Calcitonin (salmon) (trifluoroacetate salt)

Calcitonin (salmon) (trifluoroacetate salt) Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption.^1,2 It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin.³ 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.^4,5 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).⁶ 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).⁷ Formulations containing salmon calcitonin have been used to treat hypercalcemia, bone destruction by osteoporosis, and Paget's disease.²

• Einzelnachweise

  1. Foster, G.V. Calcitonin. A review of experimental and clinical investigations Postgrad. Med. J. 44(511),411-422(1968).
  2. Chesnut, C.H., III, Azria, M., Silverman, S., et al. Salmon calcitonin: A review of current and future therapeutic indications Osteoporos. Int. 19(4),479-491(2008).
  3. Wimalawansa, S.J. Amylin, calcitonin gene-related peptide, calcitonin, and adrenomedullin: A peptide superfamily Crit. Rev. Neurobiol. 11(2-3),167-239(1997).
  4. Muff, R., Bühlmann, N., Fischer, J.A., et al. An amylin receptor is revealed following co-transfection of a calcitonin receptor with receptor activity modifying proteins-1 or -3 Endocrinology 140(6),2924-2927(1999).
  5. Christopoulos, G., Perry, K.J., Morfis, M., et al. Multiple amylin receptors arise from receptor activity-modifying protein interaction with the calcitonin receptor gene product Mol. Pharmacol. 56(1),235-242(1999).
  6. Udawela, M., Christopoulos, G., Tilakaratne, N., et al. Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors Mol. Pharmacol. 69(6),1984-1989(2006).
  7. McSheehy, P.M., Farina, C., Airaghi, R., et al. Pharmacologic evaluation of the calcitonin analogue SB 205614 in models of osteoclastic bone resorption in vitro and in vivo: Comparison with salmon calcitonin and elcatonin Bone 16(4),435-444(1995).

Calcitonin (salmon) (trifluoroacetate salt) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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