63-89-8CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)([O-])OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCKILNVBDSWZSGLL-KXQOOQHDSA-N1,2-dihexadecanoyl-sn-glycero-3-phosphocholine is a phosphatidylcholine 32:0 in which the 1- and 2-acyl groups are specified as hexadecanoyl (palmitoyl). A synthetic phospholipid used in liposomes and lipid bilayers to study biological membranes. It is also a major constituent of pulmonary surfactants. It has a role as a surfactant and a mouse metabolite. It is a phosphatidylcholine 32:0 and a 1-acyl-2-hexadecanoyl-sn-glycero-3-phosphocholine. It is functionally related to a hexadecanoic acid. It is a conjugate base of a 1,2-di-O-palmitoyl-sn-glycero-3-phosphocholine.
Lipids -> Unambiguous Lipids
Lipids -> Glycerophospholipids [GP] -> Glycerophosphocholines [GP01] -> Diacylglycerophosphocholines [GP0101]
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
283.9 Ų [M+H]+ [CCS Type: DT; Buffer gas: N2; Sample Type: Human plasma; Dataset: Unambiguous Lipids]
283.19 Ų [M+CH3COO]- [CCS Type: TIMS; Method: single field calibrated]
R - Respiratory system
QR - Respiratory system
Colfosceril palmitate has shown to significantly reduce the risk of pneumothoraces, pulmonary interstitial emphysema and mortality. Unlike naturals surfactants, colfosceril palmitate reduces the risk of bronchopulmonary dysplasia, intraventricular hemorrhage and patent ductus arteriosus. In clinical placebo-controlled trials, there was a significant reduction in the number of deaths attributed to hyaline membrane disease, the incidence of pulmonary air leaks, oxygen requirements and mean airway pressure. Some reports have indicated a lack of therapeutic effect due to the absence of surfactant protein.
Treatment with colfosceril palmitate aims to reinflate a collapsed area of the lung, improve compliance and reduce intrapulmonary shunting. The actions of colfosceril palmitate are perfomed by replacing the defficient or innefective endogenous lung surfactant and thus, reducing the tension and stabilizing the alveoli from collapsing. Colfosceril palmitate will form a very thin film that will cover the surface of the alveolar cells and therefore it will reduce surface tension.
The absorption is done directly in the alveolus into the lung tissue. As the lung surfactant is distributed in the bronchi, bronchioles and alveoli, its highest concentration is at the alveolar air-fluid interface where it remains as a monolayer.
After 5 days, most of the administered dose (56%) is distributed throughout the body with renal and fecal excretion being the minor elimination pathway representing the 4 and 2% of the eliminated dose respectively. The major route of elimination is by expelled air which accounts for 28% of the administered dose.
読み込み中…
63-89-8DTXSID5046720CHEMBL1200737CHEBI:72999化学的特性white powder
Colfosceril palmitate is distributed uniformly to all lobes of the lung, distal airways and alveolar spaces. It will not enter the systemic circulation in healthy lungs, however when the integrity of the tissue is distrupted colfosceril can reach systemic circulation. Even 5 days after administration, there are traces of colfosceril palmitate retained in the body that represented 72% of the administered dose which by then have entered pathways of lipid metabolism to become tissue associated.
After 5 days of drug administration, the lung and liver would contain 10% of the administered dose and the elimination via renal excretion accounts only for 8% of the administered dose. This proved a very small renal clearance and confirmed that the major elimination route is by expired air.
用途生体膜モデル、リポソーム調製用。
使用1,2-dipalmitoyl-sn-glycero-3-phosphocholine is a major phospholipid constituent and primary surface tension lowering component of natural lung surfactant. Colfosceril Palmitate is used as pulmonary surfactant and diagnostic aid (fetal lung maturity).
一般的な説明1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine is a strong bilayer-forming lipid. It the most common phospholipid in mammalian membranes. It is also an important component of the mucosal layer of the colon.
純化方法It has three crystalline forms 1, 2 and ' which change at 60-70o and at 229o, respectively. In order to obtain a fine powder, ~2 g are dissolved in CHCl3 (15mL) and pet ether (b 35-60o) is added; the solution is evaporated to dryness in vacuo at <20o and then dried at 0.1mm over CaCl2. [Baer & Maurukas J Am Chem Soc 74 158 1952, Baer & Kates J Biol Chem 185 615 1950, Beilstein 4 IV 1463.]
定義本品は、次の化学式で表される有機化合物である。
定義ChEBI: A phosphatidylcholine 32:0 in which the 1- and 2-acyl groups are specified as hexadecanoyl (palmitoyl). A synthetic phospholipid used in liposomes and lipid bilayers to study biological membranes. It is also a major constituent of pulmonary surfactants.