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tubocurarine

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Description

Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare. [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]

isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID6000
CHEMBL ID339427
CHEBI ID9774
SCHEMBL ID121375
MeSH IDM0022137

Synonyms (67)

Synonym
gtpl2294
KBIO1_001515
DIVK1C_006571
SDCCGMLS-0066631.P001
CHEBI:9774 ,
(+)-tubocurarine
d-tubocurarine
tubocurarin
SPECTRUM4_001922
SPECTRUM_001966
NCGC00178480-01
PDSP1_001485
SPECTRUM5_000685
PDSP2_001469
isoquinoline alkaloid
jexin
(+) tubocurarine
dimethoxy(trimethyl)[?]diol
7',12'-dihydroxy-6,6'-dimethoxy-2,2',2'-trimethyltubocuraranium
C07547
57-95-4
tubocurarine
DB01199
13h-4,6:21,24-dietheno-8,12-metheno-1h-pyrido(3',2':14,15)(1,11)dioxacycloeicosino(2,3,4-ij)isoquinolinium, 2,3,13a,14,15,16,25,25a-octahydro-9,19-dihydroxy-18,29-dimethoxy-1,14,14-trimethyl-, (13ar-(13ar*,25as*))-
tubocurarine, (+)-
tubocuraranium, 7',12'-dihydroxy-6,6'-dimethoxy-2,2',2'-trimethyl-
tubocurarinum
hsdb 2152
13h-4,6:21,24-dietheno-8,12-metheno-1h-pyrido(3',2':14,15)(1,11)dioxacycloeicosino(2,3,4-ij)isoquinolinium, 2,3,13a,14,15,16,25,25a-octahydro-9,19-dihydroxy-18,29-dimethoxy-1,14,14-trimethyl-, (13ar,25as)-
KBIOSS_002526
KBIOGR_002264
KBIO2_005086
KBIO3_001990
KBIO2_007654
KBIO2_002518
SPECPLUS_000475
SPECTRUM3_001095
SPBIO_001489
SPECTRUM2_001335
BSPBIO_002770
HMS2089C06
TC9 ,
NCGC00163242-02
CHEMBL339427
tubocurarine cation
tubocurarine ion
bdbm50366799
smr002533646
MLS003882581
w9yxs298bm ,
unii-w9yxs298bm
EPITOPE ID:174836
tubocurarine [hsdb]
tubocurarine [vandf]
tubocurarine [who-dd]
SCHEMBL121375
AB00053831-03
DTXSID0048393
AB00053831_04
(1s,16r)-9,21-dihydroxy-10,25-dimethoxy-15,15,30-trimethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.2^{3,6}.1^{8,12}.1^{18,22}.0^{27,31}.0^{16,34}]hexatriaconta-3,5,8,10,12(34),18(33),19,21,24(32),25,27(31),35-dodecaen-15-ium
SR-05000001878-4
SBI-0052455.P002
Q421268
BRD-K99621550-003-03-4
13h-4,6:21,24-dietheno-8,12-metheno-1h-pyrido[3',2':14,15][1,11]dioxacycloeicosino[2,3,4-ij]isoquinolinium,2,3,13a,14,15,16,25,25a-octahydro-9,19-dihydroxy-18,29-dimethoxy-1,14,14-trimethyl-,(13ar,25a
(1s,16r)-10,25-dimethoxy-15,15,30-trimethyl-7,23-dioxa-30-aza-15-azoniaheptacyclo[22.6.2.23,6.18,12.118,22.027,31.016,34]hexatriaconta-3(36),4,6(35),8(34),9,11,18(33),19,21,24,26,31-dodecaene-9,21-diol
tubocurarine, ()-

Research Excerpts

Overview

d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) That binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM) D-Tubsurarine is a competitive inhibitor of the bindings of alpha-bungarotoxin to the acetyl choline receptor.

ExcerptReferenceRelevance
"d-Tubocurarine is a potent competitive antagonist of both the muscle-type nicotinic acetylcholine receptor (AChR) and the serotonin type-3 receptor (5HT(3)R). "( Interaction of d-tubocurarine analogs with mutant 5-HT(3) receptors.
White, MM; Yan, D, 2002
)
1.38
"d-Tubocurarine (curare) is a well-characterized competitive antagonist of nicotinic acetylcholine receptors (AChRs), and it is usually assumed that curare and agonists share a common binding site. "( Characterization of d-tubocurarine binding site of Torpedo acetylcholine receptor.
Filatov, GN; O'Leary, ME; White, MM, 1994
)
1.32
"d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM). "( Identification of amino acids contributing to high and low affinity d-tubocurarine sites in the Torpedo nicotinic acetylcholine receptor.
Chiara, DC; Cohen, JB, 1997
)
1.25
"D-Tubocurarine is a potent competitive antagonist of two members of the ligand-gated ion channel family, the muscle-type nicotinic acetylcholine receptor (AChR) and serotonin type-3 receptor (5HT3R). "( Interaction of D-tubocurarine analogs with the 5HT3 receptor.
Pedersen, SE; White, MM; Yan, D, 1998
)
1.36
"d-Tubocurarine is a competitive inhibitor of the bindings of alpha-bungarotoxin to the acetylcholine receptor."( Cholinergic sites in skeletal muscle. II. Interaction of an agonist and two antagonists with the acetylcholine site.
Almon, RR; Appel, SH, 1976
)
0.81
"d-Tubocurarine (d-TC) is a drug commonly used to produce muscle paralysis. "( d-Tubocurarine causes neuronal death when injected directly into rat brain.
Dasheiff, RM, 1985
)
1.71
"(+)-Tubocurarine was found to be a potent GABA antagonist."( A comparative study of some convulsant substances as gamma-aminobutyric acid antagonists in the feline cerebral cortex.
Hill, RG; Simmonds, MA; Straughan, DW, 1973
)
0.73

Effects

d-tubocurarine and procaine have been shown to inhibit the acetylcholinesterase of rat brain homogenate by coupled and non-competitive mechanism respectively. Tubocurarin has a structure similar to that of vecuronium, was used as the internal standard.

