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Product Details
Description |
Octreotide acetate is a synthetic somatostatin analogue that serves various functions and has diverse medical uses. By reducing watery diarrhea, it helps mitigate the loss of body fluids and minerals. Additionally, it is employed in the treatment of acromegaly, a condition characterized by excessive production of growth hormone, and in gastroenteropancreatic tumors. Octreotide acetate acts as an agonist for μ-opioid receptors and δ-opioid receptors, inhibiting the secretion of growth hormone, glucagon, insulin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. |
Function |
Stable in sterile saline solutions, octreotide acetate has a half-life of approximately 100 minutes and is administered via subcutaneous injection for palliative treatment of metastatic carcinoid tumors and VIP-secreting tumors. It proves effective in reducing symptoms such as severe diarrhea, facial flushing, and wheezing associated with carcinoid tumors, as well as in managing VIPomas, which cause profuse watery diarrhea. In acromegaly, octreotide acetate is employed when patients are unresponsive to previous pituitary radiation therapy or surgery, reducing blood levels of growth hormone and insulin-like growth factor-I (IGF-I). |
Uses |
Octreotide acetate has been explored for potential applications in conditions such as diabetes, psoriasis, Alzheimer's disease, and as an adjunctive treatment for hyperinsulinemia in patients with insulinomas. Its synthetic nature and prolonged duration of action make it a valuable therapeutic agent, inhibiting the pathologically increased secretion of various hormones and peptides within the gastro-entero-pancreatic endocrine system. |
InChI:InChI=1/C49H66N10O10S2.C2H4O2/c1-28(61)39(25-60)56-48(68)41-27-71-70-26-40(57-43(63)34(51)21-30-13-5-3-6-14-30)47(67)54-37(22-31-15-7-4-8-16-31)45(65)55-38(23-32-24-52-35-18-10-9-17-33(32)35)46(66)53-36(19-11-12-20-50)44(64)59-42(29(2)62)49(69)58-41;1-2(3)4/h3-10,13-18,24,28-29,34,36-42,52,60-62H,11-12,19-23,25-27,50-51H2,1-2H3,(H,53,66)(H,54,67)(H,55,65)(H,56,68)(H,57,63)(H,58,69)(H,59,64);1H3,(H,3,4)/t28-,29-,34-,36+,37+,38-,39-,40+,41+,42+;/m1./s1
A solid-phase method for the preparation...
Structure–activity relationship studies ...
Subcutaneous (SC) octreotide acetate effectively relieves the diarrhea and flushing associated with carcinoid syndrome but requires long-term multiple injections daily. A microencapsulated long-acting formulation (LAR) of octreotide acetate has been developed for once-monthly intramuscular dosing.
(Figure Presented) Getting the better of...
The new electrophilic trifluoromethylati...
H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OH
octreotide
Conditions | Yield |
---|---|
With ammonium acetate; pyrographite; In tetrahydrofuran; water; at 20 ℃;
|
85.6% |
D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr(ol)
octreotide
Conditions | Yield |
---|---|
In water; at 20 ℃; for 47.5h; pH=7.4; aq. phosphate buffer;
|
80% |
With phosphate buffer; air; at 25 ℃; for 48h; Yield given;
|
|
With ammonium acetate; for 48h; pH=7.0;
|
|
With air;
|
Boc-D-Phe-OH
Togni's reagent
Togni's reagent II
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