表单
solid
技术
HPLC: suitable
gas chromatography (GC): suitable
颜色
pale yellow
溶解性
ethanol: 11 mg/mL
0.1 M HCl: 30 mg/mL
DMSO: 4.8 mg/mL
包装形式
neat
SMILES字符串
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
基因信息
human ... DRD2(1813) , HTR2A(3356)
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应用
Refer to the product′s Certificate of Analysis for more information on a suitable instrument technique. Contact Technical Service for further support.
生化/生理作用
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。
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
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
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
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
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
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