BIOM20002 Lecture Notes - Lecture 40: Sympathomimetic Drug, Sildenafil, Heparin

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Lecture 40-42 how do drugs work through receptors. Agonist binding agonist is a stimulus of the receptor ---> increase in receptivity upon binding. Changed cellular biochemistry behaviour triggered by stimulus transduction. Drugs do(cid:374)(cid:859)t (cid:449)o(cid:396)k (cid:449)ithout (cid:271)i(cid:374)di(cid:374)g (cid:858)(cid:373)agi(cid:272) (cid:271)ullet(cid:859) (cid:272)o(cid:374)(cid:272)ept a perfectly selected agent that would kill the pathogens without impacting the host. Drug selectivity rather than specificity is more realistic to be the goal because for s(cid:373)all (cid:373)ole(cid:272)ules the(cid:396)e(cid:859)s a le(cid:448)el of likelihood of interaction between multiple agents. Chemical reaction rate depends on the concentration of reactants. A agonist is in vast excess of r receptor. Increase in concentration of ligands increases occupancy: ec50 is a constant for half drug response (intrinsic efficacy), different from kd which is about affinity. Efficacy: response vs. drug conc. y c n a p u c c o. Partial agonist may cause a lesser response when all the receptors are occupied.

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