WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317850
CAS#: 77-67-8
Description: Ethosuximide is a succinimide anticonvulsant, used mainly in absence seizures. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures. The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli.
Hodoodo Cat#: H317850
Name: Ethosuximide
CAS#: 77-67-8
Chemical Formula: C7H11NO2
Exact Mass: 141.08
Molecular Weight: 141.168
Elemental Analysis: C, 59.56; H, 7.85; N, 9.92; O, 22.67
Synonym: Emeside, Ethosuccimid, Ethosuximide, Ethylmethylsuccimide, Ethymal, Zarontin.
IUPAC/Chemical Name: 3-Ethyl-3-methyl-2,5-pyrrolidinedione
InChi Key: HAPOVYFOVVWLRS-UHFFFAOYSA-N
InChi Code: InChI=1S/C7H11NO2/c1-3-7(2)4-5(9)8-6(7)10/h3-4H2,1-2H3,(H,8,9,10)
SMILES Code: O=C(C(C)(CC)C1)NC1=O
Appearance: White to off-white crystalline powder.
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | Ethosuximide improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel. |
In vitro activity: | Ethosuximide at clinically relevant concentrations inhibited GIRK channels expressed in Xenopus oocytes. The inhibition was concentration-dependent, but voltage-independent, and time-independent during each voltage pulse. Reference: Neuropharmacology. 2009 Feb;56(2):499-506. https://pubmed.ncbi.nlm.nih.gov/18977371/ |
In vivo activity: | Intraperitoneal pre-treatment (30 min prior) of mice with ethosuximide (10.0–30.0 mg/kg) produced a dose-dependent inhibition of itch responses in male (Fig. 1a) and female (Fig. 1b) mice injected with histamine. Ethosuximide was also able to decrease the time mice spent scratching when co-delivered subcutaneously (100.0–1000.0 μg) with histamine in either male (Fig. 1c) or female (Fig. 1d) mice. Similarly, systemically delivered ethosuximide (10.0–30.0 mg/kg) elicited dose-dependent inhibition of scratching behaviour of male (Fig. 2a) and female (Fig. 2b) subjects that received chloroquine diphosphate. Likewise, ethosuximide produced a significant reduction of itch responses when co-delivered (100.0–1000.0 μg) with chloroquine in male (Fig. 2c) and female (Fig. 2d). Reference: Mol Brain. 2021; 14: 46. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7927410/ |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 64.0 | 453.36 | |
Ethanol | 28.0 | 198.35 | |
Water | 28.0 | 198.35 |
The following data is based on the product molecular weight 141.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | 1. Kobayashi T, Hirai H, Iino M, Fuse I, Mitsumura K, Washiyama K, Kasai S, Ikeda K. Inhibitory effects of the antiepileptic drug ethosuximide on G protein-activated inwardly rectifying K+ channels. Neuropharmacology. 2009 Feb;56(2):499-506. doi: 10.1016/j.neuropharm.2008.10.003. Epub 2008 Oct 17. PMID: 18977371. 2. Gadotti VM, Zamponi GW. Ethosuximide inhibits acute histamine- and chloroquine-induced scratching behavior in mice. Mol Brain. 2021 Mar 2;14(1):46. doi: 10.1186/s13041-021-00762-1. PMID: 33653383; PMCID: PMC7927410. 3. Kerckhove N, Boudieu L, Ourties G, Bourdier J, Daulhac L, Eschalier A, Mallet C. Ethosuximide improves chronic pain-induced anxiety- and depression-like behaviors. Eur Neuropsychopharmacol. 2019 Dec;29(12):1419-1432. doi: 10.1016/j.euroneuro.2019.10.012. Epub 2019 Nov 22. PMID: 31767519. |
In vitro protocol: | 1. Kobayashi T, Hirai H, Iino M, Fuse I, Mitsumura K, Washiyama K, Kasai S, Ikeda K. Inhibitory effects of the antiepileptic drug ethosuximide on G protein-activated inwardly rectifying K+ channels. Neuropharmacology. 2009 Feb;56(2):499-506. doi: 10.1016/j.neuropharm.2008.10.003. Epub 2008 Oct 17. PMID: 18977371. |
In vivo protocol: | 1. Gadotti VM, Zamponi GW. Ethosuximide inhibits acute histamine- and chloroquine-induced scratching behavior in mice. Mol Brain. 2021 Mar 2;14(1):46. doi: 10.1186/s13041-021-00762-1. PMID: 33653383; PMCID: PMC7927410. 2. Kerckhove N, Boudieu L, Ourties G, Bourdier J, Daulhac L, Eschalier A, Mallet C. Ethosuximide improves chronic pain-induced anxiety- and depression-like behaviors. Eur Neuropsychopharmacol. 2019 Dec;29(12):1419-1432. doi: 10.1016/j.euroneuro.2019.10.012. Epub 2019 Nov 22. PMID: 31767519. |
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