Agonist: Difference between revisions

>Sir Kibs
Added a section on partial agonists
>David Hedlund
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[[File:Efficacy spectrum.png|thumbnail|275px|Efficacy spectrum of receptor ligands]]
[[File:Efficacy spectrum.png|thumbnail|275px|Efficacy spectrum of receptor ligands]]
[[File:Inverse_agonist_3.svg|thumbnail|275px|Dose response curves of receptor ligands]]
[[File:Inverse_agonist_3.svg|thumbnail|275px|Dose response curves of receptor ligands]]
An '''agonist''' is a chemical that binds to the [[receptor]] of a cell and activates the receptor to cause a physiological response. An agonist initiates the same reaction typically produced by the binding of an endogenous ligand (such as a hormone or neurotransmitter) with a receptor.<ref>Agonist definition (Merriam-Webster) http://www.merriam-webster.com/dictionary/agonist</ref> A drug’s ability to affect a given receptor is dependent on the drug’s affinity and intrinsic efficacy towards that receptor. The affinity of a drug describes the strength of attraction between it and a given receptor, and consequently its ability to bind to that receptor. A drug with a high affinity for a receptor has a high likelihood of binding to it, while a drug with a low affinity has a lesser degree of attraction towards a receptor.  
An '''agonist''' is a chemical that binds to the [[receptor]] of a cell and activates the receptor to cause a physiological response. An agonist initiates the same reaction typically produced by the binding of an endogenous ligand (such as a hormone or neurotransmitter) with a receptor.<ref>{{Citation | title=Definition of AGONIST | url=https://www.merriam-webster.com/dictionary/agonist}}</ref> A substance's ability to affect a given receptor is dependent on the substance's affinity and intrinsic efficacy towards that receptor. The affinity of a substance describes the strength of attraction between it and a given receptor, and consequently its ability to bind to that receptor. A substance with a high affinity for a receptor has a high likelihood of binding to it, while a substance with a low affinity has a lesser degree of attraction towards a receptor.  


This contrasts the efficacy of a drug, which describes a drug's capacity to produce a response when bound to a receptor. A drug with high efficacy will produce a proportionally stronger effect than a drug of lower efficacy occupying the same number of receptors. The maximum efficacy of a drug reflects the greatest attainable response to a particular drug on a receptor set regardless of dose. A drug with a high efficacy may need to occupy less receptors to produce maximum effects, meaning it will not produce stronger effects beyond a certain dosage.   
This contrasts the efficacy of a substance, which describes a substance's capacity to produce a response when bound to a receptor. A substance with high efficacy will produce a proportionally stronger effect than a substance of lower efficacy occupying the same number of receptors. The maximum efficacy of a substance reflects the greatest attainable response to a particular substance on a receptor set regardless of dose. A substance with a high efficacy may need to occupy fewer receptors to produce maximum effects, meaning it will not produce stronger effects beyond a certain dosage.   


In contrast to an agonist, an [[antagonist]] is a chemical that binds to the receptor of a cell without causing a physiological response. Receptor antagonists work by blocking or diminishing the effects produced by endogenous or drug-induced agonism of a receptor.  
In contrast to an agonist, an [[antagonist]] is a chemical that binds to the receptor of a cell without causing a physiological response. Receptor antagonists work by blocking or diminishing the effects produced by endogenous or substance-induced agonism of a receptor.  
==Types of agonists==
==Types of agonists==
[[Receptors]] can be activated by chemicals produced by the body (endogenous) or chemicals from outside of the body (exogenous). Therefore, an endogenous agonist for a particular receptor is a chemical produced in the body that binds to and activates that receptor. For example, [[serotonin]] is the endogenous agonist of serotonin receptors.  
[[Receptors]] can be activated by chemicals produced by the body (endogenous) or chemicals from outside of the body (exogenous). Therefore, an endogenous agonist for a particular receptor is a chemical produced in the body that binds to and activates that receptor. For example, [[serotonin]] is the endogenous agonist of serotonin receptors.  
===Agonists===
===Agonists===
There are several types of agonist:
There are several types of agonist:
*A '''superagonist''' is an agonist that produces a greater effect from the receptor than the endogenous agonist, and therefore has an efficacy of over 100%.
*A '''superagonist''' is an agonist that produces a greater effect from the receptor than the endogenous agonist, and therefore has an efficacy of over 100%.
*A '''full agonist''' binds and activates a receptor with an efficacy equal to the endogenous agonist. For example, [[heroin]] mimics the action of endorphins on μ-opioid receptors in the nervous system.
*A '''full agonist''' binds and activates a receptor with an efficacy equal to the endogenous agonist. For example, [[heroin]] mimics the action of endorphins on μ-opioid receptors in the nervous system.
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==See also==
==See also==
*[[Responsible use]]
*[[Responsible use]]
*[[Scientific information]]
*[[Scientific information]]
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==External links==
==External links==
*[https://en.wikipedia.org/wiki/Agonist Agonist (Wikipedia)]
*[https://en.wikipedia.org/wiki/Agonist Agonist (Wikipedia)]
==References==
==References==
<references/>
<references />
[[Category:Neuroscience]]
 
[[Category:Pharmacology]]
 
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