5'-Guanidinonaltrindole
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| Other names | 5'-Guanidinonaltrindole, GNTI |
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5'-Guanidinonaltrindole (5'-GNTI) is an
κ opioid receptor. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist norbinaltorphimine.[1] It has a slow onset and long duration of action,[2][3] and produces antidepressant effects in animal studies.[4] It also increases allodynia by interfering with the action of the κ-opioid peptide dynorphin.[5]
In addition to activity at the KOR, 5'-GNTI has been found to act as a
positive allosteric modulator of the α1A-adrenergic receptor (EC50 = 41 nM), and this may contribute to its "severe transient effects".[6]