1038988-11-2
1038988-11-2 structure
- Name: 5HT6-ligand-1
- Chemical Name: 5HT6-ligand-1
- CAS Number: 1038988-11-2
- Molecular Formula: C20H22BrN3O2S
- Molecular Weight: 448.38
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-04-03 15:49:59
- Modify Date: 2024-01-09 11:21:05
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5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.
| Name | 5HT6-ligand-1 |
|---|
| Description | 5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM. |
|---|---|
| Related Catalog | |
| Target |
Ki: 1.43 nM (5-HT6)[1] |
| In Vivo | 5HT6-ligand-1 is extensively metabolized in rat liver microsomes whereas in human liver microsomes, 5HT6-ligand-1 is extensively metabolized (90%). The IC50 values for 5HT6-ligand-1 at CYP 3A4 is 35.97%, whereas the IC50 values at CYP 2D6 enzymes is less than 20 μM. 5HT6-ligand-1 at an oral dose of 10 mg/kg is rapidly absorbed in rats with a good oral half-life of 3.17±0.49 h with an oral bioavailability of 29±5%. The observed oral Cmax is 60±44 ng/mL and occurs at 1.83 h. 5HT6-ligand-1 displays an oral exposure of 217±92 ng h/mL. It has a clearance of 220±92 mL/min/kg with a volume of distribution of 32.6±10.7 L/kg for iv dose. Extensive rat metabolism coupled with high clearance could be the possible reason for moderate oral bioavailability showed by 5HT6-ligand-1. Oral administration of 5HT6-ligand-1 reverses the time delay induced memory deficit and statistically significant effect is observed at a dose of 10 mg/kg indicating cognitive improvement potential of the compound 6a[1]. |
| References |
| Molecular Formula | C20H22BrN3O2S |
|---|---|
| Molecular Weight | 448.38 |