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
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
| Molecular Formula | C17H24N6O4S |
| Molecular Weight | 408.475 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q01717 Gene ID: 25570.0 Gene Symbol: Trhr Target Organism: Rattus norvegicus (Rat) |
35.2 nM [Ki] | ||
Target ID: GO:0061526 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
|
| NS-3(CG3703), a TRH analog, ameliorates scopolamine-induced memory disruption in rats. | 1995 Aug |
|
| NS-3, a TRH-analog, reverses memory disruption by stimulating cholinergic and noradrenergic systems. | 1996 Feb |
|
| Effects of thyrotropin-releasing hormone and its analogs on daytime sleepiness and cataplexy in canine narcolepsy. | 1997 Aug 15 |
|
| Effects of thyrotropin-releasing hormone and its analogue, NS-3, on blood pressure, heart rate, and serum catecholamine levels in rats. | 1997 Feb |
|
| Chronic oral administration of CG-3703, a thyrotropin releasing hormone analog, increases wake and decreases cataplexy in canine narcolepsy. | 2000 Jul |
Patents
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
| Substance Class |
Chemical
Created
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admin
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Edited
Sat Dec 16 17:07:50 GMT 2023
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| Record UNII |
30MUJ6YYUY
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| Record Status |
Validated (UNII)
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C76367
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C77010
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ACTIVE MOIETY |
