Cardiovascular

AM

Adrenomedullin is a 52-amino-acid vasoactive peptide originally isolated from human pheochromocytoma. It is a potent vasodilator acting through CGRP receptors, promotes natriuresis, reduces inflammation, protects vascular endothelial barrier function, and enhances wound healing. Circulating AM levels rise in heart failure, sepsis, and critical illness — making it both a biomarker and emerging therapeutic target.

Ang(1-7) · A779 counter-regulatory

Angiotensin 1-7 is a 7-amino-acid peptide of the renin-angiotensin system (RAS) and the primary product of ACE2 enzyme activity. It opposes the vasoconstrictive, pro-inflammatory actions of Angiotensin II by acting on the Mas receptor — promoting vasodilation, natriuresis, anti-fibrosis, and anti-inflammation. Extensively studied for heart failure, hypertension, and COVID-19, it represents the counter-regulatory arm of the RAS.

Atrial Natriuretic Peptide · ANF

ANP (Atrial Natriuretic Peptide) is a 28-amino-acid cardiac hormone secreted by atrial cardiomyocytes in response to volume overload. It reduces blood pressure through natriuresis, vasodilation, and inhibition of the RAAS. Carperitide (synthetic ANP) is approved in Japan for acute heart failure. ANP is a key biomarker and drug target for heart failure and hypertension, studied alongside BNP and C-type natriuretic peptide.

APLNR ligand · apelin-13

Apelin is an endogenous peptide that acts as the ligand for the APJ receptor (APLNR), a GPCR expressed throughout the cardiovascular system. It improves cardiac output and vascular tone through both positive inotropy and vasodilation, increases nitric oxide production, and reduces oxidative stress. Research focuses on heart failure, pulmonary arterial hypertension, and its potential to replace or complement established cardiac peptides.

Brain Natriuretic Peptide · Nesiritide

BNP (B-type/brain natriuretic peptide) is a 32-amino-acid hormone secreted by ventricular cardiomyocytes in response to wall stress and volume overload. Clinically, it is the primary biomarker for heart failure diagnosis and prognosis. Recombinant BNP (nesiritide/Natrecor) was approved for acute decompensated heart failure, producing vasodilation and natriuresis. Research into modified natriuretic peptides continues for heart failure therapy.

BK · Kallidin precursor fragment

Bradykinin is a 9-amino-acid vasoactive peptide of the kinin-kallikrein system. It produces vasodilation, increased vascular permeability, pain, and inflammation by acting on B1 and B2 receptors. ACE inhibitors (a major drug class) lower blood pressure partly by preventing bradykinin degradation. Icatibant, a B2 antagonist, is approved for hereditary angioedema. Research also implicates bradykinin in COVID-19 pathology (bradykinin storm hypothesis).

DDAVP · 1-desamino-8-D-arginine vasopressin

Desmopressin (DDAVP) is a synthetic vasopressin analog modified to eliminate vasopressor activity while retaining antidiuretic potency. FDA-approved for central diabetes insipidus, nocturnal enuresis (bedwetting), and von Willebrand disease, it achieves selective V2 receptor activation. Research explores its role in cognitive enhancement, where intranasal administration shows effects on memory consolidation.

ET-1 · Big endothelin-1

Endothelin-1 (ET-1) is a 21-amino-acid vasoconstrictor peptide produced primarily by vascular endothelial cells. It is the most potent endogenous vasoconstrictor known, acting through ETA and ETB receptors on vascular smooth muscle and endothelium. Elevated ET-1 is implicated in pulmonary arterial hypertension, heart failure, and renal disease — driving the development of endothelin receptor antagonists (bosentan, ambrisentan, macitentan) as clinical drugs.

Examorelin · EP 23905

Hexarelin is one of the most potent synthetic GHRP compounds, producing the largest GH pulse among GHRPs. Beyond its GH-stimulating properties, research highlights direct cardioprotective effects through CD36 receptor binding, independent of GH or IGF-1. Studies show benefits in heart failure models, myocardial infarction recovery, and protection against ventricular dysfunction.

Victoza · Saxenda

Liraglutide is a once-daily GLP-1 receptor agonist approved for type 2 diabetes (Victoza) and obesity (Saxenda). It achieves fatty acid attachment to albumin for extended half-life, enabling daily dosing. The LEADER trial established significant cardiovascular mortality benefit in high-risk patients, and research continues into neuroprotective and anti-inflammatory properties beyond metabolic indications.

