Peptide directoryHeart, vessels & kidneys

Pyr-apelin-13

Apelin-13 with its first residue sealed, the main apelin in the heart.

Where it comes from

Made in
Heart and blood: the predominant apelin found in human heart tissue
Sent out by
With the other apelins
Acts on
  • Heart muscle
  • Vessels
  • Kidney

What it does

  • The pyroglutamate cap blocks the enzymes that chew peptides from the front, so it outlasts plain apelin-13 in blood 1
  • The form actually present in human heart tissue, which is why it, and not apelin-13, is what infusion studies use 1
  • At the receptor it behaves as apelin-13 does: vessel relaxation through the endothelium, and a stronger, faster heartbeat 2

In medicine

  • Infused in healthy volunteers and in patients with heart failure as a research probe, where it raised cardiac output and lowered systemic resistance within minutes 2
  • No approved medicine and no clinical assay. Commercial apelin kits do not report the isoforms separately, so a published apelin level is a mixture 1

Beyond the body’s own use

  • Its discovery changed what counts as the real human apelin: the peptide most earlier work had used is not the one the heart mainly holds 1
  • Analogues meant for the clinic start from this form because of its stability, and none has yet reached a registered trial
  • Nothing is in human use beyond research infusions. How much of the apelin measured in blood is this form is still unknown 1

Sources

  1. Maguire et al., [Pyr1]apelin-13 identified as the predominant apelin isoform in the human heart, Hypertension 2009
  2. Japp et al., Acute cardiovascular effects of apelin in humans, Circulation 2010

This card describes what a medicine is for and what the evidence says; it recommends nothing. Talk to your clinician about anything you read here.