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 |
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 |
|
| Distinct mechanism for antidepressant activity by blockade of central substance P receptors. | 1998 Sep 11 |
|
| Stress-induced C-fos expression in the rat locus coeruleus is dependent on neurokinin 1 receptor activation. | 1999 |
|
| The substance P antagonist L-760,735 inhibits stress-induced NK(1) receptor internalisation in the basolateral amygdala. | 1999 Nov 27 |
|
| Intra-amygdala injection of the substance P [NK(1) receptor] antagonist L-760735 inhibits neonatal vocalisations in guinea-pigs. | 2001 Jul |
|
| The selective neurokinin 1 receptor antagonist R116301 modulates photic responses of the hamster circadian system. | 2001 Mar |
|
| 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 |
|
| 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 |
|
| Chronic substance P (NK1) receptor antagonist and conventional antidepressant treatment increases burst firing of monoamine neurones in the locus coeruleus. | 2002 |
|
| Substance P (neurokinin 1) receptor antagonists enhance dorsal raphe neuronal activity. | 2002 Sep 1 |
|
| 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 |
|
| Role of neurokinin type 1 receptor in nociception at the periphery and the spinal level in the rat. | 2016 Mar |
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 13:45:00 UTC 2023
by
admin
on
Sat Dec 16 13:45:00 UTC 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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4I4P4I2E8P
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DTXSID90430978
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admin on Sat Dec 16 13:45:00 UTC 2023 , Edited by admin on Sat Dec 16 13:45:00 UTC 2023
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