ETHOTOIN - CAS 86-35-1
Catalog number: 86-35-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C11H12N2O2
Molecular Weight:
204.23
COA:
Inquire
Targets:
Sodium Channel
Description:
Ethotoin is an anticonvulsant drug. It is a sodium channel inhibitor. Ethotoin can be used for the treatment of epilepsy. It is a hydantoin, similar to phenytoin.
Purity:
95%
Appearance:
White Solid
Synonyms:
(±)-Ethotoin; 1-Ethyl-2,5-dioxo-4-phenylimidazolidine; 3-Ethyl-5-phenyl-2,4-imidazolidinedione; 3-Ethyl-5-phenylhydantoin; 3-Ethyl-5-phenylimidazolidin-2,4-dione; AC-695; Accenon; Peganone; 3-Ethyl-5-phenyl-2,4-Imidazolidinedione;
Solubility:
Chloroform, DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
anticonvulsant drug
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
90-92℃
Density:
1.197 g/cm
InChIKey:
SZQIFWWUIBRPBZ-UHFFFAOYSA-N
InChI:
InChI=1S/C11H12N2O2/c1-2-13-10(14)9(12-11(13)15)8-6-4-3-5-7-8/h3-7,9H,2H2,1H3,(H,12,15)
Canonical SMILES:
CCN1C(=O)C(NC1=O)C2=CC=CC=C2
Current Developer:
originator Recordati
1.Simultaneous measurement of phenobarbital, phenytoin, primidone, ethosuximide, and carbamazepine in serum by high-pressure liquid chromatography.
Kabra PM;Stafford BE;Marton LJ Clin Chem. 1977 Jul;23(7):1284-8.
We present a method for simultaneously determining five anticonvulsants [phenobarbital, phenytoin (diphenylhydantoin), primidone, ethosuximide, and carbamazepine] in as little as 25 microliters of serum. The proteins are precipitated with an acetonitrile solution containing hexobarbital as an internal standard. The anticonvulsants are eluted from a reversed-phase column with a mobile phase consisting of an acetonitrile/phosphate buffer (19/81 by vol) at a flow rate of 3.0 ml/min. The eluted drugs are detected by their absorption at 195 nm, and quantities estimated from their peak heights. Each analysis requires about 14 min. at an optimum column temperature of 50 degrees C. The lower unit of detection for all of these drugs is less than 10 ng. Sensitivities, for serum samples, of 1.0 mg/liter for all the drugs analyzed are attained routinely. Analytical recoveries for the five drugs varied from 97 - 107%, with good day-to-day precision (CV between 3.9 and 5.9%). Of more than 30 drugs tested for possible interference, only ethotoin interferes with the analysis of phenobarbital.
2.Comparison of the behavioral teratogenic potential of phenytoin, mephenytoin, ethotoin, and hydantoin in rats.
Minck DR;Acuff-Smith KD;Vorhees CV Teratology. 1991 Apr;43(4):279-93.
Pregnant Sprague-Dawley CD rats were orally administered either phenytoin (PHT, 200 mg/kg), mephenytoin (MPH, 100 mg/kg), ethotoin (ETH, 600 mg/kg), hydantoin (HYD, 1,200 mg/kg) or vehicle (propylene glycol) on days 7-18 of gestation. Mean (+/- S.E.) maternal serum concentrations of PHT, MPH, and ETH 1 hour after dosing on gestational day 18 were 16.0 +/- 3.3, 10.7 +/- 3.0, and 65.2 +/- 10.45, respectively, and free fractions were 16%, 18%, and 11% respectively. The free fraction for PHT is similar, but was lower for both MPH and ETH than that seen in humans. Preweaning mortality for PHT, MPH, ETH, HYD, and controls was 25%, 6.3%, 12.5%, 2.0% and 0.8%, respectively. The MPH and ETH-exposed animals weighed approximately 6.6% less than controls throughout the study; the other groups did not differ significantly. PHT offspring showed increased early locomotor activity. Only PHT-exposed animals (27%) exhibited abnormal circling behavior after weaning. PHT-circlers accounted for higher levels of activity in an open-field test and for longer straight channel swimming times. PHT-circlers and noncirclers differed from one another and controls on performance of a complex (Cincinnati) maze and on the development of the air-righting reflex.
3.Role of microtubule assembly in phenytoin teratogenic action in the sea urchin (Arbacia punctulata) embryo.
Estus S;Blumer JL Mol Pharmacol. 1989 Nov;36(5):708-15.
We evaluated the role of microtubule assembly in phenytoin (5-5-diphenylhydantoin) teratogenic activity in the sea urchin embryo. Zygotes were exposed to phenytoin or one of several phenytoin analogs within 15 min of fertilization and the frequency of the resultant malformations was assessed at the cleavage and late gastrula (prism) stages. Concomitant studies of drug uptake into zygotes and drug effects on both microtubule assembly in vitro and spindle morphology in situ were also performed. Phenytoin, 5-p-methylphenyl-5-phenylhydantoin, and 5-p-methoxyphenyl-5-phenylhydantoin were teratogenic (approaching 100% affected embryos) at both developmental stages were concentrated rapidly by the zygotes, and induced a shortened mitotic spindle in situ. In a separate in vitro system using porcine brain microtubular protein, these analogs were shown to inhibit microtubule assembly directly. The major human metabolite of phenytoin, 5-p-hydroxyphenyl-5-phenylhydantoin was teratogenic at the prism stage but induced only a 20% incidence of abnormal embryos at the first cleavage. This was attributed to the slow rate of uptake of this analog. This compound inhibited microtubule assembly in the in vitro assay and also shortened the mitotic spindle to an extent proportional to its observed weak effect on the first cleavage.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Sodium Channel Products


PF-04856264
(CAS: 1235397-05-3)

This active molecular is a human Nav1.7 voltage gated sodium channel inhibitor with the IC50 value of 28 nM. PF-04856264 inhibits the Nav channel by interacting...

