Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists

Molecular Pharmacology ofδ-Opioid Receptors

“…On the other hand, it was an antagonist in almost all of the other systems tested (Chiu et al, 1996;Mullaney et al, 1996;Neilan et al, 1999;Piñeyro et al, 2005;Tryoen-Tóth et al, 2005), except for two reports in which it behaved as a weak partial agonist both in guanosine 59-3-O-(thio)-triphosphate (GTPgS) and cAMP accumulation assays (Liu and Prather, 2002;Piñeyro et al, 2005). NTI consistently behaved as an antagonist in all systems tested (Chiu et al, 1996;Szekeres and Traynor, 1997;Neilan et al, 1999;Labarre et al, 2000), but its fluoroethyl derivatives displayed partial inverse responses in relation to ICI 174864 (Nemoto et al, 2015). NTB was without efficacy in GTPgS binding assays carried out in mDOPrs/NG108-15 cells (Szekeres and Traynor, 1997) and human DOPrs/HEK membranes (Tryoen-Tóth et al, 2005).…”

A selective delta opioid receptor antagonist based on a stilbene core

“…5 Because of this role in the addictive effects of the opioid pain medications, selective DOP receptor antagonists are gaining interest in the field of pain management and psychiatry. 6–8 …”

Correction: Tanguturi et al. Discovery of Novel Delta Opioid Receptor (DOR) Inverse Agonist and Irreversible (Non-Competitive) Antagonists. Molecules 2021, 26, 6693

“…Besides, due to adding new References, the numeration of References with respect to the original publication has been modified. References [ 2 , 3 , 4 , 5 ] will appear in the document as References [6,8–10] respectively.…”