EF-7412
EF-7412 is a dual antagonist of the 5-HT1A receptor and dopamine D2 receptor, with Ki values of 27 nM and 22 nM, respectively. EF-7412 acts as an antagonist at both pre- and postsynaptic 5-HT1A receptor sites, blocking 8-OH-DPAT (HY-112061)-induced hypothermia, behavioral syndrome, and corticosterone elevation in vivo. EF-7412 increases hypothalamic 5-HIAA/5-HT and DOPAC/DA ratios, alters 5-HT and DA neuronal activity, and slightly decreases spontaneous motor activity. EF-7412 can be used for research on 5-HT1A/D2 receptor regulation and related neural pathways.
For research use only. We do not sell to patients.
- CAS No.: 221452-76-2
- Formula: C22H33N5O4S
- Molecular Weight:463.59
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[3]|
5-HT1A Receptor 27 nM (Ki) |
Dopamine D2 receptor 22 nM (Ki) |
In Vitro
EF-7412 interacts with the rhodopsin-based 5-HT1A receptor transmembrane domain model via specific ionic and hydrogen bonds[1].
EF-7412 (compound 46) (15-90 min) potently binds to rat brain 5-HT1A (Ki = 27 nM) and D2 dopaminergic (Ki = 22 nM) receptors, with no significant affinity for α1-adrenergic, 5-HT2A, 5-HT3, 5-HT4, or benzodiazepine receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
EF-7412 (0.3-10 mg/kg; s.c.; single dose) acts as an antagonist at postsynaptic 5-HT1A receptors in rats, blocking both 8-OH-DPAT (HY-112061)-induced behavioral effects and corticosterone secretion without altering baseline measures[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss albino (male, 20-25 g)[3]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg; 0.5 mg/kg; 2.5 mg/kg; 40 mg/kg
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Administration:s.c.; single dose
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Result:Did not alter mouse rectal temperature at doses of 5, 10, and 20 mg/kg.
Completely blocked 8-OH-DPAT-induced hypothermia at 20 mg/kg when administered 15, 60, or 120 minutes before 8-OH-DPAT.
Increased the 5-HIAA/5-HT ratio in mouse hypothalamus at 10 mg/kg, an effect reversed by pretreatment with 8-OH-DPAT.
Increased the DOPAC/dopamine ratio in mouse hypothalamus at 10 mg/kg, an effect not reversed by 8-OH-DPAT.
Produced a significant slight decrease in spontaneous locomotor activity compared to vehicle controls at doses of 20 mg/kg and 40 mg/kg.
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Animal Model:Sprague Dawley (male, 200-250 g)[3]
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Dosage:0.3 mg/kg; 1 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:s.c.; single dose
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Result:Did not alter baseline flat body posture (FBP) or lower lip retraction (LLR) scores at 10 mg/kg.
Completely blocked both FBP and LLR induced by 8-OH-DPAT at 10 mg/kg.
Did not alter baseline plasma corticosterone levels at doses of 0.3, 1, 5, and 10 mg/kg.
Significantly attenuated the increase in plasma corticosterone induced by 8-OH-DPAT at 10 mg/kg.
Chemical Information
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CAS No. 221452-76-2
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Molecular Weight 463.59
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Formula C22H33N5O4S
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SMILES
O=C1N(CCCCN2CCN(CC2)C3=CC(NS(=O)(CC)=O)=CC=C3)C(C4N1CCC4)=O
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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.
Protocols
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
Purity & Documentation
References
[1]. López-Rodríguez ML, et al. Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors. J Med Chem. 2005;48(7):2548-2558. [Content Brief]
[2]. López-Rodríguez ML, et al. Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties. Bioorg Med Chem Lett. 1999;9(12):1679-1682. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EF-7412 Related Classifications
HY-182677 Related Classifications
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Keywords
- EF-7412
- 221452-76-2
- EF7412
- EF 7412
- 5-HT Receptor
- Dopamine Receptor
- dual 5-HT?A/D? antagonist
- selective over α?-adrenoceptors
- blocks 8-OH-DPAT-induced responses
- increases 5-HIAA/5-HT ratio
- increases DOPAC/DA ratio
- inhibits spontaneous locomotor activity
- mouse
- rat
- anxiety-related disorders
- depression-related disorders
- Inhibitor
- inhibitor
- inhibit