Page last updated: 2024-12-07

argiotoxin-636

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Description

argiotoxin-636: from the venom of Argiope aurantia; blocks neuromuscular transmission in insects; structure in first source. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122294
CHEMBL ID1098240
CHEBI ID34541
SCHEMBL ID17014644
MeSH IDM0557909

Synonyms (27)

Synonym
argiotoxin 636
108687-79-2
argiopin
CHEMBL1098240 ,
chebi:34541 ,
argiotoxin-636
bdbm50316373
(2s)-n-[5-[3-[3-[[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]propylamino]propylamino]pentyl]-2-[[2-(2,4-dihydroxyphenyl)acetyl]amino]butanediamide
butanediamide, n1-(16,21-diamino-21-imino-15-oxo-6,10,14,20-tetraazaheneicos-1-yl)-2-(((2,4-dihydroxyphenyl)acetyl)amino)-, (s-(r*,r*))-
ar-636
(s-(r*,r*))-n1-(16,21-diamino-21-imino-15-oxo-6,10,14,20-tetraazaheneicos-1-yl)-2-(((2,4-dihydroxyphenyl)acetyl)amino)butanediamide
argiotoxin636
ar636
argtx-636
ar 636
105029-41-2
argiopine
(2s)-n-(5-{[3-({3-[(2s)-2-amino-5-[(diaminomethylidene)amino]pentanamido]propyl}amino)propyl]amino}pentyl)-2-[2-(2,4-dihydroxyphenyl)acetamido]butanediamide
gtpl4138
argiotoxin
SCHEMBL17014644
(2s)-n-[5-[3-[3-[[(2s)-2-amino-5-guanidino-pentanoyl]amino]propylamino]propylamino]pentyl]-2-[[2-(2,4-dihydroxyphenyl)acetyl]amino]butanediamide
Q20888492
n~1~-{5-[(3-{[3-(l-arginylamino)propyl]amino}propyl)amino]pentyl}-n~2~-[(2,4-dihydroxyphenyl)acetyl]-l-aspartamide
lu7 ,
n~1~-(16,21-diamino-15-hydroxy-21-imino-6,10,14,20-tetraazahenicos-14-en-1-yl)-2-{[2-(2,4-dihydroxyphenyl)-1-hydroxyethylidene]amino}butanediimidic acid
DTXSID60909308

