2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Monoamine Transporter Serotonin Transporter Dopamine Transporter 5-HT Receptor
  4. 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.

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6-APDB

6-APDB Chemical Structure

CAS No. : 152623-93-3

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6-APDB Related Antibodies

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Description

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[1][2].

IC50 & Target

human 5-HT2B Receptor

 

In Vitro

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.

6-APDB Related Antibodies

ELISA Assay[1]

Cell Line: HEK 293 cells
Concentration: 100 μM
Incubation Time: 45 min for NA release; 15 min for dopamine, 5-HT release
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.
In Vivo

6-APDB (1-25 mg/kg; i.p.; single dose) produces dose-dependent locomotor stimulation in male Swiss-Webster mice with an ED50 of 2.80 mg/kg, and high doses induce initial activity depression followed by delayed stimulation[2].
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.

Animal Model: Sprague-Dawley (male, 320-350 g, trained to discriminate methamphetamine from vehicle)[2]
Dosage: 0.25, 0.5, 1, 2.5 mg/kg
Administration: i.p.; single dose; 40 minutes pre-test
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.
Molecular Weight

177.24

Formula

C11H15NO
CAS No.
SMILES

NC(C)CC1=CC=C2C(OCC2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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6-APDB Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

6-APDB152623-93-3Monoamine TransporterSerotonin TransporterDopamine Transporter5-HT Receptor5-HTTSERTSLC6A4DATSLC6A3Serotonin Receptor5-hydroxytryptamine Receptorrat TA1 receptorserotoninhuman SERThuman NEThuman 5-HT2β receptorshuman DATmouse TA1 receptornoradrenalinehuman 5-HT2? receptorsdopamineInhibitorinhibitorinhibit

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