Puneet Varma (Editor)

5' Guanidinonaltrindole

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Covid-19
PubChem CID  6604846
ChemSpider  21259050
Formula  C27H29N5O3
IUPHAR/BPS  1669
ChEMBL  CHEMBL330427
Molar mass  471.55 g/mol
5'-Guanidinonaltrindole
Synonyms  5'-Guanidinonaltrindole, GNTI

5'-Guanidinonaltrindole (5'-GNTI) is an opioid antagonist used in scientific research which is highly selective for the κ opioid receptor. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist norbinaltorphimine. It has a slow onset and long duration of action, and produces antidepressant effects in animal studies. It also increases allodynia by interfering with the action of the κ-opioid peptide dynorphin.

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".

References

5'-Guanidinonaltrindole Wikipedia


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