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.
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- No. CAS: 221452-76-2
- Fòrmula: C22H33N5O4S
- Peso molecular:463.59
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Almacenamiento:
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Actividad biológica
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5-HT1A Receptor 27 nM (Ki) |
Dopamine D2 receptor 22 nM (Ki) |
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.
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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No. CAS 221452-76-2
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Peso molecular 463.59
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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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- 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