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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[Central nervous system stimulants as nonspecific antagonists of morphine-induced respiratory depression]. | 1992 Sep-Oct |
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Protective effects of TRH and its analogues in chemical and genetic models of seizures. | 1997 Sep-Oct |
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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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Posatirelin for the treatment of degenerative and vascular dementia: results of explanatory and pragmatic efficacy analyses. | 1998 Jan-Feb |
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[TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin]. | 2002 |
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Treatment of vascular dementia: evidence from trials with non-cholinergic drugs. | 2004 Nov 15 |
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Effects of TRH and its analogues on primary cortical neuronal cell damage induced by various excitotoxic, necrotic and apoptotic agents. | 2009 Oct |
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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-
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C76367
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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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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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Related Record | Type | Details | ||
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ACTIVE MOIETY |