Changes: Nicotinic antagonist

Latest revision as of 18:46, September 12, 2012

Biological: Behavioural genetics · Evolutionary psychology · Neuroanatomy · Neurochemistry · Neuroendocrinology · Psychoneuroimmunology · Physiological Psychology · Psychopharmacology

A nicotinic antagonist is a type of anticholinergic which inhibits the action at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, but some centrally acting compounds such as mecamylamine and 18-methoxycoronaridine block nicotinic acetylcholine receptors in the brain and can be used for treating drug addiction.

Comparison
Mechanism	Antagonist	Preferred receptor	Clinical use
Ganglionic blocking agents	Hexamethonium	Ganglion type	none^[1]
	Mecamylamine	Ganglion type
	Trimethaphan	Ganglion type	Rarely used for blood pressure decrease during surgery^[1]
Nondepolarizing neuromuscular blocking agents	Atracurium	Muscle type	muscle relaxant in anaesthesia^[1]
	Doxacurium	Muscle type
	Mivacurium	Muscle type
	Pancuronium	Muscle type	muscle relaxant in anaesthesia^[1]
	Tubocurarine	Muscle type	Rarely used ^[1]
	Vecuronium	Muscle type	muscle relaxant in anaesthesia^[1]
Depolarizing neuromuscular blocking agents	Succinylcholine	Muscle type
Centrally acting nicotinic antagonists	18-Methoxycoronaridine	α3β4

ReferencesEdit

↑ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 149

External linksEdit

MeSH Nicotinic+antagonists

v·d·e Antiaddictives (N07B)
Nicotine dependence/ (Nicotinic agonist)	Nicotine • Dianicline • Varenicline • Lobeline • Mecamylamine • Scopolamine NDRI (Bupropion) • AA (Clonidine) • CB1 (Surinabant)
Alcohol dependence	AD inhibitor (Disulfiram, Calcium carbimide) • mGluR (Acamprosate) • Opioid receptor antagonists (Naltrexone, Nalmefene) • Topiramate • AA (Clonidine) • Baclofen
Opioid dependence	Buprenorphine • Methadone • Levacetylmethadol • Dihydrocodeine • Dihydroetorphine • AA (Clonidine) • Lofexidine • Extended Release Morphine • Extended Release Hydromorphone • Baclofen • Ibogaine
Stimulant dependence	Dextroamphetamine • NDRI (Bupropion) • DRI (Vanoxerine) • Nocaine • GABA analogue (Vigabatrin)
Benzodiazepine dependence	AA (Clonidine) • benzodiazepine (Diazepam) • Phenytoin • barbiturate (Phenobarbital)
Cocaine dependence	NDRI (Bupropion) • DRI (Vanoxerine) • Nocaine • Baclofen • GABA analogue (Vigabatrin)
Sedative-Hypnotic dependence	barbiturate (Phenobarbital) • benzodiazepine (Diazepam, Lorazepam) • AA (Clonidine) • Chloral hydrate
Template:Central nervous system navs

