Drug that inhibits the action of acetylcholine at nicotinic acetylcholine receptors
A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this type being tubocurarine,[1] but some centrally acting compounds such as bupropion, mecamylamine, and 18-methoxycoronaridine block nicotinic acetylcholine receptors in the brain and have been proposed for treating nicotine addiction.[medical citation needed]
Comparison
Mechanism
Antagonist
Preferred receptor
Clinical use
Ganglionic blocking agents
Hexamethonium
Ganglion type
None[2]
Mecamylamine
Ganglion type
Trimethaphan
Ganglion type
Rarely used for blood pressure decrease during surgery[2]
Nondepolarizing neuromuscular blocking agents
Atracurium
Muscle type
Muscle relaxant in anaesthesia[2]
Doxacurium
Muscle type
Mivacurium
Muscle type
Pancuronium
Muscle type
Muscle relaxant in anaesthesia[2]
Tubocurarine
Muscle type
Discovered in arrow poison it was the first pheripheral muscle relaxant. Rarely used since 1980s.[2]
Vecuronium
Muscle type
Muscle relaxant in anaesthesia[2]
Depolarizing neuromuscular blocking agents
Succinylcholine*
Muscle type
Centrally acting nicotinic antagonists
18-Methoxycoronaridine
α3β4
Bupropion
α3β4. α4β2, α1β1γδ
Antidepressant (NDRI)
Hydroxybupropion
α3β4. α4β2, α1β1γδ
Antidepressant (NDRI). Metabolite of bupropion.
Threohydrobupropion
α3β4.
Antidepressant (NDRI). Metabolite of bupropion.
Dextromethorphan
α3β4. α4β2, α7
Common over the counter antitussive.
Dextrorphan
α3β4. α4β2, α7
Metabolite of dextromethorphan; no accepted medical uses.
3-Methoxymorphinan
α3β4
Secondary metabolite of dextromethorphan; not used in medical practice. Unknown medical efficacy.
Note: Succinylcholine is a nicotinic agonist. See neuromuscular blocking agents page for details on the mechanism of action.
^P. Taylor (1990). In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th Ed., (A. G. Gilman et al., Eds.), pp. 166-186, New York: Pergamon Press.
^ abcdefRang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 149
and 25 Related for: Nicotinic antagonist information
ISBN 0-443-07145-4. Page 149 Media related to Nicotinicantagonists at Wikimedia Commons Nicotinic+antagonists at the U.S. National Library of Medicine Medical...
withdrawal symptoms. Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9...
Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond...
A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity...
in the autonomic nervous system, often by acting as a nicotinic receptor antagonist. Nicotinic acetylcholine receptors are found on skeletal muscle, but...
negligible affinity for the NMDA receptor but potent alpha-7 nicotinic receptor antagonist activity, may have antidepressant action. This furthers the...
Hexamethonium is a non-depolarising ganglionic blocker, a neuronal nicotinic (nAChR) receptor antagonist that acts in autonomic ganglia by binding mostly in or on...
is a dissociative anesthetic. PCP works primarily as an NMDA receptor antagonist. PCP is most commonly used in the United States. While usage peaked in...
NMDA receptor. As an antagonist of the α7 nicotinic acetylcholine receptor. However, recently (2011) direct recording of α7 nicotinic acetylcholine receptor...
names Inversine, Vecamyl) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s...
as a norepinephrine–dopamine reuptake inhibitor (NDRI) and a nicotinic receptor antagonist. However, its effects on dopamine are weak and clinical significance...
receptor antagonist or an inverse agonist at histamine receptors. Only a few currently marketed H1-antihistamines are known to function as antagonists. Histamine...
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...
widespread drug resistance. It acts as a nicotinicantagonist, dopamine agonist, and noncompetitive NMDA antagonist. The antiviral mechanism of action is...
are stimulants, others are antiviral, have competitive NMDA antagonist activity, or are nicotinic receptor antagonists. Isometheptene Heptaminol v t e...
acetylcholinesterase inhibitor. It is also a nicotinicantagonist. Cholinesterase inhibitor Nicotinicantagonist FULTON, MP; MOGEY, GA (June 1954). "Some...
negligibly active as NMDA receptor antagonists in comparison, but retain activity as potent antagonists of the α7-nicotinic acetylcholine receptor. Ketamine...
A dopamine antagonist, also known as an anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors...
Medications that lower seizure threshold include the antidepressant and nicotinicantagonist bupropion, the atypical opioid analgesics tramadol and tapentadol...
selective 5-HT3 receptor antagonist and α7-nicotinic receptor partial agonist. Tropisetron have been shown to sensitise human α7-nicotinic receptors to low concentrations...
Global Information