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词条 Muscarinic antagonist
释义

  1. Effects

  2. Comparison table

     Overview  Binding affinities  Anticholinergics  Antihistamines  Antidepressants  Antipsychotics 

  3. See also

  4. References

  5. External links

{{Infobox drug class
| Name = Muscarinic acetylcholine receptor antagonist
| Image = L-Scopolamin.svg
| Alt = Scopolamine
| Use = Allergies, Asthma, Bradycardia, Motion sickness, Parkinson's disease, etc.
| Caption = Skeletal formula of scopolamine, a nonselective antagonist of the muscarinic receptors
| Biological_target = Metabotropic acetylcholinergic receptors.
| ATC_prefix = V
| MeshID = D018727
}}

A muscarinic receptor antagonist (MRA) is a type of anticholinergic 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 and other cell membranes. Besides responding to their primary neurochemical, neurotransmitter receptors can be sensitive to a variety of other molecules. Acetylcholine receptors are classified into two groups based on this:

  • muscarinic, which respond to muscarine
  • nicotinic, which respond to nicotine

Most muscarinic receptor antagonists are synthetic chemicals; however, the two most commonly used anticholinergics, scopolamine and atropine, are belladonna alkaloids, and are naturally extracted.

Muscarinic antagonist effects and muscarinic agonist effects counterbalance each other for homeostasis.

Certain substances are known as long-acting muscarinic receptor antagonists (LAMAs).[1]

{{TOC limit|3}}

Effects

Scopolamine and atropine have similar effects on the peripheral nervous system. However, scopolamine has greater effects on the central nervous system (CNS) than atropine due to its ability to cross the blood–brain barrier. At higher-than-therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue, and reduction in rapid eye movement sleep. Scopolamine (Hyoscine) has anti-emetic activity and is, therefore, used to treat motion sickness.

Antimuscarinics are also used as anti-parkinsonian drugs. In parkinsonism, there is imbalance between levels of acetylcholine and dopamine in the brain, involving both increased levels of acetylcholine and degeneration of dopaminergic pathways (nigrostriatal pathway). Thus, in parkinsonism there is decreased level of dopaminergic activity. One method of balancing the neurotransmitters is through blocking central cholinergic activity using muscarinic receptor antagonists.

Atropine acts on the M2 receptors of the heart and antagonizes the activity of acetylcholine. It causes tachycardia by blocking vagal effects on the sinoatrial node. Acetylcholine hyperpolarizes the sinoatrial node, which is overcome by MRA and thus increases the heart rate. If atropine is given by intramuscular or subcutaneous injection, it causes initial bradycardia. This is because by i.m/s.c it acts on presynaptic M1 receptors (autoreceptors). Intake of acetylcholine in axoplasm is prevented and the presynaptic nerve releases more acetylcholine into the synapse that initially causes bradycardia.

In the atrioventricular node, the resting potential is abbreviated, which facilitates conduction. This is seen as a shortened PR-interval on an electrocardiogram. It {{clarify|date=June 2015}} has an opposite effect on blood pressure. Tachycardia and stimulation of the vasomotor center causes an increase in blood pressure. But, due to feed back regulation of the vasomotor center, there is fall in blood pressure due to vasodilation.

Important[2] muscarinic antagonists include atropine, Hyoscyamine, hyoscine butylbromide and hydrobromide, ipratropium, tropicamide, cyclopentolate, and pirenzepine.

Muscarinic antagonists such as ipratropium bromide can also be effective in treating asthma, since acetylcholine is known to cause smooth muscle contraction, especially in the bronchi.

