Quetiapine fumarate

Description

Quetiapine hemifumarate (111974-72-2) is an atypical antipsychotic agent. Antagonist at serotonin (5-HT2) and dopamine (D2) receptors, IC50s=148 and 329 nM respectively. Reverses depressive-like behavior and reduces DNA methyltransferase activity induced by maternal deprivation in a rat model. Efficacious as a monotherapy in the treatment of posttraumatic stress disorder.

Chemical properties

White Crystalline Solid

The Uses of Quetiapine fumarate

Used as an antipsychotic.  Quetiapine fumarate is a psychotropic agent belonging to a chemical class, the dibenzothiazepine derivatives. It is present in tablets as the fumarate salt. It's activity is primarily due to the parent drug. Quetiapine has affinity for D2, 5-HT2A, H1, alpha 1 and 5-HT1A receptors.

The Uses of Quetiapine fumarate

antihypertensive adrenergic receptor blocking agent with selective alpha1- and nonselective beta-adrenergic receptor blocking actions in a single substance.

The Uses of Quetiapine fumarate

Quetiapine hemifumarate salt has been used as an antagonist for β-arrestin 2 mutant T205M recruitment.

brand name

Seroquel (AstraZeneca).

General Description

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

Hazard

Human systemic effects.

Biochem/physiol Actions

Quetiapine hemifumarate is an atypical antipsychotic, a combined serotonin (5HT2) and dopamine (D2) receptor antagonist.

in vitro

quetiapine has shown affinity for various neurotransmitter receptorsincluding dopamine, serotonin, histamine, and adrenergicreceptors, quetiapine exihibited binding characteristics at the dopamine-2receptorsimilar to those of clozapine [1].

in vivo

in animal models, quetiapine exihibited a preclinical profile suggestive of antipsychotic activity with a reduced tendency to cause extrapyramidal symptoms (eps) and sustained prolactin elevation. quetiapine altered neurotensin neurotransmission and c-fos expression in limbic but not motor brain regions.in humans, quetiapine exhibited linear pharmacokinetics with a mean terminal half-life of 7 hours.the optimal dosing range for quetiapine was 150 to 750 mg/day, and recent results suggested that once-daily dosing might be suitable for some patients [1].quetiapine prevented schizophrenia and depression in hippocampal cell proliferation and bdnf expression caused by chronic restraint stress (crs) in rats in a dose-dependent manner. quetiapine (5 mg/kg) in combination with venlafaxine (2.5 mg/kg) increaseed hippocampal cell proliferation and prevented bdnf decrease in stressed rats, while each of the drugs exerted mild or no effects [2].in rats subjected to chronic-restraint stress, chronic administration of quetiapine attenuated the decrease in levels of brain-derived neurotrophic factor (bdnf) in the hippocampi. the stress-induced suppression of hippocampal neurogenesis was reversed after post-stress administration of quetiapine (10 mg/kg) for 7 or 21 days, evidenced in the numbers of pcreb-positive and brdu-labeled cells that were comparable to those in non-stressed rats but higher than those in the vehicle-treated rats [3].

storage

+4°C

References

1) Ellenbroek et al. (1996); Activity of “seroquel” (ICI 204,636) in animal models for atypical properties of antipsychotics: a comparison with clozapine; Neuropsychopharmacology 15 406 2) Saller and Salama (1993), Seroquel: biochemical profile of a potential atypical antipsychotic; Psychopharmacolgy (Berl) 112 285 3) Ignacio et al. (2017), Quetiapine treatment reverses depressive-like behavior and reduces DNA methyltransferase activity induced by maternal deprivation; Behav. Brain Res. 320 225 4) Villarreal et al. (2016), Efficacy of Quetiapine Monotherapy in Posttraumatic Stress Disorder: A Randomized, Placebo-Controlled Trial; Am. J. Psychiatry 173 1205