2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. 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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EF-7412

EF-7412 Chemical Structure

CAS No. : 221452-76-2

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EF-7412 Related Antibodies

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Description

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[1][2][3].

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.

EF-7412 Related Antibodies
In Vivo

EF-7412 (compound 46) (0.5-40 mg/kg; s.c.; single dose) acts as an antagonist at presynaptic 5-HT1A receptors in Mus musculus (blocking 8-OH-DPAT-induced hypothermia without altering baseline temperature) and modulates both serotonergic and dopaminergic neuronal activity, with a slight inhibitory effect on locomotor activity at doses of 20 mg/kg and above[3].
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.

Animal Model: Swiss albino (male, 20-25 g)[3]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 0.5 mg/kg; 2.5 mg/kg; 40 mg/kg
Administration: s.c.; single dose
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.
Animal Model: Sprague Dawley (male, 200-250 g)[3]
Dosage: 0.3 mg/kg; 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: s.c.; single dose
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.
Molecular Weight

463.59

Formula

C22H33N5O4S
CAS No.
SMILES

O=C1N(CCCCN2CCN(CC2)C3=CC(NS(=O)(CC)=O)=CC=C3)C(C4N1CCC4)=O
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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EF-7412 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:

EF-7412221452-76-2EF7412EF 74125-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptordual 5-HT?A/D? antagonistselective over α?-adrenoceptorsblocks 8-OH-DPAT-induced responsesincreases 5-HIAA/5-HT ratioincreases DOPAC/DA ratioinhibits spontaneous locomotor activitymouseratanxiety-related disordersdepression-related disordersInhibitorinhibitorinhibit

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