ExcerptReferenceRelevance
"Tubocurarine, which has a structure similar to that of vecuronium, was used as the internal standard."( Determination of vecuronium in blood by HPLC with UV and electrochemical detection: a pilot study in man.
Chou, CH; Ho, ST; Ho, W; Hu, OY, 1991
)
1
"d-Tubocurarine has been reported to inhibit the action of dopamine on mollusc neurons. "( d-Tubocurarine as a dopaminergic antagonist in the rabbit ear artery.
Nelson, SH; Steinsland, OS, 1983
)
1.71
"d-tubocurarine and procaine have been shown to inhibit the acetylcholinesterase of rat brain homogenate by coupled and non-competitive mechanism respectively, which suggests binding to enzyme peripheral sites. "( [Age changes in the allosteric properties of brain acetylcholinesterase].
Aksentsev, SL; Arinchin, NI; Konev, SV; Miliutin, AA; Okun', IM, 1976
)
0.98
"Tubocurarine, which has a structure similar to that of vecuronium, was used as the internal standard."( Determination of vecuronium in blood by HPLC with UV and electrochemical detection: a pilot study in man.
Chou, CH; Ho, ST; Ho, W; Hu, OY, 1991
)
1
"d-Tubocurarine has been shown to bind to two different sites in receptor-rich membranes."( Arrangement of the subunits of the nicotinic acetylcholine receptor of Torpedo californica as determined by alpha-neurotoxin cross-linking.
Eaton, DC; Hamilton, SL; Pratt, DR, 1985
)
0.83

Actions

d-Tubocurarine was found to produce a close correlation between the degrees of twitch strength depression and T4 for both muscles. At a higher concentration (20 microM) the drug little affected them.

ExcerptReferenceRelevance
"d-Tubocurarine was found to produce a close correlation between the degrees of twitch strength depression and T4 for both muscles."( Characterization of the train-of-four response in fast and slow muscles: effect of d-tubocurarine, pancuronium, and vecuronium.
Blake, GJ; Day, NS; Dretchen, KL; Standaert, FG, 1983
)
1.05
"d-Tubocurarine induced an increase in heart rate (+6%), a decrease in arterial pressure (-24%) and cardiac index (-17%)."( [Hemodynamic effects of vecuronium in man].
Cousin, MT; Guggiari, M; Lienhart, A; Maneglia, R; Tauvent, A; Viars, P, 1983
)
0.82
"D-tubocurarine blocked the increase in acetylcholinesterase and the decrease in spontaneous contractions caused by acetyl-beta-methylcholine."( Regulation of acetylcholinesterase in cultured muscle by chemical agents and electrical stimulation.
Walker, CR; Wilson, BW, 1976
)
0.81
"4. d-Tubocurarine (dTC) at lower concentrations (0.5-2 microM) suppressed EJPs, but at a higher concentration (20 microM) the drug little affected them."( Involvement of cholinergic nerves in excitatory junction potentials through prejunctional nicotinic receptors in the guinea-pig vas deferens.
Fukushi, Y; Wakui, M, 1987
)
0.73

Treatment

d-Tubocurarine pretreatment abolished suxamethonium-induced fasciculations completely. Alcuronium pretreatment gave protection in 93% and pancuronium pret treatment in 43% of patients.

ExcerptReferenceRelevance
"d-Tubocurarine pretreatment abolished suxamethonium-induced fasciculations completely, whereas alcuronium pretreatment gave protection in 93% and pancuronium pretreatment in 43% of patients."( Effects of precurarization on the blood pressure and heart rate changes induced by suxamethonium facilitated laryngoscopy and intubation.
Kautto, UM, 1981
)
0.82
"of d-tubocurarine (dTc) as pretreatment, followed 3 minutes later by 2 mg./kg."( Adverse effects of increased succinylcholine dose following d-tubocurarine pretreatment.
Peterson, C; Stoelting, RK,
)
0.83
"Tubocurarine pretreatment (3 mg) resulted in a significant decrease in fasciculations, but myalgia, which occurred in five patients, remained the same."( Phenytoin reduces suxamethonium-induced myalgia.
Hatta, V; Kaul, HL; Saxena, A, 1992
)
1
"Pre-treatment with tubocurarine afforded the best control of suxamethonium-induced sequelae."( A matched comparison of four suxamethonium administration techniques in patients with strabismus.
Brander, P; Cozanitis, DA; Karhunen, U; Merrett, JD, 1982
)
0.58

Toxicity

ExcerptReferenceRelevance
"Neuromuscular, circulatory, and adverse effects of intravenous succinylcholine (SCh), mg/kg, were compared in 3 groups of 40 patients each."( Diazepam prevents some adverse effects of succinylcholine.
Fahmy, NR; Lappas, DG; Malek, NS, 1979
)
0.26
" Increasing SCh dosage with pretreatment apparently did not accentuate adverse effects, and in some instances was associated with fewer such effects, than after lower-dose SCh injections without pretreatment."( Adverse effects of increased succinylcholine dose following d-tubocurarine pretreatment.
Peterson, C; Stoelting, RK,
)
0.37
"Intravenous succinylcholine (SCh) is widely used as a muscle relaxant but it is often associated with adverse effects, including muscle fasciculations, postoperative myalgia, elevated serum potassium (K+) and creatine phosphokinase (CPK), etc."( [The study of pretreatment with diphenylhydantoin or D-tubocurarine on succinylcholine-induced adverse effects].
Ho, ST; Hu, OY; Hwing, CS; Kuo, WS; Li, CH, 1990
)
0.53
" Acrylates appear to be the toxic agent."( Potentiation of atracurium toxicity in isolated rat hepatocytes by inhibition of its hydrolytic degradation pathway.
Klaunig, JE; Nigrovic, V; Schultz, NE; Smith, SL, 1987
)
0.27
" The customary assumption was made that the exudation of LDH reflects the toxic effects of the relaxants."( Comparative toxicity of atracurium and metocurine in isolated rat hepatocytes.
Klaunig, JE; Nigrovic, V; Schultz, NE; Smith, SL; Wajskol, A, 1986
)
0.27

Pharmacokinetics

This review is an attempt to bring together the pharmacokinetic data on d-tubocurarine and pancuronium with clinical observations on relaxant dosage and effect.

