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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2012/09/22 10:32:21」(JST)
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Naloxonazine |
|
Other names
NIH 10894; NSC 612113, Bis-[5-α-4,5-Epoxy-3,14-dihydroxy-17-(2-propenyl)-morphinan-6-ylidene] hydrazine dihydrochloride
|
Identifiers |
CAS number |
82824-01-9 Y |
PubChem |
9576413 |
IUPHAR ligand |
1677 |
Jmol-3D images |
Image 1 |
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C=CCN1[C@H]2[C@]3([C@]4(C5=C(C2)C=CC(=C5O[C@H]4/C(=N/N=C\6/[C@@H]7OC8=C(C=CC9=C8[C@]72[C@]([C@@H](C9)N(CC2)CC=C)(CC6)O)O)/CC3)O)CC1)O
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Properties |
Molecular formula |
C38H42N4O6 |
Molar mass |
650.76 g mol−1 |
Y (verify) (what is: Y/N?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
Infobox references |
Naloxonazine is a potent irreversible mu opioid antagonist.[1] Naloxonazine forms spontaneously in acidic solutions of naloxazone, and may be responsible for much or all of the irreversible μ opioid receptor binding displayed by the latter.[2]
See also
- Oxymorphone-3-methoxynaltrexonazine (OM-3-MNZ) a similarly structured opioid also having two complete & mirrored morphinan carbon skeletons but which is a full agonist instead.[3]
References
- ^ Naloxonazine dihydrochloride
- ^ Hahn, E. F.; Pasternak, G. W. (1982-09). "Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites". Life Sciences 31 (12-13): 1385–1388. doi:10.1016/0024-3205(82)90387-3. PMID 6292633. http://www.sciencedirect.com/science/article/pii/0024320582903873. Retrieved 2011-10-18.
- ^ Image of OM-3-MNZ
English Journal
- Antinociceptive action of botulinum toxin type A in carrageenan-induced mirror pain.
- Drinovac Vlah V1, Bach-Rojecky L2, Lacković Z3.
- Journal of neural transmission (Vienna, Austria : 1996).J Neural Transm (Vienna).2016 Dec;123(12):1403-1413. Epub 2016 Aug 9.
- "Mirror pain" or mirror-image pain (MP) is pain opposite to the side of injury. Mechanism and frequency in humans are not known. There is no consent on therapy. Here we report that unilaterally injected botulinum toxin type A (BT-A) has bilateral effect in experimental MP, thus deserves to be invest
- PMID 27506955
- µ1 -Opioid receptors in the dorsomedial and ventrolateral columns of the periaqueductal grey matter are critical for the enhancement of post-ictal antinociception.
- de Freitas RL1,2,3,4, Medeiros P1,3, Khan AU1,5, Coimbra NC6,7,8.
- Synapse (New York, N.Y.).Synapse.2016 Dec;70(12):519-530. doi: 10.1002/syn.21926. Epub 2016 Sep 6.
- Generalised tonic and tonic-clonic seizures are followed by significant increase in nociceptive thresholds in both laboratory animals and humans. The endogenous opioid peptides play a role in antinociceptive signalling, and the periaqueductal grey matter (PAG) is recruited to induce analgesia. Thus,
- PMID 27503688
- Endogenous central amygdala mu-opioid receptor signaling promotes sodium appetite in mice.
- Smith CM1,2,3, Walker LL1, Leeboonngam T1,4, McKinley MJ1,5, Denton DA6,7,8, Lawrence AJ6,2.
- Proceedings of the National Academy of Sciences of the United States of America.Proc Natl Acad Sci U S A.2016 Nov 29;113(48):13893-13898. Epub 2016 Nov 14.
- Due to the importance of dietary sodium and its paucity within many inland environments, terrestrial animals have evolved an instinctive sodium appetite that is commensurate with sodium deficiency. Despite a well-established role for central opioid signaling in sodium appetite, the endogenous influe
- PMID 27849613
Japanese Journal
- Evidence for Separate Involvement of Different μ-Opioid Receptor Subtypes in Itch and Analgesia Induced by Supraspinal Action of Opioids
- Andoh Tsugunobu,Yageta Yuichi,Konno Mitsuhiro [他],YAMAGUCHI MIYAMOTO Tomomi,TAKAHATA Hiroki,NOJIMA Hiroshi,NEMOTO Hideo,KURAISHI Yasushi
- Journal of pharmacological sciences 106(4), 667-670, 2008-04-20
- … Facial scratching following morphine was not affected by the μ1-OR antagonist naloxonazine at doses that inhibited the antinociceptive effects. …
- NAID 10024320256
- Tyr-Pro-Trp-Gly-NH_2(Tyr-W-MIF-1)analogであるTyr-D-Pro-Trp-Gly-NH_2の抗侵害作用におけるμオピオイド受容体の関与について
- 中山 大助,渡邉 廣行,藤村 務 [他],櫻田 忍
- 東北薬科大学研究誌 53, 71-76, 2006-12
- … pretreatment with the μ_1-opioid receptor antagonist naloxonazine, the κ-opioid receptor antagonist, nor-binaltorphimine, or the δ-opioid receptor antagonist naltrindole. … pretreatment with higher doses of naloxonazine, but not by pretreatment with nor-binaltorphimine or naltrindole. …
- NAID 110006392398
- Dermorphin analogueであるH-Tyr-D-Arg-Phe-β-Ala-OHおよびH-Tyr-D-Arg-Phe-β-Ala-NH_2によるcapsaicinおよびsubstance P誘発性SBL行動抑制の違いについて
- 結城 正幸,渡邉 廣行,岩田 陽子 [他],中山 大助,照井 潤,櫻田 忍
- 東北薬科大学研究誌 50, 179-184, 2003-12
- … Pretreatment with naloxonazine significantly antagonized inhibitory action of TAPA-NH_2 on substance Pinduced SBL behavioural response without antagonistic effect against DAMGO and TAPA, while antinociceptive effect of DAMGO, TAPA and TAPA-NH_2 was completely inhibited by the pretreatment with naloxone. … capsaicin was completely inhibited by the pretreatment with naloxonazine, whereas naloxone at a dose of 1 mg/kg s. …
- NAID 110004686351
Related Links
- Buy Naloxonazine dihydrochloride (CAS 82824-01-9), Potent and selective μ1-opioid receptor antagonist, from Santa Cruz Biotechnology. ... Naloxonazine dihydrochloride is a potent and selective μ 1-opioid receptor antagonist. The μ ...
- Learn and talk about Naloxonazine , and check out Naloxonazine on Wikipedia, Youtube, Google News, Google Books, and Twitter on ...
Related Pictures
★リンクテーブル★
[★]
- 英
- opioid
- 同
- 類麻薬
- 関
- 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
+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 -