Idalopirdine Hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lu AE58054 盐酸盐是一种 5-HT(6)R 拮抗剂的体内结合亲和力和效应、体外选择性和效力 (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.

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Idalopirdine (intraperitoneal injection, 5?mg/kg, daily, 28 days) Hydrochloride can reduce food intake and body weight in over-eating rat models.Idalopirdine (1 or 2?mg/kg, i.v) Hydrochloride can dose-dependently increase the gamma power during nPO electrical stimulation, enhance effect of donepezil on cortical gamma oscillations but no alteration of sleep-wake patterns in rats. Animal Model:Male Wistar rats Dosage:5?mg/kg Administration:intraperitoneal injection, daily, 28 days Result:Significantly reduced the amount of calories consumed by animals in a palatable diet and significantly reduced plasma levels of glucose, triglycerides and cholesterol.Animal Model:Male Sprague-Dawley rats Dosage:1 or 2?mg/kg Administration:i.v.Result:No significant increase in the gamma power at 1 mg/kg and significantly increased the gamma power at 2 mg/kg.Significantly enhanced and/or prolonged effect of low-dose donepezil (0.3 mg/kg) on gamma power during 60-minute nPO stimulation after donepezil administration.

Lu AE58054 Hydrochloride | Idalopirdine hydrochloride | Idalopirdine HCl

Endocrinology/Hormones

5-HT Receptor

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467458-02-2

434.84

C20H20ClF5N2O

>98% (HPLC)

In Vitro:?DMSO : ≥ 25 mg/mL (57.49 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years