NPY

Neuropeptide Y (NPY) is a 36-amino-acid peptide and the most abundant neuropeptide in the mammalian CNS, acting through Y1–Y6 receptors. It is a potent orexigenic signal (stimulating appetite and fat storage), anxiolytic agent, vasoconstrictor, and regulator of circadian rhythms. Paradoxically, peripheral NPY promotes fat accumulation while central NPY drives food intake — making it a complex but high-priority metabolic research target.

Serelaxin · H2 relaxin

Relaxin-2 is an endogenous peptide hormone structurally related to insulin, primarily known for its role in pregnancy (cervical ripening, joint laxity). Research discovered its potent anti-fibrotic properties — it remodels collagen networks in heart, kidney, lung, and liver — making it a leading candidate for fibrosis and acute heart failure. Serelaxin (recombinant relaxin) reached Phase 3 trials for acute heart failure with promising early signals but did not meet primary endpoints.

Ozempic · Wegovy

Semaglutide is a long-acting GLP-1 receptor agonist approved for type 2 diabetes (Ozempic, Rybelsus) and obesity (Wegovy). By mimicking the incretin hormone GLP-1, it enhances glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying, and reduces appetite via central hypothalamic pathways. Landmark trials demonstrate up to 15–17% body weight reduction and significant cardiovascular mortality benefit.

Elamipretide · Szeto-Schiller 31

SS-31 (elamipretide) is a tetrapeptide that selectively targets cardiolipin in the inner mitochondrial membrane, stabilizing cristae architecture and enhancing ATP synthesis efficiency. It reduces mitochondrial ROS production and protects against ischemia-reperfusion injury, heart failure, and aging-related mitochondrial dysfunction. Phase 2 trials have been conducted for heart failure with preserved ejection fraction and Barth syndrome.

Thymosin Beta-4 Fragment · Tβ4 fragment

TB-500 is a synthetic version of the active region of Thymosin Beta-4, a naturally occurring peptide found in virtually all human cells. Research shows it promotes actin polymerization and cell migration, which accelerates wound healing, muscle repair, and vascular growth. It is particularly studied for its ability to reduce inflammation and promote cardiac tissue repair.

C₂₁₂H₃₅₀N₅₆O₇₈S · 4963.44 Da

Tβ4 · LKKTETQ

Thymosin Beta-4 is the full-length 43-amino-acid peptide and one of the most abundant intracellular proteins in mammalian cells. It sequesters G-actin, regulating actin polymerization and cell motility, which underpins its role in wound healing, cardiac repair, and immune cell migration. Clinical trials have examined it for dry eye disease, epidermolysis bullosa, and cardiac repair after myocardial infarction.

UCN1 · Urocortin

Urocortin 1 (UCN1) is a 40-amino-acid member of the CRH peptide family that activates both CRHR1 and CRHR2 receptors. It has potent cardioprotective effects — improving cardiac contractility, reducing ischemia-reperfusion injury, and stimulating natriuresis — making it a significant heart failure research target. It also modulates anxiety and appetite centrally. Phase 2 trials for chronic heart failure showed improvements in cardiac function.

ADH · Antidiuretic Hormone

Vasopressin (AVP) is a 9-amino-acid neuropeptide produced in the hypothalamus and released by the posterior pituitary. It regulates water reabsorption via V2 receptors in renal collecting ducts and vasoconstriction via V1a receptors in blood vessels. Clinically used for diabetes insipidus, septic shock vasodilation, GI hemorrhage, and cardiac arrest. Extensive research also examines its roles in social bonding, memory, and stress responses.

Vasoactive Intestinal Peptide · Vasoactive Intestinal Polypeptide

VIP (Vasoactive Intestinal Peptide) is a 28-amino-acid neuropeptide with pleiotropic anti-inflammatory, bronchodilatory, and immunomodulatory effects mediated through VPAC1 and VPAC2 receptors. Research spans pulmonary arterial hypertension (inhaled VIP trials), inflammatory bowel disease, sepsis, Parkinson's disease, and CIRS (chronic inflammatory response syndrome). It suppresses Th1 cytokines and promotes Treg cell function.