Effect of butaphosphan and cyanocobalamin on postpartum metabolism and milk production in dairy cows.

O objetivo deste estudo foi determinar o efeito de butaphosphan e cianocobalamina (BTPC) no plasma e na produção de leite, em vacas leiteiras no pós-parto

[(t)Bu-d-Gly(5)]NPS, a pure and potent antagonist of the neuropeptide S receptor: In vitro and in vivo studies

Neuropeptide S (NPS) regulates various biological functions by selectively activating the NPS receptor (NPSR). Recently, the NPSR ligand [tBu-d-Gly5]NPS was generated and in vitro characterized as a pure antagonist at the mouse NPSR. In the present study the pharmacological profile of [tBu-d-Gly5]NPS has been investigated. [tBu-d-Gly5]NPS activity was evaluated in vitro in the calcium mobilization assay at the rat NPSR and in vivo in the locomotor activity and righting reflex tests in mice and in the elevated plus maze and defensive burying assays in rats. In vitro, [tBu-d-Gly5]NPS was inactive per se while it inhibited the calcium mobilization induced by 30 nM NPS (pKB 7.42). In Schild analysis experiments [tBu-d-Gly5]NPS (0.1–10 μM) produced a concentration-dependent rightward shift of the concentration–response curve to NPS, showing a pA2 value of 7.17. In mouse locomotor activity experiments, supraspinal injection of [tBu-d-Gly5]NPS (1–10 nmol) dose dependently counteracted NPS (0.1 nmol) stimulant effects. In the mouse righting reflex assay [tBu-d-Gly5]NPS (0.1–10 nmol) fully prevented the arousal-promoting action of the natural peptide (0.1 nmol). Finally, [tBu-d-Gly5]NPS (3–30 nmol) was able to completely block NPS (1 nmol) anxiolytic-like actions in rat elevated plus maze and defensive burying assays. Collectively, the present results demonstrated that [tBu-d-Gly5]NPS behaves both in vitro and in vivo as a pure and potent NPSR antagonist. This compound represents a novel and useful tool for investigating the pharmacology and neurobiology of the NPS/NPSR system

Exploring the role of neuropeptide S in the regulation of arousal: a functional anatomical study

Neuropeptide S (NPS) is a regulatory peptide expressed by limited number of neurons in the brainstem. The simultaneous anxiolytic and arousal-promoting effect of NPS suggests an involvement in mood control and vigilance, making the NPS-NPS receptor system an interesting potential drug target. Here we examined, in detail, the distribution of NPS-immunoreactive (IR) fiber arborizations in brain regions of rat known to be involved in the regulation of sleep and arousal. Such nerve terminals were frequently apposed to GABAergic/galaninergic neurons in the ventro-lateral preoptic area (VLPO) and to tyrosine hydroxylase-IR neurons in all hypothalamic/thalamic dopamine cell groups. Then we applied the single platform-on-water (mainly REM) sleep deprivation method to study the functional role of NPS in the regulation of arousal. Of the three pontine NPS cell clusters, the NPS transcript levels were increased only in the peri-coerulear group in sleep-deprived animals, but not in stress controls. The density of NPS-IR fibers was significantly decreased in the median preoptic nucleus-VLPO region after the sleep deprivation, while radioimmunoassay and mass spectrometry measurements showed a parallel increase of NPS in the anterior hypothalamus. The expression of the NPS receptor was, however, not altered in the VLPO-region. The present results suggest a selective activation of one of the three NPS-expressing neuron clusters as well as release of NPS in distinct forebrain regions after sleep deprivation. Taken together, our results emphasize a role of the peri-coerulear cluster in the modulation of arousal, and the importance of preoptic area for the action of NPS on arousal and sleep