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Merck
CN

G3416

5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate

solid, ≥98% (HPLC)

别名:

GNTI

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关于此项目

经验公式(希尔记法):
C27H29N5O3 · 2C2HF3O2 · xH2O
化学文摘社编号:
分子量:
699.60 (anhydrous basis)
MDL number:
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352202
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

solid

solubility

H2O: 30 mg/mL

storage temp.

2-8°C

Gene Information

human ... OPRK1(4986)

Application

5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate (GNTI) has been used as a selective κ opioid receptor antagonist:
  • to study the influence of opioid receptor types on the anti-hyperalgesic effect of dipeptidyl peptidase 4 (DPP4) inhibitors in inflammation
  • to study the role of κ opioid receptor in the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB)
  • to validate its inhibitory actions on Akt kinase activities

Biochem/physiol Actions

5′-Guanidinonaltrindole di(trifluoroacetate) (GNTI) is a 5‘-guanidine derivative and a selective κ opiate receptor antagonist. It is five-fold more potent and 500-fold more selective than norbinaltorphimine (nor-BNI) for the κ opioid receptor in smooth muscle preparations.

Features and Benefits

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.

Legal Information

Sold under US Patent No. 6,500,824.


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

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相关内容

Instructions


Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific Reports (2017)
Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific reports (2017)
R M Jones et al.
European journal of pharmacology, 396(1), 49-52 (2000-05-24)
5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid



全球贸易项目编号

货号GTIN
G3416-5MG04061833629949