Comparison table

Overview

SubstanceTrade namesMechanismClinical useAdverse effects
Atropine (D/L-Hyoscyamine)Symax, HyoMax, Anaspaz, Egazil, Buwecon, Cystospaz, Levsin, Levbid, Levsinex, Donnamar, NuLev, Spacol T/S and Neoquess non-selective antagonism, CNS depression[2]
  • in anaesthesia[2][3]
  • anticholinesterase poisoning[2]
  • bradycardia[2]
  • antispasmodic in gastrointestinal hypermotility[2]
  • urinary retention[2]
  • xerostomia[2]
  • blurred vision[2]
Scopolamine (L-Hyoscine) Scopace, Transderm-Scop, Maldemar, Buscopan non-selective antagonism, CNS depression[2]
  • as atropine[2]
  • motion sickness[2]
  • as atropine[2]
  • sedation[2]
Hydroxyzine Vistaril, AtaraxVery mild/negligible mechanism of action
Ipratropium Atrovent and Apovent non-selective antagonism, without any mucociliary excretion inhibition.[2] in asthma and bronchitis[2]
  • Bronchial vasodilation
Tropicamide short acting non-selective antagonism, CNS depression[2]
  • produce mydriasis and cycloplegia in diagnostics[2]
  • may cause ocular hypertension[2]
Pirenzepine M1 receptor-selective antagonist[2]
  • inhibits gastric secretion[2]
  • in peptic ulcer (not much anymore)[2]
 (fewer than non-selective ones)[2]
Diphenhydramine Benadryl, Nytol Non-selective antagonism in the central nervous system, blood vessels and smooth muscle tissues
  • for extrapyramidal symptoms from typical and atypical antipsychotic medications
  • antihistamine
  • sleep aid
  • antiparkinson agent
  • management of asthma symptoms
  • sedation
  • dry mouth
  • constipation
  • urinary retention
Doxylamine Unisom
  • antihistamine[4]
  • antiemetic
  • sleep aid
  • dizziness
  • dry mouth
Dimenhydrinate Dramamine Combination of diphenhydramine with a methylxanthine salt
  • motion sickness
Dicyclomine
  • Irritable bowel syndrome
Flavoxate Urispas
  • Urinary bladder antispasmodic
Oxybutynin Ditropan
  • overactive bladder
  • urge incontinence
Tiotropium Spiriva
  • Chronic obstructive pulmonary disease
Cyclopentolate short acting non-selective antagonism, CNS depression[2]
  • produce mydriasis and cycloplegia in diagnostics[2]
  • may cause ocular hypertension[2]
Atropine methonitrate non-selective antagonism, blocks transmission in ganglia.[2] Lacks CNS effects[31]
  • antispasmodic in gastrointestinal hypermotility[2]
Trihexyphenidyl/Benzhexol Artane Targets the M1 Muscarinic receptor Parkinson's disease Drug at relative dose has 83% activity of atropine, thus has the same side-effects
Tolterodine Detrusitol, Detrol
  • urge incontinence
Solifenacin Vesicare Competitive muscarinic acetylcholine receptor antagonist
  • overactive bladder (OAB)
  • Urgency (urge incontinence)
Darifenacin Enablex Selective for M3 receptors [5] Urinary incontinence [5] Few side effects[5]
Benztropine CogentinReduces the effects of the relative central cholinergic excess that occurs as a result of dopamine deficiency.
  • Parkinson's disease
  • extrapyramidal symptoms caused by typical and atypical antipsychotics
Mebeverine Colofac, Duspatal, DuspatalinA muscolotropic spasmolytic with a strong and selective action on the smooth muscle spasm of the gastrointestinal tract, in particular of the colon.
  • Irritable bowel syndrome in its primary form (e.g., Abdominal Pain, Bloating, Constipation, and Diarrhea).
  • Irritable bowel syndrome associated with organic lesions of the gastrointestinal tract. (e.g., diverticulosis & diverticulitis, etc.).
  • skin rashes
Procyclidine Antimuscarinic
  • Drug-induced parkinsonism, akathisia and acute dystonia
  • Parkinson disease
  • Idiopathic or secondary dystonia
Overdose produces confusion, agitation and sleeplessness that can last up to or more than 24 hours. Pupils become dilated and unreactive to light. Tachycardia (fast heart beat), as well as auditory and visual hallucinations
Aclidinium bromide Tudorza Selective long acting muscarinic antagonist
  • Bronchospasm
  • Chronic Obstructive Pulmonary Disease

