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

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
[Central nervous system stimulants as nonspecific antagonists of morphine-induced respiratory depression].
1992 Sep-Oct
Protective effects of TRH and its analogues in chemical and genetic models of seizures.
1997 Sep-Oct
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
Posatirelin for the treatment of degenerative and vascular dementia: results of explanatory and pragmatic efficacy analyses.
1998 Jan-Feb
[TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin].
2002
Treatment of vascular dementia: evidence from trials with non-cholinergic drugs.
2004 Nov 15
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
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:49:11 GMT 2023
Edited
by admin
on Fri Dec 15 15:49:11 GMT 2023
Record UNII
78U6302ARL
Record Status Validated (UNII)
Record Version
  • Download
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
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
EPA CompTox
DTXSID301318172
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
CAS
78664-73-0
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
EVMPD
SUB09981MIG
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
MESH
C055448
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
SMS_ID
100000081370
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
MERCK INDEX
m1229
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY Merck Index
INN
6310
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
FDA UNII
78U6302ARL
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
ChEMBL
CHEMBL2105243
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
PUBCHEM
71230
Created by admin on Fri Dec 15 15:49:11 GMT 2023 , Edited by admin on Fri Dec 15 15:49:11 GMT 2023
PRIMARY
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
PRIMARY
Related Record Type Details
ACTIVE MOIETY