Template:Antihypertensives and diuretics

v·d·e

Cholinergics

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Receptor ligands

mAChR

Agonists: 77-LH-28-1 • AC-42 • AC-260,584 • Aceclidine • Acetylcholine • AF30 • AF150(S) • AF267B • AFDX-384 • Alvameline • AQRA-741 • Arecoline • Bethanechol • Butyrylcholine • Carbachol • CDD-0034 • CDD-0078 • CDD-0097 • CDD-0098 • CDD-0102 • Cevimeline • cis-Dioxolane • Ethoxysebacylcholine • LY-593,039 • L-689,660 • LY-2,033,298 • McNA343 • Methacholine • Milameline • Muscarine • NGX-267 • Ocvimeline • Oxotremorine • PD-151,832 • Pilocarpine • RS86 • Sabcomeline • SDZ 210-086 • Sebacylcholine • Suberylcholine • Talsaclidine • Tazomeline • Thiopilocarpine • Vedaclidine • VU-0029767 • VU-0090157 • VU-0152099 • VU-0152100 • VU-0238429 • WAY-132,983 • Xanomeline • YM-796
Antagonists: 3-Quinuclidinyl Benzilate • 4-DAMP • Aclidinium Bromide • Anisodamine • Anisodine • Atropine • Atropine Methonitrate • Benactyzine • Benzatropine (Benztropine) • Benzydamine • BIBN 99 • Biperiden • Bornaprine • CAR-226,086 • CAR-301,060 • CAR-302,196 • CAR-302,282 • CAR-302,368 • CAR-302,537 • CAR-302,668 • CS-27349 • Cyclobenzaprine • Cyclopentolate • Darifenacin • DAU-5884 • Dimethindene • Dexetimide • DIBD • Dicyclomine (Dicycloverine) • Ditran • EA-3167 • EA-3443 • EA-3580 • EA-3834 • Elemicin • Etanautine • Etybenzatropine (Ethylbenztropine) • Flavoxate • Himbacine • HL-031,120 • Ipratropium bromide • J-104,129 • Hyoscyamine • Mamba Toxin 3 • Mamba Toxin 7 • Mazaticol • Mebeverine • Methoctramine • Metixene • Myristicin • N-Ethyl-3-Piperidyl Benzilate • N-Methyl-3-Piperidyl Benzilate • Orphenadrine • Otenzepad • Oxybutynin • PBID • PD-102,807 • Penehyclidine • Phenglutarimide • Phenyltoloxamine • Pirenzepine • Piroheptine • Procyclidine • Profenamine • RU-47,213 • SCH-57,790 • SCH-72,788 • SCH-217,443 • Scopolamine (Hyoscine) • Solifenacin • Telenzepine • Tiotropium bromide • Tolterodine • Trihexyphenidyl • Tripitamine • Tropatepine • Tropicamide • WIN-2299 • Xanomeline • Zamifenacin; Others: 1st Generation Antihistamines (Brompheniramine, chlorphenamine, cyproheptadine, dimenhydrinate, diphenhydramine, doxylamine, mepyramine/pyrilamine, phenindamine, pheniramine, tripelennamine, triprolidine, etc) • Tricyclic Antidepressants (Amitriptyline, doxepin, trimipramine, etc) • Tetracyclic Antidepressants (Amoxapine, maprotiline, etc) • Typical Antipsychotics (Chlorpromazine, thioridazine, etc) • Atypical Antipsychotics (Clozapine, olanzapine, quetiapine, etc)

nAChR

Agonists: 5-HIAA • A-84,543 • A-366,833 • A-582,941 • A-867,744 • ABT-202 • ABT-418 • ABT-560 • ABT-894 • Acetylcholine • Altinicline • Anabasine • Anatoxin-a • AR-R17779 • Butyrylcholine • Carbachol • Cotinine • Cytisine • Decamethonium • Desformylflustrabromine • Dianicline • Dimethylphenylpiperazinium • Epibatidine • Epiboxidine • Ethanol • Ethoxysebacylcholine • EVP-4473 • EVP-6124 • Galantamine • GTS-21 • Ispronicline • Lobeline • MEM-63,908 (RG-3487) • Nicotine • NS-1738 • PHA-543,613 • PHA-709,829 • PNU-120,596 • PNU-282,987 • Pozanicline • Rivanicline • Sazetidine A • Sebacylcholine • SIB-1508Y • SIB-1553A • SSR-180,711 • Suberylcholine • TC-1698 • TC-1734 • TC-1827 • TC-2216 • TC-5214 • TC-5619 • TC-6683 • Tebanicline • Tropisetron • UB-165 • Varenicline • WAY-317,538 • XY-4083
Antagonists: 18-Methoxycoronaridine • α-Bungarotoxin • α-Conotoxin • Alcuronium • Amantadine • Anatruxonium • Atracurium • Bupropion (Amfebutamone) • Chandonium • Chlorisondamine • Cisatracurium • Coclaurine • Coronaridine • Dacuronium • Decamethonium • Dextromethorphan • Dextropropoxyphene • Dextrorphan • Diadonium • DHβE • Dimethyltubocurarine (Metocurine) • Dipyrandium • Dizocilpine (MK-801) • Doxacurium • Duador • Esketamine • Fazadinium • Gallamine • Hexafluronium • Hexamethonium (Benzohexonium) • Ibogaine • Isoflurane • Ketamine • Kynurenic acid • Laudexium (Laudolissin) • Levacetylmethadol • Malouetine • Mecamylamine • Memantine • Methadone • Methorphan (Racemethorphan) • Methyllycaconitine • Metocurine • Mivacurium • Morphanol (Racemorphanol) • Neramexane • Nitrous Oxide • Pancuronium • Pempidine • Pentamine • Pentolinium • Phencyclidine • Pipecuronium • Radafaxine • Rapacuronium • Rocuronium • Surugatoxin • Suxamethonium (Succinylcholine) • Thiocolchicoside • Toxiferine • Trimethaphan • Tropeinium • Tubocurarine • Vecuronium • Xenon