ExcerptReferenceRelevance
"Data about plasma concentration, renal and biliary elimination of tubocurarine, gallamine, alcuronium and pancuronium are taken from the literature for synoptical pharmacokinetic analysis."( Comparative clinical pharmacokinetics of tubocurarine, gallamine, alcuronium and pancuronium.
Agoston, S; Buzello, W, 1978
)
0.76
" The serum half-life was prolonged 76% and the serum clearance rate decreased 60% by hypothermia (28 C)."( Pharmacokinetics and pharmacodynamics of d-tubocurarine during hypothermia in the cat.
Benet, LZ; Ham, J; Matteo, RS; Miller, RD; Roderick, LL, 1978
)
0.52
"We propose a model of drug pharmacodynamic response that when integrated with a pharmacokinetic model allows characterization of the temporal aspects of pharmacodynamics as well as the time-independent sensitivity component."( Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine.
Ham, J; Miller, RD; Sheiner, LB; Stanski, DR; Vozeh, S, 1979
)
0.49
" Spontaneous degradation of atracurium in plasma is the major route of elimination in man and contributes to a short elimination half-life (approximatively 20 min)."( [Metabolism and pharmacokinetics of atracurium].
Colin, JN; Singlas, E, 1985
)
0.27
" There was a significant difference in the pharmacokinetic parameters of all elderly patients compared with younger controls."( Pharmacokinetics and pharmacodynamics of d-tubocurarine and metocurine in the elderly.
Abraham, R; Backus, WW; Brotherton, WP; Diaz, J; Matteo, RS; McDaniel, DD, 1985
)
0.53
"The pharmacodynamic behaviour upon continuous infusion and bolus administration of pancuronium and vecuronium was studied in cats with and without ligated renal pedicles."( Pharmacodynamics of vecuronium and pancuronium in cats with and without ligated renal pedicles.
Booij, LH; Crul, JF; Van de Pol, F; Vree, TB, 1982
)
0.26
" With the use of sophisticated pharmacokinetic and pharmacodynamic models good relationships have been demonstrated between plasma concentrations of the relaxants throughout the entire range of relaxant response."( Clinical pharmacokinetics of the non-depolarising muscle relaxants.
Ramzan, MI; Shanks, CA; Somogyi, AA; Triggs, EJ; Walker, JS,
)
0.13
"01) and the elimination half-life was significantly prolonged (11."( Pharmacokinetics and pharmacodynamics of metocurine in humans with and without renal failure.
Brotherton, WP; Matteo, RS, 1981
)
0.26
" The elimination half-life (t beta 1/2) was 174 +/- 60 min in neonates, significantly longer than the values of 90 +/- 23 and 89 +/- 18 min in children and adults, respectively."( Pharmacokinetics and pharmacodynamics of d-tubocurarine in infants, children, and adults.
Cronnelly, R; Fisher, DM; Gregory, GA; Miller, RD; O'Keeffe, C; Stanski, DR, 1982
)
0.53
" To characterize the pharmacokinetic component of the increased requirement, the disposition of dTc was studied in eight patients with burns ranging from 15% to 80% of body surface area and compared with that in six nonburned surgical patients of comparable age and weight."( Pharmacokinetics of d-tubocurarine in patients with thermal injury.
Greenblatt, DJ; Lebowitz, PW; Martyn, JA; Matteo, RS; Savarese, JJ, 1982
)
0.58
" Except for a longer distribution half-life, the pharmacokinetic variables for edrophonium did not differ significantly from those for neostigmine."( Pharmacokinetics of edrophonium and neostigmine when antagonizing d-tubocurarine neuromuscular blockade in man.
Cronnelly, R; Fahey, MR; Miller, RD; Morris, RB; Stanski, DR, 1981
)
0.5
"This review is an attempt to bring together the pharmacokinetic data on d-tubocurarine and pancuronium with clinical observations on relaxant dosage and effect."( Tubocurarine and pancuronium: a pharmacokinetic view.
Ramzan, MI; Shanks, CA; Somogyi, AA; Triggs, EJ, 1980
)
1.93
" The pharmacokinetic parameters derived from this study did not differ significantly from those reported for a single dose except that the plasma clearance was less."( Pharmacokinetics of tubocurarine administered by combined i.v. bolus and infusion.
Ramzan, MI; Shanks, CA; Triggs, EJ, 1980
)
0.58
"Within the context of this study of immobilization disuse atrophy, pharmacokinetic and pharmacodynamic characterization of antagonist responses can be used to infer muscle disuse-related changes in acetylcholine receptors."( The changing pharmacodynamics of metocurine identify the onset and offset of canine gastrocnemius disuse atrophy.
Disbrow, E; Fung, DL; Gronert, GA; White, DA, 1995
)
0.29

Compound-Compound Interactions

ExcerptReferenceRelevance
" Also, neuromuscular effects of enflurane in combination with dTc or pancuronium are not significantly different from those seen suring equi-MAC isoflurane anesthesia."( Neuromuscular effects of enflurane, alone and combined with d-Tubocurarine, pancuronium, and succinylcholine, in man.
Fogdall, RP; Miller, RD, 1975
)
0.49
"The effect of trimetaphan alone and in combination with pancuronium, tubocurarine or metocurine (dimethyl tubocurarine) has been examined on the rat phrenic nerve diaphragm preparation."( The neuromuscular blocking effect of trimetaphan alone and in combination with different non-depolarizing muscle relaxants in the rat.
Pollard, BJ; van der Spek, AF, 1987
)
0.51

Dosage Studied

Cumulative dose-response curves were constructed for pancuronium, metocurine, d-tubocurarine and gallamine in 56 children anaesthetized with thiopentone, N2O/O2 and narcotic.

