[CAS NO. 310392-94-0] Wf-516
PRODUCTS SPECIFICATIONS [310392-94-0]
DESCRIPTION [310392-94-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 502.39 |
| Molecular Formula | C25H25Cl2N3O4 |
| SMILES | O[C@H](COC1=C2C=C(C3=NN=C(C)O3)OC2=CC=C1)CN(CC4)CCC4C5=CC=C(Cl)C(Cl)=C5 |
Summary
Wf-516 is an inhibitor of 5-HT reuptake , and an antagonist of 5-HT1A and 5-HT2A receptors, with K i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
IC50 & Target
|
5-HT 1A Receptor 5 nM (Ki) |
5-HT 2A Receptor 40 nM (Ki) |
In Vitro
Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats with K i of 8.1 nM and 7.9 nM, respectively [2] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Wf-516 (0.5 mg/kg, i.v.) does not induce any change in the firing activity of 5-HT neurons, but significantly blocks the inhibitory effect of 8-OHDPAT (a 5-HT autoreceptor agonist) by 70%. A full dose-response relationship between the suppression of DRN firing activity and different doses of LSD shows a significant fourfold shift to the right in the Wf-516 pretreated rats (ED 50 = 32.4 ± 1.0 μg/kg) as compared to controls (ED 50 = 7.5 ± 1.2 μg/kg). After intravenous administration of successive doses of 1.25 mg/kg of Wf-516 (up to 10 mg/kg), the effect of microiontophoretically applied 5-HT is prolonged and reaches statistical significance at 7.5 mg/kg. At this dose, the RT 50 value is increased by 53% and, by 75% at the highest dose of 10 mg/kg of Wf-516 used [1] . Oral administration of 30 mg/kg Wf-516 to these 5,7-DHT-treated rats induces a significant decrease of BPND in the hippocampus as compared with baseline, but no additional reduction of BPND is observed in the raphe nucleus. Oral ED 50 values for Wf-516 in the hippocampus and raphe nucleus are 5.3 mg/kg and 4.2 mg/kg, respectively [2] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] El Mansari M, et al. In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):351-61. Epub 2007 Nov 30.
- [2] Saijo T, et al. Presynaptic selectivity of a ligand for serotonin 1A receptors revealed by in vivo PET assays of rat brain. PLoS One. 2012;7(8):e42589.
