221452-76-2
Chemical Structure
EF-7412
- CAS No.: 221452-76-2
- Formula:C22H33N5O4S
- Molecular Weight:463.59
InChIKey: APHPLOYRLDEZMD-UHFFFAOYSA-N
SMILES: O=C1N(CCCCN2CCN(CC2)C3=CC(NS(=O)(CC)=O)=CC=C3)C(C4N1CCC4)=O
Biological Activity: 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].
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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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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]
- [3]. López-Rodríguez ML, et al. Synthesis and Structure-Activity Relationships of a New Model of Arylpiperazines. 8. 1 Computational Simulation of Ligand-Receptor Interaction of 5-HT 1A R Agonists with Selectivity over alpha1-Adrenoceptors. J Med Chem. 2005 Apr;48 (7):2548-2558.
