ニコチン受容体遮断薬、ニコチン遮断薬、ニコチン拮抗薬

WordNet

a drug that neutralizes or counteracts the effects of another drug
a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"

PrepTutorEJDIC

対立する人,敵対者,競争相手(opponent)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/09/09 12:34:19」(JST)

wiki en

A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this type being tubocurarine,^[1] but some centrally acting compounds such as bupropion, mecamylamine, and 18-methoxycoronaridine block nicotinic acetylcholine receptors in the brain and have been proposed for treating drug addiction.^{[citation needed]}

Comparison
Mechanism	Antagonist	Preferred receptor	Clinical use
Ganglionic blocking agents	Hexamethonium	Ganglion type	none^[2]
	Mecamylamine	Ganglion type
	Trimethaphan	Ganglion type	Rarely used for blood pressure decrease during surgery^[2]
Nondepolarizing neuromuscular blocking agents	Atracurium	Muscle type	muscle relaxant in anaesthesia^[2]
	Doxacurium	Muscle type
	Mivacurium	Muscle type
	Pancuronium	Muscle type	muscle relaxant in anaesthesia^[2]
	Tubocurarine	Muscle type	Rarely used ^[2]
	Vecuronium	Muscle type	muscle relaxant in anaesthesia^[2]
Depolarizing neuromuscular blocking agents	Succinylcholine*	Muscle type
Centrally acting nicotinic antagonists	18-Methoxycoronaridine	α3β4

Note: Succinylcholine is actually a nicotinic agonist. See neuromuscular blocking agents page for details on the mechanism of action.

References

^ P. Taylor (1990). In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th Ed., (A. G. Gilman et al., Eds.), pp. 166-186, New York: Pergamon Press.
^ ^a ^b ^c ^d ^e ^f Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 149

External links

Nicotinic antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)

This antihypertensive-related article is a stub. You can help Wikipedia by expanding it.

This drug article relating to the musculoskeletal system is a stub. You can help Wikipedia by expanding it.

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. ニコチンの心血管系への影響 cardiovascular effects of nicotine
2. 成人における禁煙のための薬物療法 pharmacotherapy for smoking cessation in adults
3. 成人における禁煙マネージメントの概要 overview of smoking cessation management in adults
4. タバコの喫煙と妊娠 cigarette smoking and pregnancy
5. 成人の顔面紅潮に対するアプローチ approach to flushing in adults

English Journal

Nicotinic acetylcholine receptor antagonists alter the function and expression of serine racemase in PC-12 and 1321N1 cells.

Singh NS, Paul RK, Ramamoorthy A, Torjman MC, Moaddel R, Bernier M, Wainer IW.SourceLaboratory of Clinical Investigation, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA.
Cellular signalling.Cell Signal.2013 Dec;25(12):2634-45. doi: 10.1016/j.cellsig.2013.08.025. Epub 2013 Sep 4.
Western blot analysis demonstrated that PC-12 cells express monomeric and dimeric forms of serine racemase (m-SR, d-SR) and that 1321N1 cells express m-SR. Quantitative RT-PCR and functional studies demonstrated that PC-12 cells express homomeric and heteromeric forms of nicotinic acetylcholine rece
PMID 24012499

Prevention of hemolysis-induced organ damage by nutritional activation of the vagal anti-inflammatory reflex*.

de Haan JJ, Windsant IV, Lubbers T, Hanssen SJ, Hadfoune M, Prinzen FW, Greve JW, Buurman WA.Source1Department of Surgery, NUTRIM School for Nutrition, Toxicology and Metabolism, Maastricht University Medical Centre+, Maastricht, The Netherlands. 2Department of Internal Medicine, Medisch Spectrum Twente, Enschede, The Netherlands. 3Department of Physiology, Cardiovascular Research Institute Maastricht, Maastricht University Medical Centre+, Maastricht, The Netherlands. 4Department of Surgery, Atrium Medical Center, Heerlen, The Netherlands.
Critical care medicine.Crit Care Med.2013 Nov;41(11):e361-7. doi: 10.1097/CCM.0b013e31828e9262.
OBJECTIVES: Acute hemolysis is associated with organ damage, inflammation, and impaired vascular function. Stimulation of the cholecystokinin-1 receptor-dependent vagal anti-inflammatory reflex with lipid-rich enteral nutrition was demonstrated to prevent tissue damage and attenuate inflammation. Th
PMID 24105450

Novel 2-(substituted benzyl)quinuclidines inhibit human α7 and α4β2 nicotinic receptors by different mechanisms.

Arias HR, López JJ, Feuerbach D, Fierro A, Ortells MO, Pérez EG.SourceDepartment of Medical Education, California Northstate University College of Medicine, Elk Grove, CA 95757, USA. Electronic address: hugo.arias@cnucom.org.
The international journal of biochemistry & cell biology.Int J Biochem Cell Biol.2013 Nov;45(11):2420-30. doi: 10.1016/j.biocel.2013.08.003. Epub 2013 Aug 14.
This work presents the design and synthesis of a series of novel 2-benzylquinuclidine derivatives, comprising 12 methiodide and 11 hydrochloride salts, and their structural and pharmacological characterization at the human (h) α7 and α4β2 nicotinic receptors (nAChRs). The antagonistic potency of
PMID 23954208

Japanese Journal

Nicotine Effects and the Endogenous Opioid System

Kishioka Shiroh,Kiguchi Norikazu,Kobayashi Yuka,Saika Fumihiro
Journal of Pharmacological Sciences 125(2), 117-124, 2014
… Nicotine (NIC) is an exogenous ligand of the nicotinic acetylcholine receptor (nAChR), and it influences various functions in the central nervous system. … The opioid-receptor antagonist naloxone (NLX) elicits NIC withdrawal after repeated NIC administration, and NLX-induced NIC withdrawal is inhibited by concomitant administration of an opioid-receptor antagonist. …
NAID 130004438636

Genetic Background Influences Nicotine-induced Conditioned Place Preference and Place Aversion in Mice

Ise Yuya,Mori Tomohisa,Katayama Shirou,Suzuki Tsutomu,Wang Tzu-Chueh
Journal of Nippon Medical School 81(1), 53-56, 2014
… These effects were completely reversed by the nicotinic receptor antagonist mecamylamine. …
NAID 130004147283

Possible Involvement of Endogenous Opioid System Located Downstream of α7 Nicotinic Acetylcholine Receptor in Mice With Physical Dependence on Nicotine

Ueno Keiko,Kiguchi Norikazu,Kobayashi Yuka,Saika Fumihiro,Wakida Naoki,Yamamoto Chizuko,Maeda Takehiko,Ozaki Masanobu,Kishioka Shiroh
Journal of Pharmacological Sciences 124(1), 47-53, 2014
… We evaluated increased serum corticosterone (SCS) as an indicator of NIC withdrawal, as it is a quantitative indicator of naloxone (opioid receptor antagonist, NLX)-precipitated morphine withdrawal in mice. … When an opioid receptor antagonist (naltrexone) was concomitantly administered with repeated NIC, the NLX-precipitated SCS increase was not elicited. …
NAID 130003382624