Increasing the number of 5-HT(1A)-receptors in cortex and hippocampus does not induce mnemonic deficits in mice.

Even though the role of the serotonin1A (5-HT(1A))-receptor for cognitive processes is undisputed, the exact involvement of pre- and postsynaptic sites remains unexplained. Recently, we introduced a mouse line overexpressing the 5-HT(1A)-receptor in the hippocampus and cortex. In this study we investigated in comparison to wild-type mice their cognitive abilities using the Morris water-maze task and inhibitory avoidance test.

The pharmacological rationale behind polypharmacy in heart failure.

The treatment of heart failure (HF) commonly requires a complex pharmacological regimen. Currently HF polypharmacy consists of drugs that target different factors for disease progression, such as altered hemodynamics and elevated neurohumoral factors. Even though a significant improvement of HF has been achieved by combination treatment with regard to morbidity and mortality rate, the increasing numbers and daily doses of drugs bare the risk of potential and sometimes unavoidable drug interactions.

Mice over-expressing the 5-HT(1A) receptor in cortex and dentate gyrus display exaggerated locomotor and hypothermic response to 8-OH-DPAT.

The serotonin 1A (5-HT(1A)) receptor is one of the best described receptor subtypes of the serotonergic system. Due to the complex distribution pattern, the pre- and postsynaptic localisation, the impact on various monoamines, as well as the influence on a wide range of physiological functions, the contribution of 5-HT(1A) receptors to behavioural outcomes is difficult to define. In this study, we present a new transgenic mouse model with a prominent over-expression of the 5-HT(1A) receptor in the outer cortical layers (I-III) and the dentate gyrus.

Regulation of transport of the angiotensin AT2 receptor by a novel membrane-associated Golgi protein.

Objective: Synthesis and maturation of G protein-coupled receptors are complex events that require an intricate combination of processes including protein folding, posttranslational modifications, and transport through distinct cellular compartments. Little is known concerning the regulation of G protein-coupled receptor transport from the endoplasmic reticulum to the cell surface.

Methods And Results: Here we show that the cytoplasmatic carboxy-terminal of the angiotensin AT2 receptor (AT2R) acts independently as an endoplasmic reticulum-export signal.

Reduced anxiety-related behaviour in transgenic mice overexpressing serotonin 1A receptors.

Serotonergic neurons play a major role in the modulation of emotion and behaviour. Especially knockout studies have revealed a role for the serotonin(1A) (5-HT(1A)) receptor in anxiety related behaviour. Mutant animals exhibit enhanced anxiety-like responses, possibly resulting from impaired autoinhibitory control of midbrain serotonergic neurons.

Analysis of the murine 5-HT receptor gene promoter in vitro and in vivo.

The expression level of the 5-HT(1A) receptor gene (htr1a) in the central nervous system (CNS) is implicated in the aetiology and treatment of anxiety disorders and depression. Previous studies of the murine htr1a have revealed that its proximal promoter is GC rich and TATA-less. Several functional transcription factor binding sites, including MAZ and SP1 recognition sequences, have been identified.

Regulation and function of somatostatin receptors.

This review summarizes the latest advances that have been made to elucidate the somatostatinergic system in respect to somatostatin receptor evolution, the development of receptor agonists/antagonists, receptor regulation, signal transduction, effects on cell proliferation, receptor-receptor or receptor-protein interactions and receptor function.

Vasoactive peptides, their receptors and drug development.

Vasoactive peptides with vasoconstrictor properties play an important role in many physiological and pathological conditions. The peptides act via specific receptors, most of them belonging to the group of seven transmembrane G-protein coupled receptors. These receptors have become important targets for drugs developed to inhibit vasoconstrictor actions.

High-frequency stimulation of the subthalamic nucleus enhances striatal dopamine release and metabolism in rats.

High-frequency stimulation of the subthalamic nucleus is believed to exert its main effects via the basal ganglia output structures. Previously, we have shown a concomitant increase in striatal dopamine (DA) metabolites in normal and 6-hydroxydopamine-lesioned rats. The present study was designed to determine whether this increase in striatal DA metabolites reflects enhanced intraneuronal DA turnover or, alternatively, is due to increased DA release with subsequent rapid and efficient reuptake and/or metabolism.