Drug Receptors and Effectors – Pharmacodynamics

by Pravin Shukle, MD

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    00:01 Let's talk about the different kinds of receptors and effectors that are in our body.

    00:06 The first most simple kind of receptor-effector combination is the steroid drug interaction.

    00:12 So a steroid is a lipophilic kind of molecule. It will pass through the membrane because it is lipophilic, and the receptor is somewhere on the inside of the cell.

    00:26 A transmembrane receptor is one in which that spends the entire membrane, and the surface has a port or a receptor site that binds a drug, and the activity is underneath and causes an effect within the cell.

    00:43 Tyrosine kinase is a specific kind of receptor-effector system, where the tyrosine kinase molecule binds to the drug on the surface, and the JAK portion of that receptor complex causes a change within the cell.

    01:00 An ion channel is a very common type of receptor-effector combination, where a drug might bind to a site on the ion channel and cause a flow of something in or out of the cell.

    01:14 And finally, you can have a G-protein coupled receptor. So a G-protein coupled receptor is where a drug binds to the receptor on one protein which causes a change in the G-protein to move over to another molecule to cause an effect.

    01:33 So, let's give an example of a G-protein mediated event. So here's epinephrine, and it causes cyclic AMP synthesis within the cell. So the first step is that the drug epinephrine binds to the receptor and you can see the receptor is a transmembrane protein.

    01:52 The receptor makes a change at the G-protein. And what happens is the G-protein itself dissociate and binds to an effector molecule, in this case, adenylyl cyclase.

    02:05 The effector catalyzes a reaction which increases the concentration of cyclic AMP.

    02:12 Cyclic AMP is the most common second messenger out there, and we call cyclic AMP a second messenger because it is now the second drug or second molecule that is going out to do something, the first being the drug.

    02:26 Now, that cyclic AMP causes a biological effect. So in this particular case, we're talking about an increase in heart rate, or a dilation of skeletal muscles, or it could be a breakdown of glycogen to glucose, depending on what you're talking about.

    About the Lecture

    The lecture Drug Receptors and Effectors – Pharmacodynamics by Pravin Shukle, MD is from the course Pharmacokinetics and Pharmacodynamics.

    Included Quiz Questions

    1. a lipophilic molecule that usually acts on an intracellular or nuclear receptor.
    2. a hydrophilic molecule that acts through tyrosine kinase.
    3. a lipophilic molecule that acts on a surface ion pore.
    4. a hydrophilic molecule that usually acts on an intracellular or nuclear receptor.
    1. G-protein coupled receptor complex
    2. Ion channel
    3. Steroid receptor
    4. Tyrosine kinase receptor
    5. Transmembrane proteins

    Author of lecture Drug Receptors and Effectors – Pharmacodynamics

     Pravin Shukle, MD

    Pravin Shukle, MD

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    Great lectures
    By Shannon R. on 29. November 2018 for Drug Receptors and Effectors – Pharmacodynamics

    I really love these course! Great work breaking it down and offering the quiz it really helps!