Phenserine - CAS 101246-66-6
Category: Inhibitor
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Molecular Weight:
Phenserine, an analog of physostigmine, is an acetylcholinesterase (AChE) inhibitor (IC50= 24 nM) potentially for the treatment of Alzheimer Disease (AD).
≥98% by HPLC
(3aS,8aR)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol 5-(N-phenylcarbamate); (-)-Eseroline phenylcarbamate; (-)-N-Phenylcarbamoyleseroline; (-)-Phenserine
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Why so few drugs for Alzheimer's disease? Are methods failing drugs?
Becker RE;Greig NH Curr Alzheimer Res. 2010 Nov;7(7):642-51.
Recent studies of Alzheimer's disease (AD) and other neuropsychiatric drug developments raise questions whether failures of some drugs occur due to flaws in methods. In three case studies of recent AD drug development failures with phenserine, metrifonate, and tarenflurbil we identified methodological lapses able to account for the failures. Errors in complex systems such as drug developments are both almost inescapable due to human mistakes and most frequently hidden at the time of occurrence and thereafter. We propose preemptive error management as a preventive strategy to exclude or control error intrusions into neuropsychiatric drug developments. We illustrate the functions we anticipate for a preemptive error management preventive strategy with a checklist and identify the limitations of this aspect of the proposal with three drug examples. This strategy applies core scientific practices to insure the quality of data within the current context of AD drug development practices.
Kinthada LK;Medisetty SR;Parida A;Babu KN;Bisai A J Org Chem. 2017 Aug 18;82(16):8548-8567. doi: 10.1021/acs.joc.7b01232. Epub 2017 Aug 7.
An FeCl;3;-catalyzed efficient strategy for the allylation reactions of 3-hydroxy-2-oxindoles with allyltrimethylsilane has been developed. The reaction affords a variety of 2-oxindoles having quaternary center at the pseudobenzylic position in an operationally simple and inexpensive procedure. Control experiments using enantioenriched 3-hydroxy-2-oxindole show that the reaction proceeds through in situ generated 2H-indol-2-one (8). The methodology presents an efficient and concise access to the pyrroloindoline alkaloids (±)-deoxyeseroline (1a), (±)-esermethole (1b), (±)-physostigmine (1c), (±)-phenserine (1d), and (±)-physovenine (1e). Eventually, we extrapolated the scope of this methodology to the formal total syntheses of dimeric cyclotyrptamine alkaloids (±)-chimonanthine (3a), (±)-folicanthine (3c), and (±)-calycanthine (4).
3.Kinetics of human erythrocyte acetylcholinesterase inhibition by a novel derivative of physostigmine: phenserine.
al-Jafari AA;Kamal MA;Greig NH;Alhomida AS;Perry ER Biochem Biophys Res Commun. 1998 Jul 9;248(1):180-5.
The effect of phenserine, a novel cholinesterase inhibitor, was assessed for the first time on kinetic parameters of human erythrocyte acetylcholinesterase (AChE). Phenserine (0.025-0.40 microM) inhibited the activity of human erythrocyte AChE in a concentration-dependent fashion, the IC50 was 0.0453 microM. The Michaelis-Menten constant (K(m)) for the hydrolysis of acetylthiocholine iodide was found to be 0.124 mM and the Vmax was 0.980 mumol/min/mg protein. Dixon as well as Lineweaver-Burk plots and their secondary replots indicated that the nature of the inhibition was of the noncompetitive type. The value of Ki was estimated as 0.048 microM by the primary and secondary replots of the Dixon as well as secondary replots of the Lineweaver-Burk plot. A novel relationship between Ki and substrate concentration was also identified which permits more precise prediction of the specific type of noncompetitive inhibition of various enzymes by a wide variety of drugs, chemicals and, in some circumstances, by their own substrates.
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CAS 101246-66-6 Phenserine

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