Type of receptor ligand or drug that blocks a biological response
Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor–agonist coupling.
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.[1] They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers. In pharmacology, antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors. Antagonists mediate their effects by binding to the active site or to the allosteric site on a receptor, or they may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity. Antagonist activity may be reversible or irreversible depending on the longevity of the antagonist–receptor complex, which, in turn, depends on the nature of antagonist–receptor binding. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally defined binding sites on receptors.[2]
^"Pharmacology Guide: In vitro pharmacology: concentration-response curves." GlaxoWellcome. Retrieved on December 6, 2007.
A receptorantagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than...
NMDA receptorantagonists are a class of drugs that work to antagonize, or inhibit the action of, the N-Methyl-D-aspartate receptor (NMDAR). They are commonly...
at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment...
antagonist, or serotonin receptorantagonist, is a drug used to inhibit the action of serotonin and serotonergic drugs at serotonin (5-HT) receptors....
A mineralocorticoid receptorantagonist (MRA or MCRA) or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid...
A cannabinoid receptorantagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of cannabinoidergic drug that binds...
endothelin receptorantagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: selective ETA receptorantagonists (sitaxentan...
receptor and heightens the receptor's activity; the receptorantagonists work by binding to the receptor and blocking the activation of the receptor by...
An H3 receptorantagonist is a type of antihistaminic drug used to block the action of histamine at H3 receptors. Unlike the H1 and H2 receptors which...
dopamine antagonist, also known as an anti-dopaminergic and a dopamine receptorantagonist (DRA), is a type of drug which blocks dopamine receptors by receptor...
boost the efficacy of 5-HT3 antagonists to prevent nausea and vomiting. The discovery of neurokinin 1 (NK1) receptorantagonists was a turning point in the...
receptor over the presynaptic D2 autoreceptor. Piribedil – also D3 receptor agonist and α2–adrenergic antagonist Pramipexole – also D3, D4 receptor agonist...
A muscarinic receptorantagonist (MRA), also called an antimuscarinic, is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine...
A vasopressin receptorantagonist (VRA) is an agent that interferes with action at the vasopressin receptors. Most commonly VRAs are used in the treatment...
An opioid antagonist, or opioid receptorantagonist, is a receptorantagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone...
receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is...
An orexin receptorantagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptorantagonist of one (selective...
and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens...
treatment of most patients. Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline)...
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin...
GABA receptorantagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used...
CCR5 receptorantagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process...
CB2 receptors but acts as an indirect antagonist of cannabinoid agonists. It was found to be an antagonist at the putative new cannabinoid receptor, GPR55...
An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, which are divided into two...
anticholinergics by activating nicotinic acetylcholine receptors. Caffeine (although an adenosine receptorantagonist) can counteract the anticholinergic symptoms...
H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic...
α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically...
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