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" By transgenically rescuing the double mutant, we have investigated the relationship of receptor gene dosage and composition to synaptic function."( Glutamate receptor expression regulates quantal size and quantal content at the Drosophila neuromuscular junction.
DiAntonio, A; Goodman, CS; Heckmann, M; Petersen, SA, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-acyl-amino acidA carboxamide resulting from the formal condensation of a carboxylic acid with the amino group of an amino acid.
[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 (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)60.73780.00011.617910.0000AID477280; AID477281; AID689750; AID710277; AID722025
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)300.00000.00011.700010.0000AID477281
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.04200.00071.600310.0000AID689749; AID722024
Glutamate receptor 1Homo sapiens (human)IC50 (µMol)61.92000.01901.70836.5100AID477271; AID477272; AID477273; AID477276; AID477277
Glutamate receptor 2Homo sapiens (human)IC50 (µMol)152.75000.01901.64035.5000AID477272; AID477276
Glutamate receptor 3Homo sapiens (human)IC50 (µMol)0.23000.01901.13424.8000AID477274; AID477278
Glutamate receptor 4Homo sapiens (human)IC50 (µMol)0.43000.01901.22234.8000AID477279
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)0.08700.00071.630610.0000AID689749; AID710278; AID722024
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
regulation of receptor recyclingGlutamate receptor 1Homo sapiens (human)
signal transductionGlutamate receptor 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor 1Homo sapiens (human)
synapse assemblyGlutamate receptor 1Homo sapiens (human)
long-term memoryGlutamate receptor 1Homo sapiens (human)
response to xenobiotic stimulusGlutamate receptor 1Homo sapiens (human)
response to lithium ionGlutamate receptor 1Homo sapiens (human)
positive regulation of gene expressionGlutamate receptor 1Homo sapiens (human)
neuronal action potentialGlutamate receptor 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor 1Homo sapiens (human)
spinal cord developmentGlutamate receptor 1Homo sapiens (human)
cerebral cortex developmentGlutamate receptor 1Homo sapiens (human)
receptor internalizationGlutamate receptor 1Homo sapiens (human)
response to estradiolGlutamate receptor 1Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 1Homo sapiens (human)
response to cocaineGlutamate receptor 1Homo sapiens (human)
positive regulation of membrane potentialGlutamate receptor 1Homo sapiens (human)
response to arsenic-containing substanceGlutamate receptor 1Homo sapiens (human)
response to electrical stimulusGlutamate receptor 1Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
long-term synaptic potentiationGlutamate receptor 1Homo sapiens (human)
long-term synaptic depressionGlutamate receptor 1Homo sapiens (human)
response to fungicideGlutamate receptor 1Homo sapiens (human)
cellular response to amino acid stimulusGlutamate receptor 1Homo sapiens (human)
cellular response to ammonium ionGlutamate receptor 1Homo sapiens (human)
cellular response to dsRNAGlutamate receptor 1Homo sapiens (human)
cellular response to peptide hormone stimulusGlutamate receptor 1Homo sapiens (human)
cellular response to amine stimulusGlutamate receptor 1Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationGlutamate receptor 1Homo sapiens (human)
cellular response to brain-derived neurotrophic factor stimulusGlutamate receptor 1Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 1Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 1Homo sapiens (human)
signal transductionGlutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 2Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 2Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor 2Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
calcium-mediated signalingGlutamate receptor 3Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 3Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
protein homotetramerizationGlutamate receptor 3Homo sapiens (human)
protein heterotetramerizationGlutamate receptor 3Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
long-term synaptic potentiationGlutamate receptor 3Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 3Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 3Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 4Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic processGlutamate receptor 4Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 4Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
amyloid-beta bindingGlutamate receptor 1Homo sapiens (human)
G-protein alpha-subunit bindingGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 1Homo sapiens (human)
protein bindingGlutamate receptor 1Homo sapiens (human)
glutamate receptor activityGlutamate receptor 1Homo sapiens (human)
adenylate cyclase bindingGlutamate receptor 1Homo sapiens (human)
immunoglobulin bindingGlutamate receptor 1Homo sapiens (human)
protein kinase bindingGlutamate receptor 1Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor 1Homo sapiens (human)
PDZ domain bindingGlutamate receptor 1Homo sapiens (human)
small GTPase bindingGlutamate receptor 1Homo sapiens (human)
myosin V bindingGlutamate receptor 1Homo sapiens (human)
G-protein beta-subunit bindingGlutamate receptor 1Homo sapiens (human)
beta-2 adrenergic receptor bindingGlutamate receptor 1Homo sapiens (human)
glutamate receptor bindingGlutamate receptor 1Homo sapiens (human)
identical protein bindingGlutamate receptor 1Homo sapiens (human)
protein kinase A bindingGlutamate receptor 1Homo sapiens (human)
scaffold protein bindingGlutamate receptor 1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 2Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
protein bindingGlutamate receptor 2Homo sapiens (human)
ligand-gated monoatomic cation channel activityGlutamate receptor 2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 3Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 3Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor 3Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 4Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 4Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 1Homo sapiens (human)
cell-cell junctionGlutamate receptor 1Homo sapiens (human)
cell surfaceGlutamate receptor 1Homo sapiens (human)
ER to Golgi transport vesicle membraneGlutamate receptor 1Homo sapiens (human)
postsynaptic densityGlutamate receptor 1Homo sapiens (human)
dendriteGlutamate receptor 1Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 1Homo sapiens (human)
synaptic vesicle membraneGlutamate receptor 1Homo sapiens (human)
neuromuscular junctionGlutamate receptor 1Homo sapiens (human)
early endosome membraneGlutamate receptor 1Homo sapiens (human)
dendritic spine membraneGlutamate receptor 1Homo sapiens (human)
