WordNet
- showing a fighting disposition; "highly competitive sales representative"; "militant in fighting for better wages for workers"; "his self-assertive and ubiquitous energy" (同)militant
- involving competition or competitiveness; "competitive games"; "to improve ones competitive position" (同)competitory
- subscribing to capitalistic competition (同)free-enterprise, private-enterprise
- 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
- 競争の,競争による
- 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)』「2015/09/14 04:13:09」(JST)
[Wiki en表示]
A competitive antagonist is a receptor antagonist that binds to a receptor but does not activate the receptor. The antagonist will compete with available agonist for receptor binding sites on the same receptor. Sufficient antagonist will displace the agonist from the binding sites, resulting in a lower frequency of receptor activation.
Presence of a competitive antagonist will shift an agonism dose-response curve to the right.[1] A Schild plot for a competitive antagonist will have a slope equal to 1, and the X-intercept and Y-intercept will each equal the dissociation constant of the antagonist.[1]
Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been consumed. Naloxone (also known as Narcan) is used to reverse opioid overdose caused by drugs such as heroin or morphine. Similarly, Ro15-4513 is an antidote to alcohol and flumazenil is an antidote to benzodiazepines.
A competitive antagonist can be reversible competitive antagonist or irreversible competitive antagonist.
References
- ^ a b Doseresponse curves in the presence of antagonists
Concepts in pharmacology
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Pharmacokinetics |
- (L)ADME: (Liberation)
- Absorption
- Distribution
- Metabolism
- Excretion (Clearance)
- Loading dose
- Volume of distribution (Initial)
- Rate of infusion
- Compartment
- Bioequivalence
- Bioavailability
- Onset of action
- Biological half-life
- Plasma protein binding
- Therapeutic index (LD50/ED50)
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Pharmacodynamics |
- Toxicity (Neurotoxicology)
- Dose–response relationship (Efficacy, Potency)
- Antimicrobial pharmacodynamics: Minimum inhibitory concentration/Bacteriostatic
- Minimum bactericidal concentration/Bactericide
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Agonism and
antagonism |
- Agonist: Inverse agonist
- Irreversible agonist
- Partial agonist
- Superagonist
- Physiological agonist
- Antagonist: Competitive antagonist
- Irreversible antagonist
- Physiological antagonist
- Other: Binding
- Affinity
- Binding selectivity
- Functional selectivity
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Other |
- Drug tolerance: Tachyphylaxis
- Drug resistance: Antibiotic resistance
- Multiple drug resistance
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Drug discovery
strategies |
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Related
fields/subfields |
- Pharmacogenetics
- Pharmacogenomics
- Neuropsychopharmacology (Neuropharmacology, Psychopharmacology)
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UpToDate Contents
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English Journal
- Effects of personality on the opioidergic modulation of the emotion warmth-liking.
- Burgdorf C1, Rinn C1, Stemmler G1.
- The Journal of comparative neurology.J Comp Neurol.2016 Jun 1;524(8):1712-26. doi: 10.1002/cne.23847. Epub 2015 Jul 16.
- Neurobiological research suggests there are discrete emotion systems, which are based on separate neural pathways with specific neurotransmitters (i.e., oxytocin, opioids). So far, autonomic regulation patterns of different positive emotions could not be unambiguously characterized. Warmth-liking, a
- PMID 26135853
- Dizocilpine (MK-801) impairs learning in the active place avoidance task but has no effect on the performance during task/context alternation.
- Vojtechova I1, Petrasek T2, Hatalova H3, Pistikova A4, Vales K5, Stuchlik A6.
- Behavioural brain research.Behav Brain Res.2016 May 15;305:247-57. doi: 10.1016/j.bbr.2016.03.020. Epub 2016 Mar 10.
- The prevention of engram interference, pattern separation, flexibility, cognitive coordination and spatial navigation are usually studied separately at the behavioral level. Impairment in executive functions is often observed in patients suffering from schizophrenia. We have designed a protocol for
- PMID 26970577
- Melatonin receptor activation increases glutamatergic synaptic transmission in the rat medial lateral habenula.
- Evely KM1,2, Hudson RL3, Dubocovich ML1, Haj-Dahmane S1,2.
- Synapse (New York, N.Y.).Synapse.2016 May;70(5):181-6. doi: 10.1002/syn.21892. Epub 2016 Feb 22.
- Melatonin (MLT) is secreted from the pineal gland and mediates its physiological effects through activation of two G protein-coupled receptors, MT1 and MT2 . These receptors are expressed in several brain areas, including the habenular complex, a pair of nuclei that relay information from forebrain
- PMID 26799638
Japanese Journal
- Effects of sodium benzoate on pre-pulse inhibition deficits and hyperlocomotion in mice after administration of phencyclidine
- MATSUURA Akiko,マツウラ アキコ,松浦 暁子,FUJITA Yuko,フジタ ユウコ,藤田 有子,IYO Masaomi,イヨ マサオミ,伊豫 雅臣,HASHIMOTO Kenji,ハシモト ケンジ,橋本 謙二
- ACTA NEUROPSYCHIATRICA 27(3), 159-167, 2015-01
- … Objective: A recent clinical study demonstrated that sodium benzoate (SB), a prototype competitive D-amino acid oxidase (DAAO) inhibitor, was effective in the treatment of several symptoms such as positive and negative symptoms, and cognitive impairment, in medicated patients with schizophrenia. …
- NAID 120005619665
- 移植片対宿主病と移植片対腫瘍効果における細胞外アデノシン産生系の機能解析とその薬学的制御に関する研究
- 塚本 宏樹
- 薬学雑誌. 乙号 134(10), 1021-1027, 2014
- … Severe GVHD was enhanced by repeated administration of a CD73 inhibitor or an adenosine receptor antagonist. … A competitive engraftment assay identified endogenous A2AAR signaling in donor T cells as part of a regulatory mechanism by CD73-generated adenosine. …
- NAID 130004693882
Related Links
- com·pet·i·tive an·tag·o·nist an antimetabolite. competitive antagonist, a substance that interferes with usual metabolic activity by competing for binding sites on a substrate (the substance on which an enzyme acts in a chemical ...
- Today's Paramedic quote: Blood goes round and round; air goes in and out; any variation from this is bad. - Paramedic 101. ... Competitive Antagonists What is a competitive antagonist? A competitive antagonist is a drug or ...
Related Pictures
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- 競合的遮断薬、競合的遮断剤、競合的拮抗剤
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- 競合的拮抗薬、競合的遮断薬、競合的拮抗剤
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