Binding affinities

Anticholinergics

Compound M1 M2 M3 M4 M5 Species Ref
3-Quinuclidinyl benzilate 0.035–0.044 0.027–0.030 0.080–0.088 0.034–0.037 0.043–0.065 Human [6][37]
4-DAMP 0.57–0.58 3.80–7.3 0.37–0.52 0.72–1.17 0.55–1.05 Human [38][39]
AF-DX 250 427 55.0 692 162 3020 Human [38]
AF-DX 384 30.9 6.03 66.1 10.0 537 Human [38]
AQ-RA 741 28.8 4.27 63.1 6.46 832 Human [38]
Atropine 0.21–0.50 0.76–1.5 0.15–1.1 0.13–0.6 0.21–1.7 Human [6][7][8]
Benzatropine (benztropine) 0.231 1.4 1.1 1.1 2.8 Human [6]
Biperiden 0.48 6.3 3.9 2.4 6.3 Human [6]
Darifenacin 5.5–13 47–77 0.84–2.0 8.6–22 2.3–5.4 Human [8][49]
Dicycloverine (dicyclomine) 57 (IC50) 415 (IC50) 67 (IC50) 97 (IC50) 53 (IC50) Human/rat [7]
Hexahydrodifenidol 11 200 16 76 (IC50) 83 Human/rat [7]
Hexahydrosiladifenidol 44 249 10 298 (IC50) 63 Human/rat [7]
(R)-Hexbutinol 2.09 20.9 2.14 3.02 5.50 Human [38]
Hexocyclium 2.3 23 1.4 5.5 3.7 Human/rat [7]
Himbacine 107 10.0 93.3 11.0 490 Human [38]
Ipratropium 0.49 1.5 0.51 0.66 1.7 Human [9]
Methoctramine 16–50 3.6–14.4 118–277 31.6–38.0 57–313 Human [7][38][59]
N-Methylscopolamine 0.054–0.079 0.083–0.251 0.052–0.099 0.026–0.097 0.106–0.125 Human [10]
Orphenadrine 48 213 120 170 129 Human [37]
Otenzepad (AF-DX 116) 1300 186 838 1800 (IC50) 2800 Human/rat [7]
Oxybutynin 0.66 13 0.72 0.54 7.4 Human [8]
pFHHSiD 22.4 132 15.5 31.6 93.3 Human [10]
Pirenzepine 6.3–8 224–906 75–180 17–37 66–170 Human [6][7][10][8]
Procyclidine 4.6 25 12.4 7 24 Human [6]
Propiverine 476 2970 420 536 109 Human [8]
Scopolamine (hyoscine) 1.1 2.0 0.44 0.8 2.07 Human [6]
Silahexacyclium 2.0 35 1.2 3.2 2.0 Human/rat [7]
Timepidium 34 7.7 31 18 11 Human [8]
Tiquizium 4.1 4.0 2.8 3.6 8.2 Human [8]
Trihexyphenidyl 1.6 7 6.4 2.6 15.9 Human [6]
Tripitamine (tripitramine) 1.58 0.27 38.25 6.41 33.87 Human [11]
Zamifenacin 55 153 10 68 34 Human [8]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antihistamines

Compound M1 M2 M3 M4 M5 Species Ref
Brompheniramine 25700 32400 50100 67600 28800 Human [12]
Chlorphenamine (chlorpheniramine) 19000 17000 52500 77600 28200 Human [12]
Cyproheptadine 12 7 12 8 11.8 Human [37]
Diphenhydramine 80–100 120–490 84–229 53–112 30–260 Human [6][13]
Doxylamine 490 2100 650 380 180 Human [13]
Mequitazine 5.6 14 5.3 11.1 11.0 Human [37]
Terfenadine 8710 8510 5250 30900 11200 Human [12]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antidepressants

Compound M1 M2 M3 M4 M5 Species Ref
Amitriptyline 14.7 11.8 12.8 7.2 15.7 Human [14]
Bupropion >35,000 >35,000 >35,000 >35,000 >35,000 Human [14]
Citalopram 1430 ND|No data}}ND|No data}}ND|No data}}ND|No data}} Human [15]
Desipramine 110 540 210 160 143 Human [14]
Desmethylcitalopram >10000 >10000 >10000 >10000 >10000 Human [90]
Desmethyldesipramine 404 927 317 629 121 Human [16]
Desvenlafaxine >10000 >10000 >10000 >10000 >10000 Human [17]
Dosulepin (dothiepin) 18 109 38 61 92 Human [14]
Doxepin 18–38 160–230 25–52 20–82 5.6–75 Human [13][14]
Escitalopram 1242 ND|No data}}ND|No data}}ND|No data}}ND|No data}} Human [15]
Etoperidone >35000 >35000 >35000 >35000 >35000 Human [14]
Femoxetine 92 150 220 470 400 Human [14]
Fluoxetine 702–1030 2700 1000 2900 2700 Human [14][15]
Fluvoxamine 31200 ND|No data}}ND|No data}}ND|No data}}ND|No data}} Human [15]
Imipramine 42 88 60 112 83 Human [14]
Lofepramine 67 330 130 340 460 Human [14]
Norfluoxetine 1200 4600 760 2600 2200 Human [14]
Nortriptyline 40 110 50 84 97 Human [14]
Paroxetine 72–300 340 80 320 650 Human [14][15]
Sertraline 427–1300 2100 1300 1400 1900 Human [14][15]
Tianeptine >10000 >10000 >10000 >10000 >10000 Human [18]
Trazodone >35,000 >35,000 >35,000 >35,000 >35,000 Human [13][14]
Venlafaxine >35000 >35000 >35000 >35000 >35000 Human [14]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antipsychotics

