Drug intelligence / Profile preview

norquetiapine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
01

Overview

Norquetiapine is the major active metabolite of quetiapine, an atypical antipsychotic. It exhibits a distinctive pharmacological profile and is thought to contribute to the antidepressant and anxiolytic effects of quetiapine treatment. Mechanistically, norquetiapine acts as a potent inhibitor of the noradrenaline transporter (NET), a partial agonist at 5-HT1A (serotonin) receptors, and an antagonist at presynaptic alpha-2 adrenergic, 5-HT2C, and 5-HT7 receptors. It is also an antagonist at histamine H1, alpha-1 adrenergic, and muscarinic receptors. This broad spectrum of receptor affinities confers norquetiapine an antidepressant and anxiolytic pharmacological profile that is distinct from its parent compound[1][4].

Other names
N-desalkylquetiapine
02

Targets

HTR7 (5-hydroxytryptamine receptor 7)mAChR (Muscarinic acetylcholine receptors)ADRA2A (α2A)HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA1A (α1A)HTR2C (5-hydroxytryptamine 2C receptor)

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