8-OH-DPAT (8-Hydroxy-DPAT)

Catalog No.S8447 Batch:S844701

Technical Data

Formula

C₁₆H₂₅NO

Molecular Weight

247.38

CAS No.

78950-78-4

Solubility (25°C)*

In vitro

DMSO

49 mg/mL (198.07 mM)

Ethanol

49 mg/mL (198.07 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

8-OH-DPAT (8-Hydroxy-DPAT) is a classic 5-HT1A agonist with a pIC50 of 8.19. This compound has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site, and its biological half-life is 1.5 hours.

Targets

5-HT1A ^[1]
(Cell-free)

8.19(pIC50)

In vitro

8-OH-DPAT (8-Hydroxy-DPAT) is only weakly effective at the 5-HT1B subtype, with a pIC50 of 5.42 ± 0.08 (n = 5), and has no effect on 5-HT1B binding at concentrations lower than 100 nM^[1]. This compound is able to reduce the accumulation of both autophagic-derived and photoreceptor outer segment-derived lipofuscin, increase antioxidant protection and reduce oxidative damage in cultured human RPE cells^[4].

In vivo

The selective 5-HT1A-receptor agonist 8-OH-DPAT (8-Hydroxy-DPAT) rapidly reverses the hypotensive and bradycardic responses established during severe hemorrhage with relatively little variability after intravenous administration. It is relatively lipophilic and readily crosses the blood-brain barrier^[3].

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines Retinal pigment epithelial (RPE) cells Concentrations 10 μM Incubation Time 24 h Method Cells are exposed to H2O2 (200 µM) for 1 hour and either pre-or post treated with 8-OH-DPAT (8-Hydroxy-DPAT) (10 µM) for 24 hours. In the case of pretreatment all measurements are made 24 hr after H2O2 and for post treatment this compound is added immediately following H2O2 exposure. 5HT1A agonist treatment: To assess the ability of the 5-HT1A receptor agonist to reduce lipofuscin formation in cultured RPE cells, it 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 it is sustained following discontinuation of 5-HT1A receptor agonist treatment, this compound is discontinued after 28 days and the cells maintained in basal medium or fed POS for a further 28 days. To assess its ability to remove existing lipofuscin, autophagy-derived lipofuscin and phagocytic-derived lipofuscin are allowed to accumulate as described above and then it is added every second day for up to 28 days. To confirm that it is acting via the 5-HT1A receptor agonist we include the 5-HT1A receptor antagonist S(-)-UH-301 at 5 µM in some experiments. To determine the effect of timing of its treatment on oxidative stress markers, RPE cultures are either pre-treated with it (at 1 or 10 µM) for 3 or 24 hours prior to exposure to 200 µM H2O2 for 1 hour or treated with the 5HT1A agonist for 3 or 24 hours post-exposure to H2O2. Cells not exposed to oxidative stressor serve as a negative control, and cells exposed to oxidative stressor but not it serve as a positive control. Cells exposed to it only act as an additional control.
Animal Study:^{^[2]}	Animal Models Male Lister hooded rats Dosages 0, 3.0, 10, 100 and 300 μg/kg Administration i.p.

Cell Assay:^{^[4]}

Cell lines
Retinal pigment epithelial (RPE) cells
Concentrations
10 μM
Incubation Time
24 h
Method
Cells are exposed to H2O2 (200 µM) for 1 hour and either pre-or post treated with 8-OH-DPAT (8-Hydroxy-DPAT) (10 µM) for 24 hours. In the case of pretreatment all measurements are made 24 hr after H2O2 and for post treatment this compound is added immediately following H2O2 exposure. 5HT1A agonist treatment: To assess the ability of the 5-HT1A receptor agonist to reduce lipofuscin formation in cultured RPE cells, it 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 it is sustained following discontinuation of 5-HT1A receptor agonist treatment, this compound is discontinued after 28 days and the cells maintained in basal medium or fed POS for a further 28 days. To assess its ability to remove existing lipofuscin, autophagy-derived lipofuscin and phagocytic-derived lipofuscin are allowed to accumulate as described above and then it is added every second day for up to 28 days. To confirm that it is acting via the 5-HT1A receptor agonist we include the 5-HT1A receptor antagonist S(-)-UH-301 at 5 µM in some experiments. To determine the effect of timing of its treatment on oxidative stress markers, RPE cultures are either pre-treated with it (at 1 or 10 µM) for 3 or 24 hours prior to exposure to 200 µM H2O2 for 1 hour or treated with the 5HT1A agonist for 3 or 24 hours post-exposure to H2O2. Cells not exposed to oxidative stressor serve as a negative control, and cells exposed to oxidative stressor but not it serve as a positive control. Cells exposed to it only act as an additional control.

Animal Study:^{^[2]}

Animal Models
Male Lister hooded rats
Dosages
0, 3.0, 10, 100 and 300 μg/kg
Administration
i.p.

References

https://pubmed.ncbi.nlm.nih.gov/6223827/
https://pubmed.ncbi.nlm.nih.gov/1826841/
https://pubmed.ncbi.nlm.nih.gov/12611395/

https://pubmed.ncbi.nlm.nih.gov/22509307/

+ Expand

Selleck's 8-OH-DPAT (8-Hydroxy-DPAT) Has Been Cited by 2 Publications

Single-dose psilocybin rapidly and sustainably relieves allodynia and anxiodepressive-like behaviors in mouse models of chronic pain [ Nat Neurosci, 2025, 28(11):2285-2295]	PubMed: 41039182
Targeting 5-Hydroxytryptamine Receptor 1A in the Portal Vein to Decrease Portal Hypertension [ Gastroenterology, 2024, 167(5):993-1007]	PubMed: 38906512

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