Discussion
Ask a question about 'Competitive antagonist'
Start a new discussion about 'Competitive antagonist'
Answer questions from other users
|
A
competitive antagonist is a
receptor antagonistA 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
receptorIn 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
agonistAn 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 siteIn 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 constantIn 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.