BRL-15572

5-HT1D receptor antagonist CAS# 193611-72-2

BRL-15572

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Chemical structure

BRL-15572

3D structure

Chemical Properties of BRL-15572

Cas No. 193611-72-2 SDF Download SDF
PubChem ID 9891303 Appearance Powder
Formula C25H29Cl3N2O M.Wt 479.9
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 250 mg/mL (520.97 mM; Need ultrasonic)
Chemical Name 3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol;dihydrochloride
SMILES C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl
Standard InChIKey WPEXRXMQMPOHIO-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H27ClN2O.2ClH/c26-22-12-7-13-23(18-22)28-16-14-27(15-17-28)19-24(29)25(20-8-3-1-4-9-20)21-10-5-2-6-11-21;;/h1-13,18,24-25,29H,14-17,19H2;2*1H
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.
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.
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.

Biological Activity of BRL-15572

DescriptionBRL-15572 is an antagonist of 5-HT1D receptor with a pKi value of 7.9.
Targets5-HT1D5-HT1A5-HT2B5-HT2A5-HT7  
IC507.9(pKi)7.7(pKi)7.4(pKi)6.6(pKi)6.3(pKi)  

BRL-15572 Dilution Calculator

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BRL-15572 Molarity Calculator

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Preparing Stock Solutions of BRL-15572

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0838 mL 10.4188 mL 20.8377 mL 41.6753 mL 52.0942 mL
5 mM 0.4168 mL 2.0838 mL 4.1675 mL 8.3351 mL 10.4188 mL
10 mM 0.2084 mL 1.0419 mL 2.0838 mL 4.1675 mL 5.2094 mL
50 mM 0.0417 mL 0.2084 mL 0.4168 mL 0.8335 mL 1.0419 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.4168 mL 0.5209 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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Background on BRL-15572

BRL-15572 is an antagonist of 5-HT1D receptor with pKi value of 7.9 [1].

In the in vitro binding assay, BRL-15572 shows 60-fold higher affinity for human 5-HT1D receptor than for h5-HT1B receptor. However, it also has moderately high affinity at both human 5-HT1A and human 5-HT2B receptors. It limits the use of BRL-15572 as a pharmacological tool in systems. In native tissue, BRL-15572 totally inhibits [3H] 5-CT specific binding in guinea-pig striatum. In the functional assays, BRL-15572 is potent at both [35S] GTPγS binding assay and cAMP accumulation assay. It shows a pEC50 value of 8.1 at h5-HT1D receptor expressed in CHO cell membranes. And the activity shows to be lower in the cAMP assay [1].

References:
[1] Price G W, Burton M J, Collin L J, et al. SB-216641 and BRL-15572–compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn-Schmiedeberg's archives of pharmacology, 1997, 356(3): 312-320.

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References on BRL-15572

Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors.[Pubmed:9303568]

Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):321-7.

Human cerebral cortical slices and synaptosomes, guinea-pig cerebral cortical slices and human right atrial appendages were used to study the effects of SB-216641, a preferential h5-HT1B receptor ligand, and of BRL-15572, a preferential h5-HT1D receptor ligand, on the presynaptic h5-HT1B and h5-HT1B-like autoreceptors in the human and guinea-pig brain preparations, respectively, and on the presynaptic h5-HT1D heteroreceptors in the human atrium. The brain preparations, preincubated with [3H]serotonin ([3H]5-HT), and the segments of atrial appendages, preincubated with [3H]noradrenaline, were superfused with modified Krebs' solution and tritium overflow was evoked electrically (human and guinea-pig cerebral cortex slices and human atrial appendages) or by high K+ (human cerebral cortex synaptosomes). The electrically evoked tritium overflow from guinea-pig cerebral cortex slices was reduced by the 5-HT receptor agonist 5-carboxamidotryptamine (5-CT). This effect was not modified by BRL-15572 (2 microM; concentration 154 times higher than its Ki at h5-HT1D receptors) but was antagonized by SB-216641 (0.1 microM; concentration 100 times higher than its Ki at h5-HT1B receptors; apparent pA2 8.45). SB-216641 (0.1 microM) by itself facilitated, whereas BRL-15572 (2 microM) did not affect, the evoked overflow. In human cerebral cortex slices SB-216641 (0.1 microM) also facilitated, and BRL-15572 (2 microM) again failed to affect, the electrically evoked tritium overflow. In human cerebral cortical synaptosomes, 5-CT reduced the K+-evoked tritium overflow. This response was unaffected by BRL-15572 (300 nM) but antagonized by SB-216641 (15 nM; drug concentrations 23 and 15 times higher than their Ki at h5-HT1D and h5-HT1B receptors, respectively). Both drugs, given alone, did not modify the K+-evoked tritium overflow. In human atrial appendages, the electrically evoked tritium overflow was inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors) but not by SB-216641 (30 nM; 30 times Ki at h5-HT1B receptors). Both drugs by themselves did not change the electrically evoked tritium overflow. In conclusion, SB-216641 behaves as a preferential antagonist at native human 5-HT1B receptors and BRL-15572 as a preferential antagonist at native human 5-HT1D receptors. These compounds are clearly useful tools for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies.

SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.[Pubmed:9303567]

Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.

Despite only modest homology between h5-HT1B and h5-HT1D receptor amino acid sequences, these receptors display a remarkably similar pharmacology. To date there are few compounds which discriminate between these receptor subtypes and those with some degree of selectivity, such as ketanserin, have greater affinity for other 5-HT receptor subtypes. We now report on two compounds, SB-216641 (N-[3-(2-dimethylamino) ethoxy-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-(1,1'-biphen yl)-4-carboxamide) and BRL-15572 3-[4-(3-chlorophenyl) piperazin-1-yl]-1,1-diphenyl-2-propanol), which display high affinity and selectivity for h5-HT1B and h5-HT1D receptors, respectively. In receptor binding studies on human receptors expressed in CHO cells, SB-216641 has high affinity (pKi = 9.0) for h5-HT1B receptors and has 25-fold lower affinity at h5-HT1D receptors. In contrast, BRL-15572 has 60-fold higher affinity for h5-HT1D (pKi = 7.9) than 5-HT1B receptors. Similar affinities for these compounds were determined on native tissue 5-HT1B receptors in guinea-pig striatum. Functional activities of SB-216641 and BRL-15572 were measured in a [35S]GTPgammaS binding assay and in a cAMP accumulation assay on recombinant h5-HT1B and h5-HT1D receptors. Both compounds were partial agonists in these high receptor expression systems, with potencies and selectivities which correlated with their receptor binding affinities. In the cAMP accumulation assay, results from pK(B) measurements on the compounds again correlated with receptor binding affinities (SB-216641, pK(B) = 9.3 and 7.3; BRL-15572, pK(B) = <6 and 7.1, for h5-HT1B and h5-HT1D receptors respectively). These compounds will be useful pharmacological agents to characterise 5-HT1B and 5-HT1D receptor mediated responses.

Description

BRL-15572 2Hcl is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

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