Page last updated: 2024-11-05

picrotoxin

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

Description

Cocculus: A plant genus of the family MENISPERMACEAE. Members contain sinococuline, coccuvine and other ALKALOIDS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Picrotoxin: A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

picrotoxin : A mixture consisting of equimolar amounts of picrotoxinin and picrotin found in the climbing plant Anamirta cocculus. [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]

FloraRankFlora DefinitionFamilyFamily Definition
CocculusgenusA plant genus of the family MENISPERMACEAE. Members contain sinococuline, coccuvine and other ALKALOIDS.[MeSH]MenispermaceaeA plant family of the order Ranunculales, subclass Magnoliidae, class Magnoliopsida. Members are mostly vines and shrubs and they contain isoquinoline alkaloids, some of which have been used as arrow poisons.[MeSH]

Cross-References

ID SourceID
PubMed CID31304
SCHEMBL ID16319990
MeSH IDM0016843
PubMed CID24802493
MeSH IDM0016843

Synonyms (28)

Synonym
nsc 403139
picrotoxinum
hsdb 6385
einecs 204-716-6
caswell no. 663a
picrotin, compound with picrotoxinin (1:1)
picrotoxinin - picrotin
picrotox
coques du levant [french]
picrotoxine
epa pesticide chemical code 002301
ai3-17689
indian berry
oriental berry
cocculus
cocculin
coques du levant
124-87-8
DB00466
picrotoxin [nf]
unii-zlt174dl7u
zlt174dl7u ,
gtpl4051
SCHEMBL16319990
Q416602
BP166191
picrotoxin
P-6780

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"05 mg/kg was found to be safe in red-footed tortoises, provided that treatment was not repeated at intervals of less than 7 days."( Toxicity and efficacy of ivermectin in chelonians.
Bush, M; Teare, JA, 1983
)
0.27
" From these observations, it is proposed that intrinsic functional inhibition in hippocampal circuits can reduce adverse effects of Abeta on the excitatory component."( Inhibitory neuronal activity can compensate for adverse effects of beta-amyloid in hippocampal neurons.
Graf, RA; Kater, SB, 1998
)
0.3
" In addition, its richness in bioactive compounds gives it an antioxidant potential, and it is not toxic in acute and sub-acute toxicity."( Revealing the most effective anticonvulsant part of Malvaviscus arboreus Dill. Ex Cav. and its acute and sub-acute toxicity.
Adassi, MB; Foutsop, AF; Kom, TD; Ngo Bum, E; Ngoupaye, GT; Yassi, FB, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" The method was applied to a pharmacokinetic study following intraperitoneal (i."( Simultaneous determination of the two components of picrotoxin in serum by reversed-phase high-performance liquid chromatography with application to a pharmacokinetic study in rats.
Aguilar-Veiga, E; Galan-Valiente, J; Mendez-Alvarez, E; Sierra-Marcuño, G; Sierra-Paredes, G; Soto-Otero, R, 1989
)
0.28
" This rapid and sensitive method can be used as a routine research tool in various physiological or pharmacokinetic studies especially in small animals."( Rapid measurement of the monoamine content in small volumes of rat plasma.
Chen, CF; Cheng, FC; Chia, LG; Kuo, JS; Tsai, TH, 1994
)
0.29

Compound-Compound Interactions

ExcerptReferenceRelevance
" Hence, in the present study, its (100 and 200 mg/kg) action was tested alone and in combination with phenobarbitone (20 mg/kg) and diazepam (0."( Effect of 7-nitroindazole alone and in combination with phenobarbitone and diazepam on picrotoxin-induced convulsions in rats.
Ekambaram, P; Paul, V, 2003
)
0.32
" The effect of SNP was tested alone and in combination with phenobarbitone (PB), the GABA potentiating antiepileptic drug, against picrotoxin (PCT) (5 mg/kg)-induced convulsions in rats."( Effects of sodium nitroprusside, a nitric oxide donor, on gamma-aminobutyric acid concentration in the brain and on picrotoxin-induced convulsions in combination with phenobarbitone in rats.
Ekambaram, P; Paul, V, 2005
)
0.33

