Antipsychotic agent-2 

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT_1A, 5-HT_2A, 5-HT_2C, D₂ and H₁ receptors with K_is of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability^[1].

Antipsychotic agent-2 (Compound 11) antagonizes the inhibition of Forskolin (HY-15371)-stimulated cAMP production elicited by 10^-6 M dopamine in CHO-K1 cells stably expressing human D₂ receptors, indicative of D₂ antagonistic activity (K_b=45.7 nM)^[1].
Antipsychotic agent-2 inhibits the Forskolin-stimulated cAMP production in HEK293 cells stably expressing 5-HT_1A receptors in a concentration-dependent manner, indicative of 5-HT_1A agonistic activity (EC₅₀=160 nM), while it behaves as 5-HT_2A antagonists, antagonizing the inositol phosphate production stimulated by 10^-6 5-HT in CHO-K1 cells expressing 5-HT_2A receptors (K_b=96.4 nM)^[1].
Antipsychotic agent-2 (0.1-10 μM) is a relatively low potency CYP3A4 inducer^[1].
Antipsychotic agent-2 (0.3-30 μM; 72 h) represents good safety profile and shows significant cytotoxic activity only at 30 μM concentration in SH-SY5Y cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Antipsychotic agent-2 (Compound 11; 20-80 mg/kg; i.p.; once) induces statistically significant changes in spontaneous locomotor activity in mice^[1].
Antipsychotic agent-2 (40 mg/kg; i.p.; once) decreases amphetamine-induced hyperactivity in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

395.47

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O=C(C1=NNC2=CC=CC=C21)NCCCCN3CCN(CC3)C4=CC=C(C=C4)F

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• [1]. Stępnicki P, et al. Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling. Eur J Med Chem. 2023 Apr 5;252:115285.  [Content Brief]