143482-60-4

143482-60-4 structure

Name	LOE 908 hydrochloride
Synonyms	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)

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.