ExcerptRelevanceReference
"This experiment was carried out upon the male-adulte-AF SPF-Wister Rat, anesthetized by the use of pentobarbital-Na at the only dosage of 40 mg/kg/IP and put under artificial ventilation."( [Variations in the activity of various curarizing substances as a function of the time of administration].
Agopian, B; Bouyard, P; Bruguerolle, B; Jadot, G; Mesdjian, E; Valli, M, 1975
)
0.25
" The dose-response curve to suxamethonium in tetrodotoxin 2 X 10(-7)M could be shifted to the right with tubocurarine 10(-6)M."( A mammalian muscle with the pharmacological characteristics of slow tonic muscle.
Dale, MM; Muid, R, 1978
)
0.47
"3 4-Aminopyridine causes a prallel shift to the right of the dose-response curve to Mg(2+) for blockade of nerve impulse-evoked transmitter release (in the absence of tetrodotoxin)."( 4-Aminopyridine and evoked transmitter release from motor nerve endings.
Illes, P; Thesleff, S, 1978
)
0.26
" Each of the three groups of children who were treated with one of the three curare-like agents were subdivided according to age and dose-response curves were obtained."( [Comparative study of the neuromuscular effects of 3 curare-like agents in children].
Goudsouzian, NG; Mathieu, A; Nishan, G, 1979
)
0.26
" Bell-shaped log dose-response curves were obtained for McN."( A comparative study of the effects induced by MCN-A-343 and acetylcholine on the isolated toad rectus abdominis.
Corrado, AP; Jurkiewicz, A; Simioni, LR, 1976
)
0.26
" Almost all parameters except behavior showed a distinct dose-response relationship."( Electrophysiological correlates of the behavioral effects of tubocurarine in conscious cats.
Ashorobi, RB; Guha, D; Pradhan, SN, 1979
)
0.5
"Intravenous dose-response relationships were used to correlate neuromuscular paralysis with effects on autonomic mechanisms in anaesthetized cats."( Effects on non-depolarizing neuromuscular blocking agents on peripheral autonomic mechanisms in cats.
Chapple, DJ; Hughes, R, 1976
)
0.26
"A cumulative dose-response curve for d-tubocurarine based on body weight was determined for 44 infants and children 1 day to 7 years of age during halothane, nitrous oxide and oxygen anesthesia."( Re-evaluation of dosage and duration of action of d-tubocurarine in the pediatric age group.
Donlon, JV; Goudsouzian, NG; Ryan, JF; Savarese, JJ, 1975
)
0.77
"Intravenous dose-response relationships for dimethyl tubocurarine showed that vagal blockade only became appreciable (50-83%) at doses 8-16 times those sufficient for full neuromuscular paralysis in anaesthetized cats (0."( Cardiovascular and neuromuscular effects of dimethyl tubocurarine in anaesthetized cats and rhesus monkeys.
Chapple, DJ; Hughes, R, 1976
)
0.75
" In contrast with the membrane fragments of Electrophorus, however, those of Torpedo give dose-response curves of in vitro excitation that shift towards higher concentration of the agonists by one to two orders of magnitude compared with the actual binding curves of agonists to the receptor sites."( The mode of action of the nicotinic cholinergic receptor protein in the postsynaptic membrane.
Sugiyama, H, 1978
)
0.26
" This provided data for derivation of the pharmacokinetic parameters, two plasma concentration-response curves and the dose-response curve."( Studies in man with a constant-rate infusion of tubocurarine.
Ramzan, MI; Shanks, CA; Triggs, EJ, 1979
)
0.52
" When there was no temperature change the maintenance dosage of d-TC remained constant for up to four hours denoting the equilibrium phase of the relaxant kinetics."( D-tubocurarine requirement during hypothermia.
Brown, TC; Lam, HS; Lampard, DG, 1979
)
0.98
" In 40 mM Cl- solutions, dose-response relations were determineed with ACh in the absence of presence of dTc."( Influence of chloride and sodium pump activity on carbachol- and acetylaholine-induced depolarizations in denervated rat diphragm.
Mooij, JJ, 1976
)
0.26
" 4 On the frog rectus abdominis the alkylating agent, decamethonium mustard, does not produce any 'parallel shift' of the dose-response curve for carbachol, the only result of alkylation being a decrease in maximal response, which is more pronounced in isometric than in isotonic conditions."( Isotonic and isometric responses of different tonic muscles to agonists and antagonists.
Michelson, MJ; Shelkovnikov, SA, 1976
)
0.26
" There were no fasciculations with this dosage and conditions for endotracheal intubation were excellent."( Inhibition of suxamethonium relaxation by tubocurarine and gallamine pretreatment during induction of anaesthesia in man.
Pauca, AL; Reynolds, RC; Strobel, GE, 1975
)
0.52
" Increasing SCh dosage with pretreatment apparently did not accentuate adverse effects, and in some instances was associated with fewer such effects, than after lower-dose SCh injections without pretreatment."( Adverse effects of increased succinylcholine dose following d-tubocurarine pretreatment.
Peterson, C; Stoelting, RK,
)
0.37
" A programmed level of muscle paralysis is therefore possible for use in physiological and pharmacological experiments, and in clinical practice where precise control of the degree of paralysis together with minimal dosage is advantageous."( Computer controlled muscle relaxation: a comparison of four muscle relaxants in the sheep.
Brown, WA; Cass, NM; Coles, JR; Lampard, DG, 1976
)
0.26
"Cumulative d-tubocurarine dose-response curves were determined in 35 unpremedicated adult surgical patients."( Duration of halothane anesthesia and neuromuscular blockade with d-tubocurarine.
Crique, M; Eger, EI; Miller, RD, 1976
)
0.86
" The 5-HT2 receptor antagonist ketanserin (1 microM) caused a clear rightward shift of the dose-response curve to 5-HT on the guinea-pig ganglion, but not on the mouse or rat ganglion."( Evidence that the 5-HT3 receptors of the rat, mouse and guinea-pig superior cervical ganglion may be different.
Cheshire, SH; Gilbert, MJ; Newberry, NR, 1991
)
0.28
"3-10 ng/ml) potentiated the d-Tc-induced histamine release and shifted the dose-response curve to left without changing the maximum histamine release by d-Tc."( Effects of human recombinant IL-1 on d-tubocurarine-induced histamine release from isolated rat peritoneal mast cells.
Abe, K; Oka, M; Otsuka, H, 1992
)
0.55
" In addition, the block/fade relationships for cumulative dosing and sequential dilution were the same when measurements were made at steady-state for several doses."( Relationships between block-of-twitch and train-of-four fade in the mouse phrenic nerve-diaphragm preparation.
Rosenberg, H; Slomowitz, SA; Storella, RJ, 1991
)
0.28
" The dose-response curve of R-(--)-baclofen for its inhibitory effect on the electrically-induced vasopressor response was shifted to the right by the GABAB-receptor antagonist 2-hydroxysaclofen, but was not affected by the GABAA-receptor antagonist bicuculline."( GABAB receptor-mediated inhibition of the neurogenic vasopressor response in the pithed rat.
Kohlenbach, A; Schlicker, E, 1990
)
0.28
