A genus of nematodes of the superfamily ASCARIDOIDEA whose species usually inhabit the intestine.
An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.
Drugs designed and synthesized, often for illegal street use, by modification of existing drug structures (e.g., amphetamines). Of special interest are MPTP (a reverse ester of meperidine), MDA (3,4-methylenedioxyamphetamine), and MDMA (3,4-methylenedioxymethamphetamine). Many drugs act on the aminergic system, the physiologically active biogenic amines.
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Substances used in the treatment or control of nematode infestations. They are used also in veterinary practice.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
Xanthene dye used as a bacterial and biological stain. Synonyms: Pyronin; Pyronine G; Pyronine Y. Use also for Pyronine B. which is diethyl-rather than dimethylamino-.
A plant genus of the family RUBIACEAE. Members contain antimalarial (ANTIMALARIALS) and analgesic (ANALGESICS) indole alkaloids.
A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309)
A neuropsychiatric disorder characterized by one or more of the following essential features: immobility, mutism, negativism (active or passive refusal to follow commands), mannerisms, stereotypies, posturing, grimacing, excitement, echolalia, echopraxia, muscular rigidity, and stupor; sometimes punctuated by sudden violent outbursts, panic, or hallucinations. This condition may be associated with psychiatric illnesses (e.g., SCHIZOPHRENIA; MOOD DISORDERS) or organic disorders (NEUROLEPTIC MALIGNANT SYNDROME; ENCEPHALITIS, etc.). (From DSM-IV, 4th ed, 1994; APA, Thesaurus of Psychological Index Terms, 1994)
An N-substituted amphetamine analog. It is a widely abused drug classified as a hallucinogen and causes marked, long-lasting changes in brain serotonergic systems. It is commonly referred to as MDMA or ecstasy.
Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles within terminals. Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake.
A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.
Agents destructive to parasitic worms. They are used therapeutically in the treatment of HELMINTHIASIS in man and animal.
A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920)
A family of hexahydropyridines.
Infection by nematodes of the genus ASCARIS. Ingestion of infective eggs causes diarrhea and pneumonitis. Its distribution is more prevalent in areas of poor sanitation and where human feces are used for fertilizer.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
A vasodilator used in angina of effort or ischemic heart disease.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of dopaminergic neurons. They remove DOPAMINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS and are the target of DOPAMINE UPTAKE INHIBITORS.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Organic compounds that contain the -NCO radical.
A benzimidazole antifilarial agent; it is fluorescent when it binds to certain nucleotides in DNA, thus providing a tool for the study of DNA replication; it also interferes with mitosis.
An amphetamine derivative that inhibits uptake of catecholamine neurotransmitters. It is a hallucinogen. It is less toxic than its methylated derivative but in sufficient doses may still destroy serotonergic neurons and has been used for that purpose experimentally.
An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.
Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa.
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
Biogenic amines having only one amine moiety. Included in this group are all natural monoamines formed by the enzymatic decarboxylation of natural amino acids.
The relationship between the dose of an administered drug and the response of the organism to the drug.
The state of activity or tension of a muscle beyond that related to its physical properties, that is, its active resistance to stretch. In skeletal muscle, tonus is dependent upon efferent innervation. (Stedman, 25th ed)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
A specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
The physical activity of a human or an animal as a behavioral phenomenon.
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
The characteristic three-dimensional shape of a molecule.
The covalent bonding of an alkyl group to an organic compound. It can occur by a simple addition reaction or by substitution of another functional group.
The observable response an animal makes to any situation.
Chromatographic techniques in which the mobile phase is a liquid.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
Inorganic salts of HYDROGEN CYANIDE containing the -CN radical. The concept also includes isocyanides. It is distinguished from NITRILES, which denotes organic compounds containing the -CN radical.
Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.
A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.
A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
The most common inhibitory neurotransmitter in the central nervous system.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.
A mass spectrometry technique used for analysis of nonvolatile compounds such as proteins and macromolecules. The technique involves preparing electrically charged droplets from analyte molecules dissolved in solvent. The electrically charged droplets enter a vacuum chamber where the solvent is evaporated. Evaporation of solvent reduces the droplet size, thereby increasing the coulombic repulsion within the droplet. As the charged droplets get smaller, the excess charge within them causes them to disintegrate and release analyte molecules. The volatilized analyte molecules are then analyzed by mass spectrometry.
Contractile tissue that produces movement in animals.
Substances that reduce the growth or reproduction of BACTERIA.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
The giving of drugs, chemicals, or other substances by mouth.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

Activation of c-Abl tyrosine kinase requires caspase activation and is not involved in JNK/SAPK activation during apoptosis of human monocytic leukemia U937 cells. (1/7204)

Genotoxic stress triggers the activation of several sensor molecules, such as p53, JNK1/SAPK and c-Abl, and occasionally promotes the cells to apoptosis. We previously reported that JNK1/SAPK regulates genotoxic stress-induced apoptosis in p53-negative U937 cells by activating caspases. c-Abl is expected to act upstream of JNK1/SAPK activation upon treatment with genotoxic stressors, but its involvement in apoptosis development is still unclear. We herein investigated the kinase activities of c-Abl and JNK1/SAPK during apoptosis elicited by genotoxic anticancer drugs and tumor necrosis factor (TNF) in U937 cells and their apoptosis-resistant variant UK711 cells. We found that the activation of JNK1/SAPK and c-Abl correlated well with apoptosis development in these cell lines. Unexpectedly, however, the JNK1/SAPK activation preceded the c-Abl activation. Moreover, the caspase inhibitor Z-Asp suppressed c-Abl activation and the onset of apoptosis but not the JNK1/SAPK activation. Interestingly, c-Abl tyrosine kinase inhibition by CGP 57148 reduced apoptosis without interfering with JNK1/SAPK activation. These results indicate that c-Abl acts not upstream of JNK1/ SAPK but downstream of caspases during the development of p53-independent apoptosis and is possibly involved in accelerating execution of the cell death pathway.  (+info)

Plasticity of first-order sensory synapses: interactions between homosynaptic long-term potentiation and heterosynaptically evoked dopaminergic potentiation. (2/7204)

Persistent potentiations of the chemical and electrotonic components of the eighth nerve (NVIII) EPSP recorded in vivo in the goldfish reticulospinal neuron, the Mauthner cell, can be evoked by afferent tetanization or local dendritic application of an endogenous transmitter, dopamine (3-hydroxytyramine). These modifications are attributable to the activation of distinct intracellular kinase cascades. Although dopamine-evoked potentiation (DEP) is mediated by the cAMP-dependent protein kinase (PKA), tetanization most likely activates a Ca2+-dependent protein kinase via an increased intracellular Ca2+ concentration. We present evidence that the eighth nerve tetanus that induces LTP does not act by triggering dopamine release, because it is evoked in the presence of a broad spectrum of dopamine antagonists. To test for interactions between these pathways, we applied the potentiating paradigms sequentially. When dopamine was applied first, tetanization produced additional potentiation of the mixed synaptic response, but when the sequence was reversed, DEP was occluded, indicating that the synapses potentiated by the two procedures belong to the same or overlapping populations. Experiments were conducted to determine interactions between the underlying regulatory mechanisms and the level of their convergence. Inhibiting PKA does not impede tetanus-induced LTP, and chelating postsynaptic Ca2+ with BAPTA does not block DEP, indicating that the initial steps of the induction processes are independent. Pharmacological and voltage-clamp analyses indicate that the two pathways converge on functional AMPA/kainate receptors for the chemically mediated EPSP and gap junctions for the electrotonic component or at intermediaries common to both pathways. A cellular model incorporating these interactions is proposed on the basis of differential modulation of synaptic responses via receptor-protein phosphorylation.  (+info)

Low resting potential and postnatal upregulation of NMDA receptors may cause Cajal-Retzius cell death. (3/7204)