Bioavailability

ExcerptReferenceRelevance
" Given that p-coumaric acid is reasonably well absorbed following oral consumption in man and is relatively nontoxic, it may be suitable for the formulation of a safe and effective anxiolytic functional food."( p-Coumaric acid activates the GABA-A receptor in vitro and is orally anxiolytic in vivo.
Bisson, JF; Scheepens, A; Skinner, M, 2014
)
0.4
" hM4Di has no effect in the absence of its selective, normally inactive and orally bioavailable agonist clozapine-N-oxide (CNO)."( Chemical-genetic attenuation of focal neocortical seizures.
Kätzel, D; Kullmann, DM; Nicholson, E; Schorge, S; Walker, MC, 2014
)
0.4
" Relative bioavailability of carbamazepine after administration of nanoemulsion was 160% compared to unmodified substance."( Experimental investigation of pharmacodynamics and pharmacokinetics of carbamazepine nanoemulsion.
Abramov, DA; Kapitsa, IG; Kaplun, AP; Prokhorov, DI; Sariev, AK; Seifulla, RD; Shiriaeva, MV; Voronina, TA; Zhuravko, AS, 2014
)
0.4

Dosage Studied

haloperidol (PB) shifted the dose-response curve for GABA in the presence of bicuculline methochloride to the left. ICI 154,129 was proconvulsant in the mouse picrotoxin potentiation test. PB restored the slope and the maximum response towards that of the control GABA-induced response.

