bremazocine

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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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Bremazocine

Systematic (IUPAC) name
6-ethyl- 3-[(1-hydroxycyclopropyl)methyl]- 11,11-dimethyl- 1,2,3,4,5,6-hexahydro- 2,6-methano- 3-benzazocin-8- ol or 2-(1-hydroxy- cyclopropylmethyl)- 5-ethyl- 9,9-dimethyl- 2'-hydroxy- 6,7-benzomorphan
Clinical data
Legal status	?
Routes of administration	Oral
Identifiers
CAS Registry Number	75684-07-0
ATC code	None
PubChem	CID: 1223
IUPHAR/BPS	1603
ChemSpider	1186
UNII	ISF76M2DBE Y
ChEMBL	CHEMBL1165792 Y
Chemical data
Formula	C20H29NO2
Molecular mass	315.45 g/mol
SMILES OC1(CC1)CN4[C@@H]3Cc2c(cc(O)cc2)[C@@](C3(C)C)(CC4)CC

Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress breathing.

See also

• Benzomorphan

References

English Journal

• 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

Japanese Journal

• 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

Related Links

• bremazocine .com

bremazocine.com e-mail info@bremazocine.com bremazocine.com e-mail info@bremazocine.com

• Bremazocine CAS# 75684-07-0 API Supplier, LGM Pharma

LGM Pharma is a Bremazocine CAS# 75684-07-0 API supplier based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more. ... LGM Pharma is a Bremazocine 75684-07-0 active pharmaceutical ...

Related Pictures

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★リンクテーブル★

リンク元

「オピオイド」

「オピオイド」

　　[★]

英

opioid

同

類麻薬

関

オピオイド受容体

• オピオイド受容体に結合するモルフィン様物質のことを指す。

• 内因性のオピオイドペプチドが発見され、これらは内因性オピオイドペプチドと呼ばれるようになった。

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	ーー
naltrexone	ーーー	ー	ーーー
CTOP	ーーー
diprenorphine	ーーー	ーー	ーーー
β-funaltrexamine	ーーー	ー	＋＋
naloxonazine	ーーー	ー	ー
nalorphine	ーーー		＋
pentazocine	P		＋＋
nalbuphine	ーー		＋＋
naloxone benzoylhydrazone	ーーー	ー	ー
bremazocine	＋＋＋	＋＋	＋＋＋
ethylketocyclazocine	P	＋	＋＋＋
U50,488			＋＋＋
U69,593			＋＋＋
spiradoline	＋		＋＋＋
nor-Binaltorphimine	ー	ー	ーーー
naltrindole	ー	ーーー	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　　　　－