G potency

Dissolution testing is one of the most common analytical techniques performed in a pharmaceutical analytical laboratory. It is performed primarily on oral dosage forms to determine the in vitro release of a drug from its finished dosage. Dissolution testing complements other analytical tests that are used to characterize the performance of the final dosage form (e.g., potency and related substances assay). 

The impact of formulation on virus reduction and product recovery (e.g., potency) was evaluated during terminal freeze dry/dry heat treatment studies with an unlicensed Fraction I derived product, that will be designated Protein G. As shown in Fig. 10, the optimum formulation, that achieved >4 logio PPV inactivation and 80% product recovery, was one that contained 2% albumin, no NaCl, and <0.3%o moisture by the Karl Fischer coulometric method. In contrast, freeze dry/dry heat treatment of product formulated with no albumin, 150mM NaCl and low moisture resulted in approximately 3 logio PPV reduction and 35% product recovery. Thus, minor changes in formulations such as the addition of 2% albumin may impact virus reduction and product recovery during a freeze dry/dry heat treatment. 

What combination of favorabie assay resuits is difficuit/easy (e.g., potency, clearance, hERG) ... 

Post-coital activity in the rat was on the same order as estrogenic potency, with the order being CDB-1357 (ED jqo = (3 //g/kg)/d for each of5days) >... 

Acesulfame-K is a white crystalline powder having a long (six years or more) shelf life. It readily dissolves in water (270 g/L at 20°C). Like saccharin, acesulfame-K is stable to heat over a wide range of pH. At higher concentrations, there is a detectable bitter and metallic off-taste similar to saccharin. Use of the sodium salt of feruHc acid [437-98-4] (FEMA no. 3812) to reduce the bitter aftertaste of acesulfame-K has been described (64). The sweetness potency of acesulfame-K (100 to 200x, depending on the matching sucrose concentration) (63) is considered to be about half that of saccharin, which is about the same as that of aspartame. 

Finally, some amphiphilic sweeteners, eg, aspartame, saccharin, and neohesperidin dihydrochalcone, have been shown to be capable of stimulating a purified G-protein direcdy in an in vitro assay (136). This suggests some sweeteners may be able to cross the plasma membrane and stimulate the G-protein without first binding to a receptor. This type of action could explain the relatively longer response times and the lingering of taste associated with many high potency sweeteners. 

Calcitonin. Calcitonin is available commercially from pork and salmon extracts (Calcimar, Armour) as well as by synthesis. Preparations are bioassayed on the basis of their calcium-lowering activity in comparison to the potency of pure pork calcitonin of which ca 4 p.g is equivalent to 1 MRC unit (Medical Research Council, U.K.). For clinical use, vials containing 400 units in 4 mL are available. The recommended daily dosage is 100 units to be adrninistered subcutaneously or intramuscularly because its plasma half-life is short (4—12 min). 

As in the case of the steroids, introduction of additional nuclear substituents yields morphine analogs of increased potency. The more important of these are derived from one of the minor alkaloids that occur in opium. Thebaine (14), present in crude opium in about one-tenth the amount of morphine, exhibits a reactive internal diene system that is well known to undergo various addition reactions in a 1,4 manner (e.g., bromination). Thus, reaction with hydrogen peroxide in acid may be visualized to afford first the 14-hydroxy-6-hemiketal (15). Hydrolysis yields the isolated unsaturated ketone (16). Catalytic reduction... 

In fact, a measure of the degree of confidence can be gained from the t calculation. Shown in Appendix A are columns for greater degrees of confidence. The value for df = 4 for a 98% confidence level is 3.747 and it can be seen that the experimentally calculated value is also greater than this value. Therefore, the level of confidence that these samples came from different populations is raised to 98%. However, the level of confidence in believing that these two samples came from separate populations does not extend to 99% (t = 4.604). Therefore, at the 98% confidence level this analysis indicates that the potency of human calcitonin is effectively increased by enrichment of G -protein in the cell. 

Furchgott method, 92, 95, 97-98 G-protein coupling effects on, 76 partial, 89-91, 97, 124, 260-261 potency and, 80f Agonist occupancy, 115 Aikake s information criteria, 243, 243f Alleles, 6... 

Apelin receptors activate several signalling pathways including coupling through inhibitory G-proteins (G ) and Ras-independent activation of extracellular-regulated kinases (ERKs) via protein kinase C (PKC). The apelin receptor is one of number of G-protein-coupled receptors that can act as an alternative coreceptor for entry into cells of HIV and simian immunodeficiency vims (SIV) strains in human U87 cells expressing CD4 in vitro. Apelin peptides blocks entry of HIV but display different potencies, with apelin-36 being more effective than shorter sequences [3]. 

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