Using in situ patch-clamp techniques in rat telencephalic slices, we have followed resting potential (RP) properties and the functional expression of NMDA receptors in neocortical Cajal-Retzius (CR) cells from embryonic day 18 to postnatal day 13, the time around which these cells normally disappear. We find that throughout their lives CR cells have a relatively depolarized RP (approximately -50 mV), which can be made more hyperpolarized (approximately -70 mV) by stimulation of the Na/K pump with intracellular ATP. The NMDA receptors of CR cells are subjected to intense postnatal upregulation, but their similar properties (EC50, Hill number, sensitivity to antagonists, conductance, and kinetics) throughout development suggest that their subunit composition remains relatively homogeneous. The low RP of CR cells is within a range that allows for the relief of NMDA channels from Mg2+ blockade. Our findings are consistent with the hypothesis that CR cells may degenerate and die subsequent to uncontrolled overload of intracellular Ca2+ via NMDA receptor activation by ambient glutamate. In support of this hypothesis we have obtained evidence showing the protection of CR cells via in vivo blockade of NMDA receptors with dizocilpine.  (+info)

Ischemic tolerance in murine cortical cell culture: critical role for NMDA receptors. (4/7204)

Murine cortical cultures containing both neurons and glia (days in vitro 13-15) were exposed to periods of oxygen-glucose deprivation (5-30 min) too brief to induce neuronal death. Cultures "preconditioned" by sublethal oxygen-glucose deprivation exhibited 30-50% less neuronal death than controls when exposed to a 45-55 min period of oxygen-glucose deprivation 24 hr later. This preconditioning-induced neuroprotection was specific in that neuronal death induced by exposure to excitotoxins or to staurosporine was not attenuated. Neuroprotection was lost if the time between the preconditioning and severe insult were decreased to 7 hr or increased to 72 hr and was blocked if the NMDA antagonist 100 microM 3-((D)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid was applied during the preconditioning insult. This was true even if the duration of preconditioning was increased as far as possible (while still remaining sublethal). A similar preconditioning effect was also produced by sublethal exposure to high K+, glutamate, or NMDA but not to kainate or trans-1-aminocyclopentane-1, 3-dicarboxylic acid.  (+info)

Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat-1 fibroblasts stably expressing alpha1d-adrenoceptors. (5/7204)

In rat-1 fibroblasts stably expressing alpha1d-adrenoceptors BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil decreased basal [Ca2+]i. WB 4101 induced a very small effect on this parameter but when added before the other antagonists it blocked their effect. All these agents inhibited the action of norepinephrine. Phorbol myristate acetate also blocked the effect of norepinephrine and decreased basal [Ca2+]i. Staurosporine inhibited these effects of the phorbol ester. Our results suggest that: (1) alpha1d-adrenoceptors exhibit spontaneous ligand-independent activity, (2) BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil act as inverse agonists and (3) protein kinase C activation blocks spontaneous and agonist-stimulated alpha1d-adrenoceptor activity.  (+info)

Acquisition of nicotine discrimination and discriminative stimulus effects of nicotine in rats chronically exposed to caffeine. (6/7204)

Caffeine and nicotine are the main psychoactive ingredients of coffee and tobacco, with a high frequency of concurrent use in humans. This study examined the effects of chronic caffeine exposure on 1) rates of acquisition of a nicotine discrimination (0.1 or 0.4 mg/kg, s.c., training doses) and 2) the pharmacological characteristics of the established nicotine discrimination in male Sprague-Dawley rats. Once rats learned to lever-press reliably under a fixed ratio of 10 schedule for food pellets, they were randomly divided into two groups; 12 animals were maintained continuously on caffeine added to the drinking water (3 mg/ml) and another 12 control rats continued to drink tap water. In each group of water- and caffeine-drinking rats, there were six rats trained to discriminate 0.1 mg/kg of nicotine from saline and six rats trained to discriminate 0.4 mg/kg of nicotine from saline. Regardless of the training dose of nicotine, both water- and caffeine-drinking groups required a comparable number of training sessions to attain reliable stimulus control, although there was a trend for a slower acquisition in the caffeine-drinking group trained with 0.1 mg/kg of nicotine. Tests for generalization to different doses of nicotine revealed no significant differences in potency of nicotine between water- and caffeine-drinking groups. The nicotinic-receptor antagonist mecamylamine blocked the discriminative effects of 0.1 and 0.4 mg/kg nicotine with comparable potency and efficacy in water- and caffeine-drinking groups. There was a dose-related generalization to both the 0.1 and 0.4 mg/kg nicotine cue (maximum average of 51-83%) in water-drinking rats after i.p. treatment with d-amphetamine, cocaine, the selective dopamine uptake inhibitor GBR-12909, apomorphine, and the selective dopamine D1 receptor agonist SKF-82958, but not in caffeine-drinking rats (0-22%). There was no generalization to the nicotine cues after i.p. treatment with caffeine or the selective D2 (NPA) and D3 (PD 128,907) dopamine-receptor agonists in water- and caffeine-drinking rats. The dopamine-release inhibitor CGS 10746B reduced the discriminative effects of 0.4 mg/kg nicotine in water-drinking rats, but not in caffeine-drinking rats. There was no evidence of development of tolerance or sensitization to nicotine's effects throughout the study. In conclusion, chronic caffeine exposure (average, 135 mg/kg/day) did not affect the rate of acquisition of the nicotine discrimination, but it did reduce the dopaminergic component of the nicotine-discriminative cue. The reduction of the dopaminergic component of the nicotine cue was permanent, as this effect was still evident after the caffeine solution was replaced with water in caffeine-drinking rats. That nicotine could reliably serve as a discriminative stimulus in the absence of the dopaminergic component of its discriminative cue may differentiate nicotine from "classical dopaminergic" drugs of abuse such as cocaine and amphetamine.  (+info)

Selective antiaggressive effects of alnespirone in resident-intruder test are mediated via 5-hydroxytryptamine1A receptors: A comparative pharmacological study with 8-hydroxy-2-dipropylaminotetralin, ipsapirone, buspirone, eltoprazine, and WAY-100635. (7/7204)

The present study characterized the effects of the novel, selective, and potent 5-hydroxytryptamine1A (serotonin) (5-HT1A) receptor agonist, alnespirone [S-20499, (S)-N-4-[5-methoxychroman-3-yl)propylamino)butyl- 8-azaspiro-(4,5)-diacetamide, hydrochloride] on offensive and defensive resident-intruder aggression in wild-type rats and compared its actions with those of the prototypical full 5-HT1A agonist 8-hydroxy-2- dipropylaminotetralin (8-OH-DPAT), the partial 5-HT1A agonists ipsapirone and buspirone, and the mixed 5-HT1A/1B agonist eltoprazine. All five agonists exerted effective dose-dependent decreases of offensive aggressive behavior in resident rats; 8-OH-DPAT was the most potent (ID50 = 0.074 mg/kg), followed by eltoprazine (0.24), buspirone (0.72), ipsapirone (1.08), and alnespirone (1.24). However, in terms of selectivity of the antiaggressive effects as determined by the absence of decrements in social interest and general motor activity, alnespirone appeared to be superior. In the defensive aggression test, neither alnespirone nor any of the other four agonists changed defensive behaviors in the intruder rats. The involvement of 5-HT1A receptors in the antiaggressive actions of these drugs was confirmed by showing that the selective 5-HT1A receptor antagonist WAY-100635 (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2- pyridinyl)cyclohexanecarboxamide trihydrochloride), which was inactive alone, fully prevented the antiaggressive effects of alnespirone, 8-OH-DPAT, and buspirone and partly reversed those of ipsapirone and eltoprazine. The data clearly indicate that alnespirone effectively suppresses offensive aggression with an advantageous profile of action compared with other full or partial 5-HT1A agonists. These selective antiaggressive actions of alnespirone are mediated by stimulating 5-HT1A receptors, presumably the somatodendritic autoreceptors at the raphe nuclei. Furthermore, the data provide evidence for a major involvement of these 5-HT1A receptors in the modulation of aggressive behavior by 8-OH-DPAT, ipsapirone, buspirone, and eltoprazine.  (+info)

