BRL-15572 Dihydrochloride - Moligand™, 10mM in DMSO , Agonist of 5-HT 1A receptor;Agonist of 5-HT 1B receptor;Agonist of 5-HT 1D receptor;Agonist of 5-ht 1e receptor;Agonist of 5-HT 1F receptor;Agonist of 5-HT 2A receptor;Agonist of 5-HT 2B receptor;Agoni, Agonist of 5-HT 1A receptor;Agonist of 5-HT 1B receptor;Agonist of 5-HT 1D receptor;Agonist of 5-ht 1e receptor;Agonist of 5-HT 1F receptor;Agonist of 5-HT 2A receptor;Agonist of 5-HT 2B receptor;Agonist of 5-HT 2C receptor;Agonist of 5-HT 6 receptor

CAS: 193611-72-2 Cat. No.: B408254 Molecular Weight: 479.87 PubChem CID: 9891303

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

3-(4-(3-chlorophenyl)piperazin-1-yl)-1,1-diphenylpropan-2-ol dihydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

BRL-15572 is a5-HT1Dreceptor antagonist withpKiof 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
In vitro

BRL-15572 displays high affinity and selectivity for h5-HT_1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT_1D than 5-HT_1B receptors. BRL-15572 binds to h5-HT_1B and h5-HT_1D 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-HT_1B and h5-HT_1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT_1A, 5-HT_1B, 5-HT_1E, 5-HT_1F, 5-HT_2A, 5-HT_2B, 5-HT_2C, 5-HT₆ and 5-HT₇ with pK_i of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT_1D cell line, both BRL-15572 (1 µM) shifts the 5-HT concentration response curve with pK_B of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT_1A and 5-HT_2B receptors. 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). The inhibitory effect of 5-HT on the K⁺-evoked overflow of glutamate is antagonized by the h5-HT_1D 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. The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247.

In vivo

In diabetic pithed rats, administration of the selective 5-HT_1D 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-HT_1B and 5-HT_1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572.
Cell Data

cell lines：

Concentrations：0 μM -10 μM

Incubation Time：30 minutes

Powder Purity:≥99%

Specifications

Synonyms

3-(4-(3-chlorophenyl)piperazin-1-yl)-1, 1-diphenylpropan-2-ol dihydrochloride

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST

Mechanism of action

Agonist of 5-HT 1A receptor;Agonist of 5-HT 1B receptor;Agonist of 5-HT 1D receptor;Agonist of 5-ht 1e receptor;Agonist of 5-HT 1F receptor;Agonist of 5-HT 2A receptor;Agonist of 5-HT 2B receptor;Agonist of 5-HT 2C receptor;Agonist of 5-HT 6 receptor

Names and Identifiers

• Isomeric SMILES: C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl
• Alternate CAS: 734517-40-9
• PubChem CID: 9891303
• Molecular Weight: 479.87

Associated Targets(Human)

HTR1B Tclin 5-hydroxytryptamine receptor 1B (1 Activities)

Discover Target: HTR1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A (1 Activities)

Discover Target: HTR2A

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HTR1E Tchem 5-hydroxytryptamine receptor 1E (1 Activities)

Discover Target: HTR1E

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HTR1D Tclin 5-hydroxytryptamine receptor 1D (1 Activities)

Discover Target: HTR1D

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HTR1F Tclin 5-hydroxytryptamine receptor 1F (1 Activities)

Discover Target: HTR1F

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HTR2C Tclin 5-hydroxytryptamine receptor 2C (1 Activities)

Discover Target: HTR2C

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HTR1A Tclin 5-hydroxytryptamine receptor 1A (1 Activities)

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR6 Tchem 5-hydroxytryptamine receptor 6 (1 Activities)

Discover Target: HTR6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B (1 Activities)

Discover Target: HTR2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 37 mg/mL (199.76 mM); Water: 37 mg/mL (199.76 mM); Ethanol: 37 mg/mL (199.76 mM)