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Litoxetine HCl 是一种选择性5-羟色胺(5-HT)再摄取抑制剂(SSRI)和混合5-羟色胺拮抗剂,可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下(10 nM-1 microM)引起大鼠离体食道肌肉粘膜的浓度依赖性松弛,使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl(3微摩-300微摩)与明显的松弛有关,直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性,在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力,这种效力被pCPA 处理所逆转。
Litoxetine HCl 是一种选择性5-羟色胺(5-HT)再摄取抑制剂(SSRI)和混合5-羟色胺拮抗剂,可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下(10 nM-1 microM)引起大鼠离体食道肌肉粘膜的浓度依赖性松弛,使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl(3微摩-300微摩)与明显的松弛有关,直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性,在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力,这种效力被pCPA 处理所逆转。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 693 | 现货 | |
5 mg | ¥ 1,600 | 现货 | |
10 mg | ¥ 2,390 | 现货 | |
25 mg | ¥ 3,970 | 现货 | |
50 mg | ¥ 5,780 | 现货 | |
100 mg | ¥ 7,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,390 | 现货 |
产品描述 | Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment. |
靶点活性 | [3H]-DAU 6215:0.3 microM |
体外活性 | Litoxetine HCl(0.3-3微摩尔)对5-HT曲线的高效及低效阶段表现出拮抗作用。[1] 同时,Litoxetine HCl(1及3微摩尔)对5-MeOT的反应以浓度依赖的方式向右移动。[1] |
体内活性 | Litoxetine HCl(每日两次,连续4天),一种新型特异性5-羟色胺再摄取抑制剂。[2] |
别名 | 利托西汀盐酸盐, litoxetine HCL(86811-09-8 Free base) |
分子量 | 277.79 |
分子式 | C16H20ClNO |
Smiles | [H]Cl.C1(COC2CCNCC2)=CC3=C(C=CC=C3)C=C1 |
密度 | no data available |
存储 | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 22.5 mg/mL (81 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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