2-((3-三氟甲基)苯基)组胺二马来酸酯

别名

(2-[2-(3-Trifluoromethyl)phenyl)-1H-imidazol-4-yl]ethanamine dimaleate,Compound 39

应用

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.

制备说明

2-((3-Trifluoromethyl)phenyl)histamine dimaleate is soluble in water at approximately 20 mg/ml.