Idalopirdine Hydrochloride 是一种选择性的5-HT6 受体拮抗剂，Ki为 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 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 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[1].

467458-02-2

C20H20ClF5N2O

434.83

Lu AE58054 Hydrochloride;Lu AE58054盐酸盐;Idalopirdine HCl

H2O:3 mg/mL(6.90 mM, with ultrasonic and warming),with ultrasonic and warming
DMSO:20 mg/mL(45.99 mM)
Ethanol:50 mg/mL(114.99 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years