ExcerptRelevanceReference
" The dose-response relationship and specifity of this effect were investigated."( Transient apnoea after systemic injection of GABA in the rat.
Hagmüller, K; Holzer, P, 1979
)
0.26
" Kinetic analyses of the dose-response curves for the N-methylamino acid in the presence or absence of the convulsant indicated that the number of molecules of the amino acid combining with the receptor site to produce a response was 3 for N-methylGABA, 2 for N-methylglycine, 3 for N-methyltaurine, 3 for N-methylbeta-alanine."( Effects of N-methylamino acids and convulsants on spontaneous action potentials in guinea-pig cerebellar slices.
Okamoto, K; Quastel, JH, 1977
)
0.26
" 4 In the frog spinal cord GABA depolarized the dorsal roots presumably by mimicking the activity of the transmitter depolarizing the primary afferents; sigmoidal log dose-response curves for GABA were obtained."( A comparative study of the action of gamma-aminobutyric acid and piperazine on the lobster muscle fibre and the frog spinal cord.
Constanti, A; Nistri, A, 1976
)
0.26
" 3 Studies of the dose-response relations indicated a competition between the amino acid and the convulsant at a common receptor site."( Effects of amino acids and convulsants on spontaneous action potentials in cerebellar cortex slices.
Okamoto, K; Quastel, JH, 1976
)
0.26
" Functional changes in the GABAA receptors were assayed using the effects of potentiators (benzodiazepine, barbiturate) and antagonists (picrotoxin) on the muscimol control dose-response curves."( Functional changes in GABAA receptor stimulation during the oestrous cycle of the rat.
Lindgren, S; Meyerson, B; Westerling, P, 1991
)
0.28
"In order to test the GABA hypothesis of kindling, GABA-complex antagonists were administered in a dose-response paradigm to rats that had been implanted with indwelling forebrain electrodes, but not kindled."( Secondary generalization in non-kindled rats following acute administration of GABA-complex and adenosine antagonists.
Burnham, WM; Mingo, NS, 1990
)
0.28
"25 and 200 mumol/kg as revealed by the dose-response curves obtained in both experiments."( NMDA antagonist properties of gamma-L-glutamyl-L-aspartate demonstrated on chemically induced seizures in mice.
De Barry, J; Mathis, C; Ungerer, A, 1990
)
0.28
" The dose-response relationship followed simple Michaelis-Menten kinetics, with a half-maximal response elicited at approximately 110 microM."( Effects of gamma-aminobutyric acid on skate retinal horizontal cells: evidence for an electrogenic uptake mechanism.
Malchow, RP; Ripps, H, 1990
)
0.28
" In males, a dose-response study of nimodipine's effects on seizures induced by different doses of picrotoxin was conducted."( The effect of nimodipine on picrotoxin-induced seizures.
Thomas, J, 1990
)
0.28
"In a dose-response study, the pattern of sex-associated susceptibility to picrotoxin-induced myoclonic, focal, akinetic, and generalized tonic-clonic (GTC) seizures was investigated in rats to determine whether the reported heightened susceptibility of females to seizures was a general phenomenon in rats or whether it was limited to specific types of seizures."( Gender difference in susceptibility to picrotoxin-induced seizures is seizure- and stimulation-dependent.
Thomas, J, 1990
)
0.28
" The presence of these different ICl components explains why the dose-response relationship cannot be fitted well by a single Hill equation; the fitting requires a synthesis of 3 suitable Hill equations."( GABA activates different types of chloride-conducting receptor-ionophore complexes in a dose-dependent manner.
Akaike, N; Ishizuka, S; Yasui, S, 1985
)
0.27
" Hill coefficients, determined from dose-response data, indicated that binding of at least two GABA molecules was required to activate the chloride channel."( GABA receptors on the cell-body membrane of an identified insect motor neuron.
David, JA; Pinnock, RD; Sattelle, DB; Wafford, KA, 1988
)
0.27
"Using isolated, internally perfused bullfrog dorsal root ganglion cells we have studied the dose-response curves for gamma-aminobutyric acid (GABA) in the presence of internally or externally applied GABA antagonists."( Bicuculline and picrotoxin block gamma-aminobutyric acid-gated Cl- conductance by different mechanisms.
Akaike, N; Carpenter, DO; Hattori, K; Oomura, Y, 1985
)
0.27
" Acute and long-term haloperidol administration induced significant leftward displacement of the control dose-response curves for picrotoxin but not those for strychnine or 3-mercaptopropionic acid (3-MPA)."( Behavioral aspects of GABAergic-dopaminergic interactions in the central nervous system.
