A 5-HT6 receptor antagonist
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Lu AE58054

Item No. 27335

Technical Information
Formal Name
6-fluoro-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]-1H-indole-3-ethanamine
CAS Number
467459-31-0
Molecular Formula
C20H19F5N2O
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
218, 279 nm
SMILES
FC(F)C(F)(F)COC1=CC(CNCCC2=CNC3=C2C=CC(F)=C3)=CC=C1
InChi Code
InChI=1S/C20H19F5N2O/c21-15-4-5-17-14(11-27-18(17)9-15)6-7-26-10-13-2-1-3-16(8-13)28-12-20(24,25)19(22)23/h1-5,8-9,11,19,26-27H,6-7,10,12H2
InChi Key
YBAWYTYNMZWMMJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).1 It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine (Item No. 14270), LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Arnt, J., Bang-Andersen, B., Grayson, B., et alLu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int. J. Neuropsychopharmacol. 13(8), 1021-1033 (2010).

    2. Cherian, A.K., Kucinski, A., Wu, R., et alCo-treatment with rivastigmine and idalopirdine reduces the propensity for falls in a rat model of falls in Parkinson’s disease. Psychopharmacology (Berl) 236(6), 1701-1715 (2019).