추천 제품
분석
≥98% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 32 mg/mL
H2O: insoluble
SMILES string
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
애플리케이션
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.
생화학적/생리학적 작용
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.
특징 및 장점
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.
신호어
Warning
유해 및 위험 성명서
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1 - STOT SE 3
표적 기관
Respiratory system
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
개인 보호 장비
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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
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)
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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