87 research outputs found
When fragments link: A bibliometric perspective on the development of fragment-based drug discovery
Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)-and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.
Various approaches to the synthesis of all four stereoisomers of 2-(1H- imidazol-4-yl)cyclopropylamine (cyclopropylhistamine) are described. The rapid and convenient synthesis and resolution of trans-cyclopropylhistamine is reported. The absolute configuration of its enantiomers was determined by single-crystal X-ray crystallographic analysis. The distinct transcyclopropylhistamine enantiomers were tested for their activity and affinity on the histamine
Synthesis, structure activity relationships and molecular modelling of histamine H3 receptor ligands
Timmerman, H. [Promotor]Menge, W.M.P.B. [Copromotor]Nederkoorn, P.H.J. [Copromotor
Sex- and histamine-dependent long-term cognitive effects of methamphetamine exposure
As prenatal methamphetamine (MA) exposure results in long-term hippocampus-dependent cognitive deficits, the increased MA use in women of childbearing age is of great concern. As mice are most commonly used in genetic models, we started to study the potential effects of neonatal MA exposure in female and male mice on brain function 3 months later. As histamine (HA) might mediate some effects of MA in adulthood, we also tested whether in neonates HA might mediate the long-term effects of MA using HA
Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas
The neurotransmitter histamine exerts its action through four distinct histamine receptors. The histamine
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