| Name | Idalopirdine Hydrochloride |
| Description | Idalopirdine Hydrochloride (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[1]. |
| 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[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 50 mg/mL (114.99 mM)
DMSO : 20 mg/mL (45.99 mM)
H2O : 3 mg/mL (6.90 mM, with ultrasonic and warming), Sonication and heating are recommended.
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| Keywords | Serotonin Receptor | Lu AE58054 | inhibit | 5-hydroxytryptamine Receptor | Lu AE-58054 Hydrochloride | 5-HT Receptor | Lu AE-58054 | Lu AE 58054 Hydrochloride | Lu AE 58054 | Idalopirdine | Inhibitor | Idalopirdine Hydrochloride |
| Inhibitors Related | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
