First phase activity

The effect is a nerve-mediated increased insulin secretion, particularly increased first phase activity [41-43], but the effect on glucose uptake is more pronounced. It appears that the neural response can increase the translocation of GLUT4 much like the effect of exercise and without concomitant changes in insulin concentration [44]. 

Based on Hquid—Hquid equiHbrium principles, a general model of octanol—water partitioning is possible if accurate activity coefficients can be determined. First, phase equiHbrium relationships based on activity coefficients permit Hquid—Hquid equiHbrium calculations for the biaary octanol—water system. Because the two components are almost immiscible ia each other, two phases form an octanol-rich phase containing dissolved water, and a water-rich phase containing dissolved octanol. 

When the amount of coke formed as a function of time on stream is compared to the decrease in catalytic activity (see Fig. 3), two regimes of deactivation can be noticed for the strongly deactivating catalysts, i e, a slow initial deactivation which is followed by a rapid loss of activity This first phase is characteristic of a slow transformation of the reactive carbon into less reactive coke. The second phase is attributed to carbon formed on the support which accumulates there and rapidly covers the Pt particles when its amount reaches a critical value causing the sudden decay of catalytic activity. 

Overview. Figure 10 shows, in simplified form, the activities, inputs and outputs involved in running HSPF, from a typical user s point of view. The first phase involves copying input time series, such as meteorological data, from sequential files (cards, tape, disc) to the Time Series Store (TSS). This is sometimes done in a single run but in most practical situations, where data have to be gathered from diverse sources and gaps have to be patched, several runs are made. 

The successful roll out of first phase would depend on the following preroll out activities ... 

Cyclosporine demonstrates immunosuppressive activity by inhibiting the first phase of T-cell activation. It also inhibits release of inflammatory mediators from mast cells, basophils, and polymorphonuclear cells. It is used in the treatment of both cutaneous and arthritis manifestations of severe psoriasis. The usual dose is between 2.5 and 5 mg/kg/day given in two divided doses. Adverse effects include nephrotoxicity, hypertension, hypomagnesemia, hyperkalemia, alterations in liver function tests, elevations of serum lipids, GI intolerance, paresthesias, hypertrichosis, and gingival hyperplasia. Cumulative treatment for more than 2 years may increase the risk of malignancy, including skin cancers and lymphoproliferative disorders. 

In the first phase of their research, Squibb tested a short-chain peptide isolated from the venom of the viper Bothrops jararaca, with which Vane was working in the laboratory, in human volunteers and showed that it did, indeed, inhibit the conversion of angiotensin I to angiotensin II after intravenous injection. The peptide was also shown to reduce blood pressure in patients when injected. Since the vast majority of peptides cannot be absorbed from the GI tract, Squibb scientists set out to prepare a nonpeptide compound that could be used orally and manufactured at acceptable cost. The design of a true peptidomimetic that became orally active had not been accomplished at that time. Squibb then carried out... 

Notes Analysis (Joost and Methner, Genome Biol., 3(11) research 0063.1-0063.16,2002. http //genomebiology.com/ 2002/3/11 /research/0063). Profiling is performed in two phases. The first phase consists of a panel of 25 GPCR representing the families most commonly associated with off-target effects. Once a compound shows activity in one of the assays from the first set, full dose response is run on receptors within the same target family to assess selectivity (Phase 2). 

There are at least three potential reservoirs. The first phase reflects virus produced predominantly from activated CD4+ T cells. Extracellular virus particles can be trapped on specialized cells in the germinal centers of the peripheral lymphoid tissues. These cells, known as follicular dendritic cells (FDCs), are able to retain antigenic material on their surfaces for long periods of time. This reservoir declines rapidly with a half-life of about 2 weeks. ... 

Quaternary onium salts were the first phase-transfer catalysts used subsequently, a number of compounds (linear polyethers, polypodands, crown-ethers, cryptands, cage-compounds, etc.) were found effective for the anion activation in two-phase systems. These structurally different systems must satisfy at least two fundamental conditions in order to behave as phase-transfer catalysts i) solubility in the organic phase ii) steric hindrance around the cationic center leading to a good cation-anion separation within the ion-pair. 

Conclusions. The objectives cited earlier were met. Solid trends do exist in this series can be documented, and can be used to chart new work. Significant trends in residuals encountered after the first phase of the study provided the basis for model refinement. Good support exists for the premise that we have thoroughly traversed the most attractive areas of structure/activity space in this series. 

The first phase of ToxCast profiled a chemical library of 320 environmental chemicals (309 unique structures and 11 replicates), which are mostly pesticidal actives and inerts having rich in vivo data from guideline studies. ToxCast is now in Phase II, bringing to 1060 the number of unique chemicals tested across nearly 650 diverse assays. The additional Phase II chemicals include a number of reference chemicals, consumer products, food additives, failed pharmaceuticals, data-poor chemicals being screened for potential endocrine... 

The first phase of ToxCast profiled a 309-chemical library consisting mostly of pesticidal actives as well as several other compounds of high interest. The acceptance criteria for chemical selection for inclusion in Phase I were as follows (a) availability of in vivo data from bioassays on chronic/cancer, multigenerational reproductive, and/or prenatal developmental toxicity (95% Phase I chemicals met this criteria) (b) solubility in DMSO (the vehicle for HTS assays) with a log of the octanol/water partition coefficient (logP) between -1 and +6 (97.5% met this criteria) (c) molecular weight in the range of 250-1,000 (90% met this criteria) and (d) commercially available at a purity >90% (98% met this criteria) (16). Current information about the Phase I (and Phase II) chemical library can be found at the NCCT website address http //www. epa.gov/ncct/toxcast/chemicals.html. 

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