Page last updated: 2024-12-06

minaxolone

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

Description

Minaxolone is a synthetic steroid with anti-inflammatory and immunomodulatory properties. It has been investigated for its potential therapeutic applications in various inflammatory conditions, including rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis. The synthesis of minaxolone involves several steps, starting with the modification of a steroid precursor molecule. It is believed to exert its effects by inhibiting the production of pro-inflammatory cytokines and modulating the activity of immune cells. Minaxolone is studied for its potential to provide a novel therapeutic approach for inflammatory disorders, offering a more targeted and potentially safer alternative to conventional treatments. Research into minaxolone is ongoing, and further studies are needed to fully evaluate its efficacy and safety in human subjects.'
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minaxolone: RN given refers to parent cpd(2beta,3alpha,5alpha,11alpha)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71960
CHEMBL ID2105209
SCHEMBL ID141444
MeSH IDM0074100

Synonyms (27)

Synonym
minaxolone
D05041
62571-87-3
minaxolone (usan/inn)
c.c.i. 12923
cci 12923
minaxolone [usan:inn:ban]
minaxolonum [inn-latin]
11alpha-(dimethylamino)-2beta-ethoxy-3alpha-hydroxy-5alpha-pregnan-20-one
pregnan-20-one, 11-(dimethylamino)-2-ethoxy-3-hydroxy-, (2beta,3alpha,5alpha,11alpha)-
minaxolona [inn-spanish]
1-[(2s,3s,5s,8s,9s,10s,11r,13s,14s,17s)-11-(dimethylamino)-2-ethoxy-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]ethanone
unii-737skc73l0
minaxolona
minaxolonum
737skc73l0 ,
CHEMBL2105209
cci-12923
1-[(1s,2s,4s,5s,7s,10s,11s,14s,15s,17r)-17-(dimethylamino)-4-ethoxy-5-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-14-yl]ethan-1-one
gtpl5478
minaxolone [usan]
pregnan-20-one, 11-(dimethylamino)-2-ethoxy-3-hydroxy-, (2.beta.,3.alpha.,5.alpha.,11.alpha.)-
minaxolone [inn]
minaxolone [who-dd]
SCHEMBL141444
Q6863285
DTXSID201024283

Research Excerpts

Overview

Minaxolone is a potent ligand for the neurosteroid binding site of the GABAA, receptor.

ExcerptReferenceRelevance
"Minaxolone appears to be a promising new anaesthetic worthy of further study."( An early clinical assessment of the steroid anaesthetic Minaxolone.
Dunn, GL; McChesney, J; Morison, DH; Pine, W, 1980
)
1.23
"Minaxolone proved to be a satisfactory induction agent."( Initial experience with Minaxolone. A water-soluble steroid intravenous anaesthetic agent.
Lumley, J; Morgan, M; Punchihewa, VG; Whitwam, JG, 1980
)
1.29
"Minaxolone is a potent ligand for the neurosteroid binding site of the GABAA, receptor. "( Development of tolerance in mice to the sedative effects of the neuroactive steroid minaxolone following chronic exposure.
Ford, E; Hagan, RM; Marshall, FH; Mullings, J; Oakley, NR; Stratton, SC; Worton, SP, 1997
)
1.96

Effects

Minaxolone has been withdrawn from clinical trials following equivocal toxicological findings in rats which require further investigation.

ExcerptReferenceRelevance
"Minaxolone has been withdrawn from clinical trials following equivocal toxicological findings in rats which require further investigation."( Minaxolone: an evaluation with and without premedication.
Briggs, LP; Clarke, RS; Dundee, JW; McNeill, HG, 1981
)
2.43
"Minaxolone has been used to induce anaesthesia, and in incremental doses to supplement nitrous oxide, in 100 patients undergoing minor surgical procedures. "( Initial experience with Minaxolone. A water-soluble steroid intravenous anaesthetic agent.
Lumley, J; Morgan, M; Punchihewa, VG; Whitwam, JG, 1980
)
2.01
"Minaxolone has been used for the induction and maintenance of anaesthesia in 60 patients undergoing minor surgical procedures. "( Early clinical evaluation of minaxolone: a new intravenous steroid anaesthetic agent.
Aveling, W; Campbell, D; Chang, H; Cooper, GM; Fitch, W; Prys-Roberts, C; Savege, TM; Sear, JW; Simpson, P; Waters, A, 1979
)
1.99

Actions

ExcerptReferenceRelevance
"minaxolone) additionally enhance the function of recombinant glycine receptors (GlyR)."( GABAA and glycine receptor-mediated transmission in rat lamina II neurones: relevance to the analgesic actions of neuroactive steroids.
Belelli, D; Dempster, J; Gentet, LJ; Mitchell, EA, 2007
)
1.06

Pharmacokinetics

ExcerptReferenceRelevance
" Drug uptake and retention in extravisceral tissues, represented here by the hindquarters, can result in the mean total body drug clearance being overestimated when determined by traditional systemic pharmacokinetic methods."( Uptake and elution of chlormethiazole, meperidine, and minaxolone in the hindquarters of sheep: implications for clearance calculations.
Carapetis, RJ; Mather, LE; McLean, CF; Runciman, WB; Upton, RN, 1991
)
0.53
" Further experimental evidence in support of this finding was the lack of dose dependence in any pharmacokinetic parameter following bolus doses through the clinical range of 12."( Minaxolone, a new steroidal anesthetic. Pharmacokinetics and organ extraction in sheep.
Gourlay, GK; Mather, LE; Parkin, KS,
)
1.57
" The decay in the plasma drug concentrations after the infusion could be fitted to a bi-exponential equation, indicating that the steroids were distributed according to an open two-compartment pharmacokinetic model."( Alphadione and minaxolone pharmacokinetics.
Prys-Roberts, C; Sear, JW, 1981
)
0.62

Dosage Studied

ExcerptRelevanceReference
" Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating development of tolerance."( Development of tolerance in mice to the sedative effects of the neuroactive steroid minaxolone following chronic exposure.
Ford, E; Hagan, RM; Marshall, FH; Mullings, J; Oakley, NR; Stratton, SC; Worton, SP, 1997
)
0.84
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (20)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.505710.0000AID71999
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.497310.0000AID71999
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.498810.0000AID71999
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.504610.0000AID71999
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00132.22068.3000AID71999
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00321.79008.3000AID71999
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00321.54318.3000AID71999
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.07100.00321.54318.3000AID71999
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.506510.0000AID71999
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.505710.0000AID71999
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.07100.00010.507510.0000AID71999
[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 (4)

Assay IDTitleYearJournalArticle
AID210604Therapeutic index by the ratio between LD50 to HD501997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID114282Hypnotic dose was determined by observing loss of righting reflex for a minimum period of 30 sec in 50% of treated mice after i.v. administration.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID71999The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
AID119225Effect on interval between loss of righting reflex and return to righting reflex (sleep duration) was measured at a dose twice that of hypnotic dose.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-199032 (80.00)18.7374
1990's6 (15.00)18.2507
2000's2 (5.00)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: 20.77

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

MetricThis Compound (vs All)
Research Demand Index20.77 (24.57)
Research Supply Index3.83 (2.92)
Research Growth Index4.01 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (7.14%)5.53%
Reviews5 (11.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (80.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]