824958-22-7

Upstream product

• 101740-02-7 ethyl 4-[4-(2-methoxyphenyl)piperazin-1-yl]butanoate 
• 35386-24-4 1-(2-Methoxyphenyl)piperazine 

Downstream Products

• 1020000-79-6 C₃₀H₃₂FN₅O₃ 
• 1020000-98-9 C₃₀H₃₂FN₅O₃ 
• 1020001-04-0 C₃₁H₃₅N₅O₄ 
• 1020001-07-3 C₃₁H₃₄FN₅O₄ 
• 1020001-12-0 C₃₁H₃₄FN₅O₄ 
• 1020001-14-2 C₃₁H₃₅N₅O₄ 
• 1020001-17-5 C₃₁H₃₄FN₅O₄ 
• 1020001-09-5 C₃₁H₃₅N₅O₄ 
• 1020000-60-5 C₃₀H₃₃N₅O₃ 
• 1197155-08-0 4-(4-(2-Methoxyphenyl)piperazin-1-yl)-N-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)butanamide 

Relevant academic research and scientific papers

Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT1A/5-HT7 receptor antagonists and phosphodiesterase 4/7 inhibitors with procognitive and antidepressant activity

A library of novel anilide and benzylamide derivatives of ω-(4-(2-methoxyphenyl)piperazin-1-yl)alkanoic acids as combined 5-HT1A/5-HT7 receptor ligands and phosphodiesterase PDE4B/PDE7A inhibitors was designed using a structure-based drug design approach. The in vitro studies of 33 newly synthesized compounds (7-39) allowed us to identify 22 as the most promising multifunctional 5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with PDE4B/PDE7A inhibitory activity (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM). Compound 22 exerted a very good ability to passively penetrate through biological membranes and a high metabolic stability in vitro. Moreover, the pharmacological evaluation of 22 showed its procognitive and antidepressant properties in rat behavioral tests. Compound 22 at a dose of 3 mg/kg (i.p.) significantly reversed MK-801-induced episodic memory deficits in the novel object recognition test, while at a dose of 10 mg/kg (i.p.) reduced the immobility time of animals (by about 34percent) in the forced swimming test. The antidepressant-like effect produced by compound 22 was stronger than that of escitalopram used as a reference drug. This study opens a new perspective in the search for efficacious drugs for the treatment of cognitive and depressive disorders.

Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression

5-HT7 receptor (5-HT7R) is a promising target for the treatment of depression and neuropathic pain. 5-HT7R antagonists exhibited antidepressant effects, while the agonists produced strong anti-hyperalgesic effects. In our efforts to discover selective 5-HT 7R antagonists or agonists, N-biphenylylmethyl 2- methoxyphenylpiperazinylalkanamides 1 were designed, synthesized, and biologically evaluated against 5-HT7R. Among the synthesized compounds, N-2′-chlorobiphenylylmethyl 2- methoxyphenylpiperazinylpentanamide 1-8 showed the best binding affinity with a Ki value of 8.69 nM and it was verified as a novel antagonist according to functional assays. The compound 1-8 was very selective over 5-HT1DR, 5-HT2AR, 5-HT3R, 5-HT5AR and 5-HT6R and moderately selective over 5-HT1AR, 5-HT1BR and 5-HT2CR. The novel 5-HT7R antagonist 1-8 exhibited an antidepressant effect at a dose of 25 mg/kg in the forced swimming test in mice and showed a U-shaped dose-response curve which typically appears in 5-HT7R antagonists such as SB-269970 and lurasidone.

Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents

The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Novel quinazolinone derivatives as 5-HT7 receptor ligands

5-HT7 receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT7 receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highl

COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS

The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.

N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-phenyl-1-piperazinealkylamide derivatives, and therapeutic use thereof as 5-HT7 receptor ligands

A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was prepared and their affinity for serotonin 5-HT7, 5-HT1A, and 5-HT2A receptors was measured using in vitro binding assays. In relation to

Structure-affinity relationship study on n-(1,2,3,4-tetrahydronaphthalen-1- yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine 7 receptor agents

A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1- piperazinealkylamides was prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT7, 5-HT1A, and 5-HT 2A receptors was measured by in vitro bind