- 関
- muscarinic agonist、muscarinic cholinergic agonist
WordNet
- (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
- a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
- someone involved in a contest or battle (as in an agon)
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/17 12:18:25」(JST)
[Wiki en表示]
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.
Contents
- 1 Clinical significance
- 2 Muscarinic versus nicotinic activity
- 3 Muscarinic Acetylcholine Receptor Subtypes
- 4 See also
- 5 References
- 6 External links
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 decreased 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, for glaucoma.
- Arecoline, an alkaloid present in the Betel nut.
- Pilocarpine is a drug that acts as a muscarinic receptor agonist that is used to treat glaucoma.
- Cevimeline (AF102B) (Evoxac) is a muscarinic agonist that is an Food and Drug Administration (FDA)-approved drug and used for the management of dry mouth in Sjögren's syndrome.
Muscarinic versus nicotinic activity
| Comparison of cholinergic agonists [6] |
| Substance |
Receptor specificity |
Hydrolysis by
acetylcholinesterase |
Comments |
| Muscarinic |
Nicotinic |
| Choline |
+++ |
+++ |
++ |
Essential nutrient |
| Acetylcholine |
+++ |
+++ |
+++ |
Endogenous ligand |
| Carbachol |
++ |
+++ |
- |
Used in the treatment of glaucoma |
| Methacholine |
+++ |
+ |
++ |
Used to diagnose bronchial hyperreactivity,[7] a hallmark of asthma and COPD. |
| Bethanechol |
+++ |
- |
- |
Used in bladder and gastrointestinal hypotonia. |
| Muscarine |
+++ |
- |
- |
Natural alkaloid found in certain mushrooms. Cause of mushroom poisoning |
| Nicotine |
- |
+++ |
- |
Natural alkaloid found in the tobacco plant. |
| Pilocarpine |
++ |
- |
- |
Used in glaucoma. |
| Oxotremorine |
++ |
- |
- |
Used in research to induce symptoms of Parkinson's disease. |
Muscarinic Acetylcholine Receptor Subtypes
The targets for Muscarinic agonists include the following receptors:
| Receptor/Transporter Protein |
| M1 |
| M2 |
| M3 |
| M4 |
| M5 |
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. doi:10.1016/j.nurt.2008.05.002. PMID 18625455.
- ^ 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. doi:10.1176/appi.ajp.2008.06091591. PMID 18593778.
- ^ Sellin AK, Shad M, Tamminga C. (November 2008). "Muscarinic agonists for the treatment of cognition in schizophrenia". CNS Spectrums 13 (1): 985–96. PMID 19037177.
- ^ 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. ISBN 0-443-06911-5.
- ^ Birnbaum S, Barreiro TJ (June 2007). "Methacholine challenge testing: identifying its diagnostic role, testing, coding, and reimbursement". Chest 131 (6): 1932–5. doi:10.1378/chest.06-1385. PMID 17565027.
External links
- Muscarinic Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
|
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)
|
|
|
Histamitic
|
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
|
|
|
Serotonergic
|
- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
|
|
|
|
AA
|
|
GABAergic
|
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
|
|
Glutamitic
|
- 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)
|
|
|
|
Cholinergics
|
|
|
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
- Choline
- 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
- Suberyldicholine
- 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
- Etanautine
- Etybenzatropine/Ethylbenztropine
- Flavoxate
- Himbacine
- HL-031,120
- Ipratropium bromide
- J-104,129
- Hyoscyamine
- Mamba Toxin 3
- Mamba Toxin 7
- Mazaticol
- Mebeverine
- Methoctramine
- Metixene
- N-Ethyl-3-Piperidyl Benzilate
- N-Methyl-3-Piperidyl Benzilate
- Orphenadrine
- Otenzepad
- Oxybutynin
- PBID
- PD-102,807
- PD-0298029
- 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, 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
- Butinoline
- Butyrylcholine
- Carbachol
- Choline
- Cotinine
- Cytisine
- Decamethonium
- Desformylflustrabromine
- Dianicline
- Dimethylphenylpiperazinium
- Epibatidine
- Epiboxidine
- Ethanol
- Ethoxysebacylcholine
- EVP-4473
- EVP-6124
- Galantamine
- GTS-21
- Ispronicline
- Levamisole
- Lobeline
- MEM-63,908/RG-3487
- Morantel
- Nicotine
- NS-1738
- PHA-543,613
- PHA-709,829
- PNU-120,596
- PNU-282,987
- Pozanicline
- Rivanicline
- RJR-2429
- Sazetidine A
- Sebacylcholine
- SIB-1508Y
- SIB-1553A
- SSR-180,711
- Suberyldicholine
- Suxamethonium/Succinylcholine
- 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
- Chandonium
- Chlorisondamine
- Cisatracurium
- Coclaurine
- Coronaridine
- Dacuronium
- Decamethonium
- Dextromethorphan
- Dextropropoxyphene
- Dextrorphan
- Diadonium
- DHβE
- Dihydrochandonium
- Dimethyltubocurarine/Metocurine
- Dipyrandium
- Dizocilpine/MK-801
- Doxacurium
- Esketamine
- Fazadinium
- Gallamine
- Hexafluronium
- Hexamethonium/Benzohexonium
- Hydroxybupropion
- Ibogaine
- Isoflurane
- Ketamine
- Kynurenic acid
- Laudexium/Laudolissin
- Levacetylmethadol
- Malouetine
- Mecamylamine
- Memantine
- Methadone (Levomethadone)
- Methorphan/Racemethorphan
- Methyllycaconitine
- Metocurine
- Mivacurium
- Morphanol/Racemorphan
- Neramexane
- Nitrous Oxide
- Pancuronium
- Pempidine
- Pentamine
- Pentolinium
- Phencyclidine
- Pipecuronium
- Radafaxine
- Rapacuronium
- Rocuronium
- Surugatoxin
- Thiocolchicoside
- Toxiferine
- Trimethaphan
- Tropeinium
- Tubocurarine
- Vecuronium
- Xenon
|
|
|
|
|
Reuptake inhibitors
|
|
|
Plasmalemmal
|
|
CHT Inhibitors
|
- Hemicholinium-3/Hemicholine
- Triethylcholine
|
|
|
|
Vesicular
|
|
|
|
|
|
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
|
|
|
|
BChE inhibitors
|
- Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
|
|
|
|
|
|
Others
|
|
|
Precursors
|
- Choline (Lecithin)
- Citicoline
- Cyprodenate
- Dimethylethanolamine
- 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
|
|
|
|
UpToDate Contents
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English Journal
- Identification of natural lactoylcholine in lactic acid bacteria-fermented food.
