Compounds > 4-methyl-3-methylsulfonyl-5-phenyl-4h-1,2,4-triazole
Page last updated: 2024-12-08

4-methyl-3-methylsulfonyl-5-phenyl-4h-1,2,4-triazole

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Description

4-methyl-3-methylsulfonyl-5-phenyl-4H-1,2,4-triazole: structure given in first source; selectively reverses strychnine-induced seizures [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID164013
CHEMBL ID25195
SCHEMBL ID919281
MeSH IDM0207741

Synonyms (20)

Synonym
116850-44-3
4h-1,2,4-triazole, 4-methyl-3-(methylsulfonyl)-5-phenyl-
brn 3613487
mdl 27531
4-methyl-3-(methylsulfonyl)-5-phenyl-4h-1,2,4-triazole
CHEMBL25195
4-methyl-3-methylsulfonyl-5-phenyl-1,2,4-triazole
mdl 27,531
5-phenyl-4-methyl-3-(methylsulfonyl)-4h-1,2,4-triazole
4-methyl-3-methylsulfonyl-5-phenyl-4h-1,2,4-triazole
mdl-27531
AKOS016387397
SCHEMBL919281
DPGDRICHXKQXEN-UHFFFAOYSA-N
DTXSID40151540
NS-03238
Z752028628
3-methanesulfonyl-4-methyl-5-phenyl-4h-1,2,4-triazole
mfcd00877313
EN300-11769654
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID175552Effect of compound on reflux function in spinal transected rats at 40 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID114839Effective dose required for antagonist activity against maximal electroshock induced seizures in mice when administered intraperitoneally1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175548Effect of compound on reflux function in spinal transected rats at 10 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID72576In vitro displacement of [35S]TBPS at GABA-A picrotoxin convulsant site in rat cortical membranes at 100 uM (Inactive)1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175543Effect of compound on hyperreflexia in spinal transected rats at 20 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175541Effect of compound on hyperreflexia in spinal transected rats at 10 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175546Effect of compound on hyperreflexia in spinal transected rats at 5 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID71273In vitro displacement of [3H]baclofen at GABA-B receptor in rat cortical membranes at 100 uM (Inactive)1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175553Effect of compound on reflux function in spinal transected rats at 5 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID71684In vitro displacement of [3H]muscimol from GABA-A receptor in rat cortical membranes at 100 uM (Inactive)1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID1275693Anticonvulsant activity in ip dosed Swiss mouse assessed as protection against PTZ-induced seizures administered 30 mins prior to PTZ challenge2016European journal of medicinal chemistry, Feb-15, Volume: 109The importance of triazole scaffold in the development of anticonvulsant agents.
AID1275699Anticonvulsant activity in ip dosed CD1 mouse assessed as protection against strychnine-induced seizures administered 0.5 hr prior to strychnine challenge2016European journal of medicinal chemistry, Feb-15, Volume: 109The importance of triazole scaffold in the development of anticonvulsant agents.
AID175550Effect of compound on reflux function in spinal transected rats at 20 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID40658In vitro displacement of [3H]flunitrazepam at GABA-A benzodiazepine site in rat cortical membranes at 100 uM (Inactive)1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID1275700Anticonvulsant activity in po dosed CD1 mouse assessed as protection against strychnine-induced seizures administered 0.5 hr prior to strychnine challenge2016European journal of medicinal chemistry, Feb-15, Volume: 109The importance of triazole scaffold in the development of anticonvulsant agents.
AID114848Effective dose required for antagonist activity against strychnine induced seizures in mice when administered intraperitoneally1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID196225Enhancement of 1 uM muscimol-stimulated 36Cl- uptake into rat cerebellar membrane1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID117046Dose encompassing the 50% lethal effect was recorded when administered intraperitoneally in mice1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID114835Effective dose required for antagonist activity against 3-mercaptopropionic-acid induced seizures in mice when administered intraperitoneally1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID175545Effect of compound on hyperreflexia in spinal transected rats at 40 mg/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID114842Effective dose required for antagonist activity against pentylenetetrazole-induced seizures in mice when administered intraperitoneally1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (80.00)18.2507
2000's0 (0.00)29.6817
2010's1 (20.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.53

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.53 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		1.9810amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		1.9810halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
glycine
[no description available]		1.9810alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
phenytoin
[no description available]		3.5320imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		2.3820clonidine;
imidazoline
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		1.98101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		1.9810branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		1.9810ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
flunitrazepam
Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia.		1.98101,4-benzodiazepinone;
C-nitro compound;
monofluorobenzenes		anxiolytic drug;
GABAA receptor agonist;
sedative
muscimol
Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.. muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita.		1.9810alkaloid;
isoxazoles;
primary amino compound		fungal metabolite;
GABA agonist;
oneirogen;
psychotropic drug
chlorine
Chlorine: An element with atomic symbol Cl, atomic number 17, and atomic weight 35, and member of the halogen family.		1.9810diatomic chlorine;
gas molecular entity		bleaching agent
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.9401,2,3-triazole
strychnine
Strychnine: An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.. strychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position.		2.3820monoterpenoid indole alkaloid;
organic heteroheptacyclic compound		avicide;
cholinergic antagonist;
glycine receptor antagonist;
neurotransmitter agent;
rodenticide
valproate sodium
Epilim: oral sodium valproate used as antidepressive agent. sodium valproate : The sodium salt of valproic acid.. valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid.		3.2310organic sodium saltgeroprotector
ConditionIndicatedRelationship StrengthStudiesTrials
Clasp-Knife Spasticity
[description not available]		01.9810
Palsy
[description not available]		01.9810
Absence Seizure
[description not available]		02.3820
Muscle Spasticity
A form of muscle hypertonia associated with upper MOTOR NEURON DISEASE. Resistance to passive stretch of a spastic muscle results in minimal initial resistance (a free interval) followed by an incremental increase in muscle tone. Tone increases in proportion to the velocity of stretch. Spasticity is usually accompanied by HYPERREFLEXIA and variable degrees of MUSCLE WEAKNESS. (From Adams et al., Principles of Neurology, 6th ed, p54)		01.9810
Paralysis
A general term most often used to describe severe or complete loss of muscle strength due to motor system disease from the level of the cerebral cortex to the muscle fiber. This term may also occasionally refer to a loss of sensory function. (From Adams et al., Principles of Neurology, 6th ed, p45)		01.9810
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.3820
Aura
[description not available]		03.0410
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		03.0410
Decerebrate Posturing
[description not available]		01.9810
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9810