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Details

Stereochemistry ABSOLUTE
Molecular Formula C17H28N4O4
Molecular Weight 352.4286
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POSATIRELIN

SMILES

CC(C)C[C@H](NC(=O)[C@@H]1CCCC(=O)N1)C(=O)N2CCC[C@H]2C(N)=O

InChI

InChIKey=DPNGIIPSQYKWQA-AVGNSLFASA-N
InChI=1S/C17H28N4O4/c1-10(2)9-12(17(25)21-8-4-6-13(21)15(18)23)20-16(24)11-5-3-7-14(22)19-11/h10-13H,3-9H2,1-2H3,(H2,18,23)(H,19,22)(H,20,24)/t11-,12-,13-/m0/s1

HIDE SMILES / InChI

Description

Posatirelin is a synthetic peptide that, in animal models, has been shown to improve cognitive and motor disturbances associated with aging or induced by central neurotransmission disruption. Modulation of various neurotransmission systems and activation of excitatory amino acid receptors have been suggested as possible mechanisms of action, since posatirelin increases the turnover and release of catecholamines in several brain areas as well as choline acetyltransferase activity in the cerebral cortex. In neuronal cultures, posatirelin has been shown to have trophic effects, accelerating the maturation of cerebellar granule cells and stimulating neurite growth. The benefits of posatirelin therapy in patients with late-onset Alzheimer's disease have potential clinical relevance. Significant improvements in motor, intellectual and emotional impairments were seen in posatirelin recipients. The difference in these parameters with respect to the reference and inactive drugs was significant. Posatirelin can improve cognitive and functional abilities of patients suffering from degenerative or vascular dementia. Posatirelin had been in phase III clinical trial for the treatment of cognition disorders. However, this development was discontinued.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
10 mg/day for 3-month treatment period
Route of Administration: Intramuscular