Tìm theo
Methyl aminolevulinate
Các tên gọi khác (4 ) :
  • 5-Aminolevulinic acid methyl ester
  • Aminolevulinic acid methyl ester
  • Methyl aminolevulinate
  • Methyl delta-aminolevulinate
Thuốc Gốc
Small Molecule
CAS: 33320-16-0
ATC: L01XD03
ĐG : Galderma Laboratories , http://www.galderma.com
CTHH: C6H11NO3
PTK: 145.1564
Methyl aminolevulinate is a prodrug that is metabolised to Protoporphyrin IX (a photosensitizer) used in photodynamic therapy.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H11NO3
Phân tử khối
145.1564
Monoisotopic mass
145.073893223
InChI
InChI=1S/C6H11NO3/c1-10-6(9)3-2-5(8)4-7/h2-4,7H2,1H3
InChI Key
InChIKey=YUUAYBAIHCDHHD-UHFFFAOYSA-N
IUPAC Name
methyl 5-amino-4-oxopentanoate
Traditional IUPAC Name
methyl aminolevulinate
SMILES
COC(=O)CCC(=O)CN
Độ hòa tan
Freely soluble
logP
-1.2
logS
0.18
pKa (strongest acidic)
16.12
pKa (Strongest Basic)
7.83
PSA
69.39 Å2
Refractivity
35.22 m3·mol-1
Polarizability
14.55 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : After topical application of methyl aminolevulinate, porphyrins will accumulate intracellularly in the treated skin lesions. The intracellular porphyrins (including PpIX) are photoactive, fluorescing compounds and, upon light activation in the presence of oxygen, singlet oxygen is formed which causes damage to cellular compartments, in particular the mitochondria. Light activation of accumulated porphyrins leads to a photochemical reaction and thereby phototoxicity to the light-exposed target cells.
Cơ Chế Tác Dụng : Methyl aminolevulinate is a prodrug that is metabolised to Protoporphyrin IX (a photosensitizer) used in photodynamic therapy. Photosensitization following application of methyl aminolevulinate cream occurs through the metabolic conversion of methyl aminolevulinate (prodrug) to photoactive porphyrins (PAP), which accumulates in the skin lesions to which the cream has been applied. When exposed to light of appropriate wavelength and energy, the accumulated photoactive porphyrins produce a photodynamic reaction, resulting in a cytotoxic process dependent upon the simultaneous presence of oxygen. The absorption of light results in an excited state of porphyrin molecules, and subsequent spin transfer from photoactive porphyrins to molecular oxygen generates singlet oxygen, which can further react to form superoxide and hydroxyl radicals.
Dược Động Học :
▧ Absorption :
In vitro, after 24 hours the mean cumulative absorption through human skin was 0.26% of the administered dose.
Độc Tính : The severity of local phototoxic reactions such as erythema, pain and burning sensation may increase in case of prolonged application time or very high light intensity.
Chỉ Định : For topical use, in combination with 570 to 670 nm wavelength red light illumination, in the treatment of non-hyperkeratotic actinic keratoses of the face and scalp in immunocompetent patients when used in conjunction with lesion preparation (debridement using a sharp dermal curette).
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Metvixia 16.8% cream
    Giá bán buôn : USD >82.2
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Metvix
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00992
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=157922
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507004
ChemSpider
http://www.chemspider.com/Chemical-Structure.138950.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0299-6300-02
PharmGKB
http://www.pharmgkb.org/drug/PA164784028
Wikipedia
http://en.wikipedia.org/wiki/Methyl_aminolevulinate
Drugs.com
http://www.drugs.com/mtm/methyl-aminolevulinate-topical.html
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