Compound M1 M2 M3 M4 M5 Species Ref
Amisulpride >10,000 >10,000 >10,000 >10,000 >10,000 Human [19]
Aripiprazole 6780 3510 4680 1520 2330 Human [20]
Asenapine >10000 >10000 >10000 >10000 ND|No data}} Human [116][116]
Bromperidol 7600 1800 7140 1700 4800 Human [6]
Chlorprothixene 11 28 22 18 25 Human [6]
Chlorpromazine 25 150 67 40 42 Human [6]
Clozapine 1.4–31 7–204 6–109 5–27 5–26 Human [6][116][21][22]
Cyamemazine (cyamepromazine) 13 42 32 12 35 Human [23]
N-Desmethylclozapine 67.6 414.5 95.7 169.9 35.4 Human [24]
Fluperlapine 8.8 71 41 14 17 Human [6]
Fluphenazine 1095 7163 1441 5321 357 Human [25]
Haloperidol >10000 >10000 >10000 >10000 >10000 Human [116][21]
Iloperidone 4898 3311 >10000 8318 >10000 Human [26]
Loxapine 63.9–175 300–590 122–390 300–2232 91–241 Human [6][27]
Melperone >15000 2400 >15000 4400 >15000 Human [6]
Mesoridazine 10 15 90 19 60 Human [6]
Molindone ND|No data}}ND|No data}} >10000 ND|No data}}ND|No data}} Human [28]
Olanzapine 1.9–73 18–96 13–132 10–32 6–48 Human [29][21][22]
Perphenazine ND|No data}}ND|No data}} 1848 ND|No data}}ND|No data}} Human [28]
Pimozide ND|No data}}ND|No data}} 1955 ND|No data}}ND|No data}} Human [28]
Quetiapine 120–135 630–705 225–1320 660–2990 2990 Human [29][21]
Remoxipride >10000 >10000 >10000 >10000 ND|No data}} Human [29]
Rilapine 190 470 1400 1000 1100 Human [6]
Risperidone 11000 ≥3700 13000 ≥2900 >15000 Human [6][29]
Sertindole ND|No data}}ND|No data}} 2692 ND|No data}}ND|No data}} Human [28]
Tenilapine 260 62 530 430 660 Human [6]
Thioridazine 2.7 14 15 9 13 Human [6]
Thiothixene >10000 >10000 >10000 >10000 5376 Human [30]
cis-Thiothixene 2600 2100 1600 1540 4310 Human [6]
Tiospirone 630 180 1290 480 3900 Human [6]
Trifluoperazine ND|No data}}ND|No data}} 1001 ND|No data}}ND|No data}} Human [28]
Ziprasidone ≥300 >3000 >1300 >1600 >1600 Human [21][31]
Zotepine 18 140 73 77 260 Human [6]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

See also

{{col div|colwidth=30em}}
  • Anticholinergic
  • Muscarinic agonist
  • Nicotinic acetylcholine receptor
  • Nicotinic agonist
  • Nicotinic antagonist
  • Parasympatholytic
{{colend}}

References

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25. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=fluphenazine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
26. ^{{cite journal | vauthors = Kalkman HO, Subramanian N, Hoyer D | title = Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders | journal = Neuropsychopharmacology | volume = 25 | issue = 6 | pages = 904–14 | year = 2001 | pmid = 11750183 | doi = 10.1016/S0893-133X(01)00285-8 | url = }}
27. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=loxapine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
28. ^1 2 3 4 {{cite journal | vauthors = Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL | title = H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs | journal = Neuropsychopharmacology | volume = 28 | issue = 3 | pages = 519–26 | year = 2003 | pmid = 12629531 | doi = 10.1038/sj.npp.1300027 | url = }}
29. ^1 2 3 4 5 6 7 {{cite journal | vauthors = Bymaster FP, Calligaro DO, Falcone JF, Marsh RD, Moore NA, Tye NC, Seeman P, Wong DT | title = Radioreceptor binding profile of the atypical antipsychotic olanzapine | journal = Neuropsychopharmacology | volume = 14 | issue = 2 | pages = 87–96 | year = 1996 | pmid = 8822531 | doi = 10.1016/0893-133X(94)00129-N | url = }}
30. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=thiothixene&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
31. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=ziprasidone&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}

External links

  • Effects of Muscarinic Antagonist
  • Atropine (Muscarinic Receptor Antagonist), Cardiovascular Pharmacology Concepts, Richard E. Klabunde, PhD
  • {{MeshName|Muscarinic+antagonists}}
  • {{MeshPharmaList|82018727}}
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1 : Muscarinic antagonists
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