Lu AE58054 Hydrochloride

A 5-HT6 receptor antagonist

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库存: 现货

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5mg

￥1975.00

1580.00

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10mg

￥3062.00

2450.00

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50mg

￥8100.00

6480.00

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200mg

￥18362.00

14690.00

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货号: ajci8166
CAS: 467458-02-2
别名: N-[2-(6-氟-1H-吲哚-3-基)乙基]-3-(2,2,3,3-四氟丙氧基)苄基胺单盐酸盐,Lu AE 58054 Hydrochloride
分子式: C20H20ClF5N2O
分子量: 434.83
纯度: >98%
溶解度: ≥ 21.74 mg/mL in DMSO, ≥ 51.2 mg/mL in EtOH, ≥ 3.83 mg/mL in Water with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist with Ki value of 0.83 nM [1].
The serotonin6 receptor (5-HT6R) is one of 14 known 5-HTRs in the serotonin receptor family [1]. It plays an important role in cognitive impairments associated with Alzheimer's disease and schizophrenia [2].
In the 5-HT(6) GTP gamma S efficacy assay, Lu AE58054 showed potent inhibition of 5-HT-mediated activation. Apart from medium affinity to adrenergic alpha (1B)- and alpha(1A)-adrenoreceptors, Lu AE58054 shows >50-fold selectivity compared with more than 70 targets examined [1].
In rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 with ED50 of 2.7 mg/kg. Administration of Lu AE58054 in a dose range (5–20 mg/kg) leading to above 65% 5-HT6R binding, which reversed cognitive impairment in rats treatment with phencyclidine. These results indicate that Lu AE58054 is a potent antagonist of 5-HT6Rs with good oral bioavailability in the rat model of cognitive impairment in schizophrenia [1].
参考文献:
[1]. Arnt J, Bang-Andersen B, Grayson B, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol, 2010, 13(8): 1021-1033.
[2]. Witten L, Bang-Andersen B, Nielsen SM, et al. Molecular and Cellular Pharmacology
Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo. Eur J Pharmacol, 2012, 676(1-3): 6-11.