Palermo-Neto, J; Sandoval, MR, 1989
)
0.28
" Complete dose-response curves were carried out on individual neurons, reducing error introduced by cell-to-cell variability."( Modulation of neurotransmitter action: control of the gamma-aminobutyric acid response through the benzodiazepine receptor.
Chan, CY; Farb, DH, 1985
)
0.27
" The dose-response relationships for GABA antagonism of [3H]alpha-dihydropicrotoxinin binding and for picrotoxinin antagonism of the GABA enhancement of [3H]flunitrazepam binding in cultured cortical neurons were also investigated."( The picrotoxinin binding site and its relationship to the GABA receptor complex.
Dichter, MA; Snodgrass, SR; White, WF, 1985
)
0.27
" The effect of GABA was mimicked by (-)-baclofen, which gave a dose-response curve overlapping that of GABA, while (+)-baclofen was about one hundred times less potent."( Modulatory activity of GABAB receptors on cholinergic tone in guinea-pig distal colon.
Giotti, A; Luzzi, S; Maggi, CA; Spagnesi, S; Zilletti, L, 1985
)
0.27
"5 mg/kg diazepam-morphine dose-response curve."( The possible modulation of morphine analgesia by the supramolecular GABA receptor complex.
Ayhan, IH; Palaoglu, O, 1986
)
0.27
" The dose-response relationships for strychnine and picrotoxin were investigated at fixed pressures."( Investigations into the origin of the high pressure neurological syndrome: the interaction between pressure, strychnine and 1,2-propandiols in the mouse.
Bowser-Riley, F; Daniels, S; Smith, EB, 1988
)
0.27
" Dose-response and time course studies of Ro 15-4513 against gamma-aminobutyric acid (GABA) antagonists were performed."( Interactions of the imidazodiazepine Ro 15-4513 with chemical convulsants.
Lister, RG; Nutt, DJ, 1988
)
0.27
" beta CCE and beta CCtB produced dose-related, parallel shifts in the dose-response curve for the discriminative effects of diazepam, but the magnitude of the shifts was limited: the two highest doses of beta CCE and beta CCtB produced shifts that were not significantly different in magnitude."( Beta-carbolines as antagonists of the discriminative stimulus effects of diazepam in rats.
Cook, JA; Guzman, F; Hagen, TJ; Shannon, HE, 1988
)
0.27
" Prednisolone shifted the dose-response curve of the GABA current downward."( Voltage-clamp studies of the inhibition of gamma-aminobutyric acid response by glucocorticoids in bullfrog primary afferent neurons.
Akasu, T; Ariyoshi, M, 1987
)
0.27
" VP showed a U-shaped dose-response effect."( Effects of neurohypophyseal peptide hormones on alcohol dependence and withdrawal.
Kovács, GL; Szabó, G; Telegdy, G, 1987
)
0.27
" Muscimol (2 mg/kg) and THIP (5 and 10 mg/kg) exerted the antiimmobility effect even after single dosing 1 h before the test."( Effect of GABAergic drugs in the behavioral 'despair' test in rats.
Borsini, F; Evangelista, S; Meli, A, 1986
)
0.27
"The dose-response curves for the anticonvulsive activity of sulfated and nonsulfated cholecystokinin octapeptide (CCK-8-SE and CCK-8-NS) against picrotoxin-induced (6 mg/kg SC) seizures were assessed either following or without pretreatment with a single high dose of CCK-8-SE or CCK-8-NS, to examine acute tolerance to the effect after IP injections in mice."( Multiple treatment potentiates the anticonvulsive activity of cholecystokinin octapeptides.
Kádár, T; Penke, B; Pesti, A; Telegdy, G,
)
0.13
" The log dose-response curve for depolarization was sigmoid with a mean ED(50) of 12."( Depolarizing actions of gamma-aminobutyric acid and related compounds on rat superior cervical ganglia in vitro.
Bowery, NG; Brown, DA, 1974
)
0.25
" The dose-response relation showed that picrotoxin depressed the conductance increase produced by GABA in a non-competitive manner."( A study of the action of picrotoxin on the inhibitory neuromuscular junction of the crayfish.
Takeuchi, A; Takeuchi, N, 1969
)
0.25
" No significant tolerance developed to the anticonvulsant action of PK 11195 (30 mg kg-1) even after 25 days of dosing daily."( Pro- and anti-convulsant properties of PK 11195, a ligand for benzodiazepine binding sites: development of tolerance.
File, SE, 1984
)
0.27
" PB shifted the dose-response curve for GABA in the presence of bicuculline methochloride to the left without altering the slope or the dose ratio, and not only displaced the dose-response curve for GABA in the presence of picrotoxinin but also restored the slope and the maximum response towards that of the control GABA-induced response."( Potentiation of GABAA-receptor-mediated responses by barbiturates in the guinea-pig ileum.
Kerr, DI; Ong, J, 1984
