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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
8-OH-DPAT (also known as 8-Hydroxy-DPAT) is a classic, potent and selective agonist of 5-HT1A with the potential to be used for sleep disorders. It activates 5-HT1A with a pIC50 of 8.19. 8-OH-DPAT weakly binds to 5-HT1B with pIC50 of 5.42 and pIC50 <5 for 5-HT; it has a selectivity of almost a thousand times for a subtype of the 5-HT1 binding site and a Ki of 466 nM for 5-HT7. Furthermore In cultured human RPE cells, it can decrease oxidative damage, boost antioxidant defense, and lessen the accumulation of lipofuscin produced by both autophagy and photoreceptor outer segment. In orexin-KO mice, narcoleptic-like sleep dysfunction is caused by 5-HT1A receptor dysfunction, which may also contribute to orexin deficiency-induced sleep disorders. In addition, the use of 5-HT1A receptor agonists like 8-OH-DPAT may be helpful in treating sleep disorders caused by orexin deficiencies.
| Targets |
5-HT1A Receptor ( pIC50 = 8.19 ); 5-HT7 Receptor ( pIC50 = 466 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
8-OH-DPAT (also known as 8-Hydroxy-DPAT) is a well-established, strong, and specific 5-HT1A agonist, with a pIC50 of 8.19. 8-OH-DPAT weakly binds to 5-HT1B with pIC50 of 5.42 and pIC50 <5 for 5-HT; it has a selectivity of almost a thousand times for a subtype of the 5-HT1 binding site and a Ki of 466 nM for 5-HT7. Furthermore In cultured human RPE cells, it can decrease oxidative damage, boost antioxidant defense, and lessen the accumulation of lipofuscin produced by both autophagy and photoreceptor outer segment. In orexin-KO mice, narcoleptic-like sleep dysfunction is caused by 5-HT1A receptor dysfunction, which may also contribute to orexin deficiency-induced sleep disorders. In addition, the use of 5-HT1A receptor agonists like 8-OH-DPAT may be helpful in treating sleep disorders caused by orexin deficiencies.
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| Cell Assay |
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. All measurements for the pretreatment phase are taken 24 hours after the H2O2 exposure, and for the posttreatment phase, 8-OH DPAT is added right away. Management of 5HT1A agonists: Addition of 8-OH DPAT, a 5-HT1A receptor agonist, to the culture medium at concentrations ranging from 0.1 to 20 µM is done every 48 hours to evaluate the compound's capacity to inhibit lipofuscin formation in cultured stem cells. PBS-only-receiving cells served as negative controls in all experiments, which were conducted in basal medium. In order to find out if the effects of 8-OH DPAT persist after 5-HT1A receptor agonist treatment is stopped, the cells are kept in basal medium or fed POS for an additional 28 days after the 8-OH DPAT treatment is stopped. In order to determine whether 8-OH DPAT can eliminate lipofuscin that has already been present, autophagy- and phagocytic-derived lipofuscin are allowed to build up as previously mentioned, and then 8-OH DPAT is added every two days for a maximum of 28 days. We include the 5-HT1A receptor antagonist S(-)-UH-301 at 5 µM in some experiments to verify that 8-OH DPAT is acting through the 5-HT1A receptor agonist. In order to ascertain how the timing of 8-OH DPAT treatment affects oxidative stress markers, RPE cultures are either treated with the 5HT1A agonist for 3 or 24 hours following exposure to H2O2 or pre-treated with 8-OH DPAT (at 1 or 10 µM) for 3 or 24 hours prior to exposure to 200 µM H2O2 for 1 hour. As a negative control, cells that are not subjected to an oxidative stressor are used, and as a positive control, cells that are subjected to an oxidative stressor but do not receive 8-OH DPAT. The only function of cells exposed to 8-OH DPAT is that of an extra control.
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| Animal Protocol |
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| References |
| Molecular Formula |
C16H25NO
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| Molecular Weight |
247.38
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| Exact Mass |
247.19
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| Elemental Analysis |
C, 77.68; H, 10.19; N, 5.66; O, 6.47
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| CAS # |
78950-78-4
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| Related CAS # |
8-OH-DPAT hydrobromide; 76135-31-4
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| Appearance |
Solid powder
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| SMILES |
CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O
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| InChi Key |
ASXGJMSKWNBENU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H25NO/c1-3-10-17(11-4-2)14-9-8-13-6-5-7-16(18)15(13)12-14/h5-7,14,18H,3-4,8-12H2,1-2H3
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| Chemical Name |
7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0424 mL | 20.2118 mL | 40.4236 mL | |
| 5 mM | 0.8085 mL | 4.0424 mL | 8.0847 mL | |
| 10 mM | 0.4042 mL | 2.0212 mL | 4.0424 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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