N/A
N/A 用途与合成方法
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)
Pasireotide pamoate exhibits unique high-affinity binding to human somatostatin receptors.
Pasireotide pamoate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells with an IC
50
of 0.4±0.1 nM.
Pasireotide pamoate (160mg/Kg/month; s.c.; for 4 months) decreases serum insulin levels and increases serum glucose levels in Pdx1-Cre.
Pasireotide pamoate displays a reduction in tumor activity and reduces Pancreatic Neuroendocrine Tumor (PNET) size in Pdx1-Cre.
Pasireotide pamoate increases apoptosis in PNETs in Pdx1-Cre.
Pasireotide pamoate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in in a mouse model of immune-mediated arthritis.
| Animal Model: | Eight 12-month old mice carrying the Men1 allele, Men1 floxed/floxed conditional knockout (Pdx1-Cre) |
| Dosage: | 60mg/kg |
| Administration: | Subcutaneous injection; very month; for 4 months |
| Result: | Decreased serum insulin levels and increases serum glucose levels in Pdx1-Cre. |
