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Merck
CN
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文件

安全信息

B8312

Sigma-Aldrich

BNTX maleate salt hydrate

≥98% (HPLC)

别名:

7(E)-Benzylidenenaltrexone maleate salt hydrate, BNTX-7 maleate salt hydrate, Morphinan-6-one,17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-7-(phenylmethylene)-,(5a,7E)- maleate salt hydrate

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About This Item

经验公式（希尔记法）:
C31H31NO8 · xH2O
分子量:
545.58 (anhydrous basis)
MDL编号:
MFCD12912399
UNSPSC代码:
12352200
PubChem化学物质编号:
329773306
NACRES:
NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

yellow

溶解性

DMSO: >20 mg/mL

储存温度

−20°C

SMILES字符串

O.OC(=O)\C=C/C(O)=O.Oc1ccc2C[C@H]3N(CC[C@@]45[C@@H](Oc1c24)C(=O)\C(C[C@@]35O)=C\c6ccccc6)CC7CC7

InChI

1S/C27H27NO4.C4H4O4.H2O/c29-20-9-8-18-13-21-27(31)14-19(12-16-4-2-1-3-5-16)23(30)25-26(27,22(18)24(20)32-25)10-11-28(21)15-17-6-7-17;5-3(6)1-2-4(7)8;/h1-5,8-9,12,17,21,25,29,31H,6-7,10-11,13-15H2;1-2H,(H,5,6)(H,7,8);1H2/b19-12+;2-1-;/t21-,25+,26+,27-;;/m1../s1

InChI key

AGUNLJBLOJAUKM-ZKJXOIBSSA-N

应用

BNTX, a selective nonpeptide σ1 opioid receptor (DOR1) antagonist, is used in σ opioid receptor research to help differentiate and characterized the function and role of the σ1 opioid receptor versus other σ opioid receptor subtypes. BNTX was used to help define the role of σ1 opioid receptors in neurological processes such as anxiety. It was used to help define the role of σ opioid receptors in myocardial infarct development and size.

生化/生理作用

BNTX is a selective nonpeptide δ1 opioid receptor antagonist. It antagonizes the effect of D-Pen2,5-enkephalin (a δ1 agonist 4-6 fold, but did not affect the activity of δ2 or μ agonists.<<<107>>> BNTX is used to discriminate among opioid receptor subtypes in effects such as alcohol and drug dependence. It binds 100× more tightly to δ1 than to δ2 receptors. In the tail-flick assay, antinocieceptive ED50 = 646.4 pmol/mouse.

特点和优势

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形图

Exclamation markEnvironment
GHS07,GHS09

警示用语：

Warning

危险声明

H319,H400

预防措施声明

P273 - P305 + P351 + P338

危险分类

Aquatic Acute 1 - Eye Irrit. 2

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

法规信息

监管及禁止进口产品

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Garrett J Gross et al.
Journal of cardiovascular pharmacology, 59(2), 194-197 (2011-12-02)
Eribis peptide 94 (EP 94) is a novel enkephalin derivative that binds with high potency to μ and δ opioid receptors with less affinity for the κ opioid receptor. This compound has recently been shown to produce an acute reduction
Yoshinori Miyata et al.
Bioorganic & medicinal chemistry letters, 21(16), 4710-4712 (2011-07-19)
We evaluated antimalarial and/or chloroquine-resistance reversing effects of five opioid receptor antagonists. Although none of the evaluated compounds showed antimalarial effects, some of them, especially the δ(1) receptor antagonist, 7-benzylidenenaltrexone (BNTX) exhibited potent chloroquine-resistance reversing effects in Plasmodium chabaudi.
Azusa Sugiyama et al.
Neuropharmacology, 79, 314-320 (2013-12-18)
Recently, we reported that the δ opioid receptor (DOR) agonist KNT-127 produces anxiolytic-like effects in behaving rats. Here, we report on the roles of DOR subtypes ( DOR(1) and DOR(2)) play in mediating KNT-127-induced anxiolytic-like effects. Pretreatment with the DOR(2)-selective
So Young Kim et al.
Oncotarget, 8(37), 61057-61071 (2017-10-06)
Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a potential biological anticancer agent. However, a wide range of human primary cancers, including pancreatic cancer, display resistance to apoptosis induction by TRAIL. Therefore, this resistance needs to be overcome to allow TRAIL

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