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BRL-54443
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BRL-54443图片
CAS NO:57477-39-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
BRL-54443 是一种有效的 5-HT1E/1F 受体激动剂（Ki 值分别为 1.1 nM 和 0.7 nM）；显示比其他 5-HT 和多巴胺受体高 30 倍的选择性。
Cas No.57477-39-1
别名3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
化学名3-(1-methylpiperidin-4-yl)-1H-indol-5-ol
Canonical SMILESCN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O
分子式C14H18N2O
分子量230.31
溶解度DMF: 12.5 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/mL,Ethanol: 1.4 mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BRL-54443 is a potent agonist for 5-HT1E and 5HT1F receptors (pEC50 values= 8.5 and 8.6) with more than 30-fold selectivity against human cloned 5-HT1A and more than 50-fold selectivity against a range of other 5-HT and dopamine receptors. [1]

5-HT receptor is a G-protein coupled receptor for 5-hydroxytryptamine (serotonin) that found in nerve systems. It also functions as receptor for various alkaloids and psychoactive substances.

In studies using rat brain cortical membranes, BRL-54443 causes biphasic inhibition of total [3H]-5-HT. [1] In C57BL/6J mouse aortae, BRL 54443 leads to a contraction in the presence of Ketanserin (an antagonist of 5-HT2A and 5-HT2C receptors).[3]

In Sprague Dawley rats, automated locomotor activity is reduced by BRL- 54443 administration at doses of 3 and 5 mg/kg. [2] BRL-4443 also stimulates sniffing behavior in rats. [2] In a barostat study, the intragastric volume was monitored in sedated cats at constant pressure, BRL-54443 induces a dose-dependent intragastric volume increase. [4]

References:
1.  A.M. Brown, K. Avenell, T J. Young et al. BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. 1998. Br.J.Pharmacol. 123 233P.
2.  S. Lightowler, T. Stean, N. Upton et al. Effect of BRL 54443 (3-(1-methylpiperidin-4-yl)-1H-indol-5-ol), a 5-HT1E/1F receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. 1998. Br.J.Pharmacol. 123 237P.
3.  McKune CM, Watts SW. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
4.  Janssen P, Tack J, Sifrim D et al. Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67.