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
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
Molecular Formula | C17H28N4O4 |
Molecular Weight | 352.4286 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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.
Approval Year
PubMed
Title | Date | PubMed |
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L-6-ketopiperidine-2-carbonyl-L-leucyl-L-proline amide as a novel thyrotropin releasing hormone analogue with improving effects on impaired central nervous systems functions. | 1989 Mar |
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Effect of treatment with the neuroactive peptide posatirelin on microanatomical changes of frontal cortex and hippocampus caused by lesions of the locus coeruleus. | 1997 |
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Effect of lesions of the nucleus basalis magnocellularis and of treatment with posatirelin on cholinergic neurotransmission enzymes in the rat cerebral cortex. | 1998 Aug 14 |
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Screening for cerebroprotective agents using an in vivo model of cerebral reversible depolarization in awake rats. | 2001 Nov |
Patents
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:49:11 GMT 2023
by
admin
on
Fri Dec 15 15:49:11 GMT 2023
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Record UNII |
78U6302ARL
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C76367
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Code System | Code | Type | Description | ||
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3484
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DTXSID301318172
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78664-73-0
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SUB09981MIG
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C055448
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100000081370
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m1229
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PRIMARY | Merck Index | ||
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6310
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78U6302ARL
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CHEMBL2105243
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71230
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C74407
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PRIMARY |
Related Record | Type | Details | ||
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ACTIVE MOIETY |