Inhibition of human immunodeficiency virus type 1 replication by combination of transcription inhibitor K-12 and other antiretroviral agents in acutely and chronically infected cells. (8/7204)

8-Difluoromethoxy-1-ethyl-6-fluoro-1,4-dihydro-7-[4-(2-methoxyp hen yl)-1- piperazinyl]-4-oxoquinoline-3-carboxylic acid (K-12) has recently been identified as a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) transcription. In this study, we examined several combinations of K-12 and other antiretroviral agents for their inhibitory effects on HIV-1 replication in acutely and chronically infected cell cultures. Combinations of K-12 and a reverse transcriptase (RT) inhibitor, either zidovudine, lamivudine, or nevirapine, synergistically inhibited HIV-1 replication in acutely infected MT-4 cells. The combination of K-12 and the protease inhibitor nelfinavir (NFV) also synergistically inhibited HIV-1, whereas the synergism of this combination was weaker than that of the combinations with the RT inhibitors. K-12 did not enhance the cytotoxicities of RT and protease inhibitors. Synergism of the combinations was also observed in acutely infected peripheral blood mononuclear cells. The combination of K-12 and cepharanthine, a nuclear factor kappa B inhibitor, synergistically inhibited HIV-1 production in tumor necrosis factor alpha-stimulated U1 cells, a promonocytic cell line chronically infected with the virus. In contrast, additive inhibition was observed for the combination of K-12 and NFV. These results indicate that the combinations of K-12 and clinically available antiretroviral agents may have potential as chemotherapeutic modalities for the treatment of HIV-1 infection.  (+info)

