form
solid
technique(s)
HPLC: suitable, gas chromatography (GC): suitable
color
pale yellow
solubility
ethanol: 11 mg/mL, 0.1 M HCl: 30 mg/mL, DMSO: 4.8 mg/mL
format
neat
SMILES string
CN1CCN(CC1)C2=Nc3cc(Cl)ccc3Nc4ccccc24
InChI
1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
InChI key
QZUDBNBUXVUHMW-UHFFFAOYSA-N
Gene Information
human ... DRD2(1813), HTR2A(3356)
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Application
Refer to the product′s Certificate of Analysis for more information on a suitable instrument technique. Contact Technical Service for further support.
Biochem/physiol Actions
非典型抗精神病药,对 D4 多巴胺受体比对 D2 或 D3 多巴胺受体表现出更大的亲和性;在用典型抗精神病药无效的患者中,对精神分裂症的阳性和阴性症状均表现出抗精神病疗效。
法规信息
新产品
此项目有
Henry F Vischer et al.
Bioorganic & medicinal chemistry, 18(2), 675-688 (2009-12-25)
Human cytomegalovirus (HCMV) is a widespread human pathogen, possessing onco-modulatory properties. Constitutive signaling of the HCMV-encoded chemokine receptor US28 and its ability to bind a broad spectrum of chemokines might facilitate HCMV-associated tumor progression. Novel nonpeptidergic chemotypes were identified as
Stefania Butini et al.
Journal of medicinal chemistry, 52(1), 151-169 (2008-12-17)
Dopamine D(3) antagonism combined with serotonin 5-HT(1A) and 5-HT(2A) receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D(3), serotonin 5-HT(1A) and 5-HT(2A) receptors, together with
Rogier A Smits et al.
Journal of medicinal chemistry, 49(15), 4512-4516 (2006-07-21)
A series of dibenzodiazepine derivatives was synthesized to probe the binding site of the recently discovered histamine H4 receptor (H4R). Optimization of the lead structure clozapine (2) resulted in (E)-7-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine (7j), a potent H4R agonist (H4R, pKi = 7.6). Pharmacological
Tarek K Rajji et al.
The American journal of psychiatry, 172(6), 579-585 (2015-04-11)
Clozapine's potent antagonism of muscarinic M1 receptors is thought to worsen working memory deficits associated with schizophrenia. In contrast, its major metabolite, N-desmethylclozapine (NDMC), is thought to enhance working memory via its M1 receptor agonist activity. The authors hypothesized that
Enade P Istyastono et al.
Journal of medicinal chemistry, 54(23), 8136-8147 (2011-10-19)
The histamine H(4) receptor (H(4)R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H(3) receptor (H(3)R), two acidic residues in the H(4)R binding pocket, D(3.32) and E(5.46), act as essential
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