Formulation: A solid
Formal Name: 11-(1-piperazinyl)-dibenzo[b,f][1,4]thiazepine
Purity: ≥98%
Formula Markup: C17H17N3S
Formula Weight: 295,4
Shelf life (days): 1460
CAS Number: 5747-48-8
Notes: Norquetiapine is an active metabolite of the atypical antipsychotic quetiapine (Item No. 14152).{62735} It is formed from quetiapine primarily by the cytochrome P450 (CYP) isoform CYP3A4. Norquetiapine selectively inhibits the norepinephrine transporter (NET; IC50 = 12 nM) over the serotonin (5-HT) and dopamine transporters (SERT and DAT; IC50s = 988 and >10,000 nM, respectively). It binds to the histamine H1 receptor (Ki = 3.5 nM), as well as the 5-HT receptor subtypes 5-HT1, 5-HT2, and 5-HT7 (Kis = 45-1,117 nM). It also binds to α1- and α2-adrenergic, dopamine D1-D5, and M1-M5 muscarinic receptors (Kis = 95-736, 196-1,419, and 23-453 nM, respectively). It acts as an antagonist at histamine H1, α1A- and α1D-adrenergic, as well as M1, M3, and M5 muscarinic receptors, in a concentration-dependent manner and as an agonist at the 5-HT1A receptor (EC50 = 4,898 nM). Norquetiapine (0.1, 0.5, and 1 mg/kg) reduces increases in immobility time in mice heterozygous for the gene encoding vesicular monoamine transporter 2 (Vmat2) but not in wild-type mice.
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