Bioactivity | Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1]. |
Invitro | Quetiapine (<100 μM; 24 hours) has no significant effect on cell viabilities[2].Quetiapine (10 μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner[2]. Quetiapine (10 μM) also inhibits TNF-α synthesis[2]. Cell Viability Assay[2] Cell Line: |
In Vivo | Quetiapine (10 mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination[1]. Animal Model: |
Name | Quetiapine hemifumarate |
CAS | 111974-72-2 |
Formula | C23H27N3O4S |
Molar Mass | 441.54 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Cross AJ, et al. Quetiapine and its metabolite norquetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models. Br J Pharmacol. 2016 Jan;173(1):155-66. [2]. Hanzhi Wang, et al. Quetiapine Inhibits Microglial Activation by Neutralizing Abnormal STIM1-Mediated Intercellular Calcium Homeostasis and Promotes Myelin Repair in a Cuprizone-Induced Mouse Model of Demyelination. Front Cell Neurosci. 2015 Dec 21;9:492. |