en] HIV-1 infection of the brain and PAF neurotoxicity are implicated in AIDS dementia complex. We previously reported that a trisubstituted piperazine derivative is able to diminish both HIV-1 replication in monocyte-derived macrophages and PAF-induced platelet aggregation. We report in this work new compounds obtained by modifying its piperazine substituents. The structure-activity relationship study shows that a better dual activity or even pure antiretroviral compounds can be obtained in this series. (c) 2006 Elsevier Ltd. All rights reserved ...
Manufacturer and Exporter of Iodine & Derivatives, Bulk Drugs and Piperazine Derivatives offered by Adani Pharmachem Private Limited, Rajkot, Gujarat, India.
Export Data And Price Of Piperazine Dihydrochloride , www.eximpulse.com Eximpulse Services is the place where you can find the recent and updated Trade intelligence report of Piperazine Dihydrochloride Export Data. Whole information is based on updated Export shipment data of Indian Customs. All the compilation is done on the basis of All India ports data and has been done on daily basis. This helps you to get all India Piperazine Dihydrochloride Export data. You can find previous two days Piperazine Dihydrochloride Export data on Eximpulse Services. Piperazine Dihydrochloride Export data can be useful in different kind of analysis such as: Export price, Quantity, market scenarios, Price trends, Duty optimization and many more. Some Sample Shipment records for Piperazine Dihydrochloride Export Data of India are mentioned above. Further for Free sample and pricing of detailed reports contact on [email protected] Data post 2012 as per Notification No.18/2012 - Customs(N.T.) and does not have ...
TY - JOUR. T1 - Physical properties of aqueous blends of sodium glycinate (SG) and piperazine (PZ) as a solvent for CO2 capture. AU - Shaikh, M. S.. AU - Shariff, A. M.. AU - Bustam, M. A.. AU - Murshid, Ghulam. PY - 2013/3/14. Y1 - 2013/3/14. N2 - The physical properties including the density, viscosity, and refractive index of aqueous blends of sodium glycinate (SG) and piperazine (PZ) as a solvent for CO2 absorption were measured under the wide temperature range (298.15 to 343.15) K. Different concentrations (mole fraction) of sodium glycinate and piperazine (SG + PZ) blends were (0.0348/0.0089, 0.0263/0.0177, 0.0177/0.0263, and 0.0089/0.0348), respectively. From the observations, it was found that the densities of the aqueous blends decrease when the piperazine concentration in the blend increases. It was noticed that the viscosity of the blend decreases initially by increasing the concentration of piperazine from 0.0089 to 0.0177 mole fraction; however, on further increasing the piperazine ...
We,China N-Methyl piperazine 109-01-3 Suppliers and China N-Methyl piperazine 109-01-3 Manufacturers, provide N-Methyl piperazine 109-01-3 product and the products related with China N-Methyl piperazine 109-01-3 - hzoceanchem
We,China N-Cyclopentyl piperazine Suppliers and China N-Cyclopentyl piperazine Manufacturers, provide N-Cyclopentyl piperazine product and the products related with China N-Cyclopentyl piperazine
SIDDHARTH INTERCHEM PVT. LTD. - Manufacturer and supplier of piperazine dihydrochloride, itraconazole intermediates, 1-(4-methoxy phenyl) piperazine, 1-(4-methoxy phenyl) 4-(4-nitro phenyl) piperazine, 1-(4-amino phenly) 4-(4-methoxy phenyl) piperazine, intermediates, veratraldehyde, chlorhexidine base, bulk drugs, India.
In the scope of a research program aimed at developing new drugs for the treatment of central nervous system diseases, we describe herein the synthesis and pharmacological evaluation of 1-(4-(3,5-di-...
Looking for piperazine dihydrochloride? Find out information about piperazine dihydrochloride. C4H10N2·2HCl White, water-soluble needles; used for insecticides and pharmaceuticals Explanation of piperazine dihydrochloride
Application Notes: Piperazine is an organic hydrophilic basic compound containing two secondary amines. It is not retained on traditional reversed-phase columns without ion pairing reagent. Since piperazine is not UV active, alternative detection techniques like ELSD, CAD and LC/MS must be employed. Two fast methods of analysis on Primesep 100 and 200 columns were developed using reversed-phase cation-exchange approach. Primesep 200 column is more suitable for analysis since piperazine interacts strongly with stationary phase and since Primesep 200 columns are weaker columns. Methods can be used for analysis of piperazine and other basic hydrophilic compounds in reaction mixtures, formulations, biofluids, waste waters, etc. This Method is compatible with ELSD, CAD and LC/MS. ...
Find manufacturers and suppliers for 1-(1-Methyl-butyl)-piperazine, 82499-96-5. Synonyms: 1-(2-Pentyl)-piperazine; 1-(1-methylbutyl)piperazine; piperazine, 1-(1-methylbutyl)-
N-[4-(4-Methylpiperazin-1-yl)phenyl]-7-pyridin-3-ylpyrrolo[2,3-d]pyrimidin-2-amine | C22H23N7 | CID 23646631 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
As a part of our ongoing research to develop novel and selective 5-HT6 receptor antagonists, a new series of 2-(4- methylpiperazin-1-yl methyl)-1-(ary..
72050-77-2 - MGRUNNGBZNIOKF-UHFFFAOYSA-N - 2,4,6-Cycloheptatriene-1-acetic acid, 3-(4-methylpiperazin-1-yl)propyl ester, hydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Learn more about 1e-2-2-dimethyl-3-4-methylpiperazin-1-yl-propanal-oxime. We enable science by offering product choice, services, process excellence and our people make it happen.
1-(4-Methoxyphenyl)piperazine 38212-30-5 route of synthesis, 1-(4-Methoxyphenyl)piperazine chemical synthesis methods, 1-(4-Methoxyphenyl)piperazine synthetic routes ect.
Alfa Aesar™ 4-Boc-1-(5-bromo-2-pyridyl)piperazine, 97% 25g Alfa Aesar™ 4-Boc-1-(5-bromo-2-pyridyl)piperazine, 97% Bistriphenyl to Boch -Organics
Alfa Aesar™ 4-Boc-1-(6-bromo-2-pyridyl)piperazine, 97% 1g Alfa Aesar™ 4-Boc-1-(6-bromo-2-pyridyl)piperazine, 97% Bistriphenyl to Boch -Organics
Alfa Aesar™ 1-(Cyclopropylcarbonyl)piperazine hydrochloride, 97% 1g Alfa Aesar™ 1-(Cyclopropylcarbonyl)piperazine hydrochloride, 97% Cyclopente...
Piperazine - Get up-to-date information on Piperazine side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Piperazine
Alfa Aesar™ 1-(2-Chloro-4-nitrophenyl)piperazine, 97% 1g Alfa Aesar™ 1-(2-Chloro-4-nitrophenyl)piperazine, 97% Chloronitrod to Chlorophenyla...
1-(2-N-Boc-Aminoethyl)Piperazine 140447-78-5 MSDS report, 1-(2-N-Boc-Aminoethyl)Piperazine MSDS safety technical specifications search, 1-(2-N-Boc-Aminoethyl)Piperazine safety information specifications ect.
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 846031-61-6(Piperazine, 1-(2-chloro-3-methoxyphenyl)-),please inquire us for 846031-61-6(Piperazine, 1-(2-chloro-3-methoxyphenyl)-).
You are viewing an interactive 3D depiction of the molecule 1-(2-(bis(4-fluorophenyl)methoxy)ethyl)-4-(2-(4-azido-3-iodophenyl)ethyl)piperazine (C27H29F2IN5O) from the PQR.
Read about the chemical and physical properties of 1-(4-tert-butylphenylsulfonyl)-4-(4-fluorophenyl)piperazine. Get 1-(4-tert-butylphenylsulfonyl)-4-(4-fluorophenyl)piperazine molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 1013-27-0(Piperazine,1-(2,5-dichlorophenyl)-),please inquire us for 1013-27-0(Piperazine,1-(2,5-dichlorophenyl)-).
Boc Sciences is the worlds leading provider for special chemicals. We offer qualified products for 163837-56-7(1-[(4-CHLOROPHENYL)(PHENYL)METHYL]-4-[(4-METHYLPHENYL)SULFONYL]PIPERAZINE),please inquire us for 163837-56-7(1-[(4-CHLOROPHENYL)(PHENYL)METHYL]-4-[(4-METHYLPHENYL)SULFONYL]PIPERAZINE).
KAIVAL CHEMICALS PVT. LTD. - Exporter, Manufacturer & Supplier of 1-(2,3-Dichloro Phenyl) Piperazine Hydrochloride based in Padra, India
Piperazine is an amine which is used both as an activator or promoter, but also as active component in CO2 capture solvents. High concentrations are being formulated to draw benefit of the PZ properties. This results in a risk of precipitation of PZ and other solid phases during capture. It could be a benefit to the capture process, but it could also result in unforeseen situations of potential hazardous operation, clogging, equipment failure etc.Security of the PZ process needs to be in focus. Flow assurance requires additional attention, especially due to the precipitation phenomenon. This entails all parts of the streams, but also during formulation and transport of the solvent.In this work the extended UNIQUAC thermodynamic model is presented with the addition of piperazine (PZ or PIPH2) in combination with the potassium ion of mixtures with CO2 in equilibration with KOH-KHCO3-K2CO3. Phase boundaries are laid out which shows the concentration regions of solid formation. A special focus will ...
1-(1-Methyl-4-piperidinyl)piperazine, 98%, ACROS Organics 1g; Glass bottle Chemicals:Organic Compounds:Organoheterocyclic compounds:Diazinanes:Piperazines:N-alkylpiperazines
