Tìm theo
Phenserine
Các tên gọi khác (2) :
  • (-)-eseroline phenylcarbamate
  • (-)-phenserine
Thuốc Gốc
Small Molecule
CAS: 101246-66-6
CTHH: C20H23N3O2
PTK: 337.4155
Phenserine is under development by Axonyx, a US biopharmaceutical company that focuses on treatments for dementia. Phenserine is a next generation acetylcholinesterase (AChE) inhibitor indicated for the treatment of AD. Unlike currently marketed AChE inhibitors, it has a dual mechanism of action that also includes anti-amyloid activity, which may confer disease-modifying effects in patients with AD. If this is substantiated in an ongoing clinical trial then phenserine may open the door to an entirely new type of treatment for AD. Axonyx announced on 20 September 2005 that phenserine was ineffective in two curtailed phase 3 trials.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H23N3O2
Phân tử khối
337.4155
Monoisotopic mass
337.179026995
InChI
InChI=1S/C20H23N3O2/c1-20-11-12-22(2)18(20)23(3)17-10-9-15(13-16(17)20)25-19(24)21-14-7-5-4-6-8-14/h4-10,13,18H,11-12H2,1-3H3,(H,21,24)/t18-,20+/m1/s1
InChI Key
InChIKey=PBHFNBQPZCRWQP-QUCCMNQESA-N
IUPAC Name
(3aS,8aR)-1,3a,8-trimethyl-1H,2H,3H,3aH,8H,8aH-pyrrolo[2,3-b]indol-5-yl N-phenylcarbamate
Traditional IUPAC Name
(3aS,8aR)-1,3a,8-trimethyl-2H,3H,8aH-pyrrolo[2,3-b]indol-5-yl N-phenylcarbamate
SMILES
[H][C@]12N(C)CC[C@@]1(C)C1=C(C=CC(OC(=O)NC3=CC=CC=C3)=C1)N2C
Độ tan chảy
150 °C
Độ hòa tan
5.09e-02 g/l
logP
4.25
logS
-3.8
pKa (strongest acidic)
12.86
pKa (Strongest Basic)
6.58
PSA
44.81 Å2
Refractivity
99.96 m3·mol-1
Polarizability
37.09 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Phenserine, a phenylcarbamate of physostigmine, is a reversible acetyl-selective cholinesterase inhibitor. In studies of rats with lesions of the forebrain cholinergic system, injections of phenserine was found to significantly decrease the levels of secreted beta-APP in the CSF of the rats. A study on cultured human brain cells found that phenserine reduces Abeta levels by regulating beta-APP translation.
Cơ Chế Tác Dụng : Phenserine is under development by Axonyx, a US biopharmaceutical company that focuses on treatments for dementia. Phenserine is a next generation acetylcholinesterase (AChE) inhibitor indicated for the treatment of AD. Unlike currently marketed AChE inhibitors, it has a dual mechanism of action that also includes anti-amyloid activity, which may confer disease-modifying effects in patients with AD. If this is substantiated in an ongoing clinical trial then phenserine may open the door to an entirely new type of treatment for AD. Axonyx announced on 20 September 2005 that phenserine was ineffective in two curtailed phase 3 trials. Phenserine is a highly selective, reversible acetylcholinesterase inhibitor, a mechanism of action known to improve memory and cognition in Alzheimer’s subjects. Phenserine may prove to concentrate in the brain rapidly which would reduce the incidence of drug toxicity and side effects.
Dược Động Học :
▧ Absorption :
Rapidly absorbed and cleared from the body.
▧ Half Life :
8 to 10 hours
Độc Tính : The toxicity of phenserine, a derivate of physostigmine, is dramatically less. Doses of 20 mg/kg (rats, intravenous) of phenserine have not been associated with toxicity or deaths.
Chỉ Định : For the treatment of Alzheimer's disease (AD).
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04892
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=192706
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=14900124
ChemSpider
http://www.chemspider.com/Chemical-Structure.167225.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10958
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