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LOE 908 hydrochloride

Names

[ CAS No. ]:
143482-60-4

[ Name ]:
LOE 908 hydrochloride

[Synonym ]:
2-(6,7-Dimethoxy-3,4-dihydroisoquinolin-1-yl)-2-phenyl-N,N-bis[2-(2,3,4-trimethoxyphenyl)ethyl]acetamide hydrochloride (1:1)
2-(6,7-Dimethoxy-3,4-dihydro-1-isoquinolinyl)-2-phenyl-N,N-bis[2-(2,3,4-trimethoxyphenyl)ethyl]acetamide hydrochloride (1:1)
LOE 908 hydrochloride
1-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-α-phenyl-N,N-bis[2-(2,3,4-trimethoxyphenyl)ethyl]-, hydrochloride (1:1)

Biological Activity

[Description]:

LOE 908 hydrochloride is a non-selective cation channel (NSCC) inhibitor[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Neurological Disease

[In Vitro]

LOE 908 hydrochloride 以浓度依赖方式阻断阳离子电导，IC50 为 560 nM。在电压钳位的 A7r5 细胞中，通过电压依赖的 Ca2+ 通道阻断二氢吡化物敏感的 Ba2+ 电流， IC50 为 28 μM[1]。

[In Vivo]

LOE 908 (4 or 2 mg/kg followed by 160 or 80 mg/kg; i.v.) hydrochloride 可减轻大鼠急性神经运动功能障碍[2]。 Animal Model: Adult male Sprague-Dawley rats, lateral fluid percussion brain injury model[2] Dosage: 4 mg/kg bolus followed by 160 mg/kg over 24 h or 2 mg/kg bolus followed by 80 mg/kg over 24 h Administration: Intravenous administration Result: Significantly improved neuromotor function at 48 h postinjury when compared to vehicle treatment.

[References]

[1]. Krautwurst D, et al. The isoquinoline derivative LOE 908 selectively blocks vasopressin-activated nonselective cation currents in A7r5 aortic smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 1994 Mar;349(3):301-7.  

[2]. Cheney JA, et al. The novel compound LOE 908 attenuates acute neuromotor dysfunction but not cognitive impairment or cortical tissue loss following traumatic brain injury in rats. J Neurotrauma. 2000 Jan;17(1):83-91.  

Chemical & Physical Properties

[ Molecular Formula ]:
C41H49ClN2O9

[ Molecular Weight ]:
749.289

[ Exact Mass ]:
748.312683

Related Compounds