AA 29504
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AA 29504,{2-氨基-4-(2, 4, 6-三甲基苄胺)-苯基}-氨基甲酸乙酯,是突触外GABAA受体的正向调节剂。AA 29504也是KCNQ通道开放剂retigabine的类似物,比retigabine效果差3-4倍。AA 29504对KCNQ通道的EC50值介于9.6和13.5 μM之间[2]。在爪蟾卵母细胞表达的α1β3γ2s或α4β3δ GABAA受体的试验中,AA 29504在1 μM下无激动活性,但可使GABA和gaboxadol(THIP)对两个受体的EC50值左移。AA 29504(1 μM)对α1β3γ2s受体的最大GABA响应未发生改变,但对α4β3δ受体提高了3倍[1]。
GABA可瞬时激活突触GABAA受体,导致经典的抑制性突触后电流(相位性抑制)[2]。KCNQ(也称Kv7)通道是电压依赖的钾离子通道,由五个不同的KCNQ亚基(KCNQ1-5,或称作Kv7.1-Kv7.5)的同源和异源复合体组成[3]。
在爪蟾卵母细胞中,AA 29504低于3 μM的浓度下无内在活性,但在3 μM及以上AA 29504可诱发微小的响应,且不能被bicuculline阻断。浓度为1 μM的AA 29504处理对GABAA受体和KCNQ通道无内在活性,但可左移GABA的浓度反应曲线,而不影响GABA的最大响应[1]。
在亚慢性苯环己哌啶(PCP)处理的大鼠中,AA 29504在1和4 mg/kg下急性给药可逆转PCP诱导的短缺,但中间剂量2 mg/kg则不能。AA 29504处理不影响自发活动。AA 29504处理的动物组不能显著区分熟知事物和新事物。2 mg/kg的AA 29504处理的组对左边的物体有微弱但显著的偏好[2]。
参考文献:
[1]. K. Hoestgaard-Jensen, N.O. Dalby, T.D. Wolinsky, et al. Pharmacological characterization of a novel positive modulator at α4β3δ-containing extrasynaptic GABAA receptors. Neuropharmacology, 2010, 58:702-711.
[2]. Trine Damgaard, Niels Plath, Jo C. Neill, et al. Extrasynaptic GABAA receptor activation reverses recognition memory deficits in an animal model of schizophrenia. Psychopharmacology, 2011, 214:403-413.
[3]. Henrik H. Hansen, Christina Ebbesen, Claus Mathiesen, et al. The KCNQ Channel Opener Retigabine Inhibits the Activity of Mesencephalic Dopaminergic Systems of the Rat. Journal of Pharmacology and Experimental Therapeutics, 2006, 318(3): 1006–1019.
Physical Appearance | Off-white solid |
Storage | Store at -20°C |
M.Wt | 327.42 |
Cas No. | 945828-50-2 |
Formula | C19H25N3O2 |
Solubility | <32.74mg/ml in DMSO |
Chemical Name | (E)-ethyl hydrogen (2-amino-4-((2,4,6-trimethylbenzyl)amino)phenyl)carbonimidate |
SDF | Download SDF |
Canonical SMILES | CCO/C(O)=N/C1=C(N)C=C(NCC2=C(C=C(C=C2C)C)C)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |