Intrinsic activity (IA) or efficacy refers to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC50, which is a measure of the potency of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by Stephenson (1956) to describe the way in which agonists vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system.
Agonists of lower efficacy are not as efficient at producing a response from the drug-bound receptor, by stabilizing the active form of the drug-bound receptor. Therefore, they may not be able to produce the same maximal response, even when they occupy the entire receptor population, as the efficiency of transformation of the inactive form of the drug-receptor complex to the active drug-receptor complex may not be high enough to evoke a maximal response. Since the observed response may be less than maximal in systems with no spare receptor reserve, some low efficacy agonists are referred to as partial agonists.
Intrinsic Activity of an Agonist || Junaid Asghar PhD
Intrinsic activity (IA) (often called as Efficacy) refers to the relative ability of a drug-receptor complex to produce a maximum functional response.
#IntrinsicActivity
#IntrinsicEfficacy
#JunaidAsgharPhD
Dr. Marvin Nieman, from the department of Pharmacology at Case Western Reserve University, gives a brief overview of important pharmacodynamic principles.
published: 05 Sep 2017
INTRINSIC ACTIVITY OF A DRUG & QUANTAL DOSE-RESPONSE RELATIONSHP
TALE 26 : INTRINSIC ACTIVITY OF A DRUG & QUANTAL DOSE-RESPONSE RELATIONSHP
VIDEO GUIDE
00:14
Intrinsic Activity and Quantal dose response relationship
00:24
Introduction to intrinsic activity
Classification of drugs
-Full Agonist
-Partial agonist
-Inverse agonist
-Antagonist
01:05
Full Agonist
04:41
Partial Agonist
07:03
Inverse Agonist
08:08
Antagonist
Competitive antagonist
Irreversible antagonist
Allosteric antagonist
Functional antagonist
14:32
Quantal dose response relationship
Therapeutic index
19:50
Summary
published: 29 Jul 2020
General Pharmacology 12/ Receptors/ Intrinsic activity/ Affinity
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published: 20 Jun 2019
Intrinsic activity of drug by Leena Hameed
Reference book
Lippincott illustrated Pharmacology by K. Whalen
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published: 30 Jun 2020
Intrinsic activity ,agonists antagonists types functionla anatagonism by Dr uut in Urdu
#agonists #antagonists #functionalantagonism
published: 28 Dec 2019
Intrinsic activity agonists antagonist types functional antagonism by Dr uut in English
Download "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Test and other GPAT Materials - https://play.google.com/store/apps/details?id=co.bolton.nqilv
Pharmacology is all about the study of drug and their effect on the body along with body responsible for the drug taken. The drug gives its action mainly through the receptor.
Receptors are the macromolecule or binding site located at the surface or inside the cell. They are used to recognize the signal or drug molecule and initiate the biological response.
The biological response is generally given by any drug using any of these mechanisms- (1) Enzyme (2) Ion channels (3) Transport (4) Receptor. In biochemistry and pharmacology, a receptor is a protein molecule that receives chem...
Time Stamps:
00:00 Resting State of the Receptor and Receptor Activation
01:21 Intrinsic Activity/ Intrinsic Efficacy
03:20 Intrinsic Activity of Full, Partial and Inverse Agonists
09:15 Full, Partial and Inverse Agonists on a bar graph
12:48 Concentration-Response Curve (CRC) or Dose-response Curve (DRC)
14:54 Efficacy and Potency
26:39 Spare Receptors/ Reserve Receptors
The efficacy of a drug is the maximum response achievable from a drug regardless of the drug potency.
Note that a drug may have a high efficacy but not be potent, i.e. the drug may have a high maximal response (Emax) but require a lot of the drug to do so. If an analgesic can relieve hundred percent of a patient's pain but requires 2000 mg to do so, this drug has a high efficacy but a low potency. Conversely, a drug ca...
Intrinsic activity (IA) (often called as Efficacy) refers to the relative ability of a drug-receptor complex to produce a maximum functional response.
#Intrin...
Intrinsic activity (IA) (often called as Efficacy) refers to the relative ability of a drug-receptor complex to produce a maximum functional response.
#IntrinsicActivity
#IntrinsicEfficacy
#JunaidAsgharPhD
Intrinsic activity (IA) (often called as Efficacy) refers to the relative ability of a drug-receptor complex to produce a maximum functional response.
#IntrinsicActivity
#IntrinsicEfficacy
#JunaidAsgharPhD
Dr. Marvin Nieman, from the department of Pharmacology at Case Western Reserve University, gives a brief overview of important pharmacodynamic principles.
Dr. Marvin Nieman, from the department of Pharmacology at Case Western Reserve University, gives a brief overview of important pharmacodynamic principles.
Dr. Marvin Nieman, from the department of Pharmacology at Case Western Reserve University, gives a brief overview of important pharmacodynamic principles.
TALE 26 : INTRINSIC ACTIVITY OF A DRUG & QUANTAL DOSE-RESPONSE RELATIONSHP
VIDEO GUIDE
00:14
Intrinsic Activity and Quantal dose response relationship
00:24...
TALE 26 : INTRINSIC ACTIVITY OF A DRUG & QUANTAL DOSE-RESPONSE RELATIONSHP
VIDEO GUIDE
00:14
Intrinsic Activity and Quantal dose response relationship
00:24
Introduction to intrinsic activity
Classification of drugs
-Full Agonist
-Partial agonist
-Inverse agonist
-Antagonist
01:05
Full Agonist
04:41
Partial Agonist
07:03
Inverse Agonist
08:08
Antagonist
Competitive antagonist
Irreversible antagonist
Allosteric antagonist
Functional antagonist
14:32
Quantal dose response relationship
Therapeutic index
19:50
Summary
Download "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Test and other GPAT Materials - https://play.goo...
Download "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Test and other GPAT Materials - https://play.google.com/store/apps/details?id=co.bolton.nqilv
Pharmacology is all about the study of drug and their effect on the body along with body responsible for the drug taken. The drug gives its action mainly through the receptor.
Receptors are the macromolecule or binding site located at the surface or inside the cell. They are used to recognize the signal or drug molecule and initiate the biological response.
The biological response is generally given by any drug using any of these mechanisms- (1) Enzyme (2) Ion channels (3) Transport (4) Receptor. In biochemistry and pharmacology, a receptor is a protein molecule that receives chemical signals from outside a cell. When such chemical signals bind to a receptor, they cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell.
A receptor is a protein which binds to a specific molecule. The molecule it binds is known as the ligand. A ligand may be any molecule, from inorganic minerals to organism-created proteins, hormones, and neurotransmitters. The ligand binds to the ligand-binding site on the receptor protein. When this binding happens, the receptor undergoes a conformational change. This change shapes slightly alters the protein’s function. From this, a number of things can happen. The conformational change in the receptor can cause the receptor to become an enzyme and actively combine or separate certain molecules
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Download "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Test and other GPAT Materials - https://play.google.com/store/apps/details?id=co.bolton.nqilv
Pharmacology is all about the study of drug and their effect on the body along with body responsible for the drug taken. The drug gives its action mainly through the receptor.
Receptors are the macromolecule or binding site located at the surface or inside the cell. They are used to recognize the signal or drug molecule and initiate the biological response.
The biological response is generally given by any drug using any of these mechanisms- (1) Enzyme (2) Ion channels (3) Transport (4) Receptor. In biochemistry and pharmacology, a receptor is a protein molecule that receives chemical signals from outside a cell. When such chemical signals bind to a receptor, they cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell.
A receptor is a protein which binds to a specific molecule. The molecule it binds is known as the ligand. A ligand may be any molecule, from inorganic minerals to organism-created proteins, hormones, and neurotransmitters. The ligand binds to the ligand-binding site on the receptor protein. When this binding happens, the receptor undergoes a conformational change. This change shapes slightly alters the protein’s function. From this, a number of things can happen. The conformational change in the receptor can cause the receptor to become an enzyme and actively combine or separate certain molecules
Get in touch with the solution by just clicking following links-
Facebook Page- https://www.facebook.com/pharmavideo/
Facebook Group- https://www.facebook.com/groups/solutionpharamcy
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Time Stamps:
00:00 Resting State of the Receptor and Receptor Activation
01:21 Intrinsic Activity/ Intrinsic Efficacy
03:20 Intrinsic Activity of Full, Partial ...
Time Stamps:
00:00 Resting State of the Receptor and Receptor Activation
01:21 Intrinsic Activity/ Intrinsic Efficacy
03:20 Intrinsic Activity of Full, Partial and Inverse Agonists
09:15 Full, Partial and Inverse Agonists on a bar graph
12:48 Concentration-Response Curve (CRC) or Dose-response Curve (DRC)
14:54 Efficacy and Potency
26:39 Spare Receptors/ Reserve Receptors
The efficacy of a drug is the maximum response achievable from a drug regardless of the drug potency.
Note that a drug may have a high efficacy but not be potent, i.e. the drug may have a high maximal response (Emax) but require a lot of the drug to do so. If an analgesic can relieve hundred percent of a patient's pain but requires 2000 mg to do so, this drug has a high efficacy but a low potency. Conversely, a drug can have a high potency (small amount of drug required to get 50% of the maximal response) but have a low efficacy (partial agonist).
A drug can be less potent but still highly efficacious (Emax = 100%). Do not get confused by this concept. Remember potency and efficacy are independent of each other. Refer to the graphs in this video to illustrate this concept.
This video lecture is on:
#IntrinsicActivity
#EfficacyAndPotency
#FullandPartialAgonist
#SpareReceptors
GraphPad Prism Video:
Title: How to determine EC50 (Potency) in Prism?
