Idalopirdine Hydrochloride

Research use only, not for human use.

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).(In Vitro):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.(In Vivo):In the rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 (ED50: 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.

Lu AE58054 Hydrochloride; Idalopirdine hydrochloride; Idalopirdine HCl

Endocrinology/Hormones

5-HT Receptor

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467458-02-2

434.8

C20H20ClF5N2O

>98% (HPLC)

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Cl.FC(F)C(F)(F)COc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1

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(-20℃)

With Ice Pack

≥ 2 years