1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. BRL 54443

BRL 54443 

Cat. No.: HY-13221 Purity: 99.39%
Handling Instructions

BRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.

For research use only. We do not sell to patients.

BRL 54443 Chemical Structure

BRL 54443 Chemical Structure

CAS No. : 57477-39-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
10 mg USD 92 In-stock
Estimated Time of Arrival: December 31
50 mg USD 378 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

BRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors[1].

IC50 & Target[1]

5-HT1E Receptor

1.1 nM (Ki)

5-HT1F Receptor

0.7 nM (Ki)

5-HT1A Receptor

63 nM (Ki)

5-HT1B Receptor

126 nM (Ki)

5-HT1D Receptor

63 nM (Ki)

5-HT2A Receptor

1259 nM (Ki)

5-HT2B Receptor

100 nM (Ki)

5-HT2C Receptor

316 nM (Ki)

5-HT6 Receptor

>10,000 nM (Ki)

5-HT7 Receptor

>10,000 nM (Ki)

In Vitro

Despite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors[1].
In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50=14 nM). BRL 54443 also induces contraction (-log EC50=6.52)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

230.31

Formula

C₁₄H₁₈N₂O

CAS No.

57477-39-1

SMILES

OC1=CC2=C(NC=C2C3CCN(C)CC3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (434.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3420 mL 21.7099 mL 43.4197 mL
5 mM 0.8684 mL 4.3420 mL 8.6839 mL
10 mM 0.4342 mL 2.1710 mL 4.3420 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BRL 54443BRL54443BRL-544435-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
BRL 54443
Cat. No.:
HY-13221
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