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Chemical Structure| 193611-72-2 Chemical Structure| 193611-72-2

Structure of BRL-15572 2HCl
CAS No.: 193611-72-2

Chemical Structure| 193611-72-2

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BRL-15572 2HCl is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B and exhibiting little or no affinity for a range of other receptor types.

Synonyms: BRL 15572; BRL-15572 Dihydrochloride

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Product Details of BRL-15572 2HCl

CAS No. :193611-72-2
Formula : C25H29Cl3N2O
M.W : 479.87
SMILES Code : OC(CN1CCN(C2=CC=CC(Cl)=C2)CC1)C(C3=CC=CC=C3)C4=CC=CC=C4.[H]Cl.[H]Cl
Synonyms :
BRL 15572; BRL-15572 Dihydrochloride
MDL No. :MFCD02684402
InChI Key :WPEXRXMQMPOHIO-UHFFFAOYSA-N
Pubchem ID :9891303

Safety of BRL-15572 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of BRL-15572 2HCl

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human cerebral cortex synaptosomes 1 μM 8 min BRL-15572, as an h5-HT1D receptor ligand, completely prevented the inhibitory effect of 5-HT on K+-evoked glutamate overflow but had no effect on glutamate overflow when added alone. PMC1565844
Human temporal artery rings 500 nM at least 1 hour To investigate the antagonism of BRL-15572 on 5-HT-induced contractions, results showed BRL-15572 did not antagonize the effects of 5-HT. PMC1565520
Rat dural afferent neurons 1 μM 2 minutes To verify whether BRL-15572 blocks the inhibition of voltage-gated calcium currents by sumatriptan. Results showed that BRL-15572 significantly reduced the sumatriptan-induced inhibition of calcium currents. PMC3583198
Human small muscular pulmonary arteries 0.5 μM BRL15572 (5-HT1D-selective antagonist) did not inhibit sumatriptan-induced contractions, indicating 5-HT1B receptor mediates vasoconstriction PMC1571682
Mouse dural CGRP nociceptive fibre terminations 10 nM BRL-15572, as a selective 5-HT1D antagonist, prevented sumatriptan-induced inhibition of action potential-evoked Ca2+ transient amplitude PMC3399992
Rat thoracic aorta rings 1 µM 20 minutes To investigate the effect of BRL 15572 on lerimazoline-induced contractions, results showed BRL 15572 did not significantly inhibit lerimazoline-induced contractions PMC5581967

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat CFA-induced inflammatory pain model Slice superfusion 3 μM 6 minutes BRL-15572, as a 5-HT1D receptor antagonist, blocked the sumatriptan-induced inhibition of evoked EPSCs in CFA-injected juvenile rats. PMC7393196
Pigs Pentobarbitone-anaesthetized, bilaterally vagosympathectomized pigs Intravenous 1 mg/kg Single dose Investigate the role of BRL15572 in sumatriptan-induced constriction of porcine carotid arteriovenous anastomoses. Results showed that BRL15572 (1 mg/kg) did not affect the sumatriptan-induced constriction, indicating that 5-HT1D receptors are not involved in this process. PMC1566041

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.42mL

2.08mL

1.04mL

20.84mL

4.17mL

2.08mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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