Quetiapine Fumarate (Seroquel XR; IC-204,636; ICI204,636; ICI-204636), the fumarate salt of Quetiapine, is an atypical antipsychotic drug used for the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression. It acts as a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor,
理化性质和储存条件
| Molecular Weight (MW) | 883.09 |
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| Formula | C46H54N6O8S2 |
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| CAS No. | 111974-72-2 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 36 mg/mL (40.8 mM) |
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| Water: <1 mg/mL |
| Ethanol: <1 mg/mL |
| Solubility (In vivo) | 0.5% CMC Na: 30mg/mL |
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| Synonyms | ICI-204636; ICI 204,636; ICI 204636; ICI204636; Quetiapine Fumarate; Quetiapine hemifumarate; Seroquel XR; IC-204,636; ICI204,636; ICI-204636. |
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实验参考方法
| In Vitro | In vitro activity: Quetiapine shows affinity for various neurotransmitter receptors including serotonin, dopamine, histamine, and adrenergic receptors and has binding characteristics at the dopamine-2 receptor similar to those of clozapine. |
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| In Vivo | Quetiapine has a preclinical profile suggestive of antipsychotic activity with a reduced tendency to cause extrapyramidal symptoms (EPS) and sustained prolactin elevation. Guetiapine alters neurotensin neurotransmission and c-fos expression in limbic but not motor brain regions. Quetiapine also demonstrates clozapine-like activity in a range of behavioral and biochemical tests and may possess neuroprotective properties. Quetiapine dose-dependently prevents schizophrenia and depression in hippocampal cell proliferation and BDNF expression caused by chronic restraint stress (CRS) in rats. Guetiapine (5 mg/kg) combined with Venlafaxine (2.5 mg/kg) increases hippocampal cell proliferation and prevents BDNF decrease in stressed rats, whereas each of the drugs exerts mild or no effects. Guetiapine produces selective effects on cortical and limbic regions of the brain and in particular on dopaminergic neurotransmission in these regions. Guetiapine produces lower levels of putamenal DA D2r occupancy than those reported for typical APDs. Quetiapine also produces preferential occupancy of temporal cortical DA D2r, 46.9%, but does not spare occupancy of substantia nigra DA D2r. Guetiapine attenuates the decrease in levels of brain-derived neurotrophic factor (BDNF) in the hippocampi of rats subjected to chronic-restraint stress. Guetiapine (10 mg/kg) reverses the stress-induced suppression of hippocampal neurogenesis, evidenced in the numbers of BrdU-labeled and pCREB-positive cells that are comparable to those in non-stressed rats but higher than those in the vehicle-treated rats. |
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| Animal model | Rats |
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| Formulation & Dosage | 5, 10 mg/kg |
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| References | J Clin Psychiatry. 2002;63 Suppl 13:5-11; Hippocampus. 2006;16(6):551-9. |
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