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AGN 192403 hydrochloride

 
Catalog No.
B6583
I1咪唑啉受体的配体
组合的产品项目
规格价格库存 数量
10mg
¥ 4,957.00
Ship with 10-15 days
50mg
¥ 18,072.00
Ship with 10-15 days

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A

背景

AGN 192403 hydrochloride是一种选择性的咪唑啉1受体的配体[1].

咪唑啉受体是可乐定和其他咪唑啉的主要受体.咪唑啉1受体(I1受体)通过咪唑啉抑制交感神经行为,从而降低血压.

AGN 192403 hydrochloride是一种选择性的I1受体的配体.AGN192403表现出对I1受体的亲和力,Ki值为42 nM,比可乐定效力仅低5倍.然而,AGN192403没有激动剂和拮抗剂活性.在猴子和大鼠中,AGN192403(5000 μg/kg)对血压没有影响[1].在星形胶质细胞中,AGN 192403抑制细胞色素c释放\溶酶体吖啶橙再定位\caspase-9的激活和线粒体膜电位的降低\萘醌诱导的细胞毒性.此外,AGN 192403抑制抗霉素A\鱼藤酮和线粒体呼吸抑制剂诱导的线粒体功能障碍和细胞毒性[2].在离体正常血压大鼠心脏中,AGN192403抑制moxonidine(10-6 M)诱导的心房利钠肽(ANP)的释放[3].

参考文献:
[1] unk SA1, Lai RK, Burke JE,Munk SA1, Lai RK, Burke JE,Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2. 2.1]heptane: a potent imidazoline1 receptor specific agent.Munk et al (1996) Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J.Med.Chem. 39 1193. PMID: 8632424.Stephen A. Munk,* Ronald K. Lai, James E. Burke, [1]. Munk SA, Lai RK, Burke JE, et al. Synthesis and Pharmacologic Evaluation of 2-endo-Amino-3-exoisopropylbicyclo[2.2.1]heptane: A Potent Imidazoline1 Receptor Specific Agent. J Med Chem, 1996, 39(6): 1193-1195.
[2].  Choi DH, Kim DH, Park YG, et al. Protective effects of rilmenidine and AGN 192403 on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. Free Radic Biol Med, 2002, 33(10): 1321-1333.
[3].  Mukaddam-Daher S, Menaouar A, Gutkowska J. Receptors involved in moxonidine-stimulated atrial natriuretic peptide release from isolated normotensive rat hearts. Eur J Pharmacol, 2006, 541(1-2): 73-79.

化学属性

Physical AppearanceWhite solid
StorageStore at RT
M.Wt189.73
Cas No.1021868-90-5
FormulaC10H19N·HCl
SolubilitySoluble to 100 mM in H2O
Chemical Name(1R,2R,3R,4S)-3-isopropylbicyclo[2.2.1]heptan-2-amine hydrochloride
SDFDownload SDF
Canonical SMILESCC([C@]1([H])[C@@]2([H])CC[C@]([C@@]1([H])N)([H])C2)C.Cl
运输条件 蓝冰运输或根据您的需求运输。
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化学结构

AGN 192403 hydrochloride