PoDA spring 2013-1-answers

Drug x acting as an agonist at its receptor possesses

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11. Drug X, acting as an agonist at its receptor, possesses a binding affinity of 500 nM and an efficacy of 9. What would you expect its EC50 to be in a functional assay? A. 500 nM B. 491nM C. 56 nM D. 50 nM E. 9 nM
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12. Hyperekplexia is 13. The drug haloperidol is sold by various drug companies under a number of trade names including Aloperidin™, Bioperidolo™, Duraperidol™ and Haldol™. In terms of drug nomenclature what kind of name is haloperidol? ( 0.5 marks ) Non-proprietary or official or generic name. 14. (a) Define the term drug partition coefficient. (b) In what units is the partition coefficient expressed? (c) Would you expect a higher partition coefficient to increase or decrease the rates of movement of drug molecules across lipid bilayers? ( 1.5 marks ) (a) the relative solubilities of drug in oil to water (acting as a surrogate for membrane:buffer). (b) unitless (c) increase 15. What are the three types of capillaries? Briefly explain how they differ from one another ( 3 marks ) Capillaries with maculae - Macular junctions between capillary wall cells are not continuous belts but exist as patches. Hence there are extracellular spaces around these maculae through which drugs can travel. Fenestrated capillaries are found in excretory and secretory organs. Fenestrae (windows) through cell membrane allow for drug passage. Occluded capillaries have their intercellular spaces completely blocked off ; these make up the blood-brain barrier.
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16. Fill in the blanks. In the liver, 75% of the blood entering the liver is provided by the _ portal vein ___________ while 25% is provided by the _ hepatic artery ______________________ . The blood flows into structures called _ sinusoids ________________________ where contact of blood with hepatocytes occurs. ( 1.5 marks ) 17. You have injected a rat intravenously with a drug that you previously had radiolabeled (made radioactive). When you sacrifice the rat two hours later you find that there is a high amount of radioactivity in the rat’s small intestine?
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