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
ID Source | ID |
---|---|
PubMed CID | 71960 |
CHEMBL ID | 2105209 |
SCHEMBL ID | 141444 |
MeSH ID | M0074100 |
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 |
Minaxolone is a potent ligand for the neurosteroid binding site of the GABAA, receptor.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Minaxolone has been withdrawn from clinical trials following equivocal toxicological findings in rats which require further investigation.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
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"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 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5057 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.4973 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.4988 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5046 | 10.0000 | AID71999 |
Sodium- and chloride-dependent GABA transporter 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0013 | 2.2206 | 8.3000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Sodium- and chloride-dependent GABA transporter 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0032 | 1.7900 | 8.3000 | AID71999 |
Sodium- and chloride-dependent GABA transporter 3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0032 | 1.5431 | 8.3000 | AID71999 |
Sodium- and chloride-dependent betaine transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0032 | 1.5431 | 8.3000 | AID71999 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5065 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5057 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
GABA theta subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0710 | 0.0001 | 0.5075 | 10.0000 | AID71999 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
plasma membrane | Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) |
plasma membrane | Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) |
plasma membrane | Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID210604 | Therapeutic index by the ratio between LD50 to HD50 | 1997 | Journal 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. |
AID114282 | Hypnotic 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. | 1997 | Journal 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. |
AID71999 | The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes. | 1997 | Journal 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. |
AID119225 | Effect on interval between loss of righting reflex and return to righting reflex (sleep duration) was measured at a dose twice that of hypnotic dose. | 1997 | Journal 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 32 (80.00) | 18.7374 |
1990's | 6 (15.00) | 18.2507 |
2000's | 2 (5.00) | 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] |
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.
| This Compound (20.77) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (7.14%) | 5.53% |
Reviews | 5 (11.90%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 34 (80.95%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |