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Details

Stereochemistry ABSOLUTE
Molecular Formula C17H24N6O4S
Molecular Weight 408.475
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MONTIRELIN

SMILES

C[C@H]1SC[C@H](NC1=O)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(N)=O

InChI

InChIKey=RSHMQGIMHQPMEB-IXOXFDKPSA-N
InChI=1S/C17H24N6O4S/c1-9-15(25)22-12(7-28-9)16(26)21-11(5-10-6-19-8-20-10)17(27)23-4-2-3-13(23)14(18)24/h6,8-9,11-13H,2-5,7H2,1H3,(H2,18,24)(H,19,20)(H,21,26)(H,22,25)/t9-,11+,12+,13+/m1/s1

HIDE SMILES / InChI

Description

NS-3 (montirelin, CG 3703) is an analog of thyrotrophin releasing hormone (TRH). More potent and longer acting than TRH, CG-3703 produced beneficial effects in animal models of concussion-induced unconsciousness, cerebral ischemia, memory disruption, spontaneous convulsions in rats, narcolepsy, and spinal trauma. Given its efficacy in these models, the potential indications were broadened to include seizures, nerve trauma, cognitive dysfunction, and sleep apnea.

CNS Activity

CNS Active
3913
Curator's Comment: NS-3 (montirelin hydrate, CG 3703) can readily penetrate into the rodent brain. Centrally active TRH analogue CG3703 can improve neurological outcome and survival after brain injury in rats, perhaps through direct effects on cerebral metabolism. No available data on human.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Thyrotropin-releasing hormone receptor
10
Target ID: Q01717
Gene ID: 25570.0
Gene Symbol: Trhr
Target Organism: Rattus norvegicus (Rat)
Agonist
2678
 35.2 nM [Ki]
Releasing Agent
8
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Basic research
Unknown

Approved Use

Unknown
Primary
Phase III
656
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Differential affinities of TRH analogs at the mammalian spinal cord TRH receptor: implications for therapy in spinal injuries.
1989 Sep 25
Effect of NS-3, a thyrotropin-releasing hormone analog, on in vivo acetylcholine release in rat brain: regional differences and its sites of action.
1994 Nov
NS-3 (CG3703), an analog of thyrotropin-releasing hormone, ameliorates cognitive impairment in rats.
1995 Apr
Patents

Patents

DE10025947A1
2
EP0866711B1
2

Sample Use Guides

In Vivo Use Guide
Sources: Grünenthal (1997) Montirelin—A CNS Active TRH Analogue (Grünenthal GmbH, Aachen, Germany), pp 1–34. refernce retrieved from: http://jpet.aspetjournals.org/content/305/2/410.full
Curator's Comment: There are some evidences of Motirelin effectitivity on animal models: 1) two-week oral administration of CG-3703 (16 mg/kg) significantly reduced cataplexy and daytime sleep in canine narcolepsy http://www.ncbi.nlm.nih.gov/pubmed/10869884,9236248 2) Chronic intake of CNK-602A (NS-3, montirelin, CG 3703) in a dose that does not affect plasma levels of T3 and T4 inhibits tonic convulsions in Spontaneously epileptic rats and suggest that this drug may be an effective treatment for convulsive seizures in patients with epilepsy. http://www.ncbi.nlm.nih.gov/pubmed/8603636
0.5 mg of montirelin administered over 14 days improved ratings of global clinical state in 73% of patients exhibiting “disturbances of consciousness”.
Route of Administration: Unknown
In Vitro Use Guide
Curator's Comment: Among other TRH analogs montirelin (CG-3703) at concentrations 0.1-50 μM attenuated cell damage in retinoic acid differentiated SH-SY5Y cells
NS-3 (montirelin, CG 3703) is cytoprotective at 0.1-50 μM
Name Type Language
MONTIRELIN
INN  
INN  
Official Name English
CNK-602A
Code English
montirelin [INN]
Common Name English
CG-3703
Code English
N-(((3R,6R)-6-METHYL-5-OXO-3-THIOMORPHOLINYL)CARBONYL)-L-HISTIDYL-L-PROLINAMIDE
Systematic Name English
NS-3
Code English
Classification Tree Code System Code
NCI_THESAURUS C76367
Created by admin on Sat Dec 16 17:07:50 GMT 2023 , Edited by admin on Sat Dec 16 17:07:50 GMT 2023
Code System Code Type Description
MESH
C031926
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PRIMARY
PUBCHEM
6917793
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PRIMARY
CAS
90243-66-6
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PRIMARY
SMS_ID
100000080383
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PRIMARY
ChEMBL
CHEMBL2304039
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PRIMARY
EVMPD
SUB09056MIG
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PRIMARY
FDA UNII
30MUJ6YYUY
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PRIMARY
INN
6190
Created by admin on Sat Dec 16 17:07:50 GMT 2023 , Edited by admin on Sat Dec 16 17:07:50 GMT 2023
PRIMARY
NCI_THESAURUS
C77010
Created by admin on Sat Dec 16 17:07:50 GMT 2023 , Edited by admin on Sat Dec 16 17:07:50 GMT 2023
PRIMARY
EPA CompTox
DTXSID301034132
Created by admin on Sat Dec 16 17:07:50 GMT 2023 , Edited by admin on Sat Dec 16 17:07:50 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of MONTIRELIN
SALT/SOLVATE (PARENT)
Structure of MONTIRELIN TETRAHYDRATE
NIH
NCATS
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