Aleplasinine

Structural formula
General
Non-proprietary name	Aleplasinine
other names	{5- (3-methylphenyl) -1- [4- (2-methyl-2-propanyl) benzyl] -1 H -indol-3-yl} (oxo) acetic acid ( IUPAC ) ; PAZ-417;
Molecular formula	C 28 H 27 NO 3
External identifiers / databases
PubChem	10224267
ChemSpider	8399758
DrugBank	DB12635
Wikidata	Q2640993
Drug information
Mechanism of action	PAI-1 - inhibitor
properties
Molar mass	425.5 g · mol -1
safety instructions
GHS hazard labeling ; no classification available
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Aleplasinin is an experimental drug from the group of plasminogen activator inhibitors (PAI-1 inhibitors). It is being developed by the US pharmaceutical company Wyeth and is intended to be used as a drug against Alzheimer's disease .

Mechanism of action

In Alzheimer's disease encamp senile plaques , from misfolded amyloid beta - peptides , along with neurofibrillary tangles in neurons of. This leads to necrosis of the nerve cells .

The beta-amyloid peptide activates the tissue-specific plasminogen activator tPA ( tissue plasminogen activator ), which in turn activates plasminogen which the plasmin - synthesis induced. Plasmin stimulates the breakdown of beta amyloid.

tPA in turn is inhibited by the plasminogen activator inhibitor PAI-1. In Alzheimer's disease this inhibition is increased many times over. Aleplasinin selectively inhibits PAI-1 and thus prevents inhibition of tPA. As a result, the beta-amyloid peptide is increasingly broken down and can no longer be combined with the neurofibrils in the nerve cells. This prevents necrosis.

literature

JS Jacobsen, et al., MN Pangalos: Enhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade , in: Proceedings Natural Academy Sciences , 2008 , 105 , pp. 8754-8759; doi: 10.1073 / pnas.0710823105
American Medical Association: STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL: Aleplasinin ( Memento of October 7, 2008 in the Internet Archive )

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.