Link: https://youtu.be/2js_cNqRI8Y
Time Stamps:
00:00 Resting State of the Receptor and Receptor Activation
01:21 Intrinsic Activity/ Intrinsic Efficacy
03:20 Intrinsic Activity of Full, Partial and Inverse Agonists
09:15 Full, Partial and Inverse Agonists on a bar graph
12:48 Concentration-Response Curve (CRC) or Dose-response Curve (DRC)
14:54 Efficacy and Potency
26:39 Spare Receptors/ Reserve Receptors
The efficacy of a drug is the maximum response achievable from a drug regardless of the drug potency.
Note that a drug may have a high efficacy but not be potent, i.e. the drug may have a high maximal response (Emax) but require a lot of the drug to do so. If an analgesic can relieve hundred percent of a patient's pain but requires 2000 mg to do so, this drug has a high efficacy but a low potency. Conversely, a drug can have a high potency (small amount of drug required to get 50% of the maximal response) but have a low efficacy (partial agonist).
A drug can be less potent but still highly efficacious (Emax = 100%). Do not get confused by this concept. Remember potency and efficacy are independent of each other. Refer to the graphs in this video to illustrate this concept.
This video lecture is on:
#IntrinsicActivity
#EfficacyAndPotency
#FullandPartialAgonist
#SpareReceptors
GraphPad Prism Video:
Title: How to determine EC50 (Potency) in Prism?
Link: https://youtu.be/2js_cNqRI8Y
Intrinsic activity (IA) (often called as Efficacy) refers to the relative ability of a drug-receptor complex to produce a maximum functional response.
#IntrinsicActivity
#IntrinsicEfficacy
#JunaidAsgharPhD
Dr. Marvin Nieman, from the department of Pharmacology at Case Western Reserve University, gives a brief overview of important pharmacodynamic principles.
Download "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Test and other GPAT Materials - https://play.google.com/store/apps/details?id=co.bolton.nqilv
Pharmacology is all about the study of drug and their effect on the body along with body responsible for the drug taken. The drug gives its action mainly through the receptor.
Receptors are the macromolecule or binding site located at the surface or inside the cell. They are used to recognize the signal or drug molecule and initiate the biological response.
The biological response is generally given by any drug using any of these mechanisms- (1) Enzyme (2) Ion channels (3) Transport (4) Receptor. In biochemistry and pharmacology, a receptor is a protein molecule that receives chemical signals from outside a cell. When such chemical signals bind to a receptor, they cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell.
A receptor is a protein which binds to a specific molecule. The molecule it binds is known as the ligand. A ligand may be any molecule, from inorganic minerals to organism-created proteins, hormones, and neurotransmitters. The ligand binds to the ligand-binding site on the receptor protein. When this binding happens, the receptor undergoes a conformational change. This change shapes slightly alters the protein’s function. From this, a number of things can happen. The conformational change in the receptor can cause the receptor to become an enzyme and actively combine or separate certain molecules
Get in touch with the solution by just clicking following links-
Facebook Page- https://www.facebook.com/pharmavideo/
Facebook Group- https://www.facebook.com/groups/solutionpharamcy
Instagram- https://www.instagram.com/solutionpharmacy/
Mail Us for Free Pharmacology Materials- [email protected]
LinkedIn- http://linkedin.com/in/pushpendrakpatel
Time Stamps:
00:00 Resting State of the Receptor and Receptor Activation
01:21 Intrinsic Activity/ Intrinsic Efficacy
03:20 Intrinsic Activity of Full, Partial and Inverse Agonists
09:15 Full, Partial and Inverse Agonists on a bar graph
12:48 Concentration-Response Curve (CRC) or Dose-response Curve (DRC)
14:54 Efficacy and Potency
26:39 Spare Receptors/ Reserve Receptors
The efficacy of a drug is the maximum response achievable from a drug regardless of the drug potency.
Note that a drug may have a high efficacy but not be potent, i.e. the drug may have a high maximal response (Emax) but require a lot of the drug to do so. If an analgesic can relieve hundred percent of a patient's pain but requires 2000 mg to do so, this drug has a high efficacy but a low potency. Conversely, a drug can have a high potency (small amount of drug required to get 50% of the maximal response) but have a low efficacy (partial agonist).
A drug can be less potent but still highly efficacious (Emax = 100%). Do not get confused by this concept. Remember potency and efficacy are independent of each other. Refer to the graphs in this video to illustrate this concept.
This video lecture is on:
#IntrinsicActivity
#EfficacyAndPotency
#FullandPartialAgonist
#SpareReceptors
GraphPad Prism Video:
Title: How to determine EC50 (Potency) in Prism?
Link: https://youtu.be/2js_cNqRI8Y
Intrinsic activity (IA) or efficacy refers to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC50, which is a measure of the potency of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by Stephenson (1956) to describe the way in which agonists vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system.
Agonists of lower efficacy are not as efficient at producing a response from the drug-bound receptor, by stabilizing the active form of the drug-bound receptor. Therefore, they may not be able to produce the same maximal response, even when they occupy the entire receptor population, as the efficiency of transformation of the inactive form of the drug-receptor complex to the active drug-receptor complex may not be high enough to evoke a maximal response. Since the observed response may be less than maximal in systems with no spare receptor reserve, some low efficacy agonists are referred to as partial agonists.