Cardiovascular and renal effects of novel nonpeptide nociceptin opioid peptide receptor agonists.

ABSTRACT:

Background and purpose

Partial agonists of the nociceptin opioid peptide (NOP) receptor have potential therapeutic use as antihypertensive and water diuretics (aquaretics). To date, peptide NOP receptor ligands have failed to progress in clinical trials due to poor pharmacokinetics and adverse effects. Nonpeptide, small-molecule NOP receptor ligands may be more suitable as therapeutic agents. This study investigated the cardiovascular and renal responses produced by the novel nonpeptide NOP agonists AT-403, AT-090, AT-127, and AT-039.

Experimental approach

Changes in mean arterial pressure (MAP), heart rate (HR), renal excretory function and occurrence of sedation and hyperphagia were determined before and after i.v. bolus injection or infusion of the NOP agonists in conscio

SUBMITTER: Denys IB 

PROVIDER: S-EPMC8716424 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature