DAMGO

出典: meddic

-エンケファリン

Ala(2)-MePhe(4)-Gly-ol(5)-Enkephalin、Ala(2)-MePhe(4)-Gly(5)-enkephalin

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/08/27 10:05:23」(JST)

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[Wiki en表示]

英文文献

  • Wheel running reduces high-fat diet intake, preference and mu-opioid agonist stimulated intake.
  • Liang NC1, Bello NT2, Moran TH3.
  • Behavioural brain research.Behav Brain Res.2015 May 1;284:1-10. doi: 10.1016/j.bbr.2015.02.004. Epub 2015 Feb 7.
  • The ranges of mechanisms by which exercise affects energy balance remain unclear. One potential mechanism may be that exercise reduces intake and preference for highly palatable, energy dense fatty foods. The current study used a rodent wheel running model to determine whether and how physical activ
  • PMID 25668514
  • Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
  • Yuan Y1, Zaidi SA2, Stevens DL3, Scoggins KL3, Mosier PD2, Kellogg GE2, Dewey WL3, Selley DE3, Zhang Y4.
  • Bioorganic & medicinal chemistry.Bioorg Med Chem.2015 Apr 15;23(8):1701-15. doi: 10.1016/j.bmc.2015.02.055. Epub 2015 Mar 6.
  • A series of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues were synthesized and pharmacologically characterized to study their structure-activity relationship at the mu opioid receptor (MOR). The competition binding assay showed two-atom
  • PMID 25783191
  • Activation of mu-opioid receptors in the ventrolateral orbital cortex inhibits the GABAergic miniature inhibitory postsynaptic currents in rats.
  • Qu CL1, Huo FQ2, Huang FS3, Tang JS2.
  • Neuroscience letters.Neurosci Lett.2015 Apr 10;592:64-9. doi: 10.1016/j.neulet.2015.02.045. Epub 2015 Feb 21.
  • Previous studies have indicated that mu-opioid receptors in the ventrolateral orbital cortex (VLO) are involved in antinociception in tail flick tests and GABAergic neurons or terminals express mu-opioid receptors in the VLO. The current study examined the effect of selective mu-opioid receptor agon
  • PMID 25711796

和文文献

  • Analysis of the Effects of Anesthetics and Ethanol on μ-Opioid Receptor
  • Minami Kouichiro,Sudo Yuka,Shiraishi Seiji [他],SEO Masanori,UEZONO Yasuhito
  • Journal of pharmacological sciences 112(4), 424-431, 2010-04-20
  • … </SUB><I>μ</I>OR agonist DAMGO ([D-Ala<SUP>2</SUP>,<I>N</I>-MePhe<SUP>4</SUP>,Gly-ol]-enkephalin) elicited Ca<SUP>2+</SUP>-activated Cl<SUP>−</SUP> … Ketamine, propofol, halothane, and ethanol themselves did not elicit any currents in oocytes expressing <I>μ</I>OR-G<SUB>qi5</SUB>, whereas ketamine and ethanol inhibited the DAMGO-induced Cl<SUP>−</SUP> …
  • NAID 10027909045
  • Comparison of Five Benzodiazepine-Receptor Agonists on Buprenorphine-Induced μ-Opioid Receptor Regulation
  • Poisnel Geraldine,Dhilly Martine,Le Boisselier Reynald [他],BARRE Louisa,DEBRUYNE Daniele
  • Journal of pharmacological sciences 110(1), 36-46, 2009-05-20
  • … Using 0.312 – 5 nM [3H]-DAMGO concentrations and Scatchard plot analysis, Bmax (maximal receptor density) and Kd (dissociation constant) were determined at different brain regions of interest (amygdala, cortex, hippocampus, hypothalamus, thalamus). …
  • NAID 10025736509
  • μ-Opioid Receptor Forms a Functional Heterodimer With Cannabinoid CB_1 Receptor : Electrophysiological and FRET Assay Analysis
  • Hojo Minoru,Sudo Yuka,Ando Yuko [他],MINAMI Koichiro,TAKADA Masafumi,MATSUBARA Takehiro,KANAIDE Masato,TANIYAMA Kohtaro,SUMIKAWA Koji,UEZONO Yasuhito
  • Journal of pharmacological sciences 108(3), 308-319, 2008-11-20
  • … [<sc><font size = "-2">D</font></sc>-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAMGO) or CP55,940 elicited K+ currents in Xenopus oocytes expressing μOR or CB1R together with G protein activated-inwardly rectifying K+ channels (GIRKs), respectively. …
  • NAID 10024593115

