U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
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

PubMed

TitleDatePubMed
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
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 Jun 14
[Central nervous system stimulants as nonspecific antagonists of morphine-induced respiratory depression].
1992 Sep-Oct
Protective effects of TRH and its stable analogue, RGH-2202, on kainate-induced seizures and neurotoxicity in rodents.
2001 Jan
Effects of TRH and its analogues on primary cortical neuronal cell damage induced by various excitotoxic, necrotic and apoptotic agents.
2009 Oct
Patents

Sample Use Guides

In Vivo Use Guide
Sources: DOI: 10.2165/00128413-199509980-00022
10 mg/day for 3-month treatment period
Route of Administration: Intramuscular
Name Type Language
POSATIRELIN
INN   MART.   MI  
INN  
Official Name English
POSATIRELIN [MI]
Common Name English
POSATIRELIN [MART.]
Common Name English
posatirelin [INN]
Common Name English
POSATIRELIN [JAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C76367
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
Code System Code Type Description
DRUG CENTRAL
3484
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PRIMARY
EPA CompTox
DTXSID301318172
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CAS
78664-73-0
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EVMPD
SUB09981MIG
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MESH
C055448
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SMS_ID
100000081370
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MERCK INDEX
m1229
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PRIMARY Merck Index
INN
6310
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FDA UNII
78U6302ARL
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ChEMBL
CHEMBL2105243
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PUBCHEM
71230
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NCI_THESAURUS
C74407
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
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