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Is Pharmacology Difficult Podcast PHARMACODYNAMICS-RECEPTOR OCCUPATION THEORY
Welcome all to IS PHARMACOLOGY DIFFICULT Podcast! I am Dr Radhika Vijay, in this episode, I will focus on the topic "Receptor Occupation Theory". Clark in 1937 propounded a theory of Drug action which is based on receptor occupation by specific drugs, and how the pace of a cellular function is altered by interaction between receptors and drugs. these drugs are simple molecular ligands. Drug is designated by "D", receptor designated as "R", they are governed by law of mass action, the effect produced is "E", is produced as a direct function of Drug Receptor Complex, which is designated as "DR". equation thus formed is-
D+R=DR--E. Occupation of receptor should be accompanied by ability to activate, i.e. to produce a conformational change in the receptor. This ability to bind with receptor is "Affinity", the ability to produce a functional change in receptor is "Intrinsic activity". Both are independent properties of receptor. Affinity determines concentration of a drug around receptor , and leads to formation of DRs, at high affinity, more DRs is formed at low concentration as compared to drug with low affinity. Intrinsic activity is measure to induce functional change in the receptor , it has a value from 0to 1 (nil to maximum). Accordingly, there as Agonists, Partial agonists, Antagonists. Hence there is no "All or None Law". Here comes a new "S" activity, denotes strength of stimulus, now comes the "Clark's Equation",
D+R=DR--S--E. With this comes a new chapter of definitions, which will be discussed in next session, till then do follow me here, stay tuned, do rate and review on ITunes, Apple podcasts, thank you!!
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By Dr Radhika VijayWelcome all to IS PHARMACOLOGY DIFFICULT Podcast! I am Dr Radhika Vijay, in this episode, I will focus on the topic "Receptor Occupation Theory". Clark in 1937 propounded a theory of Drug action which is based on receptor occupation by specific drugs, and how the pace of a cellular function is altered by interaction between receptors and drugs. these drugs are simple molecular ligands. Drug is designated by "D", receptor designated as "R", they are governed by law of mass action, the effect produced is "E", is produced as a direct function of Drug Receptor Complex, which is designated as "DR". equation thus formed is-
D+R=DR--E. Occupation of receptor should be accompanied by ability to activate, i.e. to produce a conformational change in the receptor. This ability to bind with receptor is "Affinity", the ability to produce a functional change in receptor is "Intrinsic activity". Both are independent properties of receptor. Affinity determines concentration of a drug around receptor , and leads to formation of DRs, at high affinity, more DRs is formed at low concentration as compared to drug with low affinity. Intrinsic activity is measure to induce functional change in the receptor , it has a value from 0to 1 (nil to maximum). Accordingly, there as Agonists, Partial agonists, Antagonists. Hence there is no "All or None Law". Here comes a new "S" activity, denotes strength of stimulus, now comes the "Clark's Equation",
D+R=DR--S--E. With this comes a new chapter of definitions, which will be discussed in next session, till then do follow me here, stay tuned, do rate and review on ITunes, Apple podcasts, thank you!!