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化驗
≥98% (HPLC)
形狀
powder
顏色
off-white
溶解度
H2O: ~20 mg/mL
儲存溫度
2-8°C
SMILES 字串
OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.NCCc1c[nH]c(n1)-c2cccc(c2)C(F)(F)F
InChI
1S/C12H12F3N3.2C4H4O4/c13-12(14,15)9-3-1-2-8(6-9)11-17-7-10(18-11)4-5-16;2*5-3(6)1-2-4(7)8/h1-3,6-7H,4-5,16H2,(H,17,18);2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
InChI 密鑰
GGDUVPKRZGATLR-SPIKMXEPSA-N
應用
2-((3-Trifluoromethyl)phenyl)histamine dimaleate has been used to study the induction of goblet cell secretion in rats3. 2-((3-Trifluoromethyl)phenyl)histamine dimaleate has also been used to study the role of H1 receptor in COX-2 regulation and prostanoid homeostasis in human vascular endothelial cells4.
生化／生理作用
2-((3-Trifluoromethyl)phenyl)histamine dimaleate was found to be the most potent and selective H1 histamine receptor agonist of a panel of compounds in functional in vitro studies on histamine H2, H3, and other neurotransmitter receptors. It showed better potency at the guinea pig H1 histamine receptor than at the human H1 histamine receptor (pKi : 5.9). The selectivity of 2-((3-Trifluoromethyl)phenyl)histamine dimaleate was found to be 2138 (H1:H2), > 64 (H1:H3), 1000 (H1:M3), 105 (H1: a1), 708 (H1:β1), and 71 (H1:5HT2A). 2-((3-Trifluoromethyl)phenyl)histamine dimaleate does not cross the blood-brain barrier.
特點和優勢
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.
準備報告
2-((3-Trifluoromethyl)phenyl)histamine dimaleate is soluble in water at approximately 20 mg/ml.
訊號詞
Danger
危險分類
Acute Tox. 3 Oral - Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
C Leschke et al.
Journal of medicinal chemistry, 38(8), 1287-1294 (1995-04-14)
New histamine derivatives characterized by a (substituted) aryl, heteroaryl, benzyl, or heteroarylmethyl substituent in the C2 position of the imidazole ring have been prepared from appropriate imidates or amidines, respectively, and 2-oxo-4-phthalimido-1-butyl acetate (1). The compounds were screened as potential
Roland Seifert et al.
The Journal of pharmacology and experimental therapeutics, 305(3), 1104-1115 (2003-03-11)
Species isoforms of histamine H2-, H3-, and H4-receptors differ in their pharmacological properties. The study aim was to dissect differences between the human H1R (hH1R) and guinea pig H1R (ghH1R). We coexpressed hH1R and gpH1R with regulators of G-protein signaling
Densen Hayashi et al.
Investigative ophthalmology & visual science, 53(6), 2993-3003 (2012-04-03)
The purpose of this study was to determine the effect of histamine and its receptors on goblet cell secretion. Cultured rat and human goblet cells were grown in RPMI 1640. Goblet cell secretion of high molecular weight glycoconjugate was measured
Xiaoyu Tan et al.
Journal of immunology (Baltimore, Md. : 1950), 179(11), 7899-7906 (2007-11-21)
Although histamine plays an essential role in inflammation, its influence on cyclooxygenases (COX) and prostanoid homeostasis is not well understood. In this study, we investigated the effects of histamine on the expression of COX-1 and COX-2 and determined their contribution
Trinidad Raices et al.
Journal of molecular endocrinology, 63(3), 187-197 (2019-08-16)
Testicular Leydig cells (LC) are modulated by several pathways, one of them being the histaminergic system. Heme oxygenase-1 (HO-1), whose upregulation comprises the primary response to oxidative noxae, has a central homeostatic role and might dysregulate LC functions when induced.
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