関連リンク

DAMGO. IUPAC name. (2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl) propanoyl]amino]propanoyl]amino]acetyl]-methylamino]- N-(2-hydroxyethyl)-3- phenylpropanamide. Other names. Ala2-MePhe4-Glyol5-Enkephalin, DAGO, ...

関連画像

John DamgoThe Cebuano Indie film “Ang Damgo ni 50 (tie) – ANG DAMGO NI ELEUTERIA Ang Damgo ni Eleuteriadependent activation of the erk1 2 pathway DAMGO.png


★リンクテーブル★
リンク元オピオイド」「アラニン(2)-メチルフェニルアラニン(4)-グリシンオール(5)-エンケファリン」「Ala(2)-MePhe(4)-Gly-ol(5)-Enkephalin

オピオイド」

  [★]

opioid
類麻薬
オピオイド受容体


作用

縮瞳

  • モルフィンと多くのμ,κアゴニストは瞳孔の縮小を引き起こす。これは瞳孔を支配する副交感神経の興奮による。μアゴニストを中毒量投与すると縮瞳し、pinpoints pupupilsはpathognomonicである。(GOO.559)

オピオイドとオピオイド類似物質の作用

GOO.552
Drugs  RECEPTOR TYPES
μ受容体 δ受容体 κ受容体
morphine +++  
methadone +++    
etorphine +++ +++ +++
levorphanol +++    
fentanyl +++    
sufentanil +++
DAMGO +++    
butorphanol P   +++
buprenorphine P   ーー
naloxone ーーー ーー
naltrexone ーーー ーーー
CTOP ーーー    
diprenorphine ーーー ーー ーーー
β-funaltrexamine ーーー ++
naloxonazine ーーー
nalorphine ーーー  
pentazocine P   ++
nalbuphine ーー   ++
naloxone benzoylhydrazone ーーー
bremazocine +++ ++ +++
ethylketocyclazocine P +++
U50,488     +++
U69,593     +++
spiradoline   +++
nor-Binaltorphimine ーーー
naltrindole ーーー
DPDPE   ++  
[[[[D-Ala2,Glu4]deltorphin]]   ++  
       
DSLET ++  
endogenous Peptides       
met-enkephalin ++ +++  
leu-enkephalin ++ +++  
β-endorphin +++ +++  
dynorphin A ++   +++
dynorphin B +++
α-neoendorphin +++
+アゴニスト ーアンタゴニスト P partial agonist

各鎮痛薬のオピオイド受容体への作用

         μ受容体 κ受容体
レミフェンタニル +++  ー
フェンタニル   +++  -
モルヒネ     +++  +
ペチジン     ++   +
トラマドール   +    -
ペンタゾシン   ー    ++
ブプレノルフィン P    ー
ナロキソン    ー    -




アラニン(2)-メチルフェニルアラニン(4)-グリシンオール(5)-エンケファリン」

  [★]

-Enkephalin
アラニン(2)-メチルフェニルアラニン(4)-グリシン(5)-エンケファリン


Ala(2)-MePhe(4)-Gly-ol(5)-Enkephalin」

  [★]

-エンケファリン

Ala(2)-MePhe(4)-Gly(5)-enkephalin、DAMGO


"http://meddic.jp/DAMGO" より作成


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