adrenomedullin receptor

Adrenomedullin (AM) (22-52), human acetate is an antagonist of calcitonin generelated peptide receptor in the hindlimb vascular bed of the cat and an adrenomedullin receptor.

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and 0.317 nM alone and with RAMP1, 2, or 3, respectively. It induces cAMP accumulation in COS-7 cells transfected with CTR2 (EC50 = 0.166 nM). Salmon calcitonin inhibits bone resorption by osteoclasts in a pit formation assay using rat bone slices (ID50 = 0.003 pg/mL) and lowers calcium level in vivo in a bioassay of hypocalcemia in rats (ED15 = 33.9 mg/kg). Formulations containing salmon calcitonin have been used to treat hypercalcemia, bone destruction by osteoporosis, and Paget's disease.

Adrenomedullin (16-31), human TFA, a fragment containing amino acid residues 16-31 of human adrenomedullin (hADM), demonstrates significant CGRP1 receptor affinity and exhibits pressor activity in the rat systemic vascular bed while lacking this effect in cats [1].

Adrenomedullin (AM) (22-52), human [22-52-Adrenomedullin human], TFA, is a C-terminal truncated analogue of adrenomedullin and acts as an adrenomedullin receptor antagonist.

Adrenomedullin 11-50 rat is a peptide fragment of adrenomedullin that possesses systemic vasodilator activity at the level of calcitonin gene-related peptide-1 (CGRP1) receptor activation. Adrenomedullin and its peptide may be used in bone growth studies.

Adrenomedullin (1-50), rat, is a 50 amino acid peptide that induces selective arterial vasodilation via activation of the CGRP1 receptor. This peptide hormone is expressed in rat adrenal glands, lung, kidney, heart, and spleen, as well as in the duodenum and submandibular glands.

Adrenomedullin (AM) (13-52), human is a 40-amino acid peptide belonging to the calcitonin gene-related peptide (CGRP) family. As a potent endothelium-dependent vasodilator, it regulates vascular tone by acting on the CGRP1 receptor and can inhibit pulmonary vasoconstriction.

Endogenous central calcitonin (CT) receptor agonist that stimulates cAMP formation at a potency 350-fold greater than CT (ED50 values are 0.2 and 71 nM respectively). Displays no activity at calcitonin-gene related peptide (CGRP) and adrenomedullin recept