Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C31H35Cl2N3O2 |
Molecular Weight | 552.535 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C[C@@H](CCN1CCC(CC1)(NC(C)=O)C2=CC=CC=C2)C3=CC=C(Cl)C(Cl)=C3)C(=O)C4=CC=CC=C4
InChI
InChIKey=PGKXDIMONUAMFR-AREMUKBSSA-N
InChI=1S/C31H35Cl2N3O2/c1-23(37)34-31(27-11-7-4-8-12-27)16-19-36(20-17-31)18-15-26(25-13-14-28(32)29(33)21-25)22-35(2)30(38)24-9-5-3-6-10-24/h3-14,21,26H,15-20,22H2,1-2H3,(H,34,37)/t26-/m1/s1
Molecular Formula | C31H35Cl2N3O2 |
Molecular Weight | 552.535 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.
Approval Year
PubMed
Title | Date | PubMed |
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The non-peptide tachykinin NK1- and NK2-receptor antagonists SR 140333 and SR 48968 prevent castor-oil induced diarrhea in rats. | 1996 |
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Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. | 1997 Jun |
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SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. | 2002 Aug 23 |
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Tachykinin receptors antagonists: from research to clinic. | 2006 Aug |
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Contractile effect of tachykinins on Suncus murinus (house musk shrew) isolated ileum. | 2008 Oct-Dec |
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Behavioral effects of saredutant, a tachykinin NK2 receptor antagonist, in experimental models of mood disorders under basal and stress-related conditions. | 2008 Sep |
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Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. | 2009 May 1 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00417118
Saredutant 100 mg once daily in the morning for a maximum of 8 weeks
Route of Administration:
Oral
Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 16:31:25 UTC 2023
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Sat Dec 16 16:31:25 UTC 2023
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Record UNII |
720U2QK8I5
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Record Status |
Validated (UNII)
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C265
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SUB10449MIG
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142001-63-6
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Saredutant
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CHEMBL308148
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR |
Tachykinin NK2 receptor antagonist that was developed by Sanofi-Aventis for anti-depressant potential
IC50
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Related Record | Type | Details | ||
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ACTIVE MOIETY |