| 产品描述: | GABA 受体激活剂;GABA Receptor Activators;产品介绍:AWD 131-138(Imepitoin ) 是低亲和力的部分苯二氮(benzodiazepine)受体激动剂,有抗痉挛和抗焦虑作用。;InformationAWD 131-138 AWD 131-138 (Imepitoin, ELB-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site. |
| 靶点: |
GABA receptor |
| 体内研究: |
AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels . Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model . |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.575 ml |
17.875 ml |
35.75 ml |
| 5 mM |
0.715 ml |
3.575 ml |
7.15 ml |
| 10 mM |
0.358 ml |
1.788 ml |
3.575 ml |
| 50 mM |
0.072 ml |
0.358 ml |
0.715 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |