Bromo-dragonFLY hydrochloride
Bromo-DragonFLY hydrochloride is an orally active benzodifuran psychoactive substance with hallucinogen-related activity. Bromo-dragonFLY hydrochloride is a 5-HT2A receptor agonist and MAO-A inhibitor that activates the Gαq-PLC-β/IP1/calcium signaling pathway and targets serotonin subtypes associated with hallucinogenic effects. Bromo-dragonFLY hydrochloride produces full substitution for the LSD stimulus in LSD-trained rats in drug discrimination experiments, induces head-twitch responses in mice, and blocks hERG potassium channels. Bromo-dragonFLY hydrochloride can be used in research related to neurological diseases.
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- CAS No.: 219986-78-4
- 화학식: C13H13BrClNO2
- 분자량:330.60
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보관:
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
- 순도&문서
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
[4]|
MAO-A 0.54 μM (IC50) |
5-HT2A Receptor 0.04 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | EC50 |
0.222 nM
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Gαq-PLC-β interaction assay in HEK293T cells expressing HA-5-HT2AR, Gαq-LgBiT, and SmBiT-PLC-β assessed by NanoGlo Live Cell substrate luminescence monitored continuously for 2 hrs after agonist addition.
Gαq-PLC-β interaction assay in HEK293T cells expressing HA-5-HT2AR, Gαq-LgBiT, and SmBiT-PLC-β assessed by NanoGlo Live Cell substrate luminescence monitored continuously for 2 hrs after agonist addition.
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S1043661826000095 |
| HEK-293T | EC50 |
6.21 nM
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miniGαq recruitment assay in HEK293T cells expressing 5-HT2AR-LgBiT and SmBiT-miniGαq assessed by NanoGlo Live Cell substrate luminescence monitored continuously for 2 hrs after agonist addition.
miniGαq recruitment assay in HEK293T cells expressing 5-HT2AR-LgBiT and SmBiT-miniGαq assessed by NanoGlo Live Cell substrate luminescence monitored continuously for 2 hrs after agonist addition.
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S1043661826000095 |
| HEK-293T | EC50 |
0.0787 nM
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Agonist activity of R-Bromo-DragonFLY at 5-HT2AR in HEK293T cells assessed by IP1 accumulation using HTRF IP-One Gq detection kit incubated 2 hrs at 37°C.
Agonist activity of R-Bromo-DragonFLY at 5-HT2AR in HEK293T cells assessed by IP1 accumulation using HTRF IP-One Gq detection kit incubated 2 hrs at 37°C.
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S1043661826000095 |
| HEK-293T | EC50 |
1.28 nM
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Ca2+ mobilization assay in HEK293T cells expressing HA-5-HT2AR using Fluo-4 Direct calcium assay kit with fluorescence monitored for 180 s after agonist addition.
Ca2+ mobilization assay in HEK293T cells expressing HA-5-HT2AR using Fluo-4 Direct calcium assay kit with fluorescence monitored for 180 s after agonist addition.
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S1043661826000095 |
In Vitro
Bromo-DragonFLY (100 μM) hydrochloride exhibits no monoamine-releasing activity in HEK-293 cell efflux assays and shows no inhibitory effect on human DAT, NET, or SERT transporters[3].
Bromo-dragonFLY (DOB-DFLY) hydrochloride binds to cloned human 5-HT2A receptors with a Ki of 0.04 nM; inhibits MAOA with an IC50 of 0.54 µM; and is not metabolized in vitro by HLM, HLC, MAO, FMO, or CYP isoenzymes[4].
Bromo-DragonFLY (2 h) hydrochloride is an agonist of 5-HT2AR in the HEK293T Gαq-PLC-β interaction assay, with an EC50 of 0.222 nM and an Emax of 111% relative to serotonin; in the HEK293T miniGαq recruitment assay, the EC50 is 6.21 nM and the Emax is 147% relative to serotonin[5].
Bromo-DragonFLY hydrochloride is the most potent agonist in the HEK293T IP1 accumulation assay, with an EC50 of 0.0787 nM and an Emax of 117% relative to serotonin; in the HEK293T Ca2+ mobilization assay, it is a potent agonist, with an EC50 of 1.28 nM and an Emax of 103% relative to serotonin[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 219986-78-4
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분자량 330.60
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화학식 C13H13BrClNO2
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SMILES
BrC1=C2OC=CC2=C(CC(C)N)C3=C1C=CO3.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[3]. Rickli A, et al. Pharmacological profile of novel psychoactive benzofurans. British journal of pharmacology. 2015 Jul;172(13):3412-25. [Content Brief]
[4]. Halberstadt AL, et al. Comparison of the behavioral responses induced by phenylalkylamine hallucinogens and their tetrahydrobenzodifuran ("FLY") and benzodifuran ("DragonFLY") analogs. Neuropharmacology. 2019 Jan;144:368-376. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bromo-dragonFLY hydrochloride Related Classifications
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