Tag: 200-300

HPLC of Formula: 84807-09-0On September 12, 2002 ,《Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1A Receptors》 was published in Journal of Medicinal Chemistry. The article was written by Orus, Lara; Perez-Silanes, Silvia; Oficialdegui, Ana-M.; Martinez-Esparza, Javier; Del Castillo, Juan-C.; Mourelle, Marisa; Langer, Thierry; Guccione, Salvatore; Donzella, Giuseppina; Krovat, Eva M.; Poptodorov, Konstantin; Lasheras, Berta; Ballaz, Santiago; Hervias, Isabel; Tordera, Rosa; Del Rio, Joaquin; Monge, Antonio. The article contains the following contents:

It has been proposed that 5-HT1A receptor antagonists augment the antidepressant efficacy of selective serotonin (5-HT) reuptake inhibitors. In a search toward new and efficient antidepressants, 1-(aryl)-3-[4-arylpiperazin-1-yl]-1-propane mol. hybrids were designed, synthesized, and evaluated for 5-HT reuptake inhibition and 5-HT1A receptor affinity. The design was based in coupling structural moieties related to inhibition of serotonin reuptake, such as benzo[b]thiophene derivatives to arylpiperazines, typical 5-HT1A receptor ligands. In binding studies, several compounds showed affinity at the 5-HT transporter and at 5-HT1A receptors. Mol. modeling studies predicted the pharmacophore elements required for high affinity binding and the features that enable to discriminate between agonist, partial agonist, or antagonist action at 5-HT1A receptors and 5-HT transporter inhibition. Solvent interactions in desolvation prior to the binding step along with enthalpy and entropy compensations might be responsible to explain agonist, partial agonist, and antagonist character. Hydrogen-bonding capability seems to be important to break hydrogen interhelical hydrogen bonds or alternatively to form other bonds upon ligand binding. Partial agonists and antagonists are unable to do this as the full agonist, which interacts closely by long-range forces or directly. The compounds showing the higher affinity at both the 5-HT transporter (Ki<50 nM) and the 5-HT1A receptors (Ki<20 nM) were further explored for their ability to stimulate [35S]GTPγS binding or to antagonize 8-hydroxy-2-di-n-propylamino-tetralin (8-OH-DPAT)-stimulated [35]GTPγS binding to rat hippocampal membranes, an index of agonist/antagonist action at 5-HT1A receptors, resp. Functional characterization was performed by measuring the antagonism to 8-OH-DPAT-induced hypothermia in mice. The experimental process involved the reaction of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0HPLC of Formula: 84807-09-0)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.HPLC of Formula: 84807-09-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Faigle, Johann W.; Blattner, Hans; Glatt, Hansruedi; Kriemler, Hans Peter; Mory, Hans; Storni, Angelo; Winkler, Tammo; Oesch, Franz published their research in Helvetica Chimica Acta on August 12 ,1987. The article was titled 《Structures and mutagenic properties of products obtained by C-nitrosation of opipramol》.Application of 3445-00-9 The article contains the following contents:

Reaction of the tricyclic psychotropic drug opipramol (I) with an excess of HNO2 gave a product mixture mutagenic to Salmonella typhimurium. The main product is a tetracyclic furoxan II (yield ca. 80%), resulting from nitrosation at C(10) and C(11) of I. II is not mutagenic. The essential mutagen is a nitroarene III, formed by contraction of the central ring of I and nitrosation at C(2). The yield of III is extremely low (<0.1%). Mutagenic nitroarenes have previously not been encountered as products from the interaction of drugs with nitrite. The results came from multiple reactions, including the reaction of 2-(4-(3-Chloropropyl)piperazin-1-yl)ethanol dihydrochloride(cas: 3445-00-9Application of 3445-00-9)

2-(4-(3-Chloropropyl)piperazin-1-yl)ethanol dihydrochloride(cas: 3445-00-9) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application of 3445-00-9

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Effects of selective dopaminergic compounds on a delay-discounting task》 was written by Koffarnus, Mikhail N.; Newman, Amy H.; Grundt, Peter; Rice, Kenner C.; Woods, James H.. Electric Literature of C17H19N5 And the article was included in Behavioural Pharmacology on August 31 ,2011. The article conveys some information:

Impulsivity is widely regarded as a multidimensional trait that encompasses two or more distinct patterns of behavior, and dopaminergic systems are implicated in the expression of impulsive behavior in both humans and animal subjects. Impulsive choice, or the tendency to choose rewards associated with relatively little or no delay, has been extensively studied in humans and animal subjects using delay-discounting tasks. Here, delay-discounting procedures were used to assess the effects of receptor-selective dopaminergic agonists, antagonists, and dopamine transporter ligands on choices of immediate vs. delayed sucrose pellets. The effects of d-amphetamine, GBR 12909, apomorphine, SKF 81297, sumanirole, pramipexole, ABT-724, SCH 23390, L-741,626, PG01037, and L-745,870 were assessed in 24 Sprague-Dawley rats. The only drugs to affect impulsive choice selectively without altering undelayed choice were the D1-like antagonist, SCH 23390 (0.01 mg/kg), and the D4 partial agonist, ABT-724 (3.2 mg/kg), which both increased impulsive choice. The shared effects of these compounds may be explained by their localization within the prefrontal cortex on different groups of neurons. None of the selective agonists and antagonists tested reduced impulsive choice, so further research is needed to determine if direct dopaminergic agonists or antagonists may be therapeutically useful in the treatment of impulse-control disorders. In the experiment, the researchers used many compounds, for example, Abt-724(cas: 70006-24-5Electric Literature of C17H19N5)

Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Electric Literature of C17H19N5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cowart, Marlon; Latshaw, Steven P.; Bhatia, Pramila; Daanen, Jerome F.; Rohde, Jeffrey; Nelson, Sherry L.; Patel, Meena; Kolasa, Teodozyi; Nakane, Masaki; Uchic, Marie E.; Miller, Loan N.; Terranova, Marc A.; Chang, Renjie; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Martino, Brenda R.; Lynch, James J. III; Sullivan, James P.; Hsieh, Gin C.; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O. published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a Dopaminergic Agent with a Novel Mode of Action for the Potential Treatment of Erectile Dysfunction》.Category: piperazines The author mentioned the following in the article:

A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 μmol/kg, with a pos. response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D4 selective agonism in this series of analogs. The experimental process involved the reaction of Abt-724(cas: 70006-24-5Category: piperazines)

Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Related Products of 85817-34-1On May 15, 2007 ,《Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2′-Substituted 6-nitroquipazines》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Lee, Jae Hak; Choi, Yong Hyun; Lim, Yoo Jin; Lee, Byoung Se; Chi, Dae Yoon; Jin, Changbae. The article conveys some information:

Five C2′-substituted 6-nitroquipazine (6-NQ) derivatives were prepared and evaluated in terms of their biol. abilities (Ki) to displace [3H]citalopram binding to serotonin transporter. The relationship between their structure and biol. activities revealed that shorter alkyl groups tend to possess higher binding affinity. Both compounds 12a (I, R1 = OH) and 12c (I, R1 = OEt) were found to have the equally highest binding affinity (Ki = 0.43 ± 0.02 nM). The results came from multiple reactions, including the reaction of (4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1Related Products of 85817-34-1)

(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Related Products of 85817-34-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Zhou, Dahui; Zhou, Ping; Evrard, Deborah A.; Meagher, Kristin; Webb, Michael; Harrison, Boyd L.; Huryn, Donna M.; Golembieski, Jeannette; Hornby, Geoffrey A.; Schechter, Lee E.; Smith, Deborah L.; Andree, Terrance H.; Mewshaw, Richard E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Studies toward the discovery of the next generation of antidepressants. Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives》.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT1A receptor antagonists. The investigation of the structure-activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study (I) exhibited equal binding affinities at 5-HT transporter (Ki = 4.9 nM), 5-HT1A receptor (Ki = 6.2 nM) and functioned as a 5-HT1A receptor antagonist. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Chubanov, V.; Schnitzler, M. Mederos; Meissner, M.; Schaefer, S.; Abstiens, K.; Hofmann, T.; Gudermann, T. published an article in British Journal of Pharmacology. The title of the article was 《Natural and synthetic modulators of SK (KCa2) potassium channels inhibit magnesium-dependent activity of the kinase-coupled cation channel TRPM7》.HPLC of Formula: 70006-24-5 The author mentioned the following in the article:

Background and Purpose Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a bifunctional protein comprising a TRP ion channel segment linked to an α-type protein kinase domain. TRPM7 is essential for proliferation and cell growth. Up-regulation of TRPM7 function is involved in anoxic neuronal death, cardiac fibrosis and tumor cell proliferation. The goal of this work was to identify non-toxic inhibitors of the TRPM7 channel and to assess the effect of blocking endogenous TRPM7 currents on the phenotype of living cells. Exptl. Approach We developed an aequorin bioluminescence-based assay of TRPM7 channel activity and performed a hypothesis-driven screen for inhibitors of the channel. The candidates identified were further assessed electrophysiol. and in cell biol. experiments Key Results TRPM7 currents were inhibited by modulators of small conductance Ca2+-activated K+ channels (KCa2.1-2.3; SK) channels, including the antimalarial plant alkaloid quinine, CyPPA, dequalinium, NS8593, SKA31 and UCL 1684. The most potent compound NS8593 (IC50 1.6 μM) specifically targeted TRPM7 as compared with other TRP channels, interfered with Mg2+-dependent regulation of TRPM7 channel and inhibited the motility of cultured cells. NS8593 exhibited full and reversible block of native TRPM7-like currents in HEK 293 cells, freshly isolated smooth muscle cells, primary podocytes and ventricular myocytes. Conclusions and Implications This study reveals a tight overlap in the pharmacol. profiles of TRPM7 and KCa2.1-2.3 channels. NS8593 acts as a neg. gating modulator of TRPM7 and is well-suited to study functional features and cellular roles of endogenous TRPM7. In the part of experimental materials, we found many familiar compounds, such as Abt-724(cas: 70006-24-5HPLC of Formula: 70006-24-5)

Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).HPLC of Formula: 70006-24-5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Zhao, Yujun; Aguilar, Angelo; Bernard, Denzil; Wang, Shaomeng published an article on February 12 ,2015. The article was titled 《Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment》, and you may find the article in Journal of Medicinal Chemistry.Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride The information in the text is summarized as follows:

A review. Design of small-mol. inhibitors (MDM2 inhibitors) to block the MDM2-p53 protein-protein interaction has been pursued as a new cancer therapeutic strategy. In recent years, potent, selective, and efficacious MDM2 inhibitors have been successfully obtained and seven such compounds have been advanced into early phase clin. trials for the treatment of human cancers. Here, we review the design, synthesis, properties, preclin., and clin. studies of these clin.-stage MDM2 inhibitors. In the part of experimental materials, we found many familiar compounds, such as 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride)

1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1) is a member of sulfones.The sulfones, like the sulfonamides, are structural analogs of para-aminobenzoic acid that interfere with folic acid metabolism by acting as competitive inhibitors of dihydropteroate synthetase. All sulfones of clinical value are derivatives of dapsone, the most widely used member of this class.Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Naylor, Alan; Judd, Duncan B.; Lloyd, Jane E.; Scopes, David I. C.; Hayes, Ann G.; Birch, Philip J. published an article in Journal of Medicinal Chemistry. The title of the article was 《A potent new class of κ-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines》.Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol The author mentioned the following in the article:

The synthesis of 4-substituted 1-(arylacetyl)-2-[(alkylamino)methyl]piperazines I [R = CO2Me, R1 = R2 = Me; R = CO2Me, R1R2 = CH2CH:CHCH2CH2; R = COR3, R1R2 = (CH2)4, R3 = H, Me, Et, Pr, CH2OMe, CH:CH2, Ph, PhCH2; R = CO2R4, R1R2 = (CH2)4, R4 = Me, Et, Pr, Ph, PhCH2] and II [X = CHOH, CO, C:CHCO2Me-(E), -(Z)] and their activities as κ-opioid receptor agonists are described. This includes a range of 4-acyl and 4-carboalkoxy derivatives with the latter series showing the greatest κ-agonist activity. In particular, Me 4-[3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate [I; R = CO2Me; R1R2 = (CH2)4] displays exceptional potency and selectivity. It showed the following activities in functional in vitro assays: rabbit vas deferens (κ-specific tissue) IC50 = 0.041 nM, rat vas deferens (μ-specific tissue) IC50 > 10 000 nM, and hamster vas deferens (δ-specific tissue) IC50 > 10 000 nM. Compound I [R = CO2Me; R1R2 = (CH2)4] is also a highly potent antinociceptive agent, as determined in the mouse acetylcholine-induced abdominal constriction test: ED50 = 0.000 52 mg/kg, s.c. The activity of I resides solely in its 3(R)-enantiomer. The κ-agonist activity in both the 4-acyl and the 4-carbamate series is sensitive to the size of the 4-substituent. In addition, it would appear that an appreciable neg. electrostatic potential in this region of the mol. is an important requirement for optimal potency.(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol) was used in this study.

(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning》 was written by Stewart, Andrew O.; Cowart, Marlon D.; Moreland, Robert B.; Latshaw, Steve P.; Matulenko, Mark A.; Bhatia, Pramila A.; Wang, Xueqing; Daanen, Jerome F.; Nelson, Sherry L.; Terranova, Marc A.; Namovic, Marian T.; Donnelly-Roberts, Diana L.; Miller, Loan N.; Nakane, Masaki; Sullivan, James P.; Brioni, Jorge D.. Category: piperazines And the article was included in Journal of Medicinal Chemistry on April 22 ,2004. The article conveys some information:

A series of subtype selective dopamine D4 receptor ligands from the heteroarylmethylphenylpiperazine class have been discovered that exhibit a remarkable structure-activity relation (SAR), revealing a substituent effect in which regiosubstitution on the terminal arylpiperazine ring can modulate functional or intrinsic activity. Other structure-dependent efficacy studies in the dopamine D4 field have suggested a critical interaction of the heteroarylmethyl moiety with specific protein microdomains in controlling intrinsic activity. The authors studies indicate that for some binding orientations, the phenylpiperazine moiety also plays a key role in determining efficacy. These data also implicate a kinetic or efficiency term, contained within measured functional affinities for agonists, which support a sequential binding and conformational stabilization model for receptor activation. The structural similarity between partial agonist and antagonist, within this subset of ligands, and lack of bioisosterism for this substituent effect are key phenomena for these hypotheses. In the experimental materials used by the author, we found Abt-724(cas: 70006-24-5Category: piperazines)

Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics