BRL-54443

￥729.21 1EA 起订

其他更新日期：2020-01-15

Selleck中国

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产品详情:

英文名称：: BRL-54443

规格：: 10mg/10mM/1mL/50mg

货号：: S2852

Selleck Chemicals美国品牌，中国库存现货，5-HT Receptor抑制剂，CAS#57477-39-1。
更多详情请访问中国唯一官方网站：
http://www.selleck.cn/products/brl-54443.html

生物活性

产品描述	BRL 54443是一种5-HT1E和5-HT1F受体激动剂，pK_i分别为8.7和9.25，对5-HT1A， 5-HT1B， 5-HT1D受体具有弱的结合亲和力。
靶点	5-HT_1E	5-HT_1F	5-HT_1A	5-HT_1B	5-HT_1D
IC50	8.7 (pK_i)	9.25 (pK_i)	7.2 (pK_i)	6.9 (pK_i)	7.2 (pK_i) ^[1]
体外研究	BRL 54443 has also measurable affinity for the 5-HT_2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT_2A receptors. ^[2]
体内研究	BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. ^[1]
临床实验
特征

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验: ^[1]

Membrane preparation and binding assay	The binding affinity of a set of 5-HT receptor agonists and antagonists (samples) at 5-HT_1F receptors is tested. To do this h5-HT_1F-HEK 293 cells are cultured in Petri dishes till 90% confluency is reached. The cells are scraped from the plates and suspended in 50 mM Tris–HCl buffer (pH 7.4). After centrifugation (23,500 × g) the pellet is suspended in 5 mM Tris–HCl buffer (pH 7.4) and homogenized with an Ultra Turrax homogeniser. The membranes are collected by centrifugation at 18,000 × g for 20 minutes, resuspended in 50 mM Tris–HCl (pH 7.4) and stored at −80 °C. At the day of the binding experiment, the membranes are defrosted and homogenized. The protein concentration is determined using the Bradford protein assay and the membranes are diluted in the assay buffer down to 65 μg protein/mL (50 mM Tris–HCl, 10 mM MgCl₂, 1 mM EGTA and 10 μM pargyline, pH 7.4). Assay mixtures (0.5 mL) contained 0.4 mL membrane preparation and 2 nM of tritiated 5-HT (118 Ci/mmol); to determine the non-specific binding 1 μM sumatriptan is added. Per sample studied 15 mixtures are created containing different concentrations (10 μM–1 pM) of the sample. The mixtures are then incubated for 60 minutes at 25 °C (protected from light), incubation is stopped by rapid filtration on a Filtermate 96. Bound radioactivity is determined by liquid scintillation counting. Data are analysed graphically with inhibition curves and IC50 values are derived. K_i values are calculated according to the equation K_i =IC50/(1+(C/K_d)), with C as the concentration of [³H]5-HT (2 nM) and K_d as the equilibrium dissociation constant of [³H]5-HT (2.61 nM).

Membrane preparation and binding assay

The binding affinity of a set of 5-HT receptor agonists and antagonists (samples) at 5-HT_1F receptors is tested. To do this h5-HT_1F-HEK 293 cells are cultured in Petri dishes till 90% confluency is reached. The cells are scraped from the plates and suspended in 50 mM Tris–HCl buffer (pH 7.4). After centrifugation (23,500 × g) the pellet is suspended in 5 mM Tris–HCl buffer (pH 7.4) and homogenized with an Ultra Turrax homogeniser. The membranes are collected by centrifugation at 18,000 × g for 20 minutes, resuspended in 50 mM Tris–HCl (pH 7.4) and stored at −80 °C. At the day of the binding experiment, the membranes are defrosted and homogenized. The protein concentration is determined using the Bradford protein assay and the membranes are diluted in the assay buffer down to 65 μg protein/mL (50 mM Tris–HCl, 10 mM MgCl₂, 1 mM EGTA and 10 μM pargyline, pH 7.4). Assay mixtures (0.5 mL) contained 0.4 mL membrane preparation and 2 nM of tritiated 5-HT (118 Ci/mmol); to determine the non-specific binding 1 μM sumatriptan is added. Per sample studied 15 mixtures are created containing different concentrations (10 μM–1 pM) of the sample. The mixtures are then incubated for 60 minutes at 25 °C (protected from light), incubation is stopped by rapid filtration on a Filtermate 96. Bound radioactivity is determined by liquid scintillation counting. Data are analysed graphically with inhibition curves and IC50 values are derived. K_i values are calculated according to the equation K_i =IC50/(1+(C/K_d)), with C as the concentration of [³H]5-HT (2 nM) and K_d as the equilibrium dissociation constant of [³H]5-HT (2.61 nM).

动物实验: ^[1]

动物模型	Adult male cats
配制	Distilled water containing 1 equivalent 2,3-dihydroxybutanedioic acid+0.9% NaCl
剂量	3 μg/kg-30 mg/kg
给药处理	s.c.