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Practical Pharm - Practical session 1 Computer simulation...

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Inhibit muscle contraction channel. Pre-sypnaptic Mu-Opioid receptor DAMGO Practical session 1: Computer simulation of agonist and antagonist actions. Task 1: Concentration response to Acetylcholine i. ii. What is the threshold concentration for a response? Approximately 3x10 -9 M iii. The response saturates at 1x10-5 iv. The EC 50 value for acetylcholine is determined form the graph to be 1x10 -5 M. v. Can any information be derived regarding agonist affinity form this graph and why? No, information regarding agonist affinity cannot be derived from the graph. Affinity of Ach is the probability of it to bind to a free receptor at any given instant. The concentration response curve measures the biological response produced when Ach binds to its receptor, not the actual binding of Ach. The dose response curve cannot be used to measure the affinity of Ach for its receptor because the physiological response produced is not a direct measure of receptor occupancy.
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vi. Why does the response initially saturate? There is a saturation response after a maximum concentration is reached. The maximum response is reached at saturation. When it is saturated the extra amount of drug will not make a difference in the response, as there is a limit to which muscle contraction can occur. vii.Draw a simple diagram showing the main steps leading form acetylcholine receptor activation to smooth muscle contraction?
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Task 2: Atropine antagonist of acetylcholine response i. ii. What is the effect of atropine on the concentration response to acetylcholine? From your answer what type of antagonist is atropine? The higher the Atropine concentration the more the dose-response curve drifts to the right. The greater concentration of atropine the longer it will take Ach response. This means that a higher concentration of Ach needs to be added in order to produce the same maximum response. At higher concentration of atropine the higher the threshold concentration of Ach. Atropine is a reversible competitive antagonist for the muscarinic Ach receptor. iii. How experimentally could you discriminate between a reversible competitive antagonist and a low concentration of an irreversible competitive antagonist?
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