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Reuptake inhibitors

Plasmalemmal


CHT Inhibitors	Hemicholinium-3 (Hemicholine; HC3) • Triethylcholine

Vesicular


VAChT Inhibitors	Vesamicol

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Enzyme inhibitors

Anabolism


ChAT inhibitors	1-(-Benzoylethyl)pyridinium • 2-(α-Naphthoyl)ethyltrimethylammonium • 3-Chloro-4-stillbazole • 4-(1-Naphthylvinyl)pyridine • Acetylseco hemicholinium-3 • Acryloylcholine • AF64A • B115 • BETA • CM-54,903 • N,N-Dimethylaminoethylacrylate • N,N-Dimethylaminoethylchloroacetate

Catabolism

AChE inhibitors

Reversible: Carbamates: Aldicarb • Bendiocarb • Bufencarb • Carbaryl • Carbendazim • Carbetamide • Carbofuran • Chlorbufam • Chloropropham • Ethienocarb • Ethiofencarb • Fenobucarb • Fenoxycarb • Formetanate • Furadan • Ladostigil • Methiocarb • Methomyl • Miotine • Oxamyl • Phenmedipham • Pinmicarb • Pirimicarb • Propamocarb • Propham • Propoxur; Stigmines: Ganstigmine • Neostigmine • Phenserine • Physostigmine • Pyridostigmine • Rivastigmine; Others: Acotiamide • Ambenonium • Donepezil • Edrophonium • Galantamine • Huperzine A • Minaprine • Tacrine • Zanapezil
Irreversible: Organophosphates: Acephate • Azinphos-methyl • Bensulide • Cadusafos • Chlorethoxyfos • Chlorfenvinphos • Chlorpyrifos • Chlorpyrifos-Methyl • Coumaphos • Cyclosarin (GF) • Demeton • Demeton-S-Methyl • Diazinon • Dichlorvos • Dicrotophos • Diisopropyl fluorophosphate (Guthion) • Diisopropylphosphate • Dimethoate • Dioxathion • Disulfoton • EA-3148 • Echothiophate • Ethion • Ethoprop • Fenamiphos • Fenitrothion • Fenthion • Fosthiazate • GV • Isofluorophate • Isoxathion • Malaoxon • Malathion • Methamidophos • Methidathion • Metrifonate • Mevinphos • Monocrotophos • Naled • Novichok agent • Omethoate • Oxydemeton-Methyl • Paraoxon • Parathion • Parathion-Methyl • Phorate • Phosalone • Phosmet • Phostebupirim • Phoxim • Pirimiphos-Methyl • Sarin (GB) • Soman (GD) • Tabun (GA) • Temefos • Terbufos • Tetrachlorvinphos • Tribufos • Trichlorfon • VE • VG • VM • VR • VX; Others: Demecarium • Onchidal (Onchidella binneyi)

BChE inhibitors

Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.

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Others


Precursors	Choline (Lecithin) • Citicoline • Cyprodenate • Dimethylethanolamine (DMAE, deanol) • Glycerophosphocholine • Meclofenoxate (Centrophenoxine) • Phosphatidylcholine • Phosphatidylethanolamine • Phosphorylcholine • Pirisudanol
Cofactors	Acetic acid • Acetylcarnitine • Acetyl-coA • Vitamin B₅ (Pantethine, Pantetheine, Panthenol)
Others	Acetylcholine releasing agents: α-Latrotoxin • β-Bungarotoxin; Acetylcholine release inhibitors: Botulinum toxin (Botox); Acetylcholinesterase reactivators: Asoxime • Obidoxime • Pralidoxime

