Synonyms: SR 48,968 | SR 48968 | SR-48,968 | SR48968 | SR48968C
Compound class:
Synthetic organic
Comment: Saredutant is a tachykinin NK2 receptor antagonist that was developed by Sanofi-Aventis for anti-depressant potential [5,7-8,10].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Anthes JC, Chapman RW, Richard C, Eckel S, Corboz M, Hey JA, Fernandez X, Greenfeder S, McLeod R, Sehring S et al.. (2002)
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. Eur J Pharmacol, 450 (2): 191-202. [PMID:12206858] |
2. Chung FZ, Wu LH, Vartanian MA, Watling KJ, Guard S, Woodruff GN, Oxender DL. (1994)
The non-peptide tachykinin NK2 receptor antagonist SR 48968 interacts with human, but not rat, cloned tachykinin NK3 receptors. Biochem Biophys Res Commun, 198 (3): 967-72. [PMID:8117304] |
3. Emonds-Alt X, Golliot F, Pointeau P, Le Fur G, Breliere JC. (1993)
Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor. Biochem Biophys Res Commun, 191 (3): 1172-7. [PMID:7682062] |
4. Emonds-Alt X, Vilain P, Goulaouic P, Proietto V, Van Broeck D, Advenier C, Naline E, Neliat G, Le Fur G, Brelière JC. (1992)
A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor. Life Sci, 50 (15): PL101-6. [PMID:1313515] |
5. Hopkins CR. (2010)
ACS chemical neuroscience molecule spotlight on Saredutant. ACS Chem Neurosci, 1 (10): 653-4. [PMID:22776916] |
6. Martin CA, Naline E, Emonds-Alt X, Advenier C. (1992)
Influence of (+/-)-CP-96,345 and SR 48968 on electrical field stimulation of the isolated guinea-pig main bronchus. Eur J Pharmacol, 224 (2-3): 137-43. [PMID:1334836] |
7. Overstreet DH, Naimoli VM, Griebel G. (2010)
Saredutant, an NK2 receptor antagonist, has both antidepressant-like effects and synergizes with desipramine in an animal model of depression. Pharmacol Biochem Behav, 96 (2): 206-10. [PMID:20470817] |
8. Rogacki N, Lopez-Grancha M, Naimoli V, Potestio L, Stevens RJ, Pichat P, Bergis OE, Cohen C, Varty GB, Griebel G. (2011)
The neurokinin NK2 antagonist, saredutant, ameliorates stress-induced conditions without impairing cognition. Pharmacol Biochem Behav, 98 (3): 405-11. [PMID:21115031] |
9. Sarau HM, Griswold DE, Potts W, Foley JJ, Schmidt DB, Webb EF, Martin LD, Brawner ME, Elshourbagy NA, Medhurst AD et al.. (1997)
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. J Pharmacol Exp Ther, 281 (3): 1303-11. [PMID:9190866] |
10. Tamburella A, Leggio GM, Micale V, Navarria A, Bucolo C, Cicirata V, Drago F, Salomone S. (2013)
Behavioural and neurochemical changes induced by stress-related conditions are counteracted by the neurokinin-2 receptor antagonist saredutant. Int J Neuropsychopharmacol, 16 (4): 813-23. [PMID:22695046] |