- Nakamura K1, Okitsu S2, Ishida R3, Tian S4, Igari N5, Amano Y6.
- Food chemistry.Food Chem.2016 Jun 15;201:185-9. doi: 10.1016/j.foodchem.2016.01.055. Epub 2016 Jan 14.
- Acetylcholine (AcCh) is a major neurotransmitter and an agonist of nicotinic and muscarinic receptors in non-neuronal systems. Artificially synthesized lactoylcholine (LaCh) has potent nicotinic activity equal to that of AcCh. In this study, we report the isolation and purification of natural AcCh a
- PMID 26868564
- Understanding the pathophysiology of the asthma-chronic obstructive pulmonary disease overlap syndrome.
- Gelb AF1, Christenson SA, Nadel JA.
- Current opinion in pulmonary medicine.Curr Opin Pulm Med.2016 Mar;22(2):100-5. doi: 10.1097/MCP.0000000000000236.
- PURPOSE OF REVIEW: The review will provide an update on the pathophysiology and studies of inflammation associated with the asthma-chronic obstructive pulmonary disease (COPD) overlap syndrome (ACOS) and the mechanism(s) responsible for persistent expiratory airflow limitation in never-smoked asthma
- PMID 26717511
- Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress.
- Jadeja RN1, Urrunaga NH2, Ahmad D3, Khurana S1.
- Data in brief.Data Brief.2015 Dec 18;6:405-9. doi: 10.1016/j.dib.2015.12.025. eCollection 2016.
- We recently demonstrated the role of M1 muscarinic receptors (M1R) in modulating oxidative stress in liver and hepatocytes (Urrunaga et al., 2015) [1]. Here we provide data regarding the effect of a novel M1R agonist, VU0357017 (Lebois et al., 2010) [2], on H2O2-mediated hepatocyte injury, the effec
- PMID 26862589
Japanese Journal
- Selective M_3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model
- AMI Nozomi,KOGA Kazumi,FUSHIKI Hiroshi,UENO Yoko,OGINO Yoshio,OHTA Hisashi
- Journal of pharmacological sciences 116(1), 81-88, 2011-05-20
- … In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). … We used a highly selective M3 muscarinic antagonist, N-(2-[3-([3R]-1-(cyclohexylmethyl)-3-piperidinyl]methylamino)-3-oxopropyl]amino-2-oxoethyl)-3,3,3-triphenyl-propioamide (J-115311). …
- NAID 10029894058
- Decreased Motility of the Lower Esophageal Sphincter in a Rat Model of Gastroesophageal Reflux Disease May Be Mediated by Reductions of Serotonin and Acetylcholine Signaling
- Saegusa Yayoi,Takeda Hiroshi,Muto Shuichi,Oridate Nobuhiko,Nakagawa Koji,Sadakane Chiharu,Nahata Miwa,Harada Yumi,Iizuka Mizuki,Hattori Tomohisa,Asaka Masahiro
- Biological & Pharmaceutical Bulletin 34(5), 704-711, 2011
- … The in vivo motility proximal to LES (% motility index) in conscious rats was decreased by atropine treatment and increased by cisapride (5-HT4 receptor agonist) treatment. … The mRNA expressions of 5-HT4 and muscarinic acetylcholine 3 receptors were significantly reduced in esophageal LES strips of GERD rats compared with sham-operated rats. …
- NAID 130000657784
Related Links
- A muscarinic receptor agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic ... In the form of pilocarpine, muscarinic receptor agonists have been used medically for a long time. M3 agonists ...
- In neurochemistry, a muscarinic receptor antagonist (MRA) is an agent that blocks the activity of the muscarinic acetylcholine receptor. Acetylcholine (often abbreviated ACh) is a neurotransmitter, whose receptor is a protein found in synapses ...
Related Pictures
★リンクテーブル★
[★]
- 英
- pilocarpine
- 化
- 塩酸ピロカルピン pilocarpine hydrochloride
- 商
- アドソルボカルピン、サラジェン、サンピロ、ピロリナ
- 関
- ムスカリン受容体
[★]
- 関
- muscarinic、muscarinic cholinergic agonist、muscarinic receptor agonist
[★]
- 英
- muscarinic agonist、muscarinic receptor agonist、muscarinic cholinergic agonist
- 関
- ムスカリン作動薬、ムスカリン作用薬、ムスカリンアゴニスト
[★]
- 関
- muscarinic agonist、muscarinic receptor agonist
[★]
- 関
- cholinergic、cholinergic agent、cholinergic drug、cholinomimetic、muscarine、muscarinic agent、muscarinic agonist
[★]
- 関
- agonist、agonistic