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
solubility
H2O: 30 mg/mL
storage temp.
2-8°C
Quality Level
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
新产品
此项目有
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
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)
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
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
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