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 |
|---|---|---|
| Effects of TRH and its analogues on primary cortical neuronal cell damage induced by various excitotoxic, necrotic and apoptotic agents. | 2009-10 |
|
| Treatment of vascular dementia: evidence from trials with non-cholinergic drugs. | 2004-11-15 |
|
| [TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin]. | 2002 |
|
| Screening for cerebroprotective agents using an in vivo model of cerebral reversible depolarization in awake rats. | 2001-11 |
|
| Protective effects of TRH and its stable analogue, RGH-2202, on kainate-induced seizures and neurotoxicity in rodents. | 2001-01 |
|
| Effect of lesions of the nucleus basalis magnocellularis and of treatment with posatirelin on cholinergic neurotransmission enzymes in the rat cerebral cortex. | 1998-08-14 |
|
| Protective effects of TRH and its analogues in chemical and genetic models of seizures. | 1998-05-05 |
|
| Posatirelin for the treatment of degenerative and vascular dementia: results of explanatory and pragmatic efficacy analyses. | 1997-03-07 |
|
| Effect of treatment with the neuroactive peptide posatirelin on microanatomical changes of frontal cortex and hippocampus caused by lesions of the locus coeruleus. | 1997 |
|
| Effect of the thyrotropin releasing hormone analogue posatirelin (RGH 2202) on microanatomical changes induced by lesions of the nucleus basalis magnocellularis in the rat. | 1997 |
|
| [Central nervous system stimulants as nonspecific antagonists of morphine-induced respiratory depression]. | 1992-09-01 |
|
| Stimulant effect of thyrotropin-releasing hormone and its analog, RGH 2202, on the diaphragm respiratory activity, and their antagonism with morphine: possible involvement of the N-methyl-D-aspartate receptors. | 1991-06-14 |
|
| 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. | 1989-03 |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:09:49 GMT 2025
by
admin
on
Mon Mar 31 18:09:49 GMT 2025
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| Record UNII |
78U6302ARL
|
| Record Status |
Validated (UNII)
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| Record Version |
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| Name | Type | Language | ||
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Preferred Name | English | ||
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Official Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| 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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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 |