Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H28ClFN2OS |
Molecular Weight | 483.04 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC(Cl)=C(C=C1C)C2=C(C)SC(=N2)N(CC#C)[C@@H](CC3CC3)C4=CC(F)=C(C)C=C4
InChI
InChIKey=IEAKXXNRGSLYTQ-DEOSSOPVSA-N
InChI=1S/C27H28ClFN2OS/c1-6-11-31(24(13-19-8-9-19)20-10-7-16(2)23(29)14-20)27-30-26(18(4)33-27)21-12-17(3)25(32-5)15-22(21)28/h1,7,10,12,14-15,19,24H,8-9,11,13H2,2-5H3/t24-/m0/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23407783 | https://www.ncbi.nlm.nih.gov/pubmed/21356230Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18672365 | http://www.pharmacodia.com/yaodu/html/v1/chemicals/5f9ce39aec46f3e8e8aebbc722d8ceeb.html
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23407783 | https://www.ncbi.nlm.nih.gov/pubmed/21356230
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18672365 | http://www.pharmacodia.com/yaodu/html/v1/chemicals/5f9ce39aec46f3e8e8aebbc722d8ceeb.html
SSR-125543 is a potent, selective, and orally active corticotropin-releasing factor 1 receptor (CRF1) antagonist (Ki value of 2nM). SSR-125543 attenuates long-term cognitive deficit induced by acute inescapable stress in mice, independently from the hypothalamic pituitary adrenal axis. SSR-125543 prevents stress-induced cognitive deficit associated with hippocampal dysfunction. SSR-125543 had been in phase II clinical trials by Sanofi for the treatment of Post-traumatic stress disorder. It is also in phase I trials for the treatment of anxiety. The compound had also been in phase II clinical trials for the treatment of major depression. However, in 2011, the research was discontinued.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01034995
20 mg, 50 mg and 100 mg daily in outpatients with major depressive disorder
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22301784
HEK 293 cells cotransfected with V1b-RL and CRHR1-YFP were preincubated for 18 h at 37 C with or without 1 uM SSR-125543 and the pharmacological properties of the V1b receptor expressed at the plasma membranes determined. SSR-125543 pretreatment significantly
increased the maximal binding capacity (Bmax) for [3
H]AVP by approximately 40% without affecting the dissociation constant (Kd).
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
639018
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
752253-39-7
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
DTXSID10996687
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
C174708
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
SUB197132
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
100000182802
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
10958
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
MFT24BX55I
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
KL-46
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
CHEMBL291657
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY | |||
|
5282340
Created by
admin on Sat Dec 16 10:35:08 GMT 2023 , Edited by admin on Sat Dec 16 10:35:08 GMT 2023
|
PRIMARY |
ACTIVE MOIETY