Tìm theo
Reboxetine
Các tên gọi khác (5 ) :
  • (S
  • Esreboxetine
  • Reboxetine
  • S)-Reboxetine
  • SID11114256
Thuốc Gốc
Small Molecule
CAS: 98769-81-4
ATC: N06AX18
CTHH: C19H23NO3
PTK: 313.3908
Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine.
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/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18/h3-11,18-20H,2,12-14H2,1H3/t18-,19-/m0/s1
InChI Key
InChIKey=CBQGYUDMJHNJBX-OALUTQOASA-N
IUPAC Name
(2S)-2-[(S)-2-ethoxyphenoxy(phenyl)methyl]morpholine
Traditional IUPAC Name
reboxetine
SMILES
[H][C@]1(CNCCO1)[C@@H](OC1=CC=CC=C1OCC)C1=CC=CC=C1
Độ tan chảy
170-171 °C (Mesylate salt)
Độ hòa tan
8 mg/mL (Mesylate salt)
logP
3.1
logS
-4.2
pKa (Strongest Basic)
7.91
PSA
39.72 Å2
Refractivity
89.48 m3·mol-1
Polarizability
34.17 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of new antidepressant class. Reboxetine is an a-ariloxybenzyl derivative of morpholine. Reboxetine is primarily used to treat depression but has also been found useful in the treatment of narcolepsy and panic disorders.
Cơ Chế Tác Dụng : Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine. Reboxetine is a selective inhibitor of noradrenaline reuptake. It inhibits noradrenaline reuptake in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine. Reboxetine does not affect dopamine or serotonin reuptake and it has low in vivo and in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.
Dược Động Học :
▧ Absorption :
Reboxetine is rapidly and extensively absorbed following oral administration.
▧ Protein binding :
98%
▧ Metabolism :
Reboxetine is metabolized by dealkylation, hydroxylation and oxidation followed by glucuronide or sulphate conjugation. It is metabolized by the cytochrome P450 CYP isoenzyme 3A4.
▧ Half Life :
12.5 hours
Độc Tính : Reports of seizures (rare) have been reported
Chỉ Định : For the treatment of clinical depression.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Davedax
  • Công ty :
    Sản phẩm biệt dược : Edronax
  • Công ty :
    Sản phẩm biệt dược : Norebox
  • Công ty :
    Sản phẩm biệt dược : Prolift
  • Công ty :
    Sản phẩm biệt dược : Solvex
  • Công ty :
    Sản phẩm biệt dược : Vestra
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00234
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=65856
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504845
ChemSpider
http://www.chemspider.com/Chemical-Structure.59268.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=35226
PharmGKB
http://www.pharmgkb.org/drug/PA144614921
Wikipedia
http://en.wikipedia.org/wiki/Reboxetine
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