GUANIDINYL NALTRINDOLE

5′-Guanidinonaltrindole di(trifluoroacetate) Salt is a selective opioid receptor antagonist. It has also been utilized to develop fluorescent methods to identify phosphopantetheinyl transferase inhibitors.

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

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.