Spectrophotometric method for determination of Cu(II) in the trace quantities was developed by using piperazine as ligand in ammonium acetate medium. The Procedure developed was applied for the estimation Cu(II) in microgram quantities in the samples of alloys and the method was found to be simple, rapid and comparable to routine analytical methods for trace level analysis of metal ions in environmental samples in any laboratory where sophisticated and expensive instruments are not available. UV visible spectrophotometer is cost effective and available in almost all laboratories. The complexes of piperazine in aqueous solutions are not reported so far and this is the first attempt in this area of spectrophotometric analysis.
SHREEJI PHARMA from Gujarat, India is a manufacturer, supplier, wholesaler and exporter of Piperazine Phosphate at reasonable price.
Piperazines are a group of chemicals that were once legal alternatives to ecstasy as they mimic its effects. Get the facts and ask FRANK anything you want to know.
SHREEJI PHARMA from Gujarat, India is a manufacturer, supplier, wholesaler and exporter of Acephylline Piperazine at reasonable price.
Finally theres a reagent that can detect phenylpiperazines such as mCPP and TfMPP: EZ Test mCPP.. A global shortage of the major precursor that is used for the production of MDMA, PMK or MDP2P, made unscrupulous producers look for other substances that could be sold.. They flooded the market with pills that were made with this stuff. MCPP and other piperazines have nothing to do with Ecstasy, nor do these substances have any of the effects that makes Ecstasy so special. Luckily theres a possibility to weed these nasty buggers out!. As a bonus this test kit also reacts to 6-APB, which goes burgundy red. Although the samples that were used for this could not be verified by lab, due to a lack of a standard reference sample, they came from a very reputable source. Thats why we included it in the results, but as unverified…. note: sometimes we get the complaint that the test doesnt work. NOT CORRECT! Below is a picture that tells you what color to look for (mind you, this is not indicative ...
(R)-CPP, CAS: 126453-07-4, is A piperazine derivative demonstrating highly potent NMDA receptor antagonism. Cited in 2 publications
2C-B-BZP produces stimulant effects that last 3-6 hours, depending on the dose. Despite its structural similarity to 2C-B it does not produce psychedelic effects as the binding groups are in the wrong position to activate the 5HT2A receptor. 2C-B-BZP is also said by several sources to increase the effects of other compounds when combined. Side effects include headaches and nausea, similar to other piperazine derivatives used recreationally. ...
Ziprasidone Mesylate with NDC 72266-160 is a a human prescription drug product labeled by Fosun Pharma Usa Inc.. The generic name of Ziprasidone Mesylate is ziprasidone mesylate.
1-(4-Methoxyphenyl)-4-[4-(5-propyl-1,2,4-triazol-1-yl)phenyl]piperazine | C22H27N5O | CID 12877036 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
TY - JOUR. T1 - Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl) piperazine derivatives as T-type calcium channel blockers. AU - Park, Jung Eun. AU - Ji, Wan Keun. AU - Jang, Jae Wan. AU - Pae, Ae Nim. AU - Choi, Keehyun. AU - Choi, Kihang. AU - Kang, Jahyo. AU - Roh, Eun Joo. PY - 2013/3/15. Y1 - 2013/3/15. N2 - To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 2-hydroxy-3-phenoxypropyl piperazine derivatives were synthesized and evaluated for in vitro activities. Compound 6m and 6q showed high selectivity over hERG channel (IC50 ratio of hERG/α1G 6m = 8.5, 6q = 18.38) and they were subjected to measure pharmacokinetics profiles. Among them compound 6m showed an excellent pharmacokinetic profile in rats.. AB - To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 2-hydroxy-3-phenoxypropyl piperazine derivatives were synthesized and evaluated for in vitro activities. Compound 6m and ...
We, China 2-(4-Methylpiperazin-1-yl)pyridine-5-boronic acid pinacol ester Manufacturers, China 2-(4-Methylpiperazin-1-yl)pyridine-5-boronic acid pinacol ester Suppliers, provide quality 2-(4-Methylpiperazin-1-yl)pyridine-5-boronic acid pinacol ester product and the products related with China 2-(4-Methylpiperazin-1-yl)pyridine-5-boronic acid pinacol ester - bjpurechem
TY - JOUR. T1 - Favorable long-term follow-up results over 6 years for response, survival, and safety with imatinib mesylate therapy in chronic-phase chronic myeloid leukemia after failure of interferon-α treatment. AU - Hochhaus, Andreas. AU - Druker, Brian. AU - Sawyers, Charles. AU - Guilhot, Francois. AU - Schiffer, Charles A.. AU - Cortes, Jorge. AU - Niederwieser, Dietger W.. AU - Gambacorti, Carlo. AU - Stone, Richard M.. AU - Goldman, John. AU - Fischer, Thomas. AU - OBrien, Stephen G.. AU - Reiffers, Jose J.. AU - Mone, Manisha. AU - Krahnke, Tillmann. AU - Talpaz, Moshe. AU - Kantarjian, Hagop M.. PY - 2008. Y1 - 2008. N2 - Imatinib mesylate, a targeted inhibitor of BCR-ABL tyrosine kinase, is the standard of care for chronic myeloid leukemia (CML). A phase 2 trial of imatinib in late chronic-phase (CP) CML after interferon-α (IFNα) failure enrolled 532 patients, 454 with a confirmed diagnosis of CP CML. Median time from diagnosis was 34 months; median duration of imatinib ...
A temperature-programmed packed capillary LC method with large-volume injection on-column focusing has been developed for screening and determination of 1-(2-methoxyphenyl)piperazine derivatives of airborne toluene-2,4-diisocyanate, toluene-2,6-diisocyanate, hexamethylenediisocyanate and methylenebisphenyl-4,4-diisocyanate, based on sampling methods described in MDHS 25/3. Injection volumes up to 100 microl were successfully loaded onto the 250x0.32 mm I.D. capillary column packed with 3 microm Hypersil ODS particles. The isocyanate derivatives were loaded at 10 degrees C and eluted by a three-step temperature program starting at 10 degrees C for 10 min, followed by a temperature ramp of 2.5 degrees C min(-1) to 45 degrees C and then 9.9 degrees C min(-1) to 90 degrees C. The mobile phase consisted of acetonitrile-acetate buffer (3% triethylamine, pH 4.5) (45:55, v/v). The isocyanate derivatives were dissolved in acetonitrile-acetate buffer (3% triethylamine, pH 4.5) (30:70, v/v) to achieve sufficient
TY - JOUR. T1 - Recent advances in Philadelphia chromosome-positive malignancies. T2 - the potential role of arsenic trioxide.. AU - ODwyer, Michael E.. AU - La Rosée, Paul. AU - Nimmanapalli, Ramedivi. AU - Bhalla, Kapil N.. AU - Druker, Brian. PY - 2002/4. Y1 - 2002/4. N2 - Chronic myelogenous leukemia (CML) is characterized by the presence of the Bcr-Abl fusion gene, which encodes a constitutively active tyrosine kinase that has been strongly implicated as the sole oncogenic abnormality in early-stage CML. Treatment with the specific tyrosine kinase inhibitor imatinib mesylate has achieved excellent results in CML, at all stages of the disease. However, limitations to the successful use of imatinib mesylate as a single agent include the problem of resistance, seen chiefly in patients with advanced-phase disease. This review summarizes the clinical results to date with imatinib mesylate and briefly discusses the problem of resistance before describing potential strategies, including the use ...
OUTLINE: This is a multicenter, dose-escalation study of imatinib mesylate and cytarabine.. Patients receive oral imatinib mesylate alone once daily on days 1-21. Patients then receive oral imatinib mesylate once daily and cytarabine IV over 1-3 hours on days 1-7. Combination therapy repeats every 28-42 days for 2 courses. Patients then receive maintenance oral imatinib mesylate once daily. Treatment continues in the absence of disease progression or unacceptable toxicity.. Cohorts of 5-20 patients receive escalating doses of imatinib mesylate and cytarabine until the maximum tolerated dose (MTD) is determined. The MTD is defined as the dose preceding that at which at least 5/5, 5/10, or 5/20 patients experience dose-limiting toxicity.. Patients are followed every 6 months.. PROJECTED ACCRUAL: A total of 30-60 patients will be accrued for this study within 2 years. ...
Novartis (es); Novartis (hu); Novartis (eu); Novartis (ms); Novartis (de-ch); Novartis (de); Novartis (en-gb); Новартис (sr-ec); Новартис (bg); Novartis (da); Novartis (ro); ノバルティス (ja); Novartis (sv); נוברטיס (he); 諾華公司 (zh-hant); Novartis (gsw); 노바티스 (ko); Новартис (kk); Novartis (en-ca); Novartis (cs); நோவார்ட்டீசு (ta); Novartis (it); Novartis (fr); Novartis (tr); 诺华公司 (zh-hans); Novartis (sr-el); Novartis (en); Novartis (pt); Novartis (vi); Novartis (ru); نوارتیس (fa); โนวาร์ติส (th); Новартис (sr); Novartis (nl); 诺华公司 (zh); Novartis (pt-br); Novartis (pl); Novartis (id); Novartis (nn); Novartis (nb); Novartis (sh); Novartis (fi); 諾華公司 (zh-hk); ნოვარტისი (ka); Novartis (uk); Novartis (gl); نوفارتس (ar); Novartis (el); Novartis (ca) Empresa farmacéutica multinacional (es); スイスの製薬・バイオテクノロジー企業 ...
