Home Neuronal Signaling 5-HT Receptor agonist 8-OH-DPAT (8-Hydroxy-DPAT)

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8-OH-DPAT (8-Hydroxy-DPAT) 5-HT Receptor agonist

8-OH-DPAT (8-Hydroxy-DPAT) is a classic 5-HT1A agonist with a pIC50 of 8.19. It 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.

8-OH-DPAT (8-Hydroxy-DPAT) 5-HT Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 247.38

Purity & Quality Control

Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Mechanism of Action

Targets
5-HT1A [1]
(Cell-free)
8.19(pIC50)

In vitro
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 it 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].
Cell Research 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 it 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, 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 this compound is sustained following discontinuation of 5-HT1A receptor agonist treatment, it 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 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.

In Vivo
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 when administered intravenously. It is relatively lipophilic and readily crosses the blood-brain barrier[3].
Animal Research 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/

Chemical Information

Molecular Weight 247.38 Formula

C16H25NO
CAS No. 78950-78-4 SDF Download SDF
Synonyms N/A
Smiles CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (198.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 49 mg/mL

Water : Insoluble


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In vivo
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