所有图片(1)
别名:
Cyclopropyl (4-[3-(1H-imidazol-4-yl)propyloxy]phenyl) ketone maleate salt, FUB 359 maleate salt
经验公式（希尔记法）:
C16H18N2O2 · C4H4O4
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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 32 mg/mL
H2O: insoluble
SMILES字符串
OC(=O)\C=C/C(O)=O.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2
InChI
1S/C16H18N2O2.C4H4O4/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14;5-3(6)1-2-4(7)8/h5-8,10-12H,1-4,9H2,(H,17,18);1-2H,(H,5,6)(H,7,8)/b;2-1-
InChI key
RLQFKEYRALXXEJ-BTJKTKAUSA-N
应用
Ciproxifan maleate has been used as a selective H3R antagonist to investigate the antidepressant potential of ciproxifan in chronic unpredictable stress (CUS) model of depression in mice. It has also been used as an H3R antagonist to develop in vivo receptor occupancy assay for histamine H3 receptors (H3R)/to determine the occupancy of exogenous H3R antagonists using non-radiolabeled GSK189254 as a tracer in the rat.
生化/生理作用
Cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone (Ciproxifan) is a species-specific histamine H3 receptor (H3R) inverse agonist. It is mainly used as a reference H3R antagonist in rodent models for neurological diseases, Alzheimer′s disease, attention deficit hyperactivity disorder (ADHD), and sleep-wake disorders. It can block monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) enzyme isoforms reversibly in humans and rats.
Potent, selective H3 histamine receptor antagonist.
特点和优势
This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语：
Warning
危险分类
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
S Hagenow et al.
Scientific reports, 7, 40541-40541 (2017-01-14)
Ciproxifan is a well-investigated histamine H3 receptor (H3R) inverse agonist/antagonist, showing an exclusively high species-specific affinity at rodent compared to human H3R. It is well studied as reference compound for H3R in rodent models for neurological diseases connected with neurotransmitter
Ramakrishna Nirogi et al.
Journal of pharmacological and toxicological methods, 65(3), 115-121 (2012-04-11)
Rapid and reliable preclinical receptor occupancy measurement at the target organ in relevant species is critical in accelerating the drug hunting process. The aim of this study was to develop in vivo receptor occupancy assay for histamine H₃ receptors (H₃R)
X Ligneau et al.
The Journal of pharmacology and experimental therapeutics, 287(2), 658-666 (1998-11-10)
Ciproxifan, i.e., cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxy) phenyl) ketone, belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling [3H]histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at
Ajeet Kumar et al.
Psychoneuroendocrinology, 101, 128-137 (2018-11-21)
The last two decades of research has established histamine (HA) as a neurotransmitter. Since H3R antagonists are known to modulate several neurotransmitters besides HA, H3R antagonists have shown potential for the treatment of different central nervous system disorders, including depression.
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