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Psychopharmacology
(Index , Outline )
Muscarine
A muscarinic receptor agonist is an agent that activates the activity of the muscarinic acetylcholine receptor . The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.
Clinical significance [ ] M1 [ ] M1-type muscarinic acetylcholine receptors play a role in cognitive processing. In Alzheimer disease (AD) amyloid formation may decrease the ability of these receptors to transmit signals leading to decrease cholinergic activity. As these receptors themselves appear relatively unchanged in the disease process, they have become a potential therapeutic target when trying to improve cognitive function in patients with AD.[1] [2] [3]
A number of muscarinic agonists have been developed and are under investigation to treat AD. These agents show promise as they are neurotrophic , decrease amyloid depositions, and improve damage due to oxidative stress . Tau -phosphorylation is decreased and cholinergic function enhanced. Notably several agents of the AF series of muscarinic agonists have become the focus of such research:. AF102B, AF150(S), AF267B . In animal models that are mimicking the damage of AD, these agents appear promising.
The agent xanomeline has been proposed as a potential treatment for schizophrenia .[4] [5]
M3 [ ] In the form of pilocarpine , muscarinic receptor agonists have been used medically for a short time.
M3 agonists
Aceclidine Arecoline Betel nut .Pilocarpine glaucoma .Cevimeline Food and Drug Administration (FDA)-approved drug and used for the management of dry mouth in Sjögren's syndrome . Muscarinic versus nicotinic activity [ ] See also [ ] References [ ]
↑ Fisher A, Brandeis R, Bar-Ner RH, Kliger-Spatz M, Natan N, Sonego H, Marcovitch I, Pittel Z. AF150(S) and AF267B: M1 muscarinic agonists as innovative therapies for Alzheimer's disease. J Mol Neurosci . 2002 Aug-Oct;19(1-2):145-53. PMID 12212772
↑ Fisher A. M1 muscarinic agonists: Their potential in treatment and as disease-modifying agents in Alzheimer's disease Drug Dev. Res. 50:291-297, 2000. [1]
↑ Fisher A (July 2008). Cholinergic treatments with emphasis on m1 muscarinic agonists as potential disease-modifying agents for Alzheimer's disease . Neurotherapeutics 5 (3): 433–42. ↑ Shekhar A, Potter WZ, Lightfoot J, et al. (July 2008). Selective Muscarinic Receptor Agonist Xanomeline as a Novel Treatment Approach for Schizophrenia. Am J Psychiatry 165 (8): 1033–9. ↑ Sellin AK, Shad M, Tamminga C. (November 2008). Muscarinic agonists for the treatment of cognition in schizophrenia . CNS Spectrums 13 (1): 985–96. ↑ Unless else specified in boxes, then reference is: Table 10-3 in: Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). Rang & Dale's pharmacology , Edinburgh: Churchill Livingstone.
External links [ ]
Cholinergics
Receptor ligands
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 BenzilateN -Methyl-3-Piperidyl BenzilateOrphenadrine • 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)
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
Reuptake inhibitors
Plasmalemmal
CHT Inhibitors
Hemicholinium-3 (Hemicholine; HC3) • Triethylcholine
Enzyme 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 -DimethylaminoethylacrylateN ,N -Dimethylaminoethylchloroacetate
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
Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
Others
Choline (Lecithin ) • Citicoline • Cyprodenate • Dimethylethanolamine (DMAE, deanol) • Glycerophosphocholine • Meclofenoxate (Centrophenoxine) • Phosphatidylcholine • Phosphatidylethanolamine • Phosphorylcholine • Pirisudanol
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
