Home Neuronal Signaling 5-HT Receptor antagonist BRL-15572 Dihydrochloride

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BRL-15572 Dihydrochloride 5-HT Receptor antagonist

Cat.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.
BRL-15572 Dihydrochloride 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 479.87

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Quality Control

Batch: S267701 DMSO]96 mg/mL]false]Ethanol]40 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Chemical Information, Storage & Stability

Molecular Weight 479.87 Formula

C25H27ClN2O.2HCl

 Storage (From the date of receipt)
CAS No. 193611-72-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 96 mg/mL ( (200.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 40 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Features
A selective 5-HT1D/1B receptor antagonist.
Targets/IC50/Ki
5-HT1D [1]
7.9(pKi)
5-HT1A [1]
7.7(pKi)
5-HT2B [1]
7.4(pKi)
5-HT2A [1]
6.6(pKi)
5-HT7 [1]
6.3(pKi)
5-HT2C [1]
6.2(pKi)
5-HT1B [1]
6.1(pKi)
5-HT1F [1]
6(pKi)
5-HT6 [1]
5.9(pKi)
5-HT1E [1]
5.2(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]
References
  • https://pubmed.ncbi.nlm.nih.gov/16173953/
  • https://pubmed.ncbi.nlm.nih.gov/17880377/
  • https://pubmed.ncbi.nlm.nih.gov/15224175/

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