v·d·e Muscle relaxants (M03)
Peripherally acting (primarily antinicotinic, neuromuscular-blocking drugs)	curare alkaloids (Alcuronium, Dimethyltubocurarine, Tubocurarine) - choline derivatives (Suxamethonium) - other quaternary ammonium compounds (Atracurium, Cisatracurium, Doxacurium chloride, Fazadinium bromide, Gallamine, Hexafluronium, Mivacurium chloride, Pancuronium, Pipecuronium bromide, Rocuronium bromide, Vecuronium) - other (Botulinum toxin)
Centrally acting	carbamic acid esters (Phenprobamate, Carisoprodol, Methocarbamol, Styramate, Febarbamate), Baclofen, Chlormezanone, Chlorzoxazone, Cyclobenzaprine, Lorazepam, Mephenesin, Orphenadrine, Phenyramidol, Pridinol, Tetrazepam, Thiocolchicoside, Tizanidine, Tolperisone
Directly acting	Dantrolene

v·d·e

Neuromodulation

Types

Enzyme: Inducer • Inhibitor
Ion channel: Opener • Blocker
Receptor: Agonist • Antagonist • Positive allosteric modulator (PAM) • Negative allosteric modulator (NAM) • Inverse agonist
Transporter [Reuptake]: Enhancer (RE) • Inhibitor (RI) • Releaser (RA)
Miscellaneous: Precursor • Cofactor

Classes

Enzyme

see Enzyme inhibition

Ion channel

Calcium channel blocker (CCB) • Potassium channel blocker (PCB) • Sodium channel blocker (SCB) • Potassium channel opener (PCO)

Receptor &
transporter

BA/M


Adrenergic	Adrenergic receptor agonist (α, β (1, 2)) • Adrenergic receptor antagonist (α (1, 2), β) • Adrenergic reuptake inhibitor (ARI)
Dopaminergic	Dopamine receptor agonist • Dopamine receptor antagonist • Dopamine reuptake inhibitor (DRI)
Histaminergic	Histamine receptor agonist • Histamine receptor antagonist (H₁, H₂, H₃)
Serotonergic	Serotonin receptor agonist • Serotonin Receptor Antagonist (5-HT₃) • Serotonin reuptake inhibitor (SRI) • Serotonin reuptake enhancer (SRE)


GABAergic	GABA receptor agonist • GABA receptor antagonist • GABA reuptake inhibitor (GRI)
Glutamatergic	Glutamate receptor agonist (AMPA) • Glutamate receptor antagonist (NMDA)

Cholinergic

Acetylcholine receptor agonist (Muscarinic, Nicotinic) • Acetylcholine receptor antagonist (Muscarinic, Nicotinic (Ganglionic, Muscular))

Endocannabinoid

Cannabinoid receptor agonist • Cannabinoid receptor antagonist

Opioid

Opioid receptor agonist • Opioid receptor antagonist

Other

Adenosine reuptake inhibitor (AdoRI) • Angiotensin II receptor antagonist • Endothelin receptor antagonist • NK₁ receptor antagonist • Vasopressin receptor antagonist

Miscellaneous

Cofactor (see Enzyme cofactors) • Precursor (see Amino acids)

v·d·e Receptor agonists, antagonists, and reuptake inhibitors
Dopamine receptor	Dopamine agonist • Dopamine antagonist • Dopamine reuptake inhibitor
5-HT (serotonin) receptor	Serotonin receptor agonist • Serotonin antagonist (5-HT₃) • Serotonin uptake inhibitor (SSRI)
Adrenergic receptor	Adrenergic agonist (Alpha, Beta₂) • Adrenergic antagonist (Alpha, Beta) • Adrenergic uptake inhibitor
Acetylcholine receptor	Cholinergic (Muscarinic, Nicotinic) • Anticholinergic (Muscarinic, Nicotinic) • Acetylcholinesterase inhibitor
Histamine receptor	Histamine agonist • Histamine antagonist (H₁, H₂)
GABA receptor	GABA agonist • GABA antagonist
NMDA receptor	NMDA receptor antagonist

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 {{Cholinergics}}
 {{Muscle relaxants}}
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 {{Receptor agonists and antagonists}}

Wikia

Changes: Nicotinic antagonist

Latest revision as of 18:46, September 12, 2012

ReferencesEdit

External linksEdit