Page last updated: 2024-12-07

s 135

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

Description

S 135: GABA receptor agonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	113637
CHEMBL ID	3144843
MeSH ID	M0164457

Synonyms (8)

Synonym
s 135
2-(5-methylthien-3-yl)-2,5-dihydro-3h-pyrazolo(4,3-c)quinolin-3-one
3h-pyrazolo(4,3-c)quinolin-3-one, 2,5-dihydro-2-(5-methyl-3-thienyl)-
104679-67-6
CHEMBL3144843
2-(5-methylthiophen-3-yl)-2,5-dihydro-3h-pyrazolo[4,3-c]quinolin-3-one
2-(5-methylthiophen-3-yl)-1,2-dihydro-3h-pyrazolo[4,3-c]quinolin-3-one
DTXSID20909122

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (9)

Assay ID	Title	Year	Journal	Article
AID40967	Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors.
AID348954	Displacement of [3H]diazepam from GABAA/BzR in rat brain membrane	2008	European journal of medicinal chemistry, Jul, Volume: 43, Issue:7	Quantitative structure-activity relationship studies of a series of non-benzodiazepine structural ligands binding to benzodiazepine receptor.
AID110217	Ability to inhibit pentylenetetrazole (PTZ) induced convulsions in mice after peroral administration at 75 mg/Kg; Range is between (0.47-0.94)	1987	Journal of medicinal chemistry, Mar, Volume: 30, Issue:3	A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors.
AID39938	Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor	1996	Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14	Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
AID131056	Inverse agonist activity of orally administered compound against a subcutaneous dose of 75 mg/kg of PTZ-induced convulsions in mice	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors.
AID110218	Ability to inhibit pentylenetetrazole (PTZ) induced convulsions in mice after peroral administration at 90 mg/Kg	1987	Journal of medicinal chemistry, Mar, Volume: 30, Issue:3	A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors.
AID131059	Inverse agonist activity of orally administered compound against a subcutaneous dose of 90 mg/kg of PTZ-induced convulsions in mice	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors.
AID40966	Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex	1987	Journal of medicinal chemistry, Mar, Volume: 30, Issue:3	A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors.
AID493017	Wombat Data for BeliefDocking	2002	European journal of medicinal chemistry, Mar, Volume: 37, Issue:3	Local intersection volume: a new 3D descriptor applied to develop a 3D-QSAR pharmacophore model for benzodiazepine receptor ligands.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	3 (37.50)	18.7374
1990's	3 (37.50)	18.2507
2000's	2 (25.00)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (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: 50.29

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.

Metric	This Compound (vs All)
Research Demand Index	50.29 (24.57)
Research Supply Index	2.20 (2.92)
Research Growth Index	4.29 (4.65)
Search Engine Demand Index	80.94 (26.88)
Search Engine Supply Index	2.17 (0.95)

This Compound (50.29)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	8 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
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.	2.67	3	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic
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.	1.98	1	ethyl ester; imidazobenzodiazepine; organofluorine compound	antidote to benzodiazepine poisoning; GABA antagonist
reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.	1.97	1	alkaloid ester; methyl ester; yohimban alkaloid	adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic
carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.	2.67	3	monohydroxyquinoline; quinolone	bacterial xenobiotic metabolite
dimethylformamide Dimethylformamide: A formamide in which the amino hydrogens are replaced by methyl groups.. N,N-dimethylformamide : A member of the class of formamides that is formamide in which the amino hydrogens are replaced by methyl groups.	1.97	1	formamides; volatile organic compound	geroprotector; hepatotoxic agent; polar aprotic solvent
norharman norharman: RN given refers to parent cpd. beta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring.	2.04	1	beta-carbolines; mancude organic heterotricyclic parent	fungal metabolite; marine metabolite
2-phenylpyrazolo(4,3-c)quinolin-3(5h)-one 2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one: a mixed agonist/antagonist of the benzodiazepine receptor	2.39	2
beta-carboline-3-carboxylic acid ethyl ester beta-carboline-3-carboxylic acid ethyl ester: isolated from brain tissue & urine; extremely potent displacer of diazepam from brain benzodiazepam receptors; structure in first source	2.38	2	beta-carbolines
beta-carboline-3-carboxylic acid methyl ester beta-carboline-3-carboxylic acid methyl ester: structure given in first source	2.4	2	beta-carbolines
deoxyglucose Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.	1.97	1
harman harman: a beta-carboline; RN given refers to parent cpd; structure. harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A.	2.04	1	harmala alkaloid; indole alkaloid fundamental parent; indole alkaloid	anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; plant metabolite
1-Ethyl-9H-pyrido[3,4-b]indole [no description available]	2.04	1	harmala alkaloid

Condition	Relationship Strength	Studies
Absence Seizure [description not available]	2.37	2
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.	2.37	2
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	1.97	1
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	1.97	1
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.	1.97	1

chemdatabank.com