"Seventy neonatal to adolescent general surgical patients were studied to create an individual dose-response curve for the long-acting neuromuscular blocking agents, alcuronium and d-tubocurarine."( Dose response of alcuronium and d-tubocurarine in infants, children and adolescents.
Brown, TC; Clare, D; Meretoja, OA, 1990
)
0.75
" The dose-response values obtained were fitted to a regression embedded in a split plot factorial experimental design such as both to control and to measure effects of variation among preparations, order of administration, time, and level of block."( Interaction among agents that block end-plate depolarization competitively.
Waud, BE; Waud, DR, 1985
)
0.27
" The relative cutaneous histamine-releasing ability of each drug was derived from calculated dose-response relationships."( Comparative cutaneous histamine release by neuromuscular blocking agents.
Galletly, DC, 1986
)
0.27
" Dose-response profiles (i) have characteristic shapes for different nicotinic agonists, (ii) are described by three operationally defined parameters, and (iii) reflect different affinities of agonists for binding sites that control receptor activation and functional inhibition."( An isotopic rubidium ion efflux assay for the functional characterization of nicotinic acetylcholine receptors on clonal cell lines.
Cullen, MJ; Lukas, RJ, 1988
)
0.27
" Sepsis at 2 weeks caused an approximate 8% body weight loss, a significant decrease in maximal tension and at least a 3- to 5-fold shift to the right in dose-response curves to d-tubocurarine."( Intraperitoneal endotoxin but not protein malnutrition shifts d-tubocurarine dose-response curves in mouse gastrocnemius muscle.
Martyn, J; Tomera, JF, 1989
)
0.71
" At the conclusion of this training period, a pharmacokinetic and pharmacodynamic study of the MTC dose-response relationship was performed."( Exercise produces sensitivity to metocurine.
Gronert, GA; Matteo, RS; Shafer, SL; White, DA, 1989
)
0.28
"To evaluate possible potentiation of neuromuscular blocking effect of a combination of vecuronium and d-tubocurarine, cumulative dose-response curves were constructed to compare the potency of this combination with vecuronium and d-tubocurarine given alone."( Vecuronium and d-tubocurarine combination: potentiation of effect.
Ferres, CJ; Gibson, FM; Mirakhur, RK, 1985
)
0.82
" Atropine sulphate administered locally into the skin antagonised the response to carbachol: the dose-response curve for carbachol was shifted to the right without any depression of the maximum of the curve."( Effects of locally and systemically administered cholinoceptor antagonists on the secretory response of human eccrine sweat glands to carbachol.
Bradshaw, CM; Longmore, J; Szabadi, E, 1985
)
0.27
" A biphasic dose-response curve was observed, the first part of which was saturable and had an EC50 value of approximately 10 microM."( ATP-induced cation influx in myotubes is additive to cholinergic agonist action.
Eriksson, H; Häggblad, J; Heilbronn, E, 1985
)
0.27
" After steady-state subtherapeutic (less than 10 mg/l), therapeutic (10-20 mg/l), and toxic (greater than 20 mg/l) concentrations of theophylline, dose-response curves for dTC were determined and compared with controls that received no theophylline."( Concentration-dependent interaction of theophylline with d-tubocurarine.
Basta, S; Fuke, N; Kim, CS; Martyn, J, 1987
)
0.52
" After AZA or saline administration, dose-response (DR) curves for inhibition of gastrocnemius twitch tension by dTC were constructed."( Azathioprine fails to alter the dose-response curve of d-tubocurarine in rats.
Glidden, RS; Martyn, JA; Tomera, JF, 1988
)
0.52
"To determine the potencies of neostigmine, pyridostigmine, and edrophonium in reversing pancuronium and d-tubocurarine blockade, dose-response curves were established for first twitch height recovery and train-of-four ratio."( Dose-response curves for edrophonium, neostigmine, and pyridostigmine after pancuronium and d-tubocurarine.
Antzaka, C; Bevan, DR; Donati, F; McCarroll, SM; McCready, D, 1987
)
0.71
" The dose-response curves for pancuronium were similar using the two methods, and resulted in an ED95 (dose required to produce 95% block of the twitch height) of 60 and 59 micrograms kg-1 using single-dose and cumulative-dose methods respectively."( Dose-response curves for pancuronium and tubocurarine: comparison of single and cumulative dose techniques.
Gibson, FM; Mirakhur, RK, 1987
)
0.54
"The disposition of d-tubocurarine (dTc) was assessed when a bolus and infusion dosage regimen was used to obtain relaxation during major orthopedic surgery on the spine."( The pharmacokinetics of d-tubocurarine with surgery involving salvaged autologous blood.
Avram, MJ; Bowsher, DJ; Ronai, AK; Shanks, CA, 1985
)
0.89
" The dose-response curve was usually linear even with concentrations of 10(-2) M acetylcholine, indicating that the conductance change was probably proportional to the concentration of acetylcholine or carbachol."( A linear dose-response curve at the motor endplate.
Harrington, L, 1973
)
0.25
" Log dose-response curves for acetylcholine and carbachol were constructed in the presence of triethylcholine, tubocurarine and physostigmine, in both innervated and denervated chick biventer cervicis muscles."( Actions of acetylcholine and carbachol on the chick biventer cervicis muscle.
Marshall, IG, 1971
)
0.46
" The dose-response curves for both inhibitors are unchanged by prostigmine."( The action of tubocurarine and atropine on the normal and denervated rat diaphragm.
Beránek, R; Vyskocil, F, 1967
)
0.61
"Neuromuscular blocking agents can be evaluated in anesthetized cats, dogs, or rhesus monkeys using dose-response relationships to assess the degree of separation between neuromuscular blocking activity and effects on cardiovascular and autonomic systems."( Experimental and clinical evaluation of neuromuscular blocking agents.
Hughes, R, 1984
)
0.27
" No evidence supporting the concept that dosage should be related to patient's weight was found."( Reduction of post-suxamethonium pain by pretreatment with four non-depolarizing agents.
Bennetts, FE; Khalil, KI, 1981
)
0.26
" These alpha 2-agonists also inhibited the uptake of 45Ca evoked by carbachol with similar dose-response curve to inhibition of catecholamine secretion."( Inhibition by alpha 2-adrenoceptor agonists of the secretion of catecholamines from isolated adrenal medullary cells.
Izumi, F; Kobayashi, H; Sakurai, S; Wada, A; Yanagihara, N, 1983
)
0.27
" The findings strongly suggest a non-cytotoxic secretory process requiring the presence of two quaternary ammonium groups as suggested by the rarity of release with tubocurarine; inhibition of succinyldicholine (suxamethonium)-induced histamine release by serum cholinesterase treatment, acetylcholine and tubocurarine; and the bell-shaped dose-response curve, particularly with suxamethonium."( Characteristics of basophil histamine release by neuromuscular blocking drugs in patients with anaphylactoid reactions.
