| Size | Price | Stock | Qty |
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| Targets |
pKi: 8.23 (Melatonin MT2 receptor) and 8.95 (Melatonin MT1 receptor)[2]
8-M-PDOT targets the melatonin MT2 receptor as a selective agonist. It binds to human recombinant MT2 receptors with a pKi of 8.95 (Ki ≈ 1.12 nM), compared to a pKi of 8.23 for MT1 receptors. This selectivity makes it a valuable tool for dissecting MT2-specific signaling pathways and their physiological roles. |
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| ln Vitro |
In vitro, 8-M-PDOT is a potent and selective MT2 receptor agonist. It binds to human recombinant MT2 receptors with high affinity (pKi = 8.95; Ki = 1.12 nM) and shows 5.2- to 20-fold selectivity over MT1 receptors (pKi = 8.23). Its activity makes it a valuable tool for studying MT2 receptor function and pharmacology.
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| ln Vivo |
Treatment with 8-M-PDOT (10 µg/µL) injected into the dorsal striatum via bilateral cannulas for 30 minutes in male Wistar rats has anxiolytic-like effects [2].
In vivo, 8-M-PDOT exhibits anxiolytic-like activity. As a selective MT2 agonist, it can be used to study the role of MT2 receptors in anxiety, sleep, and circadian rhythms. It has been shown to have anxiolytic-like effects in animal models. Its in vivo efficacy supports the therapeutic potential of MT2 agonists for anxiety disorders. |
| Enzyme Assay |
In vitro receptor binding assays for 8-M-PDOT involve measuring its affinity for MT1 and MT2 receptors. Radioligand binding studies using ³H-melatonin or other melatonin ligands are performed on membranes from cells expressing the receptors. The compound is incubated with increasing concentrations, and pKi values are calculated from competition binding curves. Functional assays measure its ability to activate MT2-mediated signaling pathways.
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| Cell Assay |
For in vitro cell-based assays, cells expressing MT1 or MT2 receptors are cultured and treated with 8-M-PDOT at various concentrations. Receptor activation is measured by quantifying the inhibition of forskolin-stimulated cAMP accumulation or other downstream signaling pathways. Its selectivity for MT2 is confirmed by comparing its effects on cells expressing MT1 receptors. Cell viability is assessed by standard assays.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (280-320 g) with Rotenone[2]
Doses: 10 µg/µL Route of Administration: Administrated into the dorsal striatum by bilateral cannulas; for 30 minutes Experimental Results: Increased percentage of time spent in the open arms and in the number of open arms entries. In vivo animal studies with 8-M-PDOT are conducted in models of anxiety and circadian rhythm disorders. The compound is administered systemically, and its anxiolytic-like effects are assessed using behavioral tests such as the elevated plus maze or light-dark box. Its effects on sleep-wake cycles can be assessed using electroencephalography (EEG) recordings. |
| ADME/Pharmacokinetics |
8-M-PDOT (CAS: 134865-70-6) has a molecular weight of 233.31 g/mol and a molecular formula of C14H19NO2. Appearance: solid. Purity: ≥99% (HPLC). Storage: Room temperature. Solubility: DMSO. The compound is a selective MT2 receptor agonist with anxiolytic-like activity.
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| Toxicity/Toxicokinetics |
8-M-PDOT is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a selective MT2 agonist, it may have effects on sleep and circadian rhythms. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
N-(8-methoxy-1,2,3,4-tetrahydronaphth-2-yl)propionamide is a member of the tetrahydronaphthyl group of compounds.
8-M-PDOT (AH-002) is a selective agonist of the melatonin MT2 receptor, exhibiting 5.2-fold to 20-fold selectivity for MT2 over MT1. It binds to human recombinant MT2 receptors with a Ki of 1.12 nM (pKi = 8.95) and has anxiolytic-like activity. It has a molecular weight of 233.31 g/mol and a molecular formula of C14H19NO2. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C₁₄H₁₉NO₂
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|---|---|
| Molecular Weight |
233.31
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| Exact Mass |
233.142
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| CAS # |
134865-70-6
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| PubChem CID |
5170952
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| Appearance |
White to off-white solid powder
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| Density |
1.09g/cm3
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| Boiling Point |
447.8ºC at 760 mmHg
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| Flash Point |
224.6ºC
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| Vapour Pressure |
3.27E-08mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
2.469
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC(=O)NC1CCC2=C(C1)C(=CC=C2)OC
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| InChi Key |
RVIGBTUDFAGRTQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19NO2/c1-3-14(16)15-11-8-7-10-5-4-6-13(17-2)12(10)9-11/h4-6,11H,3,7-9H2,1-2H3,(H,15,16)
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| Chemical Name |
N-(8-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)propionamide
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| Synonyms |
AH-002,8 MPDOT AH002,8 M PDOTAH 002, 8-M-PDOT
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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 |
| 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) |
DMSO : ~100 mg/mL (~428.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 7.5 mg/mL (32.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 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: ≥ 7.5 mg/mL (32.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 75.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2861 mL | 21.4307 mL | 42.8614 mL | |
| 5 mM | 0.8572 mL | 4.2861 mL | 8.5723 mL | |
| 10 mM | 0.4286 mL | 2.1431 mL | 4.2861 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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