BRL 54443

Name: BRL 54443
Brand: Tocris Bioscience
SKU: 1129

Tocris Bioscience a Bio-Techne Brand

Catalog # 1129

Citations (2)

COA / SDS

Discontinued Product

1129 has been discontinued. View all 5-HT1E Receptor Agonists products.

Key Product Details

Description:	Potent 5-ht1E and 5-HT1F agonist
Chemical Name:	5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
Molecular Weight:	230.31

View Full Technical Details for BRL 54443

Biological Activity for BRL 54443

BRL 54443 is a potent 5-ht_1E/1F receptor agonist (pEC₅₀ values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pK_i values are 8.7. 8.9, 7.2, 6.9, 7.2, 5.9, 7.0, 6.5, 1E, _1F, _1A, _1B, _1D, _2A, _2B, _2C, ₄, ₇, D₂ and D₃ receptors respectively). Induces 5-HT_2A receptor-mediated mouse aortic contraction in vitro (pEC₅₀ = 6.52). Active in vivo.

Technical Data for BRL 54443

M. Wt	230.31
Formula	C₁₄H₁₈N₂O
Storage	Desiccate at +4°C
CAS Number	57477-39-1
PubChem ID	2438
InChi Key	WKNFADCGOAHBPG-UHFFFAOYSA-N
Smiles	CN1CCC(CC1)C1=CNC2=CC=C(O)C=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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References for BRL 54443

References are publications that support the biological activity of the product.

McKune and Watt Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J.Pharmacol.Exp.Ther. 2001 PMID: 11259531
Brown BRL 54443, a potent agonist with selectivity for human cloned 5-HT_1E and 5-HT_1F receptors. Br.J.Pharmacol.
Lightowler Effect of BRL 54443 (3-(1-methylpiperidin-4-yl)-1H-indol-5-ol), a 5-HT_1E/1F receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. Br.J.Pharmacol.

Citations for BRL 54443 (2)

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Citations are publications that use Bio-Techne products. Selected citations for BRL 54443 include:

Klein et al. (2011) Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. Br J Pharmacol. 337:860
PMID: 21422162
Müller et al. (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One. 4:e6453
PMID: 19649285

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Product Documents for BRL 54443

COA

Certificate of Analysis

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