Histamine neurons are exclusively located in the posterior hypothalamus, and project their
fibers to almost all regions of the human brain. Although a significant amount of research …

Highlights•Increase in K p, uu, br/CL int translates into higher drug brain unbound
exposure•The performance of current in silico K p, uu, br models is moderate•A deep …

The central histaminergic neuron system modulates the wakefulness, sleep–awake cycle,
appetite control, learning and memory, and emotion. Previous studies have reported …

Introduction: H1 antihistamines are often used in the medication for allergic diseases,
coughs and colds, and insomnia, with or without prescription, even though their sedative …

Aims The strength of sedation due to antihistamines can be evaluated by using positron
emission tomography (PET). The purpose of the present study is to measure histamine H1 …

Antihistamines often are self-administered at night as over-the-counter (OTC) sleep aids, but
their next-day residual sedative effect has never been evaluated using a reliable quantitative …

BACKGROUND: The central histaminergic neuron system modulates various brain
functions, including eating behavior. We hypothesized that women have higher density of …

Positron emission tomography (PET) is increasingly used in drug discovery and
development for evaluation of CNS drug disposition and for studies of disease biomarkers to …

Some histamine H1 receptor (H1R) antagonists induce adverse sedative reactions caused
by blockade of histamine transmission in the brain. Desloratadine is a second‐generation …

The antihistamines have been divided into first and second generation drugs, according to
their pharmacokinetic properties, structural characteristics and adverse effects. The effects …