Characterization of Pyrrolidinyl-hexahydro-pyranopiperazines as a Novel Kappa Opioid Receptor Agonist Scaffold

Autor: Brian Reed, Michael Miller, Mayako Michino, Eduardo R. Butelman, Ariel Ben-Ezra, Philip Pikus, Michelle Morochnik, Yuli Kim, Amy Ripka, Joseph Vacca, Mary Jeanne Kreek
Rok vydání: 2022
Předmět:
Zdroj: ACS Chemical Neuroscience. 13:1849-1856
ISSN: 1948-7193
DOI: 10.1021/acschemneuro.2c00258
Popis: The kappa agonist structure-activity relationship around the novel, pyrrolidinyl substituted pyranopiperazine scaffold was developed. More specifically, the dichloroPhenylAcetamide-Pyrrolidinyl-PyranoPiperazine (PAPPP) core A was the focus of our work. The modulation of kappa receptor potency/G-protein activation and arrestin recruitment with respect to changes of the piperazine R group in A was demonstrated. Reduced β
Databáze: OpenAIRE