Methoxyflurane
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Methoxyflurane (DA-759) is a volatile anesthetic and nephrotoxic agent. Methoxyflurane is metabolized by CYP450 to inorganic fluoride, dichloroacetic acid, and oxalate-related products, which accumulate in the renal tubules and inhibit Na, K-ATPase and Na-K-2Cl transport, leading to proximal tubular mitochondrial injury, ADH-resistant polyuria, and renal dysfunction. Methoxyflurane enhances chloride currents of GABAA α2β1 and glycine α1 receptors, positively modulates 5-HT3 receptors, and inhibits nicotinic acetylcholine receptors and voltage-gated calcium channels, reducing catecholamine secretion. Methoxyflurane is used in research on neurological diseases and kidney diseases.
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- Reinheit : 98.0%
- CAS. Nr.: 76-38-0
- Formel: C3H4Cl2F2O
- Molecular Weight:164.97
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[7]|
GABAAR |
GlyR α1 |
5-HT3 Receptor |
In Vitro
Methoxyflurane inhibits Carbamoylcholine chloride (HY-B1208)-evoked catecholamine secretion in bovine adrenal chromaffin cells with an IC50 of 230-250 μM, and inhibits high K+-evoked secretion with an IC50 of approximately 1200 μM, without affecting basal secretion[6].
Methoxyflurane reduces Carbamoylcholine chloride- and high K+-evoked 45Ca2+ influx in bovine adrenal chromaffin cells, and for K+ stimulation, this reduction is sufficient to account for the inhibition of catecholamine secretion[6].
Methoxyflurane inhibits Carbamoylcholine chloride-evoked 22Na+ influx in bovine adrenal chromaffin cells, and this inhibition is sufficient to account for the reduction in catecholamine secretion[6].
Methoxyflurane (0.2-5 mM; acute application) potentiates EC20 GABA responses at human GABAA α2β1 receptors expressed in HEK 293 cells with EC50 0.25 mM and Emax 135%[7].
Methoxyflurane (0.2-5 mM; acute application) potentiates EC20 glycine responses at human glycine α1 receptors expressed in HEK 293 cells with EC50 0.54 mM and Emax 120%[7].
Methoxyflurane (2 mM; acute application) fails to potentiate GABAA α2 (S270I) β1, α2 (A291W) β1, and α2β1 (M286W) receptors in HEK 293 cells while retaining potentiation at α2β1 (S265I)[7].
Methoxyflurane (2 mM; acute application) retains potentiation at glycine α1 (S267I) but not at glycine α1 (A288W) in HEK 293 cells[7].
Methoxyflurane (2 mM; acute application) does not potentiate human GABAC ρ1 receptors in HEK 293 cells, producing -4.9% modulation of EC20 GABA responses[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fischer 344 (principal model) and Buffalo (strain comparison)[1]
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Dosage:0.5% for 180 min; 0.75% for 360 min
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Administration:inhalation; 180 min; 360 min
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Result:Fischer 344 and Buffalo rats metabolized Methoxyflurane to a greater extent than the other three rat strains, with higher serum and urine inorganic fluoride activity.
Only Fischer 344 rats developed functional and pathological evidence of a renal lesion after Methoxyflurane.
Renal functional and morphological changes were proportional to Methoxyflurane dose; polyuria after Methoxyflurane anesthesia or direct inorganic fluoride injection was ADH-resistant.
At 24 hr after 0.5% Methoxyflurane for 180 min, proximal convoluted tubular cells showed swollen mitochondria and some indentation of the nucleus.
At 24 hr after 0.75% Methoxyflurane for 360 min, there was pronounced mitochondrial swelling, degeneration, and rupture.
Injection of inorganic fluoride (NaF) produced a much greater degree of renal insufficiency in Fischer 344 rats than in Buffalo rats, and sodium fluoride injection in Fischer 344 rats resulted in dose-related polyuric renal insufficiency and pathological abnormalities similar to those after Methoxyflurane anesthesia.
Enzyme induction increased defluorination and nephrotoxicity, whereas SKF 525A (Proadifen hydrochloride) (HY-B1311) resulted in decreased defluorination and an attenuated renal lesion.
Gentamicin (HY-A0276A) and Methoxyflurane adverse renal functional and pathological effects were additive in Fischer 344 rats.
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Animal Model:Sprague-Dawley (male, initial body weight 40-50 g)[3]
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Dosage:0.13% (sleeping time); 0.13% followed 96 h later by 0.5% (tolerance experiment)
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Administration:inhalation; 7 h/day for 1, 2, 3, 4, 5, 10, and 15 consecutive days; inhalation; 7 h/day for 10 consecutive days; then inhalation for 5 h 96 h later
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Result:Sleeping time after Methoxyflurane 0.13% was 96 minutes on day 1, 68 minutes on day 2, 43 minutes on day 3, 43 minutes on day 4, 34 minutes on day 5, 22 minutes on day 10, and 21 minutes on day 15.
Sleeping time decreased 79% between the first and fifteenth day of Methoxyflurane exposure.
After prior exposure to 0.13% Methoxyflurane 7 h/day for 10 days, exposure to 0.5% Methoxyflurane for 5 h resulted in 43% mortality (n=21).
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 76-38-0
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Appearance Liquid
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Molecular Weight 164.97
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Formel C3H4Cl2F2O
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Color Colorless to light yellow
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SMILES
COC(F)(F)C(Cl)Cl
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Synonyms
DA-759
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (291 KB)
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SDS (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Hot Topics
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Methoxyflurane Related Classifications
HY-B0718 Related Classifications
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Keywords
- Methoxyflurane
- 76-38-0
- DA-759
- DA759
- DA 759
- Potassium Channel
- GABA Receptor
- 5-HT Receptor
- nAChR
- Calcium Channel
- KcsA
- Gamma-aminobutyric acid Receptor
- γ-Aminobutyric acid Receptor
- Serotonin Receptor
- 5-hydroxytryptamine Receptor
- Nicotinic acetylcholine receptors
- Ca2+ channels
- Ca channels
- 5-HT3 receptors
- Na+/K+ ATPase
- defluorination
- inorganic fluoride
- nephrotoxicant
- nicotinic receptor
- polyuric renal insufficiency
- proximal tubular necrosis
- volatile anaesthetic
- voltage-gated calcium channels
- Inhibitor
- inhibitor
- inhibit