Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene.
AID679189TP_TRANSPORTER: uptake in Xenopus laevis oocytes1994Nature, Dec-08, Volume: 372, Issue:6506
Drug excretion mediated by a new prototype of polyspecific transporter.
AID1441978Inhibition of Kv1.1 (unknown origin)2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves That Improves Their Impaired Axonal Conduction.
AID241212Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry.
AID681422TP_TRANSPORTER: inhibition of E1S uptake (E1S: 40 uM, TEA: 1000 uM) in Xenopus laevis oocytes1999The Journal of biological chemistry, May-07, Volume: 274, Issue:19
Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain.
AID1210824AUC (0 to infinity) in Oct1/Oct2-knockout FVB mouse at 10 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.
AID680501TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical)(Doxorubicin: 3 uM, TEA: 100 uM) in MDR1-expressing LLC-PK1 cells2000European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Sep, Volume: 11, Issue:3
Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines.
AID679199TP_TRANSPORTER: inhibition of dTub uptake in Xenopus laevis oocytes2000Biochemical pharmacology, Jul-15, Volume: 60, Issue:2
Role of organic cation transporters in the renal secretion of nucleosides.
AID679156TP_TRANSPORTER: inhibition of MPP+ uptake in Xenopus laevis oocytes2000The Journal of pharmacology and experimental therapeutics, Mar, Volume: 292, Issue:3
Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).
AID679498TP_TRANSPORTER: inhibition of MPP+ uptake in Xenopus laevis oocytes1997Molecular pharmacology, Jun, Volume: 51, Issue:6
Cloning and functional expression of a human liver organic cation transporter.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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 (3,769)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990994 (26.37)18.7374
1990's1370 (36.35)18.2507
2000's1026 (27.22)29.6817
2010's348 (9.23)24.3611
2020's31 (0.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 40.75

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

MetricThis Compound (vs All)
Research Demand Index40.75 (24.57)
Research Supply Index8.27 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index67.14 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (40.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (0.26%)5.53%
Reviews29 (0.75%)6.00%
Case Studies2 (0.05%)4.05%
Observational1 (0.03%)0.25%
Other3,835 (98.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Physiology and Pathologic Role of Endothelium-Derived Hyperpolarizing Factor in Humans [NCT00166166]Phase 2174 participants (Actual)Interventional2002-07-31Terminated(stopped due to Limited clinical staff)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00166166 (11) [back to overview]Change in Tissue Plasminogen Activator (t-PA) Release
NCT00166166 (11) [back to overview]Change in Tissue Plasminogen Activator (t-PA) Release After Fluconazole and Bradykinin Administration
NCT00166166 (11) [back to overview]Change in Tissue Plasminogen Activator (t-PA) Release After Fluconazole, Tetraethylammonium (TEA), and Bradykinin Administration
NCT00166166 (11) [back to overview]Change in Tissue Plasminogen Activator (t-PA) Release After Tetraethylammonium (TEA) and Bradykinin Administration
NCT00166166 (11) [back to overview]Forearm Blood Flow (FBF) After Sodium Nitroprusside Administration
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After Administration of L-NG-monomethyl Arginine (L-NMMA)
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After Administration of L-NG-monomethyl Arginine (L-NMMA) and Tetraethylammonium (TEA)
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After Fluconazole Administration
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After Fluconazole and Tetraethylammonium (TEA) Administration
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After L-NG-monomethyl Arginine (L-NMMA) and Fluconazole Administration
NCT00166166 (11) [back to overview]Percent Change in Forearm Blood Flow (FBF) After Tetraethylammonium (TEA) Administration

Change in Tissue Plasminogen Activator (t-PA) Release

Individual net t-PA release at each time point were calculated by the following formula: net release = (Cv-CA) x {FBF x [101-hematocrit/100]}, where Cv and CA represent the concentration of t-PA in the brachial vein and artery, respectively. Change is the difference of t-PA at baseline and t-PA after bradykinin 400 ng/min (NCT00166166)
Timeframe: Baseline, 30 minutes

Interventionng/mL (Mean)
Healthy Controls5.6

[back to top]

Change in Tissue Plasminogen Activator (t-PA) Release After Fluconazole and Bradykinin Administration

Individual net t-PA release at each time point were calculated by the following formula: net release = (Cv-CA) x {FBF x [101-hematocrit/100]}, where Cv and CA represent the concentration of t-PA in the brachial vein and artery, respectively. Change is the difference of t-PA after fluconazole and t-PA after bradykinin 400 ng/min (NCT00166166)
Timeframe: 30 minutes, 60 minutes

