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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- CAS. Nr.: 152623-93-3
- Formel: C11H15NO
- Molecular Weight:177.24
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Biologische Aktivität
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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. Nr. 152623-93-3
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Molecular Weight 177.24
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Formel C11H15NO
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SMILES
NC(C)CC1=CC=C2C(OCC2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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