neuronal cell body membraneGlutamate receptor 1Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneGlutamate receptor 1Homo sapiens (human)
neuronal cell bodyGlutamate receptor 1Homo sapiens (human)
dendritic spineGlutamate receptor 1Homo sapiens (human)
dendritic shaftGlutamate receptor 1Homo sapiens (human)
axonal spineGlutamate receptor 1Homo sapiens (human)
neuron spineGlutamate receptor 1Homo sapiens (human)
postsynaptic membraneGlutamate receptor 1Homo sapiens (human)
presynaptic active zone membraneGlutamate receptor 1Homo sapiens (human)
recycling endosomeGlutamate receptor 1Homo sapiens (human)
recycling endosome membraneGlutamate receptor 1Homo sapiens (human)
excitatory synapseGlutamate receptor 1Homo sapiens (human)
synaptic membraneGlutamate receptor 1Homo sapiens (human)
presynapseGlutamate receptor 1Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 1Homo sapiens (human)
glutamatergic synapseGlutamate receptor 1Homo sapiens (human)
postsynaptic density, intracellular componentGlutamate receptor 1Homo sapiens (human)
perisynaptic spaceGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 1Homo sapiens (human)
dendritic spineGlutamate receptor 1Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
external side of plasma membraneGlutamate receptor 2Homo sapiens (human)
postsynaptic densityGlutamate receptor 2Homo sapiens (human)
dendriteGlutamate receptor 2Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 2Homo sapiens (human)
asymmetric synapseGlutamate receptor 2Homo sapiens (human)
neuronal cell bodyGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
excitatory synapseGlutamate receptor 2Homo sapiens (human)
postsynapseGlutamate receptor 2Homo sapiens (human)
postsynaptic endocytic zoneGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic membraneGlutamate receptor 3Homo sapiens (human)
parallel fiber to Purkinje cell synapseGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 3Homo sapiens (human)
dendritic spineGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendriteGlutamate receptor 4Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 4Homo sapiens (human)
neuronal cell bodyGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
extracellular vesicleGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 4Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 4Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID477277Inhibition of GluA1 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID722025Inhibition of rat GluA1 receptor flip form expressed in Xenopus laevis oocyte assessed as glutamate-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
AID710278Antagonist activity at rat glutamate N1/2A receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
AID477279Inhibition of GluA4 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID1713545Inhibition of tyrosinase in mouse B16-F10 cells at 0.421 uM using L-DOPA as substrate incubated for 30 mins followed by substrate addition and measured after 40 mins2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477271Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as effect of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID710276Antagonist activity at rat GluK1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
AID1713536Mixed type inhibition of mushroom tyrosinase using L-DOPA as substrate assessed as enzyme-substrate complex constant measured for 15 mins by UV-vis spectrophotometry based Line-weaver Burk plot analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID1713533Inhibition of mushroom tyrosinase using L-DOPA as substrate measured for 15 mins by UV-vis spectrophotometry2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477275Inhibition of recombinant GluA4 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477272Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as effect of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID1713535Mixed type inhibition of mushroom tyrosinase using L-DOPA as substrate assessed as inhibitory constant measured for 15 mins by UV-vis spectrophotometry based Line-weaver Burk plot analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID1713541Inhibition of melanin production in mouse B16-F10 cells incubated for 48 hrs2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID1713538Cytotoxicity against human M4Be cells assessed as reduction in cell viability at 42.1 uM incubated for 6 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477282Selectivity ratio of IC50 for rat recombinant GluA1A2 receptor flop isoform to IC50 for rat recombinant GluA1 receptor flop isoform2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID722024Inhibition of rat GluN1/2A receptor expressed in Xenopus laevis oocyte assessed as glutamate and glycine-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
AID1713534Inhibition of mushroom tyrosinase using DHICA as substrate measured for 15 mins by UV-vis spectrophotometry2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID722023Selectivity ratio of IC50 for rat GluA1 receptor flip form to IC50 for rat GluN1/2A receptor2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
AID689749Inhibition of rat GluN1/2A expressed in xenopus laevis oocytes assessed as inhibition of glycine-evoked current at membrane potential of -60 mV by voltage-clamp electrophysiology2011Journal of natural products, Mar-25, Volume: 74, Issue:3
Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.
AID477276Inhibition of recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID710277Antagonist activity at rat GluA1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
AID477278Inhibition of GluA3 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID689750Inhibition of rat GluA1 expressed in xenopus laevis oocytes assessed as inhibition of glutamate-evoked current at membrane potential of -60 mV by voltage-clamp electrophysiology2011Journal of natural products, Mar-25, Volume: 74, Issue:3
Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.
AID477281Inhibition of rat recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID1713548Reduction in alpha-MSH-induced tyrosinase expression in mouse B16-F10 cells at 0.041 uM incubated for 48 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477280Inhibition of rat recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID1713549Reduction in alpha-MSH-induced TRP-1 expression in mouse B16-F10 cells at 0.041 uM incubated for 48 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477273Inhibition of recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID1713537Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability at 42.1 uM incubated for 6 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.
AID477274Inhibition of recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (50)

TimeframeStudies, This Drug (%)All Drugs %
pre-199016 (32.00)18.7374
1990's23 (46.00)18.2507
2000's3 (6.00)29.6817
2010's8 (16.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other53 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]