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Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent[1] | [IC 50]
SSTR2: 37.6 nM (EC50); SSTR3: 31.3 nM (EC50); SSTR4: 10.5 nM (EC50) | [References]
[1] Dasgupta P, et al. Pharmacological Characterization of Veldoreotide as a Somatostatin Receptor 4 Agonist. Life (Basel). 2021 Oct 12;11(10):1075. DOI:10.3390/life11101075
[2] Pl?ckinger U, et al. DG3173 (somatoprim), a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue, effectively reduces GH secretion in human GH-secreting pituitary adenomas even in Octreotide non-responsive tumours. Eur J Endocrinol. 2012 Feb;166(2):223-34. DOI:10.1530/EJE-11-0737 |
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