Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C26H28F7N5O2 |
Molecular Weight | 575.5216 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](O[C@H]1OCCN(CC2=C(CN(C)C)N=NN2)[C@H]1C3=CC=C(F)C=C3)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F
InChI
InChIKey=USRYEHHMJIRICK-ZNZBMKLDSA-N
InChI=1S/C26H28F7N5O2/c1-15(17-10-18(25(28,29)30)12-19(11-17)26(31,32)33)40-24-23(16-4-6-20(27)7-5-16)38(8-9-39-24)14-22-21(13-37(2)3)34-36-35-22/h4-7,10-12,15,23-24H,8-9,13-14H2,1-3H3,(H,34,35,36)/t15-,23+,24-/m1/s1
Molecular Formula | C26H28F7N5O2 |
Molecular Weight | 575.5216 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://adisinsight.springer.com/drugs/800024616Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/9733503 | https://www.ncbi.nlm.nih.gov/pubmed/11595206 | https://www.ncbi.nlm.nih.gov/pubmed/15875166 | https://www.ncbi.nlm.nih.gov/pubmed/26690860
Sources: http://adisinsight.springer.com/drugs/800024616
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/9733503 | https://www.ncbi.nlm.nih.gov/pubmed/11595206 | https://www.ncbi.nlm.nih.gov/pubmed/15875166 | https://www.ncbi.nlm.nih.gov/pubmed/26690860
L-760735 is a non-peptide substance P receptor (Neurokinin 1 (NK1) receptor) antagonist. It exerts anxiolytic, antidepressant and antinociceptive actions in animals. Merck was developing an L- 760735 as a potential antidepressant.
Originator
Sources: http://adisinsight.springer.com/drugs/800024616
Curator's Comment: # Merck & Co
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL249 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9733503 |
0.3 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Sources: https://www.ncbi.nlm.nih.gov/pubmed/26690860 |
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
An NK1 receptor antagonist affects the circadian regulation of locomotor activity in golden hamsters. | 1998 Jul 27 |
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The substance P antagonist L-760,735 inhibits stress-induced NK(1) receptor internalisation in the basolateral amygdala. | 1999 Nov 27 |
|
The selective neurokinin 1 receptor antagonist R116301 modulates photic responses of the hamster circadian system. | 2001 Mar |
|
Chronic psychosocial stress in tree shrews: effect of the substance P (NK1 receptor) antagonist L-760735 and clomipramine on endocrine and behavioral parameters. | 2005 Sep |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15875166
Tree shrews were subjected to a 7-day period of psychosocial stress before receiving daily oral administration of L-760735 (10 mg/kg/day)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25929203
Curator's Comment: Treatment of human intervertebral disc cells with L-760735 was able to suppress expression of IL-1β, IL-6, and IL-8 in a dose-dependent manner.
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 13:45:00 GMT 2023
by
admin
on
Sat Dec 16 13:45:00 GMT 2023
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Record UNII |
4I4P4I2E8P
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Record Status |
Validated (UNII)
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Record Version |
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