medchem_403_ps_3 - phenoxybenzamine. MedChem 563P...

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MedChem 563P Conference Sections: Winter Quarter 2009 Tu 10:30-11:20 T473 Th 9:30-10:20 T625 Problem Set # 3 1. (a) Describe the main adrenergic receptor classes and describe some key distinctions for each type (i.e. tissue localization, response to stimuli, pharmacological exploits, etc.) (b) Of the adrenergic receptor classes you listed in (a), rank the relative potency of the thre e agonists shown below for each at α and β receptors. 2. Apply the SAR features of adrenergic agonists to the following compound and describe the effects of changes at each site. How do you get selective β vs. α adrenergic a gonists?
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MedChem 563P Conference Sections: Winter Quarter 2009 Tu 10:30-11:20 T473 Th 9:30-10:20 T625 Problem Set # 3 3. (a) Below are the structures of a few adrenergic antagonists. Discuss the pharmacological activity and selectivity of each as well as therapeutic use. (b) Show mechanistically how a highly reactive species is formed spontaneously from
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Unformatted text preview: phenoxybenzamine. MedChem 563P Conference Sections: Winter Quarter 2009 Tu 10:30-11:20 T473 Th 9:30-10:20 T625 Problem Set # 3 4. Show the major routes of Propranolol metabolism and draw the major metabolites formed. 5. (a) Describe the source of histamine and how it is stored. Write a mechanism to account for its formation from a common amino acid. What are some physiological effects of endogenous histamine release in humans? Histamine (b) Draw the mechanism for the oxidation of histamine to its carboxylic acid metabolite. 6. Describe the SAR for analogs of histamine that act at H1 and H2 receptors. MedChem 563P Conference Sections: Winter Quarter 2009 Tu 10:30-11:20 T473 Th 9:30-10:20 T625 Problem Set # 3 7. What is the expected receptor target for each of the compounds below and indicate a major therapeutic use. What key structural aspect of one of the agents can be used to rationalize potential drug-drug interactions?...
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This note was uploaded on 01/31/2010 for the course MEDCH 563 taught by Professor Wendell during the Spring '10 term at University of Washington.

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medchem_403_ps_3 - phenoxybenzamine. MedChem 563P...

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