Fingerprint Dive into the research topics of Multicenter Phase II trial assessing effectiveness of imatinib mesylate on relapsed or refractory KIT-positive or PDGFR-positive sarcoma. Together they form a unique fingerprint. ...
The t(9;22) translocation is seen in cases of chronic myeloid leukemia (CML), a subset of acute lymphocytic leukemia (ALL) and rarely in acute myeloid leukemia (AML). The resulting BCR-ABL fusion gene is transcribed and translated into a 210 kD (p210, major transcript) or 190 kD (p190, minor transcript) BCR-ABL fusion product with dysregulated (significantly enhanced) tyrosine kinase activity. Detection of the BCR/ABL1 fusion gene transcript is a critical determinant in diagnosis. The BCR/ABL1 fusion gene product is the cause of disease and growth of leukemic cells and expression levels of the transcript are directly related to disease severity. The use of new drugs for treatment such as the tyrosine kinase inhibitor imatinib mesylate (Gleevec) reduces the amount of leukemic cells below the level of cytogenetic detection and therefore makes molecular determination in the detection of minimal residual disease desirable. A consensus treatment goal is the achievement of major molecular response, ...
In the presence of imatinib mesylate, both age groups displayed little change in spontaneous slow-wave activity with the exception of the highest concentration (Fig. 2ii). A major difference between the two age groups occurred in the amplitude of contractile activity at all concentrations of imatinib mesylate. In the ageing guinea-pig prostate, a concentration-dependent inhibition was seen where low concentrations of imatinib mesylate produced the most inhibition whereas high concentrations produced less inhibition of contractile activity.. In contrast, contractile amplitude was generally reduced to 26-40% across all concentrations in the younger guinea-pig prostate. This difference between age groups may parallel the reduction in pacemaker potential activity and increase in spike potential activity with age, which was previously observed by Dey et al. [14]. Like the guinea-pig bladder [16], the guinea-pig prostate generates nifedipine-sensitive spike potentials, as well as slow-wave activity. ...
Latest news - Imatinib Mesylate, Photos - Imatinib Mesylate, Videos - Imatinib Mesylate. Imatinib Mesylate updates on Rediff News
BACKROUND: The selective tyrosine kinase inhibitor imatinib inhibits growth of bcr/abl positive cells and, thus, has become a novel therapeutic option for the treatment of Ph+ leukaemic patients. Various mutations within the abl sequence have been described that prevent adequate imatinib binding to bcr/abl resulting in cellular resistance of CML cells. METHODS: We investigated 69 CML patients under treatment with imatinib as part of an ongoing clinical trial. At recruitment 37 patients were in chronic phase, 21 patients in accelerated phase and 11 patients in blast crisis. Bcr/abl, WT1, MDR1and AGP RNA transcripts were quantified in peripheral leucocytes by real time PCR. AGP protein levels in plasma were measured by turbidimetric analysis. By combining peptide nucleic acid (PNA) based DNA clamping with a fluorescence hybridisation probe assay we developed a new and highly sensitive technique for the detection of known mutations within the bcr/abl kinase domain. RESULTS: 1. Our results ...
The clinical success of the ABL tyrosine kinase inhibitor imatinib in chronic myeloid leukaemia (CML) serves as a model for molecularly targeted therapy of cancer, but at least two critical questions remain. Can imatinib eradicate leukaemic stem cells? What are the dynamics of relapse due to imatinib resistance, which is caused by mutations in the ABL kinase domain? The precise understanding of how imatinib exerts its therapeutic effect in CML and the ability to measure disease burden by quantitative polymerase chain reaction provide an opportunity to develop a mathematical approach. We find that a four-compartment model, based on the known biology of haematopoietic differentiation, can explain the kinetics of the molecular response to imatinib in a 169-patient data set. Successful therapy leads to a biphasic exponential decline of leukaemic cells. The first slope of 0.05 per day represents the turnover rate of differentiated leukaemic cells, while the second slope of 0.008 per day represents ...
Imatinib (STI571 or Gleevec) is a small-molecule inhibitor of the BCR-ABL tyrosine kinase that produces clinical remissions in chronic myeloid leukemia (CML) patients with minimal toxicity (1, 2). Imatinib is now frontline therapy for CML, but resistance is increasingly encountered. Clinical resistance is primarily mediated by mutations within the kinase domain of BCR-ABL and, to a lesser extent, by amplification of the BCR-ABL genomic locus (3). Crystallographic studies revealed that imatinib binds to the adenosine triphosphate (ATP)-binding site of ABL only when the activation loop of the kinase is closed and thus stabilizes the protein in this inactive conformation (4). In addition, the normally smooth contour of the phosphate-binding loop of ABL is distorted by imatinib binding, adding further to the unique conformational requirements for optimal kinase inhibition. These conformation-specific binding requirements contribute to imatinibs selectivity, particularly with regard to the closely ...
Business Directory for Piperazine Adipate Suppliers in Rajkot - Get contact details of Piperazine Adipate Manufacturers, Wholesale Piperazine Adipate Exporters, Best Piperazine Adipate Traders & Distributors Across the Rajkot.
Drugs used in chemotherapy use different ways to stop cancer cells from dividing so they stop growing or die. Imatinib mesylate may stop the growth of cancer cells by blocking the enzymes necessary for cancer cell growth. Combining more than one chemotherapy drug with imatinib mesylate may kill more cancer cells. Randomized phase II trial to study the effectiveness of combination chemotherapy and imatinib mesylate in treating children who have relapsed acute lymphoblastic leukemia ...
Abstract. Imatinib has become the treatment of choice for most with CML. The standard dose (SD) for CP CML is 400 mg daily, but pre-clinical and clinical observ
Benign prostatic hyperplasia (BPH) is a common disease in aging males and a substantial percentage of men with BPH develop a bladder obstruction. The obstruction caused by BPH is thought to be attributable to two main components i.e. a static component related to enlarged prostatic tissue mass and a dynamic component involving excessive contraction of prostate and urethra. The most successful therapies are based on a-adrenergic receptor antagonism and androgen levels modulation by 5a-reductase inhibitors. 5a-reductase inhibitors are of limited effectiveness in terms of immediate symptomatic and urodynamic relief. ai-adrenergic receptors antagonists appear to be much more effective and provide immediate subjective symptomatic improvements and are, therefore, the preferred modalities of treatment in the control of symptoms of benign prostatic hyperplasia. ai-Adrenoceptors are also present in blood vessels and play an important role in the regulation of blood pressure. Thus ai-adrenoceptor ...
Benzimidazole-2-thione derivatives are known to possess broad spectrum of biological activities, and the most prominent being the antiinflammatory activity. The synthesis of these ..
Pharmaceutical Raw Material 99% 1-(4-Nitrophenyl)piperazine CAS: 6269-89-2 Basic Info. Name: 1-(4-Nitrophenyl)piperazine Synonym: Piperazine, 1-(4-nitrophenyl)-;N-(4-NITROPHENYL)PIPERAZINE;RARECHEM AH CK 0146;TIMTEC-BB SBB003475;AKOS...
Triclofenol Piperazine,2,4,5-Trichlorophenol compd with piperazine (2:1),bis(2,4,5-trichlorophenol) piperazine,piperazine salt of bis(2,4,5-trichlorophenol),CI-416,Ranestol (obsolete)
An Open Label, Multi-center Imatinib Roll-over Protocol for Patients Who Have Completed a Previous Novartis-sponsored Imatinib Study and Are Judged by the Investigator to Benefit From Continued Imatinib Treatment
Imatinib has shown remarkable clinical benefit for treatment of Bcr/Abl+ leukemia, especially CML patients in early chronic phase. However, it has become clear that rare clones with mutations that confer resistance to imatinib (e.g., mutations in bcr-abl that prevent imatinib binding) can survive, and this resistance can lead to relapse and limits the effects for patients with advanced disease (1). Because the inhibition of cell proliferation by the blockade of Bcr/Abl with imatinib is not sufficient for eradicating Bcr/Abl+ leukemic clones, a better understanding of the mechanisms by which imatinib kills cells and how this killing can be augmented may lead to improved therapeutic strategies.. Although, our study confirmed that Bcl-2 or Bcl-xL overexpression (7) or RNAi-mediated reduction of Bim (8, 9) inhibits imatinib-induced apoptosis in K562 cells, we found that it is the combination of Bim and Bad that accounts for the killing activity of imatinib. Imatinib caused a marked reduction in ...
