Calcitonin (8-32), salmon, is a highly selective amylin receptor antagonist. Calcitonin, a hormone involved in calcium and phosphorus metabolism, is primarily produced by the parafollicular or C cells in the thyroid gland of mammals.
Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus.
Amylin is a peptide that displays 50% homology with calcitonin gene-related peptide (CGRP), Amylin is colocalized with somatostatin in endocrine cells of the gastric fundus. In isolated mouse stomach, amylin caused a concentration-dependent decrease in ac
Amylin (8-37), rat, is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Also known as islet amyloid precursor peptide (IAPP), Amylin is co-secreted with insulin.
Pramlintide is a non-amyloidogenic analog of the antidiabetic peptide hormone amylin that contains proline residues substituted at positions 25, 28, and 29. It stimulates cAMP production in HEK293 cells expressing human amylin receptor 1a (AMY1a), AMY2a, and AMY3a (EC50s = 0.35, 22.9, and 0.89 nM, respectively). Pramlintide inhibits human islet amyloid polypeptide fibrilization in a concentration-dependent manner. In vivo, pramlintide (200 pg/kg) reduces brain levels of amyloid-β (1-40) and increases spontaneous alternation in the Y-maze in the Tg2576 transgenic mouse model of Alzheimer's disease.
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.