8-OH-DPAT (8-Hydroxy-DPAT) is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A. 8-OH-DPAT has high affinity at 5-HT7 with a Ki of 466 nM.
In vivo, 8-OH-DPAT (1 mg/kg) significantly increases wakefulness and reduces the duration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout (KO) mice. 8-OH-DPAT (1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice.
| Cell Experiment | |
|---|---|
| Cell lines | Retinal pigment epithelial (RPE) cells |
| Preparation method | Cells are exposed to H2O2 (200 µM) for 1 hour and either pre-or post treated with 8-OH DPAT (10 µM) for 24 hours. In the case of pretreatment all measurements are made 24 hr after H2O2 and for post treatment 8-OH DPAT is added immediately following H2O2 exposure. 5HT1A agonist treatment: To assess the ability of the 5-HT1A receptor agonist, 8-OH DPAT, to reduce lipofuscin formation in cultured RPE cells, this compound is added to the culture medium every 48 hours at concentrations ranging from 0.1 to 20 µM. All experiments are undertaken in basal medium, and cells receiving vehicle alone (PBS) acted as negative controls. To determine if the effect of 8-OH DPAT is sustained following discontinuation of 5-HT1A receptor agonist treatment, 8-OH DPAT treatment is discontinued after 28 days and the cells maintained in basal medium or fed POS for a further 28 days. To assess the ability of 8-OH DPAT to remove existing lipofuscin, autophagy-derived lipofuscin and phagocytic-derived lipofuscin are allowed to accumulate as described above and then 8-OH DPAT is added every second day for up to 28 days. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Lister hooded rats |
| Formulation | isotonic saline |
| Dosages | 0, 3.0, 10, 100 and 300 μg/kg |
| Administration | i.p. |
| Molecular Weight | 247.38 |
| Formula | C16H25NO |
| CAS Number | 78950-78-4 |
| Solubility (25°C) | DMSO: ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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