Tìm theo
Ethylmorphine
Các tên gọi khác (5 ) :
  • Dionine
  • Ethyl morphine
  • Ethylmorphine
  • SID144206163
  • SID50113064
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 76-58-4
CTHH: C19H23NO3
PTK: 313.3908
A narcotic analgesic and antitussive. It is metabolized in the liver by ethylmorphine-N-demethylase and used as an indicator of liver function. It is not marketed in the US but is approved for use in various countries around the world. In the US it is a schedule II drug (single-entity) and schedule III drug (in combination products).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H23NO3
Phân tử khối
313.3908
Monoisotopic mass
313.167793607
InChI
InChI=1S/C19H23NO3/c1-3-22-15-7-4-11-10-13-12-5-6-14(21)18-19(12,8-9-20(13)2)16(11)17(15)23-18/h4-7,12-14,18,21H,3,8-10H2,1-2H3/t12-,13+,14-,18-,19-/m0/s1
InChI Key
InChIKey=OGDVEMNWJVYAJL-LEPYJNQMSA-N
IUPAC Name
(1S,5R,13R,14S,17R)-10-ethoxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10,15-tetraen-14-ol
Traditional IUPAC Name
ethylmorphine
SMILES
[H][C@@]12OC3=C(OCC)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1([H])C=C[C@@H]2O
Độ tan chảy
199-201 °C
Độ hòa tan
2610 mg/L (at 20 °C)
logP
1.7
logS
-2.6
pKa (strongest acidic)
13.78
pKa (Strongest Basic)
9.19
PSA
41.93 Å2
Refractivity
89.35 m3·mol-1
Polarizability
34.17 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ethylmorphine is metabolized by the enzyme cytochrome P450 2D6 to morphine. Morphine is a narcotic pain management agent indicated for the relief of pain in patients who require opioid analgesics for more than a few days. Morphine interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, morphine exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Morphine appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.
Cơ Chế Tác Dụng : A narcotic analgesic and antitussive. It is metabolized in the liver by ethylmorphine-N-demethylase and used as an indicator of liver function. It is not marketed in the US but is approved for use in various countries around the world. In the US it is a schedule II drug (single-entity) and schedule III drug (in combination products). Ethylmorphine is metabolized by the liver enzyme cytochrome P450 2D6 to morphine. The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. Morphine first acts on the mu-opioid receptors. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation. It has been shown that morphine binds to and inhibits GABA inhibitory interneurons. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Dược Động Học :

▧ Metabolism :
After ingestion, ethylmorphine is converted to morphine in the human liver by the CYP450-isozyme CYP2D6, similarly to codeine.
Chỉ Định : Ethylmorphine is an analgesic used for pain relief.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Erfa
    Sản phẩm biệt dược : Codethyline
  • Công ty : Merck
    Sản phẩm biệt dược : Dionina
  • Công ty : Meda
    Sản phẩm biệt dược : Lepheton
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01466
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5359271
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505092
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07537
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07929
ChemSpider
http://www.chemspider.com/Chemical-Structure.4514250.html
Wikipedia
http://en.wikipedia.org/wiki/Ethylmorphine
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