SML3361
Imepitoin
≥98% (HPLC)
别名:
1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one, 1-(4-Chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one, AWD 131-138, AWD131-138, ELB138
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关于此项目
经验公式（希尔记法）:
C13H14ClN3O2
化学文摘社编号:
分子量:
279.72
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
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
Biochem/physiol Actions
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.
signalword
Warning
hcodes
Hazard Classifications
Repr. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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.
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML3361-50MG | 04065268375020 |
| SML3361-10MG | 04065268375013 |