apelin-13-peptide has been researched along with Hypotension* in 2 studies
2 other study(ies) available for apelin-13-peptide and Hypotension
| Article | Year |
|---|---|
The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment.
The apelinergic system is an important player in the regulation of both vascular tone and cardiovascular function, making this physiological system an attractive target for drug development for hypertension, heart failure and ischemic heart disease. Indeed, apelin exerts a positive inotropic effect in humans whilst reducing peripheral vascular resistance. In this study, we investigated the signaling pathways through which apelin exerts its hypotensive action. We synthesized a series of apelin-13 analogs whereby the C-terminal Phe Topics: Animals; Antihypertensive Agents; Apelin Receptors; beta-Arrestins; Blood Pressure; Cyclic AMP; HEK293 Cells; Humans; Hypotension; Intercellular Signaling Peptides and Proteins; Male; Rats, Sprague-Dawley; Receptors, G-Protein-Coupled; Signal Transduction | 2018 |
C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action.
Apelin is the endogenous ligand of the APJ receptor, a member of the G protein-coupled receptor family. This system plays an important role in the regulation of blood pressure and cardiovascular functions. To better understand the role of its C-terminal Phe(13) residue on ligand binding, receptor signaling, and hypotension, we report a series of modified analogues in which Phe(13) was substituted by unnatural amino acids. These modifications delivered new compounds exhibiting higher affinity and potency to inhibit cAMP accumulation compared to apelin-13. In particular, analogues Bpa(13) or (α-Me)Phe(13) were 30-fold more potent to inhibit cAMP accumulation than apelin-13. Tyr(OBn)(13) substitution led to a 60-fold improvement in binding affinity and induced stronger and more sustained drop in blood pressure compared to apelin-13. Our study identified new potent analogues of apelin-13, which represent valuable probes to better understand its structure-function relationship. Topics: Amino Acid Substitution; Animals; Apelin; Blood Pressure; Cyclic AMP; Hypotension; Intercellular Signaling Peptides and Proteins; Ligands; Male; Rats; Rats, Sprague-Dawley; Receptors, G-Protein-Coupled; Signal Transduction; Structure-Activity Relationship | 2015 |