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1001202-16-9 N-[(9H-Fluoren-9-ylmethoxy)carbonyl]glycylglycylglycylglycine

Synonyms

N-[(9H-Fluoren-9-ylmethoxy)carbonyl]glycylglycylglycylglycine;
Glycine, N-[(9H-fluoren-9-ylMethoxy)carbonyl]glycylglycylglycyl-;
Fmoc-Gly-Gly-Gly-Gly;
3-({[(9H-fluoren-9-yl)methoxy]carbonyl}amino)-2-sulfopropanoic acid;
2-[[2-[[2-[[2-(9H-fluoren-9-ylmethoxycarbonylamino)acetyl]amino]acetyl]amino]acetyl]amino]acetic acid;
N-[(9H-Fluoren-9-ylmethoxy)carbonyl]glycylglycylglycylglycine USP/EP/BP;
N-Fmoc-glycylglycylglycylglycine

inner Packing

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outer packing

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Applications

Terlipressin is a white powder with a molecular formula of C52H74N16O15S2, a molecular weight of 1227.37000, a density of 1.46 g/cm3, a boiling point of 1824ºC at 760 mmHg, and a chemical name of n-α-triglycyl-8-lysine-vasopressin. The flash point was 1056.9ºC, the refractive index was 1.664, and the vapor pressure was 0mmHg at 25°C.
In patients with liver cirrhosis, vascular anastomosis and portal venous pressure increase may occur between the congested veins entering the portal circulation and the body veins. Anastomosis most often occurs between the azygos vein and the lower end of the esophagus, namely esophageal varices. When they expand, they become thick and can rupture into the esophageal cavity, causing hematemesis and endangering life. Injections of the pituitary hormone vasopressin can control bleeding. It causes severe constriction of the internal blood vessels which reduces the portal pressure. However, the effect of vasopressin injection is short-lived and can cause side effects such as colic, coronary constriction, and increased fibrinolysis. This product is a precursor of vasopressin. After injection into the blood, the glycyl group in the molecule is catalyzed by enzymes to produce a continuously low level of vasopressin. It produced the desired effect on portal vein blood pressure, but the change in arterial blood pressure was much smaller than with vasopressin, and there was little increase in fibrinolytic blood. The effect can be maintained for about 4 ~ 6h after one injection.
Terlivasopressin is a new synthetic long-acting vasopressin preparation, which belongs to a precursor drug with no activity itself. After the action of aminopeptidase, the 3 glycanyl residues at the n-terminal of terlivasopressin are removed in vivo, the active lysine vasopressin is slowly "released". It is this "slow release" mechanism that allows it to maintain smooth muscle contraction for up to 10 hours after a single dose, whereas vasopressin is active for only 20-40 minutes at the same dose. On the other hand, due to the slow enzymatic hydrolysis, the lysine vasopressin in circulation can not reach the toxic level, so the use of terlivasopressin is relatively safe. The pharmacological effect of terlivasopressin is to shrink visceral vascular smooth muscle and reduce visceral blood flow (such as reducing the blood flow to the mesentery, spleen, uterus, etc.), thus reducing the blood flow and portal venous pressure. On the other hand, terlivasopressin can also reduce the effect of plasma renin concentration, thus increasing the renal blood flow in patients with hepatorenal syndrome. Improve kidney function and increase urine volume. At present, terlivasopressin is the only drug that can improve the survival rate of patients with esophageal variceal rupture and hemorrhage. It used to be mainly used in the clinical treatment of variceal rupture and hemorrhage. In addition, terlivasopressin has also been successfully used in liver and kidney synthesis, and may also play a beneficial role in complicated refractory shock and cardiopulmonary resuscitation. Compared with vasopressin, it has a long-lasting effect, does not cause dangerous complications, including pro-fibrinolysis and serious complications in the cardiovascular system, and is easy to use (can be injected intravenously), so it is more suitable for the rescue and treatment of critically ill patients, clinical Application.

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