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Merck
모든 사진(1)

주요 문서

G3416

Sigma-Aldrich

5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate

solid, ≥98% (HPLC)

동의어(들):

GNTI

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About This Item

실험식(Hill 표기법):
C27H29N5O3 · 2C2HF3O2 · xH2O
CAS Number:
Molecular Weight:
699.60 (anhydrous basis)
UNSPSC 코드:
12352202
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

solid

solubility

H2O: 30 mg/mL

저장 온도

2-8°C

유전자 정보

human ... OPRK1(4986)

애플리케이션

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

생화학적/생리학적 작용

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.

특징 및 장점

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.

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

Eyeshields, Gloves, type N95 (US)


시험 성적서(COA)

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문서 라이브러리 방문

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)
C T Chan et al.
Molecular imaging and biology, 11(3), 144-158 (2008-12-03)
Protein phosphorylation mediated by protein kinases controls numerous cellular processes. A genetically encoded, generalizable split firefly luciferase (FL)-assisted complementation system was developed for noninvasive monitoring phosphorylation events and efficacies of kinase inhibitors in cell culture and in small living subjects
Ryan Loh et al.
Behavioural brain research, 323, 1-10 (2017-01-26)
Previous work from our laboratory has shown that nonspecific kappa opioid receptor (KOR) antagonism in primary somatosensory cortex (S1) can inhibit acquisition for the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB). Although studies have demonstrated that KOR activation can alter
W C Stevens et al.
Journal of medicinal chemistry, 43(14), 2759-2769 (2000-07-14)
The indole moiety in the delta-opioid antagonist, naltrindole (2, NTI), was employed as a scaffold to hold an "address" for interaction with the kappa-opioid receptor. The attachment of the address to the 5'-position of the indole moiety was based on

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