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

Add time:09/02/2019    Source:sciencedirect.com

We synthesized derivatives of the δ opioid receptor (DOR) antagonists naltrindole (NTI) and compound 1 that were modified with small alkyl or fluorinated ethyl substituents on the 17-nitrogen. Although the derivatives showed decreased binding affinities for the opioid receptors, their selectivities for the DOR were higher than the parent compounds NTI and compound 1. Surprisingly, 17-fluoroethyl NTI derivatives exerted DOR inverse agonistic activities. The DOR inverse agonism of compounds 4c–e was less efficacious but significant, as compared with a standard DOR inverse agonist ICI-174864. On the other hand, compound 1 and its derivatives with small alkyl or monofluoroethyl substituents were partial agonists, but the derivatives having di- or trifluoroethyl group showed neither agonistic nor inverse agonistic activities.

We also recommend Trading Suppliers and Manufacturers of NALTRINDOLE HYDROCHLORIDE (cas 111469-81-9). Pls Click Website Link as below: cas 111469-81-9 suppliers

Prev:Short communicationAntinociception after intracerebroventricular administration of naltrindole in the mouse
Next:ArticlesThe Effects of Intravenous Naltrindole and Naltrindole 5′-Isothiocyanate on Sufentanil-Induced Respiratory Depression and Antinociception in Rats)