- 関
- noncompetitive antagonist
WordNet
- used to express refusal or denial or disagreement etc or especially to emphasize a negative statement; "no, you are wrong"
- a negative; "his no was loud and clear"
- referring to the degree to which a certain quality is present; "he was no heavier than a child" (同)no more
- not in any degree or manner; not at all; "he is no better today"
- quantifier; used with either mass nouns or plural count nouns for indicating a complete or almost complete lack or zero quantity of; "we have no bananas"; "no eggs left and no money to buy any"; "have you no decency?"; "did it with no help"; "Ill get you there in no time"
- 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"
- the fifth of the seven canonical hours; about 3 p.m.
PrepTutorEJDIC
- 《名詞の前に置いて》『一つも』(『一人も,少しも』)・・・『ない』 / 《補語につけて》『決して・・・でない』 / 《省略文で》・・・なし;・・・お断り / 《話》少ししか(あまり)・・・ない / (肯定の問いに対して)『いいえ』;(否定の問いに対して)はい,ええ / 《not, norの前に挿入して》『いや』,否 / 《形容詞の前に置その形容詞を否定して》…どころではない / 《比較級の前に置いて》ちっとも…でない,…と全く同じ / 《… or no の形で》…であってもなくても / 《驚き・困惑・不信などを表して》とんでもない / 《単数形で》『拒否』,「『いいえ』」という返事 / 《複数形で》反対[投]票
- 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)』「2017/05/30 06:17:10」(JST)
[Wiki en表示]
The term "non-competitive antagonism" (sometimes called non-surmountable antagonists)[citation needed] can be used to describe two distinct phenomena: one in which the antagonist binds to the active site of the receptor, and one in which the antagonist binds to an allosteric site of the receptor.[1] While the mechanism of antagonism is different in both of these phenomena, they are both called "non-competitive" because the end-results of each are functionally very similar. Unlike competitive antagonists, which affect the amount of agonist necessary to achieve a maximal response but do not affect the magnitude of that maximal response, non-competitive antagonists reduce the magnitude of the maximum response that can be attained by any amount of agonist. This property earns them the name "non-competitive" because their effects cannot be negated, no matter how much agonist is present. In functional assays of non-competitive antagonists, depression of the maximal response of agonist dose-response curves, and in some cases, rightward shifts, is produced.[2] The rightward shift will occur as a result of a receptor reserve (also known as spare receptors)[3] and inhibition of the agonist response will only occur when this reserve is depleted.
An antagonist that binds to the active site of a receptor is said to be "non-competitive" if the bond between the active site and the antagonist is irreversible or nearly so.[1] This usage of the term "non-competitive" may not be ideal, however, since the term "irreversible competitive antagonism" may also be used to describe the same phenomenon without the potential for confusion with the second meaning of "non-competitive antagonism" discussed below.
The second form of "non-competitive antagonists" act at an allosteric site.[1] These antagonists bind to a distinctly separate binding site from the agonist, exerting their action to that receptor via the other binding site. They do not compete with agonists for binding at the active site. The bound antagonists may prevent conformational changes in the receptor required for receptor activation after the agonist binds.[4] Cyclothiazide has been shown to act as a reversible non-competitive antagonist of mGluR1 receptor.[5]
References
- ^ a b c eds, David E. Golan, ed.-in-chief ; Armen H. Tashjian, Jr., deputy ed. ; Ehrin J. Armstrong, April W. Armstrong, associate (2008). Principles of pharmacology : the pathophysiologic basis of drug therapy (2nd ed.). Philadelphia, Pa., [etc.]: Lippincott Williams & Wilkins. p. 25. ISBN 978-0-7817-8355-2. Retrieved 2012-02-05.
- ^ Vauquelin G, Van Liefde I, Birzbier BB, Vanderheyden PM; Van Liefde; Birzbier; Vanderheyden (2002). "New insights in insurmountable antagonism". Fundamental & clinical pharmacology. 16 (4): 263–72. doi:10.1046/j.1472-8206.2002.00095.x. PMID 12570014.
- ^ Stephenson RP (1997). "A modification of receptor theory. 1956". Br. J. Pharmacol. 120 (4 Suppl): 106–20; discussion 103–5. doi:10.1111/j.1476-5381.1997.tb06784.x. PMC 3224279 . PMID 9142399. of the original article.
- ^ D.E. Golan, A.H Tashjian Jr, E.J. Armstrong, A.W. Armstrong. (2007) Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy Lippincott Williams & Wilkins ISBN 0-7817-8355-0
- ^ Surin A, Pshenichkin S, Grajkowska E, Surina E, Wroblewski JT; Pshenichkin; Grajkowska; Surina; Wroblewski (2007). "Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists". Neuropharmacology. 52 (3): 744–54. doi:10.1016/j.neuropharm.2006.09.018. PMC 1876747 . PMID 17095021.
UpToDate Contents
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English Journal
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- PMID 28522210
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- Lindquist BE1, Shuttleworth CW1.
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- PMID 27217381
Japanese Journal
- The Phenylquinazoline Compound S-4893 is a Non-Competitive Cytokinin Antagonist that Targets Arabidopsis Cytokinin Receptor CRE1 and Promotes Root Growth in Arabidopsis and Rice
- Arata Yuto,Nagasawa-Iida Asako,Uneme Hideki [他],NAKAJIMA Hiroki,KAKIMOTO Tatsuo,SATO Ryo
- Plant and cell physiology 51(12), 2047-2059, 2010-12-01
- NAID 10028056531
- フォルマリン誘発疼痛における Agmatine の鎮痛効果は非競合的NMDA受容体阻害薬で増強される
- 静岡 吉克,有吉 亨,仲西 修,福原 佳世子,山本 悟,山本 美佐,石川 敏三
- Pain research : the journal of the Japanese Society for the Study of Pain = 日本疼痛学会誌 25(1), 55-63, 2010-03-15
- NAID 10026443927
- フォルマリン誘発疼痛におけるAgmatine の鎮痛効果は非競合的NMDA 受容体阻害薬で増強される
- 静岡 吉克,有吉 亨,仲西 修,福原 佳世子,山本 悟,山本 美佐,石川 敏三
- PAIN RESEARCH 25(1), 55-63, 2010
- … follows, 1) Non-treated (saline, it. … the sum of the first (0 - 5 min) is 14/min and the sum of the second (20 - 60 min) is 147/min. All drugs diminished the sum of the second phase 32 - 68% compared with non-treated animals but did not affect the first phase. …
- NAID 130004651914
Related Links
- competitive antagonism the antagonism which blocks or reverses the effects of an agonist, provided that the antagonist is given at an appropriate dosage. The antagonism is completely reversible, and an increase in the biophasic ...
- I cant understand the following concepts: Q1. in case of non-competitive antagonist why is the potency same and efficacy reduced Q2. in case of competitive ... 1) A non-competitive antagonist works at a different receptor binding ...
★リンクテーブル★
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- 英
- noncompetitive antagonist、non-competitive antagonist
- 関
- 非競合的遮断薬
[★]
- 英
- noncompetitive antagonist、non-competitive antagonist
- 関
- 非競合的拮抗薬
[★]
- 関
- non-competitive antagonist
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- 関
- compete、competition、competitively、competitiveness、contest、rival
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- 関
- number of experiment、sample size
- pの前の[n]はmと記載する。synptom→symptom
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- 関
- un