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Usage

Uses

Used in Pharmaceutical Research:
Guanidinonaltrindole is used as a selective κ opioid receptor antagonist for studying the influence of opioid receptor types on the anti-hyperalgesic effect of dipeptidyl peptidase 4 (DPP4) inhibitors in inflammation. This application helps researchers understand the role of κ opioid receptors in pain management and the development of new pain relief therapies.
Used in Neuroscience Research:
In the field of neuroscience, Guanidinonaltrindole is used as a selective κ opioid receptor antagonist to study the role of κ opioid receptors in forebrain-dependent associative tasks, such as Whisker-Trace Eyeblink conditioning (WTEB). This application aids in understanding the neural mechanisms underlying learning and memory processes.
Used in Enzyme Inhibition Studies:
Guanidinonaltrindole is also used to validate its inhibitory actions on Akt kinase activities. This application is crucial for developing fluorescent methods to identify phosphopantetheinyl transferase inhibitors, which are essential for studying enzyme function and regulation in various biological processes.

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.