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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

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

PubMed

TitleDatePubMed
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

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
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:09:49 GMT 2025
Edited
by admin
on Mon Mar 31 18:09:49 GMT 2025
Record UNII
78U6302ARL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POSATIRELIN [MI]
Preferred Name English
POSATIRELIN
INN   MART.   MI  
INN  
Official 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 Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
Code System Code Type Description
DRUG CENTRAL
3484
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
EPA CompTox
DTXSID301318172
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
CAS
78664-73-0
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
EVMPD
SUB09981MIG
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
MESH
C055448
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
SMS_ID
100000081370
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
MERCK INDEX
m1229
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY Merck Index
INN
6310
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
FDA UNII
78U6302ARL
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
ChEMBL
CHEMBL2105243
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
PUBCHEM
71230
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
NCI_THESAURUS
C74407
Created by admin on Mon Mar 31 18:09:49 GMT 2025 , Edited by admin on Mon Mar 31 18:09:49 GMT 2025
PRIMARY
Related Record Type Details
ACTIVE MOIETY