An active metabolite of quetiapine
货号:ajcx26620
CAS:5747-48-8
分子式:C17H17N3S
分子量：295.4
溶解度:DMF: 16 mg/mL,DMSO: 3 mg/mL,Ethanol: 5 mg/mL,PBS (pH 7.2): 0.25 mg/mL
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Norquetiapine is an active metabolite of the atypical antipsychotic quetiapine .¹It 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 H₁receptor (K_i= 3.5 nM), as well as the 5-HT receptor subtypes 5-HT₁, 5-HT₂, and 5-HT₇(K_is = 45-1,117 nM). It also binds to α₁- and α₂-adrenergic, dopamine D₁-D₅, and M₁-M₅muscarinic receptors (K_is = 95-736, 196-1,419, and 23-453 nM, respectively). It acts as an antagonist at histamine H₁, α_1A- and α_1D-adrenergic, as well as M₁, M₃, and M₅muscarinic receptors, in a concentration-dependent manner and as an agonist at the 5-HT_1Areceptor (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.

1.Jensen, N.H., Rodriguiz, R.M., Caron, M.G., et al.N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine’s antidepressant activityNeuropsychopharmacology33(10)2303-2312(2008)