Quetiapine fumarate Inhibitor CAS No. 111974-72-2

Product Name	Quetiapine fumarate
Synonyms	Seroquel, ICI 204,636, quetiapine XR
CAS No.	111974-72-2
Molecular Weight	883.09
Formula	C₄₆H₅₄N₆O₈S₂
Chemical Structure

Biological activities

Quetiapine fumarate is a fumarate of quetiapine. Quetiapine is a novel antipsychotic drug and is used for treatment of schizophrenia, bipolar disorder, and major depressive disorder. Quetiapine exhibits high affinity for brain serotonin (5-HT_{2) and dopamine (DA) D-2 receptors with IC50 of 148 and 329 nM, respectively. Quetiapine markedly exhibits lower affinity for DA D-1 receptors with an IC50 of 1.2 µM. In cell population studies, acute treatment with quetiapine selectively increases the number of spontaneously active A10 DA cells.^[1] Quetiapine possesses some affinity for α_{1, α_{2 and 5-HT_{1A receptors with IC50 of 90, 270 and 720 nM, respectively. ^[2] Quetiapine exhibits the greatest degree of selectivity in reversing the actions of amphetamine at lower doses in A10 with an ED50 of 0.6 mg/kg, whereas it is 3 mg/kg in A9. ^[1] Acute administration of quetiapine is shown to suppress tacrine-induced tremulous jaw movements with an ED_{50 of 7.22 mg/kg. ^[3]}}}}}

Protocols

Quetiapine is dissolved in 0.1% (v/v) hydroxyproylmethylcellulose, 0.1% (v/v) Tween 80 in distilled water. ^[2]

References

[1] Swerdlow NR, et al. Seroquel restores sensorimotor gating in phencyclidine- treated rats. J Pharmacol Exp Ther. 1996, 279(3): 1290-1299. 閵嗏偓閵嗏偓 [2] Saller CF, et al. Seroquel: biochemical profile of a potential atypical antipsychotic. Psychopharmacology (Berl). 1993, 112(2-3): 285-292. 閵嗏偓閵嗏偓 [3] Betz A, et al. Quetiapine (Seroquel) shows a pattern of behavioral effects similar to the atypical antipsychotics clozapine and olanzapine: studies with tremulous jaw movements in rats. Psychopharmacology (Berl). 2005, 179(2): 383-392. 閵嗏偓閵嗏偓

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