)
0.27
" 5 Methohexitone and thiopentone produced a biphasic dose-response on the K+-stimulated release of both amino acids; low concentrations enhanced release, high concentrations depressed release."( The effects of anaesthetics on the uptake and release of amino acid neurotransmitters in thalamic slices.
Kendall, TJ; Minchin, MC, 1982
)
0.26
" From an analysis of the dose-response curve of GABA with or without ibotenate, it is suggested that ibotenate acts on the GABA receptor in the crayfish neuromuscular junction."( Inhibitory action of ibotenic acid on the crayfish neuromuscular junction.
Ishida, M; Shinozaki, H, 1980
)
0.26
" The log dose-response curves for GABA and muscimol appeared to be parallel, but were not parallel to that for dopamine."( GABA and muscimol inhibit the release of prolactin from dispersed rat anterior pituitary cells.
Besser, GM; Delitala, G; Grossman, A; Yeo, T, 1981
)
0.26
" Step clamp data were used to construct dose-response curves."( Voltage clamp analysis of inhibitory synaptic action in crayfish stretch receptor neurons.
Adams, PR; Banks, FW; Constanti, A, 1981
)
0.26
" For MES testing, mice were injected with either reserpine, yohimbine, propranolol, haloperidol or metergoline prior to dosing with TET."( Pharmacological and biochemical evaluation of triethyltin's anticonvulsant effects.
Fox, DA,
)
0.13
" ICI 154,129 was proconvulsant in the mouse picrotoxin potentiation test; the dose-response curve had a low ceiling and was biphasic."( In vivo studies with ICI 154,129, a putative delta receptor antagonist.
Cowan, A; Gmerek, DE,
)
0.13
" In the dose-response curves for DMPP-evoked CA secretion, the inhibitory action of PT (0."( Effect of picrotoxin on adrenal catecholamine secretion.
Hayashi, E; Okada, T; Yamada, S; Yamanaka, K, 1983
)
0.27
") administered in combination with naloxone and picrotoxin shifted dose-response curves for both naloxone and picrotoxin to the right."( Comparison of the effects of naloxone and picrotoxin on schedule-controlled responding in the pigeon: possible GABA-antagonistic effects of naloxone.
Carter, RB; Leander, JD, 1984
)
0.27
" Anisatin shifted the dose-response curve for GABA-induced depolarization in the primary afferent terminal to the right and also reduced the maximum response to GABA."( Anisatin, a potent GABA antagonist, isolated from Illicium anisatum.
Kudo, Y; Oka, JI; Yamada, K, 1981
)
0.26
" When applied topically to cortex, muscimol blocks focal penicillin, bicuculline, and picrotoxin discharges in a dose-response relationship."( Anticonvulsant effects of muscimol.
Collins, RC, 1980
)
0.26
"Experiments on isolated mice (CC57W males) have demonstrated that GABA antagonists (bicuculline, picrotoxin, thiosemicarbazide) increase the desocializing effects of isolation (enhance aggression and reduce intraspecies sociability), while GABA-positive drugs (muscimol, gamma-acetylenic GABA) within a certain dosage range diminish aggression and favour a temporary recovery of sociability."( [GABA-ergic correlates of aggression and intraspecies sociability of mice subjected to isolation].
Poshivalov, VP, 1981
)
0.26
" 3 The actions of Sl 75 102 were in nearly all respects identical to those of GABA; parameters examined were the effects on membrane potential and input conductance, desensitization, dose-response characteristics and sensitivity to the GABA antagonists, bicuculline and picrotoxin."( SL 75 102 as a gama-aminobutyric acid agonist: experiments on dorsal root ganglion neurones in vitro.
Desarmenien, M; Feltz, P; Headley, PM; Santangelo, F, 1981
)
0.26
" These sites appear to be interdependent since analysis of the shift in the DPH dose-response curve by PTX and vice versa, showed neither truly non-competitive nor competitive interaction."( On the action of the anticonvulsant 5,5-diphenylhydantoin and the convulsant picrotoxin in crayfish stretch receptor.
Aickin, CC; Deisz, RA; Lux, HD, 1981
)
0.26
" The log dose-response relationship obtained from 6 preparations was sigmoidal and had an ED(50) of 13 muM."( The effect of gamma-aminobutyric acid on the input conductance and membrane potential of Ascaris muscle.
Martin, RJ, 1980
)
0.26
" GABA dose-response characteristics of wild type and mutant receptors were very similar."( A unique amino acid of the Drosophila GABA receptor with influence on drug sensitivity by two mechanisms.
ffrench-Constant, RH; Jackson, MB; Zhang, HG, 1994
)
0.29
"0 mg/kg induced a significant leftward displacement of the control dose-response curve constructed for apomorphine (0."( Effect of manipulation of the GABA system on dopamine-related behaviors.