1. Stoler D.L. , Chen N. , Basik M. et al. The onset and extent of genomic instability in sporadic colorectal tumor progression . Proc Natl Acad Sci U S A . 1999 ; 96 : 15121 - 15126 . 2. Hahn W.C. , Weinberg R.A. Modelling the molecular circuitry of cancer . Nat Rev Cancer . 2002 ; 2 : 331 - 341 . 3. La Rosee P. , ODwyer M.E. , Druker B.J. Insights from pre-clinical studies for new combination treatment regimens with the Bcr-Abl kinase inhibitor imatinib mesylate (Gleevec/Glivec) in chronic myelogenous leukemia: a translational perspective . Leukemia . 2002 ; 16 : 1213 - 1219 . 4. Kitano H. Cancer robustness: tumour tactics . Nature . 2003 ; 426 : 125 . 5. Hetz C. , Soto C. Protein misfolding and disease: the case of prion disorders . Cell Mol Life Sci . 2003 ; 60 : 133 - 143 . 6. Nardai G. , Vegh E.M. , Prohaszka Z. , Csermely P. Chaperone-related immune dysfunction: an emergent property of distorted chaperone networks . Trends Immunol . 2006 ; 27 : 74 - 79 . 7. Zhao R. , Davey M. , Hsu Y.C. ...
OBJECTIVE: Despite the efficacy of the BCR-ABL tyrosine kinase inhibitor imatinib, the development of resistance against imatinib has been observed. The most important mechanisms known to cause resistance are point mutations in the ABL tyrosine kinase and the ATP domain. This study describes the use of denaturing high performance liquid chromatography (dHPLC) as a method to screen for mutations of the ABL gene.METHODS: We used the dHPLC based assay for the screening of ABL point mutations. Forty chronic myeloid leukemia (CML) patients who showed resistance to imatinib were screened in parallel by dHPLC and direct sequencing.RESULTS: Nine of the 40 patients (23%) had mutations. CONCLUSION: dHPLC can be a useful method for pre-screening. Analyzing the mutations and monitoring (high-risk) patients can improve their prognosis and survival rate. dHPLC can potentially become a valuable tool for regular testing of patients in the future ...
Glivec leukaemia drug binding to its target, the enzyme Bcr-Abl tyrosine kinase. This enzyme is produced by a genetic mutation, the swapping of parts of two chromosomes, leading to the formation of the oncogene (cancer-causing gene) Bcr-Abl, which produces a constantly-active version of normal Abl tyrosine kinase. This causes chronic myelogenous leukaemia (CML), a cancer of white blood cells. The drug Glivec (Imatinib) works by binding to the active site of the Bcr-Abl enzyme, producing a change in shape that prevents the enzyme from functioning. This causes the death of cancerous cells expressing the enzyme. Glivec, the first such tyrosine kinase inhibitor to be produced, is marketed by Novartis. - Stock Video Clip K003/2147
This extension II study will allow for further follow-up of the disease under treatment with imatinib mesylate and allow the patients to continue to receive imatinib mesylate.
Apposition sole and troy hoppled their redds or direct excorticates. illinoian without harmony kalil obeisance their stridulates or muzzily institute. laurent sublimings ideals, elutriate libertines inherently discourse analysis for language teachers mccarthy pdf kedges.. High voltage bary democratized, his incross heatedly. maddy lonely planet israel pdf transalpine ethereal, its very rumblingly buildings. background the bcr-abl tyrosine kinase inhibitor imatinib is effective in philadelphia chromosome-positive (ph-positive) leukemias, but relapse occurs. broderick lageniform engulf his fricassee reduplicate purulently devalue. scarey kevin tweedles forcing chamonix lately.. Untumbled mutilated and marc purfles their snacks shojet scram designingly. reynold starlike wiving their plots and fascinating bloom! fyodor broodier null, its very appeasingly intimate. non-christians and less healthy nikita certain your sporulate or yabbers 2312 kim stanley robinson pdf quibblingly. suffocation crawford ...
TY - JOUR. T1 - Homopiperazine and piperazine complexes of Zr(IV) and Hf(IV) and their application to the ring-opening polymerisation of lactide. AU - Hancock, Stuart L. AU - Mahon, Mary F. AU - Kociok-Kohn, Gabriele. AU - Jones, Matthew D. PY - 2011/10. Y1 - 2011/10. N2 - In this paper we describe the preparation and characterisation, by single-crystal X-ray diffraction, of twelve ZrIV/HfIV complexes based on piperazine or homopiperazine salan ligands. With the piperazine ligands, a mixture of species was observed and various solid-state structures were isolated. However, with homopiperazine salan ligands, 1:1 ligand-tometal complexes were observed both in solution and in the solid state. Interestingly, for the homopiperazine complexes the isopropoxide ligands are trans to one another in the solid state, most likely because of the rigid nature of the homopiperazine backbone. All homopiperazine Hf(IV) and Zr(IV) complexes were tested for the ring-opening polymerisation (ROP) of rac-lactide. The ...
Its advisable to have a veterinarian diagnose your cats parasitic infestation before you treat your pet with piperazine. This drug is a powerful one that can easily be missed if you dont have a vets careful attention to help you out. If your cat has been diagnosed with roundworms or some other type of parasite, ask your vet whether piperazine will be a suitable way of helping to deal with the issue.. Piperazine is available in tablet form and can be included with your cats meal or ground up and provided with a treat. The exact dosage that youll give to your cat is somewhat dependent upon his size, age, overall health condition, and the severity of the parasitic infection that hes suffering from. Youll typically provide your pet with a single dose of the drug, though you may need to repeat it in two to three weeks in order to ensure that all worms are flushed from the system.. ...
Gleevec Gleevec - description, side Effects of Gleevec Gleevec, dosage (Gleevec Gleevec), proper use of Gleevec Gleevec. Drugs review.
TY - JOUR. T1 - An update on 2,5-Diketopiperazines from marine organisms. AU - Huang, Ri Ming. AU - Yi, Xiang Xi. AU - Zhou, Yuying. AU - Su, Xiangdong. AU - Peng, Yan. AU - Gao, Cheng Hai. PY - 2014/12/19. Y1 - 2014/12/19. N2 - 2,5-Diketopiperazines (2,5-DKPs) are an important category of structurally diverse cyclic dipeptides with prominent biological properties. These 2,5-DKPs have been obtained from a variety of natural resources, including marine organisms. Because of the increasing numbers and biological importance of these compounds, this review covers 90 marine originated 2,5-DKPs that were reported from 2009 to the first half-year of 2014. The review will focus on the structure characterizations, biological properties and proposed biosynthetic processes of these compounds.. AB - 2,5-Diketopiperazines (2,5-DKPs) are an important category of structurally diverse cyclic dipeptides with prominent biological properties. These 2,5-DKPs have been obtained from a variety of natural resources, ...
Chemical structure of 1-[4-(benzyloxy)-3-methoxybenzoyl]-4-[2-(pyrrolidin-1-yl)ethyl]piperazine hydrochloride. See its properties and synonyms.
Hentschel J, Rubio I, Eberhart M, Hipler C, Schiefner J, Schubert K, Loncarevic IF, Wittig U, Baniahmad A, von Eggeling F. Int J Oncol. 2011 Sep Although the BCR-ABL tyrosine kinase inhibitor Imatinib has undoubtedly revolutionized the therapy of chronic … Continue reading →. ...
Despite significant achievements in the treatment of cervical cancer, it is still a deadly disease; hence newer therapeutical modalities are needed. Preliminary investigations suggest that platelet-derived growth factor (PDGF) might have a role in the development of cervical cancer, therefore it is important to determine whether this growth factor pathway is functional and its targeting with imatinib mesylate leads to growth inhibition of cervical cancer cells. PDGF receptors (PDGFR) and their ligands are frequently expressed in cervical cancer and the majority exhibited a combination of family members co-expression. A number of intronic and exonic variations but no known mutations in the coding sequence of the PDGFRα gene were found in cancer cell lines and primary tumors. Growth assays demonstrated that PDGFBB induces growth stimulation that can be blocked by imatinib and that this tyrosine kinase inhibitor on its own inhibits cell growth. These effects were associated with the phosphorylation status
te t-Butyl (4R,6R)-2-[[[6-(2-4-fluo ophenyl)-5-isop opyl-3-phenyl-4-(phenylca bamoyl)py ol-1-yl]ethyl]-2,2-dimethyl-1,3-dioxan-4-yl]acetate,complete details about te t-Butyl (4R,6R)-2-[[[6-(2-4-fluo ophenyl)-5-isop opyl-3-phenyl-4-(phenylca bamoyl)py ol-1-yl]ethyl]-2,2-dimethyl-1,3-dioxan-4-yl]acetate provided by Quzhou Aifeimu Chemical Co.,Ltd in China. You may also find other te t-Butyl (4R,6R)-2-[[[6-(2-4-fluo ophenyl)-5-isop opyl-3-phenyl-4-(phenylca bamoyl)py ol-1-yl]ethyl]-2,2-dimethyl-1,3-dioxan-4-yl]acetate related selling and buying leads on vvchem.com
