A potent agonist of 5-HT1E and 5-HT1F
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BRL 54443

Item No. 21263

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1-methyl-4-piperidinyl)-1H-indol-5-ol
CAS Number
57477-39-1
Molecular Formula
C14H18N2O
Formula Weight
230.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12.5 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mLEthanol: 1.4 mg/mL
λmax
278 nm
SMILES
OC1=CC=C2C(C(C3CCN(C)CC3)=CN2)=C1
InChi Code
InChI=1S/C14H18N2O/c1-16-6-4-10(5-7-16)13-9-15-14-3-2-11(17)8-12(13)14/h2-3,8-10,15,17H,4-7H2,1H3
InChi Key
WKNFADCGOAHBPG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    10 mg

    $98

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    25 mg

    $229

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    50 mg

    $423

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    Product Description

    BRL 54443 is a potent agonist of the serotonin (5-HT) receptor subtypes 5-HT1E and 5-HT1F (Ki values are 1.1 and 0.7 nM, respectively).1 It displays more than 30-fold selectivity over other 5-HT and dopamine receptors. At higher concentrations, BRL 54443 induces 5-HT2A-mediated contraction of mouse thoracic aorta strips in vitro (pEC50 = 6.5).2 It significantly reduces formalin-induced pain in rat hind paw.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Klein, M.T., Dukat, M., Glennon, R.A., et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: A comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J. Pharmacol. Exp. Ther. 337(3), 860-867 (2011).

    2. McKune, C.M., and Watts, S.W. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J. Pharmacol. Exp. Ther. 297(1), 88-95 (2001).

    3. Granados-Soto, V., Argüelles, C.F., Rocha-González, H.I., et al. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats. Neuroscience 165(2), 561-568 (2010).