CAS 630-93-3 Phenytoin Sodium

Phenytoin Sodium
(CAS: 630-93-3)

Phenytoin Sodium is a potent multi-channel blocker, which blocks Na+, K+ and Ca 2+ channels and selectively blocks persistent INaP over shorter INaP actions.

CAS 159138-80-4 Cariporide

Cariporide
(CAS: 159138-80-4)

Cariporide, also known as HOE-642, is a selectiveNa+/H+exchange inhibitor, also known as the Na+/H+ antiporter, which functions to improve cellular integrity fo...

CAS 5369-03-9 QX 314 chloride

QX 314 chloride
(CAS: 5369-03-9)

QX 314 chloride, a membrane-impermeant lidocaine derivative, is a blocker of voltage-activated Na+ channels. QX-314 elicits a long-lasting decrease in the respo...

AZD-3161
(CAS: 1369501-46-1)

AZD 3161 is a Nav1.7-voltage-gated-sodium-channel-inhibitor originated by AstraZeneca. Phase-I clinical trials in Pain and Neuropathic pain was discontinued.

PF 04885614

PF 04885614 is a potent and selective Nav1.8 inhibitor (IC50 = 53 nM for human NaV1.8 channel), with selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNa...

CAS 1262618-39-2 GS967

GS967
(CAS: 1262618-39-2)

GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhyth...

Funapide
(CAS: 1259933-16-8)

Funapide is a Nav1.7 and Nav1.8 voltage-gated sodium channel inhibitor under the development by Xenon Pharmaceuticals and Teva Pharmaceutical Industries. It is ...

CAS 42971-09-5 Vinpocetine

Vinpocetine
(CAS: 42971-09-5)

Vinpocetine is a Phosphodiesterase inhibitor and selective for PDE1. It also blocks voltage-gated Na+ channels.

CAS 484598-36-9 ProTx II

ProTx II
(CAS: 484598-36-9)

ProTx II is a selective NaV1.7 channel blocker with 100-fold selectivity over other sodium channel subtypes.

CAS 5875-06-9 Proxymetacaine hydrochloride

Proxymetacaine hydrochloride
(CAS: 5875-06-9)

Proparacaine Hydrochloride is a topical ophthalmic anesthetic, acting by inhibiting the voltage-gated sodium channels. IC50(ED50): 3.4 mM.

CAS 925463-91-8 Jingzhaotoxin III

Jingzhaotoxin III
(CAS: 925463-91-8)

Jingzhaotoxin III is a selective blocker of NaV1.5 channels with IC50 value of 348 nM. It is selective for NaV1.5 channels and shows no effect on other isoforms...

CAS 34183-22-7 Propafenone hydrochloride

Propafenone hydrochloride
(CAS: 34183-22-7)

Propafenone is a Class 1C antiarrhythmic as sodium channel blocker by slowing the influx of sodium ions into the cardiac muscle cells.

CAS 132112-35-7 Ropivacaine Hydrochloride

Ropivacaine Hydrochloride
(CAS: 132112-35-7)

Ropivacaine hydrochloride is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

CAS 24003-58-5 QX 314 bromide

QX 314 bromide
(CAS: 24003-58-5)

QX 314, a membrane impermeable quaternary derivative of lidocaine, selectively blocks sodium channels on nociceptive neurons when delivered intracellularly via ...

CAS 5370-01-4 Mexiletine Hydrochloride

Mexiletine Hydrochloride
(CAS: 5370-01-4)

Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.

PF-05241328
(CAS: 1387633-03-5)

PF-05241328, a purely acidic molecule, is a selective inhibitor of human Nav1. 7 voltage-dependent sodium channels (IC50= 31nM) for the treatment of pain. But P...

VX-150

VX-150 is a NaV1.8 blocker which is currently in a phase II clinical trial for the treatment of patients with acute pain. Study shows that VX-150 significantly ...

Psalmotoxin 1

Psalmotoxin 1 (PcTx1) is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker (IC50 = 0.9 nM) and not other members of the family. The blockade i...

CAS 161804-20-2 Benzamil hydrochloride

Benzamil hydrochloride
(CAS: 161804-20-2)

Benzamil hydrochloride is a Na+/Ca2+ exhanger (NCX) inhibitor (IC50 ~ 100 nM) and an epithelial sodium channel (ENaC) blocker. Benzamil is an analogue of amilor...

Chemical Structure

CAS 86-35-1 ETHOTOIN

Quick Inquiry

Verification code

Featured Items