Page last updated: 2024-11-07

gabazine

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

Gabazine, also known as SR 95531, is a selective and competitive antagonist of the GABAA receptor. It is a synthetic compound with a chemical structure similar to the neurotransmitter GABA. Gabazine has a high affinity for the GABAA receptor, blocking the binding of GABA and preventing the opening of the chloride ion channel. This action inhibits the inhibitory effects of GABA, leading to an increase in neuronal activity. Gabazine is primarily used as a research tool to study the role of GABAA receptors in the brain. Its ability to block the effects of GABA allows researchers to investigate the role of GABAergic neurotransmission in various physiological processes, such as learning and memory, anxiety, and epilepsy. Gabazine is also being investigated as a potential therapeutic agent for a variety of neurological disorders, including anxiety disorders, insomnia, and Parkinson's disease.'

Cross-References

ID SourceID
PubMed CID107895
MeSH IDM0142643

Synonyms (32)

Synonym
104104-50-9
6-amino-5-methyl-3-(4-methoxyphenyl)-1-pyridaziniumbutyric acid br
1(6h)-pyridazinebutanoic acid, 6-imino-3-(4-methoxyphenyl)-, monohydrobromide
6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinebutanoic acid monohydrobromide
99460mg420 ,
unii-99460mg420
sr 95531 hydrobromide
6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinebutanoic acid hydrobromide
c15h17n3o3.hbr
sr 95531 hydrobromide (gabazine)
HB0901
AKOS024456498
4-(6-imino-3-(4-methoxyphenyl)pyridazin-1(6h)-yl)butanoic acid hydrobromide
J-001107
SR-01000597905-1
sr-01000597905
CS-0028033
HY-103533
BCP21630
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid;hydrobromide
Q5515280
EX-A3488
G-216
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid;hydrobromide.
gabazine hydrobromide
6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinebutanoic acid, monohydrobromide
DTXSID40908798
AS-56048
6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinebutanoic acid, monohydrobromide;gabazine hydrobromide
A901095
BS43265
F87729
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.07400.00020.561410.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.07400.00020.635210.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.07400.00020.621710.0000AID239462
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.07400.00020.675810.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.07400.00020.646910.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.07400.00020.671210.0000AID239462
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.07400.00020.557710.0000AID239462
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.07400.00020.640310.0000AID239462
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.07400.00020.570810.0000AID239462
GABA theta subunitRattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.07400.00020.656110.0000AID239462
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID239462Displacement of [3H]muscimol from rat brain gamma-aminobutyric-acid GABA-A receptor2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID132660Electrophysiology using Whole-cell patch-clamp recordings in mouse embryos2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID71386Affinity for GABA-B receptor by inhibiting GABA uptake into rat brain synaptosomes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID248086In vitro concentration required to inhibit peak currents in cerebral cortical neurones of rat2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID72302Displacement of [3H]GABA from gamma-aminobutyric-acid A (GABA-A) receptor1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Structure and molecular modeling of GABAA receptor antagonists.
AID72134Binding affinity, determined by its ability to displace the [3H]GABA from Gamma-aminobutyric acid A (GABA-A) receptor site of rat brain membranes1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists.
AID72457Affinity for GABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
[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-19901 (20.00)18.7374
1990's1 (20.00)18.2507
2000's3 (60.00)29.6817
2010's0 (0.00)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: 42.72

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

MetricThis Compound (vs All)
Research Demand Index42.72 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index57.52 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.72)

All Compounds (24.57)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]