WordNet

showing favoritism
being or affecting only a part; not total; "a partial description of the suspect"; "partial collapse"; "a partial eclipse"; "a partial monopoly"; "partial immunity"
(biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
someone involved in a contest or battle (as in an agon)

PrepTutorEJDIC

(また『part』)『一部分の』,部分的な;不完全な / 不公平な,偏った / 《補語にのみ用いて》(…が)特に好きで《+『to』+『名』》

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/11/05 04:03:56」(JST)

wiki en

Agonists

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone.^[1] Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.^[2]

Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, and norclozapine.

References[edit]

^ N. E. Williams and T. N. Calvey (2001). Principles and Practice of Pharmacology for Anaesthetists. Blackwell Publishing. ISBN 0-632-05605-3
^ Zhu BT (2005). "Mechanistic explanation for the unique pharmacologic properties of receptor partial agonists". Biomed. Pharmacother. 59 (3): 76–89. doi:10.1016/j.biopha.2005.01.010. PMID 15795100.

This pharmacology-related article 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. オピオイド系薬剤を用いた癌疼痛のマネージメント：至適鎮痛作用 cancer pain management with opioids optimizing analgesia
2. 緊急時のオピオイド離脱 opioid withdrawal in the emergency setting
3. 癌免疫療法の原則 principles of cancer immunotherapy
4. 出産後の避妊手術 postpartum sterilization
5. 成人におけるノンレム睡眠からの覚醒障害 disorders of arousal from non rapid eye movement sleep in adults

English Journal

Short-term, low-dose varenicline administration enhances information processing speed in methamphetamine-dependent users.

Kalechstein AD1, Mahoney JJ 3rd2, Verrico CD2, De La Garza R 2nd2.
Neuropharmacology.Neuropharmacology.2014 Oct;85:493-8. doi: 10.1016/j.neuropharm.2014.05.045. Epub 2014 Jun 12.
Long-term, high-dose methamphetamine (METH) use is associated with decrements in neurocognition and, given the association between impaired neurocognition and poorer treatment outcomes in individuals dependent on alcohol and drugs, it is considered to be a neglected area of critical concern. The obj
PMID 24930359

Pharmacological evaluation of the anxiolytic-like effects of EMD 386088, a partial 5-HT6 receptor agonist, in the rat elevated plus-maze and Vogel conflict tests.

Jastrzębska-Więsek M1, Siwek A2, Partyka A3, Kubacka M4, Mogilski S4, Wasik A3, Kołaczkowski M5, Wesołowska A3.
Neuropharmacology.Neuropharmacology.2014 Oct;85:253-62. doi: 10.1016/j.neuropharm.2014.05.036. Epub 2014 Jun 4.
The 5-HT6 is one of the most recent additions to the 5-HT receptor family. Its pharmacological profile and anatomical distribution is suggestive of a putative role in mood disorders. Most of preclinical evidence suggests an anxiolytic-like action of 5-HT6 receptor antagonists. Evaluation the anxioly
PMID 24905144

d-cycloserine injected into the dorsolateral periaqueductal gray induces anxiolytic-like effects in rats.

Gomes FV1, Kakihata AM2, Semedo AC2, Hott SC2, Uliana DL2, Guimarães FS3, Resstel LB3.
Behavioural brain research.Behav Brain Res.2014 Sep 1;271:374-9. doi: 10.1016/j.bbr.2014.06.009. Epub 2014 Jun 13.
d-cycloserine (DCS) is a partial agonist of the glycine site coupled to the NMDA receptor (NMDAR). As a consequence, depending on the doses used it can function as an agonist or antagonist at this site. In rodents, anxiolytic-like effects have been observed after the systemic administration of high
PMID 24931794

Japanese Journal

Pharmacology and in Vitro Profiling of a Novel Peroxisome Proliferator-Activated Receptor γ Ligand, Cerco-A

Wakabayashi Kenji,Hayashi Shinko,Matsui Yumi,Matsumoto Takuo,Furukawa Akihiro,Kuroha Masanori,Tanaka Naomi,Inaba Tomoko,Kanda Shoichi,Tanaka Jun,Okuyama Ryo,Wakimoto Satoko,Ogata Tsuneaki,Araki Kazushi,Ohsumi Jun
Biological & Pharmaceutical Bulletin 34(7), 1094-1104, 2011
… Here we report the identification and characterization of a non-thiazolidinedione PPARγ partial agonist, Cerco-A, which is a derivative of the natural product, (?)-cercosporamide. … In PPARγ transcriptional activation assay and an adipocyte differentiation assay, Cerco-A was a potent partial agonist of PPARγ. …
NAID 130000738102

Related Pictures

★リンクテーブル★

リンク元	「アンタゴニスト」「アゴニスト」「部分アゴニスト」「部分作用薬」「部分刺激薬」
関連記事	「partial」

「アンタゴニスト」

　　[★]

英: antagonist
同: 拮抗薬、遮断薬、類似体拮抗物質 analog inhibitor

アゴニスト	作用薬	agonist	内因性の化学情報伝達物質と同じ受容体に結合し、同じ生理作用を呈する
アンタゴニスト	拮抗薬	antagonist	内因性の化学情報伝達物質と同じ受容体に結合するが、生理作用を呈しない
	部分作用薬	partial agonist	拮抗薬のうち、弱いながら生理作用を呈する
	部分拮抗薬	partial antagonist	拮抗薬のうち、弱いながら生理作用を呈する

「アゴニスト」

　　[★]

英: agonist
同: 作用薬、作動薬
関

アゴニスト	作用薬	agonist	内因性の化学情報伝達物質と同じ受容体に結合し、同じ生理作用を呈する
アンタゴニスト	拮抗薬	antagonist	内因性の化学情報伝達物質と同じ受容体に結合するが、生理作用を呈しない
	部分作用薬	partial agonist	拮抗薬のうち、弱いながら生理作用を呈する
	部分拮抗薬	partial antagonist	拮抗薬のうち、弱いながら生理作用を呈する