parasympathomimetics

副交感神経刺激薬

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parasympathomimetic、parasympathomimetic agent

WordNet

1. having an effect similar to that resulting from stimulation of the parasympathetic nervous system; "parasympathomimetic drugs slow the heart rate"

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2018/08/30 02:03:01」(JST)

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A parasympathomimetic drug, sometimes called a cholinomimetic drug, is a substance that stimulates the parasympathetic nervous system (PSNS). These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS. Chemicals in this family can act either directly by stimulating the nicotinic or muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibiting cholinesterase, promoting acetylcholine release, or other mechanisms.

Some chemical weapons such as sarin or VX, non-lethal riot control agents such as tear gas, and insecticides such as diazinon fall into this category.

Structure activity relationships for parasympathomimetic drugs

For a cholinergic agent, the following criteria describe the structure activity relationship:

1. Ing's Rule of 5: there should be no more than five atoms between the nitrogen and the terminal hydrogen for muscarinic (or cholinergic) activity;
2. the molecule must possess a nitrogen atom capable of bearing a positive charge, preferably a quaternary ammonium salt;
3. for maximum potency, the size of the alkyl groups substituted on the nitrogen should not exceed the size of a methyl group;
4. the molecule should have an oxygen atom, preferably an ester-like oxygen capable of participating in a hydrogen bond;
5. there should be a two-carbon unit between the oxygen atom and the nitrogen atom.

Pharmaceuticals/Supplements

Direct-acting

These act by stimulating the nicotinic or muscarinic receptors.

• Choline esters
  • Acetylcholine (all acetylcholine receptors)
  • Bethanechol (M3 receptors)
  • Carbachol (all muscarinic receptors and some nicotinic receptors)
  • Methacholine (all muscarinic receptors)
• Plant alkaloids
  • Arecoline
  • Nicotine
  • Muscarine
  • Pilocarpine (M3 receptors)

Indirect-acting

Indirect acting parasympathomimetic substances may be either reversible cholinesterase inhibitors, irreversible cholinesterase inhibitors or substances that promote ACh release or anti-adrenergics. The latter inhibits the antagonistic system, the sympathetic nervous system.

• Reversible cholinesterase inhibitors
  • Donepezil
  • Edrophonium
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Rivastigmine
  • Tacrine
  • Caffeine (non-competitive)
  • Huperzine A
• Irreversible cholinesterase inhibitors
  • Echothiophate
  • Isoflurophate
  • Malathion
• ACh release promoters
  • Alpha GPC
  • Cisapride
  • Droperidol
  • Domperidone
  • Metoclopramide
  • Risperidone
  • Paliperidone
  • Trazodone – via blockade of the α adrenergic receptors
• Anti-adrenergics: See also alpha blocker and beta blocker
  • Clonidine (α-receptor agonist, α₂ > α₁, giving negative feedback)
  • Methyldopa (α₂ agonist, giving negative feedback)
  • Propranolol (β-receptor antagonist)
  • Atenolol (β₁ antagonist)
  • Prazosin (α₁ antagonist)
  • Oxymetazoline (partial α2 adrenergic agonist)

See also

• Sympathomimetic drug

External links

• Parasympathomimetics at the US National Library of Medicine Medical Subject Headings (MeSH)

English Journal

• Novel multitarget-directed tacrine derivatives as potential candidates for the treatment of Alzheimer's disease.

• Wu WY1,2, Dai YC1,2, Li NG1,2, Dong ZX1,2, Gu T1,2, Shi ZH1,3, Xue X1,2, Tang YP1,2, Duan JA1,2.
• Journal of enzyme inhibition and medicinal chemistry.J Enzyme Inhib Med Chem.2017 Dec;32(1):572-587. doi: 10.1080/14756366.2016.1210139.
• PMID 28133981

• A comparison of sugammadex and neostigmine for reversal of rocuronium-induced neuromuscular blockade in children.

• Ammar AS1, Mahmoud KM1, Kasemy ZA1.
• Acta anaesthesiologica Scandinavica.Acta Anaesthesiol Scand.2017 Apr;61(4):374-380. doi: 10.1111/aas.12868. Epub 2017 Feb 10.
• PMID 28185260

• New tacrine-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates.

• Eghtedari M1, Sarrafi Y2, Nadri H3, Mahdavi M4, Moradi A3, Homayouni Moghadam F5, Emami S6, Firoozpour L4, Asadipour A7, Sabzevari O8, Foroumadi A9.
• European journal of medicinal chemistry.Eur J Med Chem.2017 Mar 10;128:237-246. doi: 10.1016/j.ejmech.2017.01.042. Epub 2017 Feb 1.
• PMID 28189905

Japanese Journal

• 幼弱ラットがっ下せんの交感神経性α１‐受容体機能の加齢変化にみられる性差

• 歯科基礎医学会雑誌 27(3), 909-932, 1985
• NAID 130004001392

• 薬物性排尿障害の臨床研究

• 泌尿器科紀要 28(5), p501-507, 1982-05
• NAID 120002260075

• 下部尿路の尿流動態研究 : V. Alpha adrenergic blockerによる神経因性膀胱機能障害の治療

• 日本泌尿器科學會雜誌 69(8), 988-999, 1978-08-20
• NAID 110003042316

Related Links

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• PARASYMPATHOMIMETICS |authorSTREAM - Upload ...

Parasympathomimetics : The main effect produced by these drugs resemble the effect of parasympathetic stimulation. On the basis of their mode of action they can be divided into two groups. Direct acting Mechanism of action of ...

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★リンクテーブル★

リンク元	「parasympathomimetic agent」
拡張検索	「indirect parasympathomimetics」「indirectly acting parasympathomimetics」
関連記事	「parasympathomimetic」

「parasympathomimetic agent」

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• 副交感神経刺激薬、副交感神経作動薬

関

parasympathomimetic、parasympathomimetics

「indirect parasympathomimetics」

　　[★] 副交感神経間接作動薬

「indirectly acting parasympathomimetics」

　　[★] 副交感神経間接作動薬

「parasympathomimetic」

　　[★]

• adj.

• 副交感神経刺激様の

• n.

• 副交感神経刺激薬

関

parasympathomimetic agent、parasympathomimetics