YL-0919 inhibits the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells with IC50 values of 1.78±0.34 nM and 1.93±0.18 nM, respectively.
|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|
The role of activation of the 5-HT1A receptor and adenylate cyclase in the antidepressant-like effect of YL-0919, a dual 5-HT1A agonist and selective serotonin reuptake inhibitor.
Qin JJ, et al. Neurosci Lett. 2014 Oct 17;582:104-8. PMID: 25220701.
Antidepressant-like activity of YL-0919: a novel combined selective serotonin reuptake inhibitor and 5-HT1A receptor agonist.
Chen HX, et al. PLoS One. 2013 Dec 18;8(12):e83271. PMID: 24367588.
|Related 5-HT Receptor Products|
8-OH-DPAT (8-Hydroxy-DPAT) is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A.
Idalopirdine hydrochloride is a potent and selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM.
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.
GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
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