Assem, ES, 1984
)
0.46
" For each drug at each temperature, a dose-response curve for twitch depression was constructed."( Pancuronium, unlike other nondepolarizing relaxants, retains potency at hypothermia.
Bartkowski, RR; Horrow, JC, 1983
)
0.27
"A cumulative dose-response study for metocurine was performed on 11 burned and 11 non-burned children during thiopentone, nitrous oxide in oxygen and narcotic anaesthesia."( Metocurine requirements and plasma concentrations in burned paediatric patients.
Goudsouzian, NG; Kaplan, RF; Liu, LM; Martyn, JA; Matteo, RS; Szyfelbein, SK, 1983
)
0.27
" The effect of d-TC and local anaesthetics on the dose-response relationship between ionophoretically applied L-glutamate and synaptic current suggested that both acted as non-competitive inhibitors."( Voltage-dependent drug blockade of L-glutamate activated channels of the crayfish.
Dekin, MS; Edwards, C, 1983
)
0.27
" The dose-response curves for the induction period were slightly steeper in patients with RF."( Dose-response of tubocurarine in patients with and without renal failure.
Alanen, T; Heino, A; Orko, R; Rosenberg, PH, 1984
)
0.61
" Cumulative dose-response curves to SCh were shifted to the right in a nearly parallel manner by (+)- and (-)-propranolol which were about equiactive."( Curare-like effect of propranolol on rat extraocular muscles.
Chiarandini, DJ, 1980
)
0.26
"The dose-response relationship, onset, duration of action, atropine requirement, and pharmacokinetic variables of edrophonium were determined in infants and children during N2O-halothane anesthesia."( Clinical pharmacology of edrophonium in infants and children.
Cronnelly, R; Fisher, DM; Miller, RD; Sharma, M, 1984
)
0.27
" Dose-response curves to dimethyl tubocurarine (MTC) were determined during anesthesia with pentobarbital sodium-N2O."( Canine gastrocnemius disuse atrophy: resistance to paralysis by dimethyl tubocurarine.
Gronert, GA; Matteo, RS; Perkins, S, 1984
)
0.78
" The inhibition showed a sigmoid log10 dose-response relationship."( Effects of eugenol on rat phrenic nerve and phrenic nerve-diaphragm preparations.
Brodin, P; Røed, A, 1984
)
0.27
"Cumulative dose-response curves of suxamethonium, tubocurarine, and pancuronium were constructed in 142 patients under enflurane and halothane anesthesia, and neuroleptic anesthesia (control group)."( Differential increase in potency of neuromuscular blocking agents by enflurane and halothane.
Schuh, FT, 1983
)
0.52
"Cumulative dose-response curves were constructed for pancuronium, metocurine, d-tubocurarine and gallamine in 56 children anaesthetized with thiopentone, N2O/O2 and narcotic."( The dose response effect of long-acting nondepolarizing neuromuscular blocking agents in children.
Ali, HH; Goudsouzian, NG; Liu, LM; Martyn, JJ, 1984
)
0.49
"After bolus intravenous dosing of d-tubocurarine (d-TC) to rats, the twitch heights of the tibialis anterior muscle indirectly stimulated were followed, and its decrease was defined as pharmacologic response of d-TC."( Kinetics of d-tubocurarine disposition and pharmacologic response in rats.
Kakemi, M; Katayama, K; Kitamura, K; Koizumi, T; Morino, A, 1983
)
0.9
" To explain sigmoidal dose-response curves, a two-site model is already sufficient."( Interaction of cholinergic ligands with the purified acetylcholine receptor protein. I. Equilibrium binding studies.
Maelicke, A; Prinz, H, 1983
)
0.27
" Dosage regimens have been designed using knowledge of the disposition kinetics of the relaxants to provide for continuous adequate relaxation during prolonged surgical procedures."( Clinical pharmacokinetics of the non-depolarising muscle relaxants.
Ramzan, MI; Shanks, CA; Somogyi, AA; Triggs, EJ; Walker, JS,
)
0.13
" Neuromuscular block produced by neomycin was cumulative despite rapid and apparent full recovery of twitch tension and an interval of 3 h between dose-response studies."( Cumulation of neomycin and its residual potentiation of tubocurarine in the cat.
Durant, NN; Katz, RL; Lee, C, 1981
)
0.51
"Cumulative dose-response curves were constructed in man for tubocurarine, pancuronium, gallamine and alcuronium from data obtained during barbiturate-narcotic-nitrous oxide anaesthesia."( Dose-response curves for four neuromuscular blockers using continuous i.v. infusion.
Ramzan, MI; Shanks, CA; Triggs, EJ; Walker, JS, 1981
)
0.5
" Cumulative dose-response curves for inhibition of evoked thumb adduction were constructed at each frequency on log probit scales and the ED50 and ED95 values were determined."( Stimulus frequency and dose-respone curve to d-tubocurarine in man.
Ali, HH; Savarese, JJ, 1980
)
0.52
" The dosage pattern consisted of a loading phase before any IEMG depression was detected, an onset phase during which a moderate amount of drug was required to achieve increasing paralysis, and a maintenance phase during which a substantially constant and relatively low infusion rate was required."( Dosage patterns of non-depolarizing neuromuscular blockers in the sheep.
Brown, WA; Cass, N; Lampard, DG; Ng, KC, 1980
)
0.26
"This review is an attempt to bring together the pharmacokinetic data on d-tubocurarine and pancuronium with clinical observations on relaxant dosage and effect."( Tubocurarine and pancuronium: a pharmacokinetic view.
Ramzan, MI; Shanks, CA; Somogyi, AA; Triggs, EJ, 1980
)
1.93
" 22Na+ efflux induced by carbamylcholine (Carb) and the partial agonist phenyltrimethylammonium (PTA) is assessed by determining dose-response relations using three approaches: (1) a filtration assay measuring responses on the 10-s time scale, (2) the same filtration assay after blocking different fractions of the receptor sites with alpha-bungarotoxin (alpha-BgTx), and (3) a rapid-mix quenched-flow technique which permits measurement of the initial rate of 22Na+ efflux on the millisecond time scale."( Permeability control by cholinergic receptors in Torpedo postsynaptic membranes: agonist dose-response relations measured at second and millisecond times.
Cohen, JB; Neubig, RR, 1980
)
0.26
" Over the physiological range of concentrations of potassium and calcium, 36% and 27% variation in dosage can be expected."( Interaction of calcium and potassium with neuromuscular blocking agents.
Waud, BE; Waud, DR, 1980
)
0.26
"The potencies of suxamethonium, pancuronium, and tubocurarine were increased, as shown by a parallel shift to the left of cumulative dose-response curves, following normovolaemic haemodilution before operation."( Influence off haemodilution on the potency of neuromuscular blocking drugs.
Schuh, FT, 1981
)
0.52
"These results indicate that crossover dosing of nondepolarizing muscle relaxants may have synergistic effects."( The effect of d-tubocurarine priming on an ED95 dose of vecuronium bromide.
Barlow, IK; Dombrowski, DL; Miguel, RV,
)
0.48
" This report assessed dose-response relations of the competitive antagonist dTC (AN) and their modification (AN') by advancing endotoxicosis."( E. coli endotoxin affinity at the nicotinic2 receptor: receptor theory revisited, ilumina nostros occulae.
