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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C1N=C(CN1C2=CC=C(C=C2)Cl)N3CCOCC3
InChI
1S/C13H14ClN3O2/c14-10-1-3-11(4-2-10)17-9-12(15-13(17)18)16-5-7-19-8-6-16/h1-4H,5-9H2
InChI key
IQHYCZKIFIHTAI-UHFFFAOYSA-N
生化/生理作用
Benzodiazepine-binding site GABAA receptor partial positive allosteric modulator (PAM) with in vivo efficacy in animal models of seizure and epilepsy.
Imepitoin (AWD 131-138; ELB 138) is a g-aminobutyric acid A (GABAA) receptor partial positive allosteric modulator (PAM) that targets the benzodiazepine (BZD)-binding site at the α/γ2-interface. Imepitoin enhances GABA current (% response/[GABA] alone in µM/receptor complex = 320/3/α1β2γ2, 310/25/α1β3γ2, 460/8/α2β2γ2, 590/12/α3β2γ2 and 290/3/α5β2γ2 using Xenopus oocytes expressing respective rat receptor complex) with ~2% the potency and 17-27% the efficacy of diazepam toward α1β2γ2. Imepitoin exhibits in vivo therapeutic efficacy in animal models of seizure and epilepsy.
警示用语：
Warning
危险声明
危险分类
Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Sevil Yasar et al.
European journal of pharmacology, 465(3), 257-265 (2003-04-19)
AWD 131-138 [1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one], a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models, was studied in squirrel monkeys trained to discriminate intramuscular (i.m.) injections of midazolam (0.3 mg/kg) from injections of vehicle. Diazepam produced
E Sigel et al.
Neuroscience letters, 245(2), 85-88 (1998-05-30)
Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2 were expressed in Xenopus oocytes in a functionally active form. At all subunit combinations, AWD 131-138 dose-dependently stimulated GABA currents. At 10 microM AWD
Wolfgang Löscher et al.
Pharmacological research, 77, 39-46 (2013-09-24)
Recently, the imidazolinone derivative imepitoin has been approved for treatment of canine epilepsy. Imepitoin acts as a low-affinity partial agonist at the benzodiazepine (BZD) site of the GABAA receptor and is the first compound with such mechanism that has been
Chris Rundfeldt et al.
CNS drugs, 28(1), 29-43 (2013-12-21)
Although benzodiazepines (BZDs) offer a wide spectrum of antiepileptic activity against diverse types of epileptic seizures, their use in the treatment of epilepsy is limited because of adverse effects, loss of efficacy (tolerance), and development of physical and psychological dependence.
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