不可逆的遮断薬、非可逆的拮抗薬

WordNet

incapable of being reversed; "irreversible momentum toward revolution"
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

逆にできない,裏返しできない / (決定などが)取り消しできない,変更できない
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）』「2013/01/03 01:55:01」(JST)

wiki en

An irreversible antagonist is a type of antagonist that binds permanently to a receptor, either by forming a covalent bond to the active site, or alternatively just by binding so tightly that the rate of dissociation is effectively zero at relevant time scales.^[1] This permanently deactivates the receptor and is usually followed by rapid internalisation and recycling of the non-functional receptor protein. Irreversible enzyme inhibitors that act similarly are clinically used and include drugs such as aspirin, omeprazole and monoamine oxidase inhibitors.^[2]

Examples

Naloxazone
Phenoxybenzamine

References

^ Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p25. ISBN 0-07-144343-6
^ Rang and Dale's Pharmacology. (6th edition, 2007). p19. ISBN 0-443-06911-5

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English Journal

Histamine induces human lung fibroblast-mediated collagen gel contraction via histamine H1 receptor.

Horie M1, Saito A, Yamauchi Y, Mikami Y, Sakamoto M, Jo T, Nakajima J, Takizawa H, Nagase T, Kohyama T.
Experimental lung research.Exp Lung Res.2014 Jun;40(5):222-36. doi: 10.3109/01902148.2014.900155.
ABSTRACT Background: Airway remodeling is implicated in irreversible airflow limitation of refractory asthma, which includes increased smooth muscle mass and subepithelial fibrosis. Activated fibroblasts acquire contractile phenotype to participate in tissue contraction and structural alteration of
PMID 24809793

Acute-Phase Protein α1-Antitrypsin--A Novel Regulator of Angiopoietin-like Protein 4 Transcription and Secretion.

Frenzel E1, Wrenger S, Immenschuh S, Koczulla R, Mahadeva R, Deeg HJ, Dinarello CA, Welte T, Marcondes AM, Janciauskiene S.
Journal of immunology (Baltimore, Md. : 1950).J Immunol.2014 Apr 23. [Epub ahead of print]
The angiopoietin-like protein 4 (angptl4, also known as peroxisome proliferator-activated receptor [PPAR]γ-induced angiopoietin-related protein) is a multifunctional protein associated with acute-phase response. The mechanisms accounting for the increase in angptl4 expression are largely unknown. T
PMID 24760148

Desensitization of Functional μ-opioid Receptors Increases Agonist Off-rate.

Williams JT.
Molecular pharmacology.Mol Pharmacol.2014 Apr 18. [Epub ahead of print]
Desensitization of μ-opioid receptors (MORs) develops over 5-15 min following application of some but not all opioid agonists and lasts for 10s of min following agonist removal. The decrease in function is receptor selective (homologous) and could result from (1) a reduction in receptor number or (
PMID 24748657

Japanese Journal

Roles of Histamine in Exercise-Induced Fatigue: Favouring Endurance and Protecting against Exhaustion

Niijima-Yaoita Fukie,Tsuchiya Masahiro,Ohtsu Hiroshi [他],Yanai Kazuhiko,Sugawara Shunji,Endo Yasuo,Tadano Takeshi
Biological and Pharmaceutical Bulletin 35(1), 91-97, 2012
… Mice given a histamine H1-receptor antagonist [fexofenadine (peripherally acting) or pyrilamine (peripherally and centrally acting)] or an irreversible HDC inhibitor (α-fluoromethylhistidine) displayed less PW endurance than control mice. … Ranitidine (H2-receptor antagonist) tended to reduce endurance. …
NAID 130001872348

Reversion-inducing cysteine-rich protein with Kazal motifs interferes with epidermal growth factor receptor signaling

Kitajima Shunsuke,Miki T.,Takegami Yujiro,Kido Y.,Noda M.,Hara Eiji,Shamma Awad,Takahashi Chiaki
Oncogene 30(6), 737-750, 2011-02-10
… The reversion-inducing cysteine-rich protein with Kazal motifs (RECK) gene had been isolated as an antagonist to RAS signaling; … In contrast, short hairpin RNA-mediated depletion of RECK induced irreversible growth arrest along with several features of the Arf, Trp53 and Cdkn1a-dependent cellular senescence. …
NAID 120002907445

Current perspective on the role of the thrombin receptor in cerebral vasospasm after subarachnoid hemorrhage

Hirano Katsuya,Hirano Mayumi
Journal of Pharmacological Sciences 114(2), 127-133, 2010
… is an irreversible process, as it is initiated by the proteolytic removal of the N-terminal region. … antagonist prevents the PAR<SUB>1</SUB> …
NAID 130000336361