2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Antipsychotic agent-2

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability.

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Antipsychotic agent-2 Chemical Structure

Antipsychotic agent-2 Chemical Structure

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Antipsychotic agent-2 Related Antibodies

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Description

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability[1].

IC50 & Target

5-HT1A Receptor

160 nM (EC50)

5-HT2A Receptor

96.4 nM (Kb)

D2 Receptor

45.7 nM (Kb)

In Vitro

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 (Kb=45.7 nM)[1].
Antipsychotic agent-2 inhibits the Forskolin-stimulated cAMP production in HEK293 cells stably expressing 5-HT1A receptors in a concentration-dependent manner, indicative of 5-HT1A agonistic activity (EC50=160 nM), while it behaves as 5-HT2A antagonists, antagonizing the inositol phosphate production stimulated by 10-6 5-HT in CHO-K1 cells expressing 5-HT2A receptors (Kb=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 Related Antibodies
In Vivo

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.

Animal Model: Naive Swiss male mice, amphetamine-induced hyperactivity[1]
Dosage: 40 mg/kg
Administration: IP, once
Result: Decreased amphetamine-induced hyperactivity.
Molecular Weight

395.47

Formula

C22H26FN5O
SMILES

O=C(C1=NNC2=CC=CC=C21)NCCCCN3CCN(CC3)C4=CC=C(C=C4)F
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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Antipsychotic agent-2 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:

Antipsychotic agent-2Antipsychotic agent2Antipsychotic agent 25-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorCHO-K1CYP3A4ForskolincAMPHEK293spontaneous locomotor activityInhibitorinhibitorinhibit

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