BRL-54443 |
カタログ番号GC17130
One-Click Copy Product Info
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BRL-54443 は強力な 5-HT1E/1F 受容体アゴニストです (Ki 値はそれぞれ 1.1 nM と 0.7 nM)。他の 5-HT およびドーパミン受容体よりも 30 倍以上の選択性を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57477-39-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 57477-39-1 | SDF | |
| Chemical Name | 3-(1-methylpiperidin-4-yl)-1H-indol-5-ol | ||
| Canonical SMILES | CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O | ||
| Formula | C14H18N2O | M.Wt | 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 | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.342 mL | 21.7099 mL | 43.4197 mL |
| 5 mM | 868.4 μL | 4.342 mL | 8.6839 mL |
| 10 mM | 434.2 μL | 2.171 mL | 4.342 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)