Catalog No.S2677

BRL-15572 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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BRL-15572 Chemical Structure

BRL-15572 Chemical Structure
Molecular Weight: 479.87

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

BRL-15572 is available in the following compound libraries:

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description BRL-15572 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.
Targets 5-HT1D [1] 5-HT1A [1] 5-HT2B [1] 5-HT2A [1]

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IC50 7.9(pKi) 7.7(pKi) 7.4(pKi) 6.6(pKi)
In vitro BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 µM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4]
In vivo In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572. [5]
Features A selective 5-HT1D/1B receptor antagonist.

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines CHO cells expressing the h5-HT1B or h5-HT1D receptors
Concentrations 0 μM -10 μM
Incubation Time 30 minutes
Method [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 µ M), with or without BRL-15572. The reaction is started by the addition of 10 µL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Non-specific binding is determined by addition of unlabelled GTPγS (10 µM), prior to the addition of cells. The reaction is stopped by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Radioactivity is determined by liquid scintillation spectrometry.

Animal Study: [5]

Animal Models Male Wistar rats with diabetes
Formulation 20% propylene glycol
Dosages 1 mg/kg, 2 mg/kg
Administration Administered via i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Price GW, et al. Naunyn Schmiedebergs Arch Pharmacol. 1997, 356(3), 312-320.

[2] Schlicker E, et al. Naunyn Schmiedebergs Arch Pharmacol. 1997, 356(3), 321-327.

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Chemical Information

Download BRL-15572 SDF
Molecular Weight (MW) 479.87


CAS No. 193611-72-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 96 mg/mL (200.05 mM)
Ethanol 40 mg/mL (83.35 mM)
Water <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 20 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3-(4-(3-chlorophenyl)piperazin-1-yl)-1,1-diphenylpropan-2-ol dihydrochloride

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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