5'-guanidinonaltrindole

5'-Guanidinonaltrindole (5'-GNTI) is a selective, highly potent small-molecule antagonist of the kappa-type opioid receptor (KOR), with a Ki of approximately 0.18 nM. It is a guanidine derivative of the selective delta-opioid receptor antagonist naltrindole, first reported in 2000 by Jones and Portoghese. 5'-GNTI exhibits high selectivity for KOR over the mu-opioid receptor (MOR) and delta-opioid receptor (DOR). Additionally, it has been identified as a positive allosteric modulator of the alpha-1A adrenergic receptor. In animal models, 5'-GNTI demonstrates a slow onset and long duration of action, producing antidepressant-like effects and inducing scratching behavior. It is widely utilized as a pharmacological research tool and has no approved therapeutic indications or active clinical development.

Other names

5'-GNTI5'-guanidinonaltrindole di-trifluoroacetate5'-guanidinonaltrindole hydrochloride5'-guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinanGNTI