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- 5. Compute for the AST (Aspartate Aminotransferase activity) of 0.10 mL serum sample mixed with 1mL of reagent which yielded a A Abs/min reading of 0.003 at 340 nm with a molar absorptivity of 0.00622.Which of these heterocyclic drugs is likely to be the least soluble in water? Use the Fsp³ parameter to decide. OH Tramadol Chemical Formula: C16H25NO2 YOUR OW Pantoprazole Torasemide Chemical Formula: C16H15F2N3O4S Chemical Formula: C16H20N4O3S Temazepam -OH Chemical Formula: C16H13CIN₂O2 Tioconazole Chemical Formula: C16H13C3N₂OS A. Tramadol B. Pantoprazole C. Torasemide D. Temazepam E. Toconazole1. Compare the binding-site locations in the brain for enkephalins and the prescription painkillers morphine and codeine. 2. Compare the structures of the peptide neurotransmitters Met-enkephalin and Leu-enkephalin in terms of what they have in common. how they differ? 3. what is the unusual structure feature present in the molecule glutathione? 4. what is the major biochemical function of glutathione?
- An experiment was carried out to measure the reaction rate of hydrolysis of acetylcholme (substrate) with serum enzymes (Eadie, 1949). In the experiment, two experiments were conducted, namely experiment 1 without using a prostigmine inhibitor and experiment 2 using a prostigmine inhibitor at 1.5 x 10^-7 mol/l. the data obtained are: a. Is prostigmine competitive or noncompetitive inhibitor? b. determine the value of km and rmax for the two experiments, compare6. For a 1:1 ligand-receptor binding interaction that is modeled by X + Y XY : (A) Show how the fraction of ligand-receptor binding (fo) is represented by the [X] [X]+ K, equation of f, (i.e., derive this expression for this reaction beginning eg with the relationship for K = f([X].[X],[XY]) under equilibrium conditions). (B) shown to the right for this reaction, what is the estimated value of Keg? Give your answer in units of M. For the data plot 0.9 0.8 0.7 0.6 문 0.5 0.4 0.3 0.2 0.1 0.0000 0.0050 0.0100 0.0150 0.0200 0.0250 0.0300 0.0350 0.0400 [X) (mM)How is a condition such as diabetes a good example of the failure of a set point in humans?
- Which of the following neurotransmitters is associated with inhibition exclusively? GABA acetylcholine glutamate norepinephrineDuring an SAR effort to identify tyrosine kinase inhibitors, it was found that compound 2 was significantly more potent and selective than compound 1. To what might you attribute this improvement in activity and selectivity? Explain. IC-5 micromolar IC-0.1 mromolar1 What's true about Purdue Pharma and OxyContin? (Select all that apply] O OxyContin is an opioid painkiller introduced to the U.S. by Purdue in 1996 as a 12-hour timed-release dosage of oxycodone. O By crushing or dissolving the 12-hour pills, drug abusers could ingest the entire dose at one time, thus causing fatal overdoses, The Sackler-family-owned Purdue Pharma, maker of OxyContin, used unethical marketing practices. Such practices led Purdue to become the major contributor to the opiold crisis that caused the deaths of 400,000 individuals, CPurdue's aggressive marketing of OxyContin included visiting doctors, paying for their meals and travel, providing gifts, and funding pain treatment groups. M Purdue has earned in excess of $30 billion since OxyContin arrived on the market. ASome of the company's marketing messages minimized the potential for OxyContin to lead to addiction, for which it paid over $600 million in fines in 2007. Purdue announced in September 2019 that it had…
- A tetrapeptide, glutamate-glycine-alanine-lysine, is prepared at at concentration of 1 mM (0.001 M) and is measured in the standard setup (pathlength of 1 cm). What is the approximate absorbance of this peptide at 280 nm? Hint: if the peptide contained a single tryptophan, the answer would be about 10. 10 280 1 0From a medicinal chemistry (and a pharmacologist) perspective, functional groups provide specific properties and behaviors that allow drug molecules to exert their desired PD and PK effects. The key point here is that each individual group within a drug molecule can serve to provide one or more specific roles, tasks, or functions. The following table summarizes a series of drug discovery lead optimization for targeting a certain renal disease. Explain the basis for changing the R- functionality at the para- position. Please explain in as much detail as you need and by using scientific justifications, which one of the 4 candidates (526-529), presents the most viable investigational drug candidate, given the information provided below? N- `N' 'N' R- Drug Code R IC30 (nM) Half-Life (tı2), Minutes 526 CH;O 104 6 527 CF;0 1110 95 528 CH;CH, 11 <5 529 CH,CF, 14 96Which physicochemical properties are useful for prediction of the oral bioavailability of drug molecules? Use naproxen and propranolol as examples in your answer.
