2-((2-环丙基苯氧基)甲基)-4,5-二氢-1H-咪唑盐酸盐

用途

Cirazoline hydrochloride (LD 3098 hydrochloride) 是一种强有力的竞争性 α1A 肾上腺素受体 (α1A-AR) 的全激动剂,α1B-AR 和 α1D-AR 的部分激动剂,Ki 值分别为 120 nM, 960 nM 和 660 nM。

名称

[ CAS 号 ]:
40600-13-3

[ 中文名 ]:
西拉唑啉盐酸盐

[ 英文名 ]:
Cirazoline hydrochloride

[英文别名 ]:

Cirazoline HCl
Phenserine
EINECS 254-995-3
Cirazoline hydrochloride
MFCD00274034

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[体外研究]

盐酸吡唑啉(5-10μM；24小时)不会改变GIC存活率,只能对抗哌唑嗪诱导的GIC死亡[1]。细胞活力测定[1]细胞系：胶质母细胞瘤起始细胞浓度：5μM；10μM孵育时间：24小时结果：不影响GIC细胞存活。

[体内研究]

盐酸恶唑啉(饮用水；40μM；9个月)在TST中表现出显著的不稳定性降低和增强小鼠的神经发生[1]。动物模型：B6/CBA小鼠[1]剂量：40μM给药：饮水；40μM；9个月结果：CAMα1A-AR小鼠抗抑郁样表型逆转。

[参考文献]

[1]. Doze VA, et al. alpha(1A)- and alpha(1B)-adrenergic receptors differentially modulate antidepressant-like behaviorin the mouse.Brain Res. 2009 Aug 18;1285:148-57.

[2]. Suzana Assad Kahn , et al. The Anti-Hypertensive Drug Prazosin Inhibits Glioblastoma Growth via the PKCδ-dependent Inhibition of the AKT Pathway. EMBO Mol Med. 2016 May 2;8(5):511-26.

物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
409.5ºC at 760mmHg

[ 分子式 ]:
C₁₃H₁₇ClN₂O

[ 分子量 ]:
252.74000

[ 闪点 ]:
201.4ºC

[ 精确质量 ]:
252.10300

[ PSA ]:
33.62000

[ LogP ]:
2.51090

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
2-8°C

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

The contribution of d-tubocurarine-sensitive and apamin-sensitive K-channels to EDHF-mediated relaxation of mesenteric arteries from eNOS-/- mice.

J. Cardiovasc. Pharmacol. 59(5) , 413-25, (2012)

The nature of the potassium channels involved in determining endothelium-derived hyperpolarizing factor-mediated relaxation was investigated in first-order small mesenteric arteries from male endothel...

Different response of ANP secretion to adrenoceptor stimulation in renal hypertensive rat atria.

Peptides 29(7) , 1207-15, (2008)

Sympathetic nervous system and atrial natriuretic peptide (ANP) system play fundamental roles in the regulation of cardiovascular functions. Overactivity of sympathetic nervous system can lead into ca...

Attenuation of store-operated Ca2+ entry and enhanced expression of TRPC channels in caudal artery smooth muscle from Type 2 diabetic Goto-Kakizaki rats.

Clin. Exp. Pharmacol. Physiol. 37(7) , 670-8, (2010)

1. Previously, we found that Ca(2+) entry from the extracellular space via alpha(1)-adrenoceptor-activated, Ca(2+)-permeable channels, but not voltage-gated Ca(2+) channels, is impaired in endothelium...

更多文献

2-((2-环丙基苯氧基)甲基)-4,5-二氢-1H-咪唑盐酸盐

用途

名称

生物活性

物理化学性质

安全信息

文献

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