Idalopirdine hydrochloride displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. In vivo, orally administered Idalopirdine hcl potently inhibited striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157, with an ED(50) of 2.7 mg/kg.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 20 mg/mL|
Characterization of [³H]Lu AE60157 ([³H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine₆ (5-HT₆) receptors in vivo.
Witten L, et al. Eur J Pharmacol. 2012 Feb 15;676(1-3):6-11. PMID: 22155399.
Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats.
Arnt J, et al. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33. PMID: 20569520.
|Related 5-HT Receptor Products|
LY344864 is a selective 5-HT1F receptor agonist with an affinity of 6 nM (Ki).
YL-0919 is a novel 5-HT1A receptor agonist and selective serotonin reuptake inhibitor.
8-OH-DPAT (8-Hydroxy-DPAT) is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A.
PRX-08066 is a a novel 5-hydroxytryptamine receptor 2B antagonist with IC50 of 3.4 nM.
MIN-101 (Roluperidone) is a novel compound with affinities for 5-HT2A and sigma-2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.