Palermo-Neto, J; Sandoval, MR, 1995
)
0.29
" In the case of the wild type receptor, fipronil blocked GABA-induced currents inducing both a shift to the right in the GABA dose-response curve and depressing the maximum amplitude of responses to GABA."( Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila melanogaster.
Baylis, HA; Buckingham, SD; Hosie, AM; Sattelle, DB, 1995
)
0.29
" This effect which was quantified in terms of numbers of tongue protrusions, was dose-dependent: a bell-shaped dose-response was found (50-500 ng)."( Interactions of the subthalamic nucleus and the subpallidal area in oro-facial dyskinesia: role of GABA and glutamate.
Cools, AR; Helfrich, SE; Spooren, WP, 1995
)
0.29
" The ED50 values 4 h after oral dosing were 13."( Topiramate: preclinical evaluation of structurally novel anticonvulsant.
Davis, CB; Dodgson, SJ; Gardocki, JF; Maryanoff, BE; Nortey, SO; Raffa, RB; Schupsky, JJ; Shank, RP; Vaught, JL,
)
0.13
" Diazepam shifted the dose-response curve for muscimol-stimulated flux to about 4-fold lower concentrations without affecting the maximum response."( Reconstitution of purified GABAA receptors: ligand binding and chloride transporting properties.
Dunn, SM; Thuynsma, RP, 1994
)
0.29
" These two current components have different dose-response characteristics for GABA, with the nondesensitizing component being activated more effectively and reaching its peak amplitude at lower agonist concentrations than the desensitizing one."( GABA responses and their partial occlusion by glycine in cultured rat medullary neurons.
Faber, DS; Lewis, CA, 1993
)
0.29
" Pretreatment of rats with venom increased the minimum convulsant dose of picrotoxin, impaired convulsion generalization and displaced to the left the dose-response curve for picrotoxin."( Behavioural and electroencephalographic effects of Tityus serrulatus scorpion venom in rats.
Dorce, VA; Sandoval, MR, 1993
)
0.29
" Acute and long-term dosing increased both rearing and locomotion frequencies observed in an open field."( Behavioral effects of acute and long-term administration of catnip (Nepeta cataria) in mice.
Bernardi, MM; Gorniak, SL; Massoco, CO; Silva, MR; Spinosa, MS, 1995
)
0.29
" In aged rats, the dose-response curve was shifted to the left, indicating an increase in the potency of GABA to inhibit [3H]t-butylbicycloorthobenzoate binding."( GABAA receptor binding in the aging rat inferior colliculus.
Albin, RL; Caspary, DM; Milbrandt, JC; Turgeon, SM, 1996
)
0.29
" It is suggested that changes in the structure of DSIP are accompanied by alterations in the strength of the effects of this peptide on horizontal and convulsive activity after dosage into the reticular part of the substantia nigra."( Effect of intranigral dosage with delta-sleep-inducing peptide and its analogs on movement and convulsive activity in rats.
Brusentsov, AI; Godlevskii, RS; Mikhaleva, II; Prudchenko, IA; Shandra, AA; Vast'yanov, AI; Zaporozhan, VN,
)
0.13
" For example, receptors formed by perch-rho 1B subunits were more sensitive to GABA than the receptors formed by other GABA-rho subunits, the dose-response curves for the various receptors revealed different Hill coefficients, and there were differences in the kinetics of the GABA-induced currents."( Molecular and pharmacological properties of GABA-rho subunits from white perch retina.
Dowling, JE; Qian, H; Ripps, H, 1998
)
0.3
" Furthermore, coexpression of wild-type rho1 and gamma2S subunits was found to shift the GABA dose-response curve."( Evidence for coassembly of mutant GABAC rho1 with GABAA gamma2S, glycine alpha1 and glycine alpha2 receptor subunits in vitro.
Lipton, SA; Pan, ZH; Zhang, D; Zhang, X, 2000
)
0.31
" The dose-response relationship for the intrathecal-intraventricular infusion paralleled that of the IV infusion but was shifted to the left by an order of magnitude."( Both cerebral GABA(A) receptors and spinal GABA(A) receptors modulate the capacity of isoflurane to produce immobility.
Dutton, R; Eger, EI; Sonner, J; Stabernack, C; Zhang, Y, 2001
)
0.31
" VS-3 neuron GABA receptors were activated by muscimol and inhibited by picrotoxin but not bicuculline, and their dose-response relationship had an EC(50) of 103."( Peripheral GABAergic inhibition of spider mechanosensory afferents.
French, AS; Panek, I; Sekizawa, S; Seyfarth, EA; Torkkeli, PH, 2002
)
0.31
" In this report, we show that ATP elicits Ca(2+) responses producing a monophasic dose-response curve with an EC(50) value of 24."( GABAB receptor-mediated presynaptic potentiation of ATP ionotropic receptors in rat midbrain synaptosomes.
