Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C26H28F7N5O2.ClH |
| Molecular Weight | 611.983 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.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=VZBKOBSSEVXFNF-QIRDZIKRSA-N
InChI=1S/C26H28F7N5O2.ClH/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);1H/t15-,23+,24-;/m1./s1
DescriptionCurator'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
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
Approval Year
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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| Distinct mechanism for antidepressant activity by blockade of central substance P receptors. | 1998 Sep 11 |
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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 |
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| Intra-amygdala injection of the substance P [NK(1) receptor] antagonist L-760735 inhibits neonatal vocalisations in guinea-pigs. | 2001 Jul |
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| Comparison of the phenotype of NK1R-/- mice with pharmacological blockade of the substance P (NK1 ) receptor in assays for antidepressant and anxiolytic drugs. | 2001 Nov |
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| Anxiolytic actions of the substance P (NK1) receptor antagonist L-760735 and the 5-HT1A agonist 8-OH-DPAT in the social interaction test in gerbils. | 2001 Oct 12 |
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| The substance P (NK1) receptor antagonist L-760735 inhibits fear conditioning in gerbils. | 2003 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 |
|
| Substance P Receptor Antagonist Suppresses Inflammatory Cytokine Expression in Human Disc Cells. | 2015 Aug 15 |
Patents
Sample Use Guides
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
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9809076
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DTXSID30430977
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E4C3XGZ4U7
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188923-01-5
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admin on Fri Dec 15 15:51:46 GMT 2023 , Edited by admin on Fri Dec 15 15:51:46 GMT 2023
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
