BRL-544435-HT1E/1F receptor agonist,potent and selective CAS# 57477-39-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 57477-39-1 | SDF | Download SDF |
| PubChem ID | 2438 | Appearance | Powder |
| Formula | C14H18N2O | M.Wt | 230.31 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (434.20 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-(1-methylpiperidin-4-yl)-1H-indol-5-ol | ||
| SMILES | CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O | ||
| Standard InChIKey | WKNFADCGOAHBPG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H18N2O/c1-16-6-4-10(5-7-16)13-9-15-14-3-2-11(17)8-12(13)14/h2-3,8-10,15,17H,4-7H2,1H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | A potent 5-ht1E/1F receptor agonist (pEC50 values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pKi values are 8.7. 8.9, 7.2, 6.9, 7.2, 5.9, 7.0, 6.5, < 6, < 6, 6.3 and 6.2 for human 5-HT1E, 1F, 1A, 1B, 1D, 2A, 2B, 2C, 4, 7, D2 and D3 receptors respectively). Induces 5-HT2A receptor-mediated mouse aortic contraction in vitro (pEC50 = 6.52). Active in vivo. |
BRL-54443 Dilution Calculator
BRL-54443 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.342 mL | 21.7099 mL | 43.4197 mL | 86.8395 mL | 108.5493 mL |
| 5 mM | 0.8684 mL | 4.342 mL | 8.6839 mL | 17.3679 mL | 21.7099 mL |
| 10 mM | 0.4342 mL | 2.171 mL | 4.342 mL | 8.6839 mL | 10.8549 mL |
| 50 mM | 0.0868 mL | 0.4342 mL | 0.8684 mL | 1.7368 mL | 2.171 mL |
| 100 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 0.8684 mL | 1.0855 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Influence of 5-HT1 receptor agonists on feline stomach relaxation.[Pubmed:15178373]
Eur J Pharmacol. 2004 May 25;492(2-3):259-67.
Sumatriptan is known for its stomach relaxing properties in both humans and cats, but the receptor involved has not been characterized. In a barostat study the intragastric volume was monitored in sedated cats at constant pressure. The maximum intragastric volume increase after subcutaneous or intravenous administration of saline or agonists was registered [mean (n=4-5)]. Sumatriptan (0.01-1 mg kg(-1)) induced a dose-dependent intragastric volume increase vs. saline (4-15 vs. 5 ml, respectively) that was sometimes accompanied by retching after 8-10 min. Pre-treatment with nitric oxide-synthase inhibitors and different 5-HT(1) receptor antagonists N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-cyclohexanecarboxami de(WAY-100635), 2-methyl-4-(5-methyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-carboxylic-acid[4-methoxy- 3-(4-methyl-piperazin-1-yl)-phenyl]amide(GR-127935), N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan-amide(5-HTP-DP) and 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine-HCl(NAN-190) did not affect the sumatriptan-induced effect. Alniditan (5-HT(1A/1D) receptor agonist) and flesinoxan (5-HT(1A) receptor agonist) did not induce significant intragastric volume changes. The 5-HT(1F) receptor agonists 5-hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole(BRL-54443) and (R)-(+)-N-(3-dimethylamino-1,2,3,4-tetrahydro-9H-carbazol-6-yl)-4-fluorobenzamide (LY-344864; 0.003-3 mg kg(-1)) however induced a dose-dependent intragastric volume increase (6-36 and 5-26 ml, respectively), no retching was seen. Our results suggest that stimulation of 5-HT(1F) receptors induces feline stomach relaxation. Whether the sumatriptan-induced gastric relaxation in cats is due to interaction with 5-HT(1F) receptors could not be proven absolutely in view of the lack of selective 5-HT(1F) receptor antagonists.
Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling.[Pubmed:11259531]
J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
The purpose of this study was to characterize pharmacologically the 5-HT receptor(s) mediating contraction in the mouse aorta and the pathways these receptors are coupled with to mediate contraction. We hypothesized that a 5-HT2A receptor, as in the rat, mediates contraction by activating L-type calcium channels, phospholipase C (PLC), and tyrosine kinase(s). Endothelium-denuded aortic strips were placed in a tissue bath for measurement of isometric contractile force. 5-HT, the 5-HT2A receptor agonist alpha-methyl-5-HT, and partial 5-HT2A receptor agonist (+/-)-2,5-dimethoxy-4-iodoamphetamine hydrochloride (+/--DOI) caused the most potent and efficacious contraction. The 5-HT(1E/1F) receptor agonist BRL 54443 also induced contraction (-log EC(50) = 6.52); however, the 5-HT2A receptor antagonist ketanserin antagonized this contraction. Our hypothesis was further supported by the finding that antagonists with affinity for the 5-HT2A receptor, ketanserin, 1-(1-naphthyl)piperazine, spiperone, and LY53857, reduced 5-HT-induced contraction. A correlation of 0.927 was found between literature-derived compound binding affinities for the agonists and antagonists at the 5-HT2A receptor of the rat and the data generated in our experiments (-log EC(50) and pK(B) values). The L-type calcium channel blockers nifedipine and nitrendipine, PLC inhibitor 2-nitro-4-carboxyphenyl N,N-diphenylcarbamate, and tyrosine kinase inhibitors genistein and PD 098,059 all shifted and/or reduced maximum contraction to 5-HT. We conclude that contraction to 5-HT in the mouse aorta is mediated primarily by a 5-HT2A receptor and is coupled to L-type calcium channels, PLC, and tyrosine kinases.
