Tìm theo
Renzapride
serotonin receptor agonists
Thuốc Gốc
Small Molecule
CAS: 112727-80-7
CTHH: C16H22ClN3O2
PTK: 323.818
Renzapride is currently in Phase III clinical development in the United States for the treatment of constipation-predominant irritable bowel syndrome (IBS-C). It is also potentially effective for irritable bowel syndrome with alternating stool pattern (IBS-A). It is being developed by Alizyme of the UK. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
323.818
Monoisotopic mass
323.14005467
InChI
InChI=1S/C16H22ClN3O2/c1-22-15-11(4-5-12(18)14(15)17)16(21)19-13-6-8-20-7-2-3-10(13)9-20/h4-5,10,13H,2-3,6-9,18H2,1H3,(H,19,21)
InChI Key
InChIKey=YFUAYKVMQVBSNG-UHFFFAOYSA-N
IUPAC Name
4-amino-N-{1-azabicyclo[3.3.1]nonan-4-yl}-3-chloro-2-methoxybenzamide
Traditional IUPAC Name
4-amino-N-{1-azabicyclo[3.3.1]nonan-4-yl}-3-chloro-2-methoxybenzamide
SMILES
COC1=C(C=CC(N)=C1Cl)C(=O)NC1CCN2CCCC1C2
Độ hòa tan
1.95e-01 g/l
logP
1.14
logS
-3.2
pKa (strongest acidic)
14.68
pKa (Strongest Basic)
8.8
PSA
67.59 Å2
Refractivity
88.74 m3·mol-1
Polarizability
33.47 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Renzapride is a substituted benzamide which acts on the upper gastrointestinal tract. It has been shown to enhance stomach emptying in normal subjects; doses of 2 and 5 mg decreasing by 21 and 37% respectively the volume of gastric contents aspirated 80 min after a test meal. Renzapride was found to reduce the oro-caecal transit time as assessed by the lactulose/breath hydrogen method in a dose related manner from 0.2 to 5 mg; the later dose producing a 62% reduction.
Cơ Chế Tác Dụng : Renzapride is currently in Phase III clinical development in the United States for the treatment of constipation-predominant irritable bowel syndrome (IBS-C). It is also potentially effective for irritable bowel syndrome with alternating stool pattern (IBS-A). It is being developed by Alizyme of the UK. [Wikipedia] Renzapride is a full serotonin 5-HT4 receptor agonist and partial serotonin 5-HT3 receptor antagonist.
Chỉ Định : For the treatment of constipation-predominant irritable bowel syndrome (IBS-C).
... loading
... loading