Competitive antagonist
Encyclopedia
A competitive antagonist is a receptor antagonist
that binds to a receptor
but does not activate the receptor. The antagonist will compete with available agonist
for receptor binding site
s on the same receptor. Sufficient antagonist will displace the agonist from the binding sites, resulting in a lower frequency of receptor activation.
Presence of a competitive antagonist will shift an agonism dose-response curve to the right. A Schild plot for a competitive antagonist will have a slope equal to 1, and the X-intercept and Y-intercept will each equal the dissociation constant
of the antagonist.
A competitive antagonist can be reversible competitive antagonist or irreversible competitive antagonist.
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
that binds to a receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
but does not activate the receptor. The antagonist will compete with available agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
for receptor binding site
Binding site
In biochemistry, a binding site is a region on a protein, DNA, or RNA to which specific other molecules and ions—in this context collectively called ligands—form a chemical bond...
s on the same receptor. Sufficient antagonist will displace the agonist from the binding sites, resulting in a lower frequency of receptor activation.
Presence of a competitive antagonist will shift an agonism dose-response curve to the right. A Schild plot for a competitive antagonist will have a slope equal to 1, and the X-intercept and Y-intercept will each equal the dissociation constant
Dissociation constant
In chemistry, biochemistry, and pharmacology, a dissociation constant is a specific type of equilibrium constant that measures the propensity of a larger object to separate reversibly into smaller components, as when a complex falls apart into its component molecules, or when a salt splits up into...
of the antagonist.
A competitive antagonist can be reversible competitive antagonist or irreversible competitive antagonist.