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.

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 (H₁:5HT_2A). 2-((3-Trifluoromethyl)phenyl)histamine dimaleate does not cross the blood-brain barrier.

Potent and selective H₁ histamine receptor agonist.

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.

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