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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/11/02 20:25:06」(JST)

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  • Mu, delta, and kappa opioid receptor agonists induce peripheral antinociception by activation of endogenous noradrenergic system.
  • Romero TR, Guzzo LS, Duarte ID.SourceDepartment of Pharmacology, Institute of Biological Sciences, ICB-UFMG, Belo Horizonte, Minas Gerais, Brazil.
  • Journal of neuroscience research.J Neurosci Res.2012 Aug;90(8):1654-61. doi: 10.1002/jnr.23050. Epub 2012 Apr 2.
  • Opioid receptor agonists induce noradrenaline release in the supraspinal, spinal, and peripheral sites. Endogenous noradrenaline release can induce an antinociceptive effect by activation of the α(2) adrenoceptor. This interaction between the opioid and the adrenergic systems could be the alternati
  • PMID 22473744
  • δ-Opioid receptor agonist SNC80 induces central antinociception mediated by Ca2+ -activated Cl- channels.
  • Pacheco Dda F, Pacheco CM, Duarte ID.SourceDepartment of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais School of Biological Sciences and Health, University Center Newton Paiva, Belo Horizonte, Brazil.
  • The Journal of pharmacy and pharmacology.J Pharm Pharmacol.2012 Aug;64(8):1084-9. doi: 10.1111/j.2042-7158.2012.01472.x. Epub 2012 May 22.
  • OBJECTIVES: The aim of this study was to determine whether Ca(2+)-activated Cl(-) channels (CaCCs) are involved in central antinociception induced by the activation of µ-, δ- and κ-opioid receptors.METHODS: The nociceptive threshold for thermal stimulation was measured using the tail-flick test i
  • PMID 22775211


  • オピエートのフロンティア電子密度の統計解析
  • 水上 善博
  • 滋賀大学教育学部紀要. 3, 自然科学 54, 35-39, 2004
  • … molecular orbital calculations.Calculated opiates are morphine, oxymorphone, levorphanol, nalorphine, naloxone, levallorphan, heroin, codeine, etorphine, dihydromorphine, normorphine, pentazocine, apomorphine, buprenorphine, butorpahnol, dihydrocodeine, oxycodone, thebaine, bremazocine, cyclazocine, ketocyclazocine, naloxazone, naltrexazone, oxymorphazone.25 molecules have common molecular skeleton that includes 10 atoms(one nitrogen atom, one oxygen atom and 8 carbon atoms).Electron densities of HOMO on these 10 atoms are used to perform principal …
  • NAID 110001183530
  • Bremazocine Recognizes the Difference in Four Amino Acid Residues to Discriminate Between a Nociceptin/Orphanin FQ Receptor and Opioid Receptors
  • SEKI Takahiro,MINAMI Masabumi,KIMURA Chiaki,UEHARA Tomoya,NAKAGAWA Takayuki,SATOH Masamichi
  • The Japanese journal of pharmacology 77(4), 301-306, 1998-08-01
  • … We investigated the molecular basis of the discrimination between nociceptin/orphanin FQ receptor (NociR) and opioid receptors (OPRs) by bremazocine, a non-type-selective opioid ligand. … Construction of several chimeric receptors between NociR and κ-opioid receptor (KOPR) and mutant NociRs followed by binding experiments with [<SUP>3</SUP>H]bremazocine showed that the mutation of only four amino acid residues of NociR, Ala<SUP>216</SUP>, Val<SUP>279</SUP>, Gln<SUP>280</SUP> …
  • NAID 10008193474

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File:Bremazocine structure.png - Wikimedia benzomorphans 8 cac alazocine bremazocine  cac alazocine bremazocine dezocineBremazocine is a κ-opioid receptor Bremazocine is a κ-opioid receptor Chemical structure of Phenazocine.







  • 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)


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


         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    -