310392-94-0
310392-94-0 structure
- Name: Wf-516
- Chemical Name: Wf-516
- CAS Number: 310392-94-0
- Molecular Formula: C25H25Cl2N3O4
- Molecular Weight: 502.390
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-04-17 10:30:22
- Modify Date: 2024-01-10 18:51:06
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Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
| Name | Wf-516 |
|---|---|
| Synonyms |
1-Piperidineethanol, 4-(3,4-dichlorophenyl)-α-[[[2-(5-methyl-1,3,4-oxadiazol-2-yl)-4-benzofuranyl]oxy]methyl]-, (αS)-
(2S)-1-[4-(3,4-Dichlorophenyl)-1-piperidinyl]-3-{[2-(5-methyl-1,3,4-oxadiazol-2-yl)-1-benzofuran-4-yl]oxy}-2-propanol |
| Description | Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity. |
|---|---|
| Related Catalog | |
| Target |
Ki: 5 nM (Human 5-HT1A receptor), 40 nM (Human 5-HT2A receptor)[1] |
| In Vitro | Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats with Ki of 8.1 nM and 7.9 nM, respectively[2]. |
| 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 (ED50 = 32.4 ± 1.0 μg/kg) as compared to controls (ED50 = 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 RT50 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 ED50 values for Wf-516 in the hippocampus and raphe nucleus are 5.3 mg/kg and 4.2 mg/kg, respectively[2]. |
| Animal Admin | A series of 6 and 5 dynamic PET scans is performed for each rat approximately 5 h and 30 min after oral and intraperitoneal pretreatments with graded doses of Wf-516 (vehicle only, 1, 3, 10, 30 and 100 mg/kg) and pindolol (vehicle only, 1, 3, 10 and 30 mg/kg), respectively. Scans for the same individual rat receiving Wf-516 (n = 4) and pindolol (n = 3) are conducted more than 2 weeks and 1 week apart, respectively. PET imaging is also carried out for rats receiving oral administration of 30 mg/kg fluvoxamine dissolved in 0.5%HPMC 30 min before pindolol treatment in order to investigate the effects of fluvoxamine-induced increase of endogenous 5-HTs on the measurements of 5-HT1A receptor occupancies. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 683.7±65.0 °C at 760 mmHg |
| Molecular Formula | C25H25Cl2N3O4 |
| Molecular Weight | 502.390 |
| Flash Point | 367.3±34.3 °C |
| Exact Mass | 501.122223 |
| LogP | 3.60 |
| Vapour Pressure | 0.0±2.2 mmHg at 25°C |
| Index of Refraction | 1.616 |
| Storage condition | 2-8℃ |