Tìm theo
Levallorphan
Các tên gọi khác (8 ) :
  • Levallofano
  • Levallorphan
  • Lévallorphane
  • Levallorphanum
  • Levalorfano
  • Lorfan
  • Naloxiphan
  • SID144205558
narcotic antagonists, antidotes
Thuốc Gốc
Small Molecule
CAS: 152-02-3
CTHH: C19H25NO
PTK: 283.4079
An opioid antagonist with properties similar to those of naloxone; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H25NO
Phân tử khối
283.4079
Monoisotopic mass
283.193614427
InChI
InChI=1S/C19H25NO/c1-2-10-20-11-9-19-8-4-3-5-16(19)18(20)12-14-6-7-15(21)13-17(14)19/h2,6-7,13,16,18,21H,1,3-5,8-12H2/t16-,18+,19+/m0/s1
InChI Key
InChIKey=OZYUPQUCAUTOBP-QXAKKESOSA-N
IUPAC Name
(1R,9R,10R)-17-(prop-2-en-1-yl)-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2(7),3,5-trien-4-ol
Traditional IUPAC Name
levallorphan
SMILES
[H][C@@]12CCCC[C@@]11CCN(CC=C)[C@@H]2CC2=C1C=C(O)C=C2
Độ tan chảy
181 °C
Độ hòa tan
633 mg/L
logP
3.48
logS
-4
pKa (strongest acidic)
10.36
pKa (Strongest Basic)
9.41
PSA
23.47 Å2
Refractivity
87.24 m3·mol-1
Polarizability
32.68 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Levallorphan, an opioid antagonist similar to naloxone, is used to treat drug overdoses. Levallorphan differs from naloxone in that it also possesses some agonist properties. It is an analogue of levelorphanol that counteracts the actions of narcotic analgesics such as morphine. It is used especially in the treatment of respiratory depression due to narcotic overdoses. Levallorphan prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.
Cơ Chế Tác Dụng : An opioid antagonist with properties similar to those of naloxone; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683) Levallorphan antagonizes opioid effects by competing for the same receptor sites. It binds to the opioid mu receptor and the nicotinic acetylcholine receptor alpha2/alpha3.
Dược Động Học :
▧ Absorption :
Rapidly absorbed.
▧ Metabolism :
Hepatic.
▧ Half Life :
1 hour
Độc Tính : Oral, rat LD50: 109±4 mg/kg
Chỉ Định : For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Takeda
    Sản phẩm biệt dược : Lorfan
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00504
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5359371
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505682
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07069
ChemSpider
http://www.chemspider.com/Chemical-Structure.4514267.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749284
Wikipedia
http://en.wikipedia.org/wiki/Levallorphan
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