Search results for "PIP"
showing 10 items of 1156 documents
Structure–activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of RO…
2007
ROCK has been implicated in many diseases ranging from glaucoma to spinal cord injury and is therefore an important target for therapeutic intervention. In this study, we have designed a series of 1-(4-(1H-indazol-5-yl)piperazin-1-yl)-2-hydroxy(or 2-amino) analogs and a series of 1-(4-(1H-indazol-5-yl amino)piperidin-1-yl)-2-hydroxy(or 2-amino) inhibitors of ROCK-II. SR-1459 has IC50 = 13 nM versus ROCK-II while the IC50s for SR-715 and SR-899 are 80 nM and 100 nM, respectively. Many of these inhibitors, especially the 2-amino substituted analogs for both series, are modest/potent CYP3A4 inhibitors as well. However, a few of these inhibitors (SR-715 and SR-899) show strong selectivity for R…
Experimental Evidence of Leaks in Elastic Pipes
2016
Several studies have been carried out in recent decades to establish a relationship between total head and leaks. In literature, the leakage governing equations have been analysed in light of pipe materials, water head, leak dimension or shape. Most of these contributions questioned the classical Torricelli equation, demonstrating through experimental evidence that the classical orifice law can give unsatisfactory results. Nevertheless, starting from the Torricelli equation, other exponential or linear governing equations have been proposed as mathematical models able to reproduce the leakages in water distribution systems (WDSs). To investigate the validity of the proposed governing equati…
Effects of Onshore and Offshore Environmental Parameters on the Leading Edge Erosion of Wind Turbine Blades: A Comparative Study
2021
Abstract The presence of rain-induced leading edge erosion of wind turbine blades (WTBs) necessitates the development of erosion models. One of the essential parameters for erosion modeling is the relative impact velocity between rain droplets and the rotating blade. Based on this parameter, the erosion damage rate of a WTB is calculated to estimate the expected leading edge lifetime. The environmental conditions that govern this parameter have site-specific variations, and thus, rain and wind loading on a turbine differ for onshore and offshore locations. In addition, there are wave loads present in the offshore environment. The present paper tries to provide guidelines for erosion modelin…
The Peptide Hemopressin Acts through CB1Cannabinoid Receptors to Reduce Food Intake in Rats and Mice
2010
Hemopressin is a short, nine amino acid peptide (H-Pro-Val-Asn-Phe-Lys-Leu-Leu-Ser-His-OH) isolated from rat brain that behaves as an inverse agonist at the cannabinoid receptor CB1, and is shown here to inhibit agonist-induced receptor internalization in a heterologous cell model. Since this peptide occurs naturally in the rodent brain, we determined its effect on appetite, an established central target of cannabinoid signaling. Hemopressin dose-dependently decreases night-time food intake in normal male rats and mice, as well as in obeseob/obmale mice, when administered centrally or systemically, without causing any obvious adverse side effects. The normal, behavioral satiety sequence is …
Hypothalamic CB1 cannabinoid receptors regulate energy balance in mice.
2012
Cannabinoid type 1 (CB(1)) receptor activation is generally considered a powerful orexigenic signal and inhibition of the endocannabinoid system is beneficial for the treatment of obesity and related metabolic diseases. The hypothalamus plays a critical role in regulating energy balance by modulating both food intake and energy expenditure. Although CB(1) receptor signaling has been implicated in the modulation of both these mechanisms, a complete understanding of its role in the hypothalamus is still lacking. Here we combined a genetic approach with the use of adeno-associated viral vectors to delete the CB(1) receptor gene in the adult mouse hypothalamus and assessed the impact of such ma…
Pied-piping domains and adjunction coincide in Finnish
2012
It is well-known thatwh-pronouns may pied-pipe their containing host phrases as they move to their final scope positions. In Finnish, such pied-piping requires further that awh-element is situated at the left edge of host phrases, a position in which it ends up either through base generation or throughwh-movement. This article investigates which independent properties define such pied-piping domains. An empirical generalization will be defended according to which a phrase constitutes such pied-piping domain if and only if it is adjoinable. The hypothesis that pied-piping domains are islands is put into question. Secondarywh-movement, pied-piping and adjunction are thus intrinsically linked …
Chemical composition and biological activities of Artemisia judaica essential oil from southern desert of Jordan
2016
Abstract Ethnopharmacologic relevance Artemisia judaica L. (Arabic name: Beithran ), is a medicinal and aromatic plant growing in the valley bottoms of desert areas, particularly in the southern desert of Jordan nearest to the Jordan-Saudi Arabia borders and in Wadi Araba in the Southern Badia. In Jordan, A. judaica is widely used in traditional medicine being recommended by aboriginal Bedouins in the North Badia region of Jordan as calmative. Furthermore, it is used for the treatment of stomach ache, heart diseases, sexual weakness, diabetes, gastro-intestinal disorders and external wounding. Additionally, other folk medicines of the Arabic region commonly use this aromatic plant for the t…
Śródziemnomorskie kody polskości w twórczości Jana Parandowskiego
2020
One is used to regarding Jan Parandowski (1895–1978) as a great connoisseur of the ancient world and a kind of “Olympic” writer with a distance to his own time and space. A thorough exam-ination of his literary essays, short stories and novels hardly proves this opinion. Treating Polish his-tory and culture, especially of the Renaissance epoch, as originating from and inspired by the ancient Roman/Greek tradition (“Poland is situated in the Mediterranean”), he conceals at the same time an evidently emotional approach to national legacy. There are several modes in which he evokes unique Polish history in the 19th century, with the great but problematic heritage of Romanticism as well as the …
Słowo, które staje się obrazem, w tradycji chrześcijan syryjskich
2017
Word which becomes an image in the tradition of Syriac Christians. The paper examines the subject of figurative art in the theological space of the tradition of Syriac Churches. Even if in the early stage of their existence those communities were an integral part of Byzantine Empire, they developed a totally different pattern of the imaging, which didn’t consist in icons or in the other forms of the traditional art. The main focus of the Syriac theological painting was to use the written word. Such an approach wasn’t a result of any prohibition inherited from the Jewish tradition or of an internal iconoclasm, but it arises from the mentality and spiritual sensitivity of the people from the …
Macrocycles prepared from lithocholic acid, piperazine and isomeric pyridine dicarboxylic acids and their selective affinities towards sodium and pot…
2001
Abstract Two novel macrocycles prepared from lithocholic acid, piperazine and pyridine dicarboxylic acids (2,6- and 3,5-isomers), have been characterized by 13C NMR and ESI–MS techniques. In case of the pyridine-2,6-dicarboxylate derivative, the molecular formula of the cycle was C59H87O6N3 (I), while the pyridine-3,5-dicarboxylate derivative (II) was a trimeric structure by molecular mass when compared with I. Furthermore, cycle I showed a special affinity towards potassium cation, while II possessed significant proton and sodium cation recognition properties.