Interventionng/mL (Mean)
Healthy Controls4.4

[back to top]

Change in Tissue Plasminogen Activator (t-PA) Release After Fluconazole, Tetraethylammonium (TEA), and Bradykinin Administration

Individual net t-PA release at each time point were calculated by the following formula: net release = (Cv-CA) x {FBF x [101-hematocrit/100]}, where Cv and CA represent the concentration of t-PA in the brachial vein and artery, respectively. Change is the difference of t-PA after fluconazole and tetraethylammonium (TEA) and t-PA after bradykinin 400 ng/min (NCT00166166)
Timeframe: 60 minutes, 90 minutes

Interventionng/mL (Mean)
Healthy Controls1.6

[back to top]

Change in Tissue Plasminogen Activator (t-PA) Release After Tetraethylammonium (TEA) and Bradykinin Administration

Individual net t-PA release at each time point were calculated by the following formula: net release = (Cv-CA) x {FBF x [101-hematocrit/100]}, where Cv and CA represent the concentration of t-PA in the brachial vein and artery, respectively. Change is the difference of t-PA after Tetraethylammonium (TEA) and t-PA after bradykinin 400 ng/min (NCT00166166)
Timeframe: 30 minutes, 60 minutes

Interventionng/mL (Mean)
Healthy Controls0.03

[back to top]

Forearm Blood Flow (FBF) After Sodium Nitroprusside Administration

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph after administration of sodium nitroprusside. Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. (NCT00166166)
Timeframe: 5 minutes

InterventionmL min^-1 * 100 mL^-1 (Mean)
Healthy Controls10.4
Risk Factors10.9

[back to top]

Percent Change in Forearm Blood Flow (FBF) After Administration of L-NG-monomethyl Arginine (L-NMMA)

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph after administration of L-NG-monomethyl Arginine (L-NMMA). Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference in FBF from baseline and after L-NMMA administration. (NCT00166166)
Timeframe: Baseline, 5 minutes

Interventionpercent change (Mean)
Healthy Controls-29
Risk Factors-23

[back to top]

Percent Change in Forearm Blood Flow (FBF) After Administration of L-NG-monomethyl Arginine (L-NMMA) and Tetraethylammonium (TEA)

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph after administration of L-NG-monomethyl Arginine (L-NMMA) and Tetraethylammonium (TEA). Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference in FBF from after L-NMMA administration and after TEA administration. (NCT00166166)
Timeframe: 5 minutes, 10 minutes

Interventionpercent change (Mean)
Healthy Controls-38
Risk Factors-39

[back to top]

Percent Change in Forearm Blood Flow (FBF) After Fluconazole Administration

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph at rest and after administration of fluconazole. Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference from baseline FBF and after fluconazole administration. (NCT00166166)
Timeframe: Baseline, 5 minutes

Interventionpercent change (Mean)
Healthy Controls-13
Risk Factors-17

[back to top]

Percent Change in Forearm Blood Flow (FBF) After Fluconazole and Tetraethylammonium (TEA) Administration

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph after administration of fluconazole and Tetraethylammonium (TEA) administration. Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference from FBF after fluconazole administration and after Tetraethylammonium (TEA) administration. (NCT00166166)
Timeframe: 5 minutes, 10 minutes

Interventionpercent change (Mean)
Healthy Controls-22

[back to top]

Percent Change in Forearm Blood Flow (FBF) After L-NG-monomethyl Arginine (L-NMMA) and Fluconazole Administration

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph after L-NMMA administration and administration of fluconazole. Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference in FBF after L-NMMA administration and then fluconazole administration. (NCT00166166)
Timeframe: 5 minutes, 10 minutes

Interventionpercent change (Mean)
Healthy Controls-26
Risk Factors-26

[back to top]

Percent Change in Forearm Blood Flow (FBF) After Tetraethylammonium (TEA) Administration

Simultaneous forearm blood flow (FBF) measurements were obtained in both arms using a dual-channel venous occlusion strain gauge plethysmograph at rest and after administration of tetraethylammonium (TEA). Flow measurements were recorded for approximately 7 seconds, every 15 seconds up to eight times and a mean FBF value was computed. Percent change is the difference from baseline FBF and after TEA administration. (NCT00166166)
Timeframe: Baseline, 5 minutes

Interventionpercent change (Mean)
Healthy Controls-18
Risk Factors-24

[back to top]