Tìm theo
Remoxipride
Các tên gọi khác (10 ) :
  • a-33547
  • FLA-731
  • Remoxiprida
  • Remoxipride
  • Remoxipridum
  • Romoxipride
  • Roxiam
  • SID11112836
  • SID11113786
  • SID26751966
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 80125-14-0
ATC: N05AL04
CTHH: C16H23BrN2O3
PTK: 371.269
An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
371.269
Monoisotopic mass
370.089205259
InChI
InChI=1S/C16H23BrN2O3/c1-4-19-9-5-6-11(19)10-18-16(20)14-13(21-2)8-7-12(17)15(14)22-3/h7-8,11H,4-6,9-10H2,1-3H3,(H,18,20)/t11-/m0/s1
InChI Key
InChIKey=GUJRSXAPGDDABA-NSHDSACASA-N
IUPAC Name
3-bromo-N-{[(2S)-1-ethylpyrrolidin-2-yl]methyl}-2,6-dimethoxybenzamide
Traditional IUPAC Name
remoxipride
SMILES
CCN1CCC[[email protected]]1CNC(=O)C1=C(OC)C=CC(Br)=C1OC
Độ hòa tan
74 mg/L
logP
2.10
logS
-3.5
pKa (strongest acidic)
13.06
pKa (Strongest Basic)
8.4
PSA
50.8 Å2
Refractivity
90.56 m3·mol-1
Polarizability
36.25 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Remoxipride, a substituted benzamide, is a selective D2 receptor antagonist. It has been shown to be effective in the treatment of schizophrenia. Some antipsychotics block domapinergic receptors as well as cholinergic, noradrenergic and histaminergic receptors. Remoxipride was developed to act specifically on the dopamine D2 receptor. As a consequence, several undesired side effects can occur. Patients often feel they are not taking any antipsychotic drug. It has a potent affinity for the sigma receptor, but it is unclear whether it is a sigma agonist or antagonist. The contribution of this property to its clinical profile is unknown. Blocking the D2 dopamine receptor is known to cause relapse in patients that have achieved remission from depression, and such blocking also counteracts the effectiveness of SSRI medication.
Cơ Chế Tác Dụng : An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. [PubChem] Remoxipride acts as an antagonist at the D2 dopamine receptor. It is believed that overactivity of dopamine systems in the mesolimbic pathway may contribute to the "positive symptoms" of schizophrenia (such as delusions and hallucinations), whereas problems with dopamine function in the mesocortical pathway may be responsible for the "negative symptoms", such as avolition, flat emotional response and alogia. Therefore, by decreasing the levels of dopamine in these pathways, it is thought that remoxipride is able to reduce the symptoms of schizophrenia, particularily the "positive symptoms".
Dược Động Học :
▧ Absorption :
Rapidly absorbed. Absolute bioavailability is 90%.
▧ Protein binding :
89-98%
▧ Metabolism :
No active metabolites
▧ Half Life :
4-7 hours
Chỉ Định : Remoxipride is an atypical antipsychotic once used for the treatment of schizophrenia.
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