Kukulka, SP; Lilford, K; Martyn, JA; Tomera, JF, 1994
)
0.29
" Previous studies combined mutagenesis, expression in Xenopus oocytes, and dose-response analysis to examine contributions of these tyrosines to agonist affinity."( Conserved tyrosines in the alpha subunit of the nicotinic acetylcholine receptor stabilize quaternary ammonium groups of agonists and curariform antagonists.
Kreienkamp, HJ; Papanikolaou, F; Quiram, P; Sine, SM; Taylor, P, 1994
)
0.29
" All the effects of Con A, that is, on the peak amplitude, desensitization, dose-response relationship of ACh induced current and binding of [3H]alpha-bungarotoxin, could be recovered by D-mannose, a competitive inhibitor of Con A binding to its receptor."( Interaction of concanavalin A and wheat germ agglutinin with Helix acetylcholine receptors.
Arvanov, VL; Ayrapetian, SN; Tsai, MC; Walker, RJ, 1993
)
0.29
" Dose-response curves yielded an EC50 of about 50 microM."( Patch-clamp analysis of glycine-induced currents in chick ciliary ganglion neurons.
Berg, DK; Zhang, ZW, 1995
)
0.29
" A rightward shift of the dose-response curve due to endotoxin was observed."( Interaction of lipopolysaccharide endotoxin produced from Escherichia coli with D-tubocurarine at the nicotinic2 receptor and adenosine 3':5' cyclic monophosphate during physiological contraction in skeletal muscle.
Tomera, JF, 1996
)
0.52
" The 50% and 90% inhibitory concentrations (IC50, IC90) of Vb, d-Tc and SCh were determined form dose-response curves."( [Neuromuscular effects of vecuronium d-tubocurarine and succinylcholine in malnourished rat's diaphragm].
Tajiri, O, 1996
)
0.56
" 177, 13), was used to calculate the dissociation constant of d-tubocurarine at various temperatures (10-37 degrees C) from the parallel shift of the acetylcholine dose-response curve to the right by effective doses of d-tubocurarine."( Thermodynamics of the interaction of d-tubocurarine with nicotinic receptors of mammalian skeletal muscle in vitro.
Banerjee, B; Ganguly, DK, 1996
)
0.8
" Six groups of adult rats were given 10 mg/kg THA twice daily by gavage for 1, 2, 4, or 8 wk (chronic THA groups), or 1 mL of saline twice daily by gavage for 1-8 wk (control), or IV THA approximately 20 min before (acute), and the cumulative dose-response curves of dTC at the tibialis and soleus muscles were determined during indirect train-of-four stimulation in the anesthetized, mechanically ventilated rat."( The effects of chronic tacrine therapy on d-tubocurarine blockade in the soleus and tibialis muscles of the rat.
Donati, F; Eshelby, D; Fox, GS; Ibebunjo, C; Tchervenkov, JI, 1997
)
0.56
" The presence or absence of weakness, in vivo dose-response relationships for d-tubocurarine, and serum anti-nAchR antibody titers were assayed in separate experiments."( Cecal ligation and puncture peritonitis model shows decreased nicotinic acetylcholine receptor numbers in rat muscle: immunopathologic mechanisms?
Goto, F; Kunimoto, F; Morita, T; Takahashi, K; Tsukagoshi, H, 1999
)
0.53
" On Day 8, the nerve-evoked peak twitch tensions, tetanic tensions, and fatigability, and the dose-response curves of d-tubocurarine in the tibialis cranialis muscle were measured in vivo and related to muscle mass or expression of AChRs."( Prednisolone-induced muscle dysfunction is caused more by atrophy than by altered acetylcholine receptor expression.
Fink, H; Ibebunjo, C; Khiroya, R; Martyn, J; Shin, YS, 2000
)
0.52
" Drug combinations containing equipotent concentrations of two agents were tested and dose-response curves were determined."( Isobolographic analysis of non-depolarising muscle relaxant interactions at their receptor site.
Dipp, NC; Fokt, RM; Kindler, CH; Paul, M; Yost, CS, 2002
)
0.31
" A dose-response curve has been prepared for Calliphora erythrocephala."( d-tubocurarine chloride: effect on insects.
Larsen, JR; Miller, DM; Yamamoto, T, 1966
)
0.97
" DMPX (10 microM) caused a leftward shift of the inhibitory dose-response curves for d-tubocurarine (0."( Endogenous adenosine prevents post-tetanic release facilitation mediated by alpha3beta2 nicotinic autoreceptors.
Correia-de-Sá, P; Faria, M; Timóteo, MA, 2003
)
0.54
"5 mg kg(-1)), we studied in vivo dose-response relationships for d-tubocurarine (d-Tc) and AChR binding using [125I]alpha-bungarotoxin as a ligand."( Chronic intraperitoneal endotoxin treatment in rats induces resistance to d-tubocurarine, but does not produce up-regulation of acetylcholine receptors.
Goto, F; Hinohara, H; Kunimoto, F; Morita, T; Okano, N, 2003
)
0.78
" In therapeutic dosage of 6 to 12 mg."( The sublingual administration of curare.
MAYER, H; NEFF, WB, 1953
)
0.23
" Dose-response curves were established for the noradrenaline-induced (10(-12) to 10(-7) mol/kg) increase of diastolic blood pressure in pithed rats treated with tubocurarine, propranolol, and atropine."( Reduction of vascular noradrenaline sensitivity by AT1 antagonists depends on functional sympathetic innervation.
Dendorfer, A; Dominiak, P; Raasch, W; Ziegler, A, 2004
)
0.52
" These actions of ethanol on neuromuscular transmission may affect the dosage of neuromuscular blockers required in patients who have imbibed significant amounts of alcohol."( Post-junctional interactions between neuromuscular blocking agents and ethanol at the mouse neuromuscular junction.
Searl, TJ; Silinsky, EM, 2010
)
0.36
" NF449 produced a greater rightward shift of the dose-response inhibition curve for d-TC than did suramin."( Study of the reversal effect of NF449 on neuromuscular blockade induced by d-tubocurarine.
Chen, YH; Hsiao, G; Huang, SS; Hung, YS; Lin, MJ; Su, CC; Su, HH; Su, TR, 2011
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
nicotinic antagonistAn antagonist at the nicotinic cholinergic receptor.
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
drug allergenAny drug which causes the onset of an allergic reaction.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
bisbenzylisoquinoline alkaloidA type of benzylisoquinoline alkaloid whose structures are built up of two benzylisoquinoline units linked by ether bridges. Various structural patterns resulting from additional bridging between the two units by direct carbon-carbon bridging or by methylenedioxy groups are common.
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency8.91250.35487.935539.8107AID624170
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
[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 2Homo sapiens (human)IC50 (µMol)78.80000.40003.10009.7000AID721751
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)9.60000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50 (µMol)55.50000.16003.95718.6000AID721752
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)9.40000.01002.765610.0000AID721754
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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 processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