Gómez-Villafuertes, R; Gualix, J; Miras-Portugal, MT; Pintor, J, 2003
)
0.32
" The magnitude of the leftward shift in the agonist dose-response curve for the two mutant combinations was in agreement with a subunit stoichiometry of 3alpha:2beta."( Stoichiometry of recombinant heteromeric glycine receptors revealed by a pore-lining region point mutation.
Beato, M; Burzomato, V; Groot-Kormelink, PJ; Sivilotti, LG, 2003
)
0.32
" Dose-response (D-R) curves and kinetic measurements of GABA rho(1) currents were carried out in the presence or absence of antagonists."( Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor.
Calvo, DJ; Goutman, JD, 2004
)
0.32
" The duration of treatment (6-8 weeks) and dosage were comparable in all studies."( Treatment of vertigo with a homeopathic complex remedy compared with usual treatments: a meta-analysis of clinical trials.
Klein, P; Schneider, B; Weiser, M, 2005
)
0.33
" In the presence of 300 microM Lu(3+), dose-response curves for GABA-evoked currents showed a significant enhancement of the maximum amplitude and an increase of the apparent affinity."( Analysis of macroscopic ionic currents mediated by GABArho1 receptors during lanthanide modulation predicts novel states controlling channel gating.
Calvo, DJ; Escobar, AL; Goutman, JD, 2005
)
0.33
" At low concentration, bilobalide (3 microM) caused a parallel right shift and surmountable GABA maximal response of the GABA dose-response curve characteristic of a competitive antagonist."( Mixed antagonistic effects of bilobalide at rho1 GABAC receptor.
Chebib, M; Duke, RK; Huang, SH; Johnston, GA; Sasaki, K; Wada, K, 2006
)
0.33
" When dosed at 10mg/kg, beta-acids increased, in the elevated plus maze, open arm entries reducing in parallel those in closed arms."( Evidence that the beta-acids fraction of hops reduces central GABAergic neurotransmission.
Avallone, R; Baraldi, M; Brusiani, F; Losi, G; Puia, G; Rivasi, M; Zanoli, P; Zavatti, M, 2007
)
0.34
" Separate groups of rats received bilateral intra-VTA injections of the GABA-A antagonist picrotoxin (34 ng/side, n = 7; 68 ng/side, n = 8), GABA-A agonist muscimol (14 ng/side, n = 8), GABA-B agonist baclofen (56 ng/side, n = 7; 100 ng/side, n = 6), picrotoxin (68 ng/side) co-injected with the GABA-B antagonist 2-hydroxysaclofen (100 ng/side, n = 7; 2 microg/side, n = 8) or artificial cerebrospinal fluid (aCSF, n = 6) to assess the effects of the various compounds on the cocaine self-administration dose-response curve."( Contribution of ventral tegmental GABA receptors to cocaine self-administration in rats.
Backes, EN; Hemby, SE, 2008
)
0.35
" In contrast to the chronic treatment, an acute application of fluoxetine in slices induces a leftward shift in the dose-response curve of the 5-HT-induced potentiation."( Chronic fluoxetine bidirectionally modulates potentiating effects of serotonin on the hippocampal mossy fiber synaptic transmission.
Haneda, E; Ikeda, Y; Kobayashi, K; Suzuki, H, 2008
)
0.35
" After the repeated attacks epilepsy model had been established successfully, model rats were randomly divided into model group, Tianbingtiaodu capsule low dosage (0."( [Effects of Tianbingtiaodu capsule on improvement of learning and memory abilities and expression of NMDAR1 of epileptic rats in the hippocampus].
Jia, XM; Liu, CY; Pei, L; Pei, YR; Wang, Y, 2010
)
0.36
" It is important to mention that the highest dosage of the AcOEt (1000 mg/kg) produced a severe suppression or isoelectric EEG activity (EEG flattening), recognized as a comatose state, suggesting a neurotoxic effect at this dosage."( Pharmacological and toxicological effects of Ruta chalepensis L. on experimentally induced seizures and electroencephalographic spectral power in mice.
Carmona-Aparicio, L; González-Trujano, ME; Martínez-Vargas, D; Santos-Valencia, F; Urbina-Trejo, E; Villasana-Salazar, B, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,937)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901705 (43.31)18.7374
1990's958 (24.33)18.2507
2000's809 (20.55)29.6817
2010's407 (10.34)24.3611
2020's58 (1.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.12

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 Index53.12 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index82.82 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (6.25%)5.53%
Trials6 (0.15%)5.53%
Reviews0 (0.00%)6.00%
Reviews68 (1.64%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies8 (0.19%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other30 (93.75%)84.16%
Other4,053 (98.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]