6-APDB
6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse.
For research use only. We do not sell to patients.
- CAS No.: 152623-93-3
- Formula: C11H15NO
- Molecular Weight:177.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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human 5-HT2B Receptor |
6-APDB (Multiple concentrations; 10 min pre-incubation, 10 min monoamine uptake incubation) inhibits monoamine uptake in NET-, DAT-, and SERT-expressing HEK 293 cells, with highest potency for NET, intermediate potency for SERT, and lowest potency for DAT, resulting in a low DAT:SERT ratio indicative of preferential serotonergic activity[1].
6-APDB (100 μM; 45 min NA release, 15 min dopamine, 5-HT release) induces transporter-mediated release of noradrenaline, dopamine, and 5-HT from monoamine transporter-expressing HEK 293 cells[1].
6-APDB (Multiple concentrations) acts as a low-potency partial agonist at human 5-HT2A receptors and a high-potency partial agonist at human 5-HT2B receptors in HEK 293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK 293 cells
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Concentration:100 μM
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Incubation Time:45 min for NA release; 15 min for dopamine, 5-HT release
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Result:Induced by a high concentration of the compound (100 μM) after preloading the transporter-transfected cells with the respective radiolabelled monoamine.
Induced transporter-mediated release of noradrenaline, dopamine, and 5-HT similarly to methamphetamine and MDMA.
6-APDB (0.25-2.5 mg/kg; i.p.; single dose; 40 minutes pre-test) only partially substitutes for the discriminative stimulus effects of methamphetamine in trained male Sprague-Dawley rats, and high doses suppress response rates[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 320-350 g, trained to discriminate methamphetamine from vehicle)[2]
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Dosage:0.25, 0.5, 1, 2.5 mg/kg
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Administration:i.p.; single dose; 40 minutes pre-test
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Result:At 1 mg/kg, produced discrimination responses of 33±21% for methamphetamine, 53±21% for cocaine, and 67±21% for DOM, respectively.
At 2.5 mg/kg, almost completely inhibited the responses.
Chemical Information
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CAS No. 152623-93-3
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Molecular Weight 177.24
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Formula C11H15NO
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SMILES
NC(C)CC1=CC=C2C(OCC2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Rickli A, et al. Pharmacological profile of novel psychoactive benzofurans. Br J Pharmacol. 2015;172(13):3412-3425. [Content Brief]
[2]. Dolan SB, et al. Discriminative stimulus and locomotor effects of para-substituted and benzofuran analogs of amphetamine. Drug Alcohol Depend. 2017;180:39-45. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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