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)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

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 membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID1346452Human KCa2.3 (Calcium- and sodium-activated potassium channels)2001Neuropharmacology, May, Volume: 40, Issue:6
Pharmacological characterisation of the human small conductance calcium-activated potassium channel hSK3 reveals sensitivity to tricyclic antidepressants and antipsychotic phenothiazines.
AID1346792Human ZAC (ZAC)2003The Journal of biological chemistry, Jan-10, Volume: 278, Issue:2
A novel class of ligand-gated ion channel is activated by Zn2+.
AID1346442Human KCa2.2 (Calcium- and sodium-activated potassium channels)2000FEBS letters, Mar-10, Volume: 469, Issue:2-3
SK2 encodes the apamin-sensitive Ca(2+)-activated K(+) channels in the human leukemic T cell line, Jurkat.
AID1346449Human KCa2.1 (Calcium- and sodium-activated potassium channels)2000British journal of pharmacology, Feb, Volume: 129, Issue:4
The pharmacology of hSK1 Ca2+-activated K+ channels expressed in mammalian cell lines.
AID1346452Human KCa2.3 (Calcium- and sodium-activated potassium channels)2004Molecular pharmacology, Mar, Volume: 65, Issue:3
An apamin- and scyllatoxin-insensitive isoform of the human SK3 channel.
AID1346438Rat KCa2.2 (Calcium- and sodium-activated potassium channels)2000British journal of pharmacology, Mar, Volume: 129, Issue:5
Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
AID1346449Human KCa2.1 (Calcium- and sodium-activated potassium channels)1996Science (New York, N.Y.), Sep-20, Volume: 273, Issue:5282
Small-conductance, calcium-activated potassium channels from mammalian brain.
AID1346438Rat KCa2.2 (Calcium- and sodium-activated potassium channels)1997The Journal of biological chemistry, Sep-12, Volume: 272, Issue:37
Determinants of apamin and d-tubocurarine block in SK potassium channels.
AID1346438Rat KCa2.2 (Calcium- and sodium-activated potassium channels)1996Science (New York, N.Y.), Sep-20, Volume: 273, Issue:5282
Small-conductance, calcium-activated potassium channels from mammalian brain.
AID1346449Human KCa2.1 (Calcium- and sodium-activated potassium channels)2000British journal of pharmacology, Mar, Volume: 129, Issue:5
Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1509244Binding affinity to MET in CD-1 mouse cochlea outer hair cells measured at -104 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1525543Binding affinity to soluble acetylcholine receptor (unknown origin)2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
Why Some Targets Benefit from beyond Rule of Five Drugs.
AID721752Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID721751Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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 (4,245)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903492 (82.26)18.7374
1990's508 (11.97)18.2507
2000's182 (4.29)29.6817
2010's58 (1.37)24.3611
2020's5 (0.12)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 63.29

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

MetricThis Compound (vs All)
Research Demand Index63.29 (24.57)
Research Supply Index8.48 (2.92)
Research Growth Index3.99 (4.65)
Search Engine Demand Index113.62 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (63.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials149 (3.20%)5.53%
Reviews83 (1.78%)6.00%
Case Studies77 (1.65%)4.05%
Observational0 (0.00%)0.25%
Other4,352 (93.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]