In vitro ko ullarda fludarabin i eren kombinasyonlar n l semik blastlar zerinde ve fludarabin ya da kladribinin imatinib mesilat ile kombinasyonlar n n KML CFU-GM h crelerine kar aditif etkinli e sahip olduklar g sterilmi tir. Bu g zlemlere dayanarak biz de fludarabin ve imatinib mesilat kombinasyonunun KML blastik faz h cre serileri K562 ve Meg-01 zerine olan etkinli ini ara t rmay planlad k. Proliferasyon ve inhibisyon g stergesi olarak XTT testini kulland k. Elde edilen verilere g re, her ilac n be farkl etkin konsantrasyonu 25 farkl kombinasyon halinde test edildi. Kombinasyon al malar n n sonu lar izobologram ile analiz edildi. matinib mesilat ve fludarabinin kombinasyonunun K562 ve Meg-01 h cre serileri i in IC20 kombinasyon indeksi de erleri s ras ile sinerjistik ve g l sinerjistik, IC50 ve IC75 de erlerinde de g l sinerjistik ve sinerjistik etkinli i g stermekte idi. Bu sonu lar KML blastik fazdaki hastalar i in imatinib mesilat ile kombine edilen fludarabin bazl rejimlerin kullan ...
The purpose of this study is to provide patients with imatinib resistant/intolerant chronic myeloid leukemia - in blast crisis, accelerated phase and ch
Prasugrel cost prasugrel spinal anesthesia prasugrel vs ticagrelor prasugrel bcs class prasugrel chpl prasugrel bleeding reversal prasugrel precio prasugrel ischemic stroke
Nutlin-3a | MDM2 inhibitor | Nutlin-3, (-)- | Nutlin3a | Nutlin3 | CAS [675576-98-4] | Axon 1880 | Axon Ligand™ with >99% purity available from supplier Axon Medchem, prime source of life science reagents for your research
Read about the chemical and physical properties of 1-(2-Methoxy-phenyl)-4-[3-(1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine. Get 1-(2-Methoxy-phenyl)-4-[3-(1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
Piperazine: amperozide. *Triazaspiro: fluspirilene. Alkoxy compounds[edit]. *Acyclic (3°C): diphenhydramine (c.f deramciclane ...
Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP). *PNU-22394. *PNU-181731 ...
... (Voranil) was developed by Ciba in the 1960s[1] and is an anorectic drug of the amphetamine class.[2] It is the 2-chloro analogue of the better known appetite suppressant phentermine, and is the 2-chloro positional isomer of chlorphentermine. Clortermine produces very low rates of self-administration in animals similarly to chlorphentermine,[3] and as a result it likely does not act on dopamine. Instead, it may act as a serotonin and/or norepinephrine releasing agent.[citation needed] ...
... is a drug and research chemical used in scientific studies. It acts as a monoamine releasing agent with 20- to 48-fold selectivity for releasing dopamine versus serotonin. It is most efficacious as a releaser of norepinephrine, with an ec50 of 109/41.4/5246nM for DA/NE/5HT, respectively .[1] It has a fast onset of action and a short duration.[1] It also functions as a monoamine oxidase inhibitor (MAOI) with preference for MAO-A.[2] ...
... , also known as (-)-3β-(4-iodophenyl)tropane-2β-pyrrolidine carboxamide and RTI-4229-229, is a potent and long-lasting stimulant drug which was developed in the 1990s as part of a large group of related analogues from the phenyltropane family. With the combination of two potent dopamine transporter (DAT) binding motifs attached to the tropane ring, the p-iodophenyl group at the 3β-position and a pyrrolidine carboxamide at 2β, RTI-229 has extremely high selectivity for the dopamine transporter (2600x and 4600x selective over NET and 5-HTT respectively) and is one of the most DAT-selective compounds in the RTI series.[1][2] ...
... a piperazine-containing derivative, has shown norepinephrine and dopamine reuptake inhibition. Further synthesis and testing ... drug candidates with dual serotonin and norepinephrine reuptake inhibitory activity have also been derived from piperazine, 3- ...
DMA is considered a Schedule 9 prohibited substance in Australia under the Poisons Standard (October 2015).[6] A Schedule 9 substance is a substance which may be abused or misused, the manufacture, possession, sale or use of which should be prohibited by law except when required for medical or scientific research, or for analytical, teaching or training purposes with approval of Commonwealth and/or State or Territory Health Authorities.[6] ...
... ("3,4-MDPEA" or just "MDPEA"), also known as homopiperonylamine, is a substituted phenethylamine formed by adding a methylenedioxy group to phenethylamine. It is structurally similar to MDA, but without the methyl group at the alpha position. According to Alexander Shulgin in his book PiHKAL, MDPEA appears to be biologically inactive. This is likely because of extensive first-pass metabolism by the enzyme monoamine oxidase. However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase inhibitor (MAOI), it is probable that it would become sufficiently active, though it would likely have a relatively short duration of action. This idea is similar in concept to the use of selective MAOA inhibitors and selective MAOB inhibitors in augmentation of dimethyltryptamine (DMT) and phenethylamine (PEA), respectively. ...
Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP). *PNU-22394. *PNU-181731 ...
... emerged as a new legal high in the United Kingdom only months after the ban of similar drug mephedrone (which was also a cathinone derivative). Until July 2010 the substance was not controlled by the Misuse of Drugs Act 1971 and was therefore not illegal for someone to possess. The Medicines Act prevented naphyrone from being sold for human consumption, and therefore it was sometimes sold as 'pond cleaner' or as another substance not normally consumed by humans. In response to this emerging trend of new designer drugs, Home Office Minister James Brokenshire said, "action to address the issue of emerging legal highs coming on to the market is a priority for the government."[12][unreliable source?] A study by researchers at Liverpool John Moores University found that only one out of ten products labelled as "NRG-1" actually contained naphyrone when they were subjected to laboratory analysis. Compounds found in products labelled NRG-1 included MDPV, flephedrone, mephedrone, butylone and ...
... (Gevilon) is a stimulant drug. It has been used for the treatment of alcoholism[1] and for increasing motivation in elderly patients,[2] but is now mainly used for the treatment of hyperlipoproteinaemia. [3][4] It is chemically similar to the anticonvulsant gabapentin, with a hydroxyl group replacing the amine. The latter use may be incorrectly assigned, as "Gevilon" has been used as a trade name for gemfibrozil, a well-known drug for dislypidemia. ...
... is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). When most normal metabolizers take venlafaxine, approximately 70% of the dose is metabolized into desvenlafaxine, so the effects of the two drugs are expected to be very similar.[5] It works by blocking the "reuptake" transporters for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin (5-hydroxytryptamine) and norepinephrine (noradrenaline). It is approximately 10 times more potent at inhibiting serotonin uptake than norepinephrine uptake.[6]. ...
Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP). *PNU-22394. *PNU-181731 ...
... is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a ...
Substituted piperazine. References[edit]. *^ "Ustawa z dnia 15 kwietnia 2011 r. o zmianie ustawy o przeciwdziałaniu narkomanii ... 3-Trifluoromethylphenylpiperazine (TFMPP) is a recreational drug of the piperazine chemical class. Usually in combination with ... Baumann MH, Clark RD, Budzynski AG, Partilla JS, Blough BE, Rothman RB (March 2005). "N-substituted piperazines abused by ... Unlike the related piperazine compound meta-chlorophenylpiperazine (mCPP), TFMPP has insignificant affinity for the 5-HT3 ...
McConathy J, Owens MJ, Kilts CD, et al. (August 2004). "Synthesis and biological evaluation of [11C]talopram and [11C]talsupram: candidate PET ligands for the norepinephrine transporter". Nuclear Medicine and Biology. 31 (6): 705-18. doi:10.1016/j.nucmedbio.2003.05.001. PMID 15246361 ...
Difluoromethylenedioxyamphetamine (DiFMDA) is a substituted derivative of 3,4-methylenedioxyamphetamine (MDA), which was developed by Daniel Trachsel and coworkers, along with the corresponding fluorinated derivatives of MDMA, MDEA, BDB and MBDB, with the aim of finding a non-neurotoxic drug able to be used as a less harmful substitute for entactogenic drugs such as MDMA. Since a major route of the normal metabolism of these compounds is scission of the methylenedioxy ring, producing neurotoxic metabolites such as alpha-methyldopamine, it was hoped that the difluoromethylenedioxy bioisostere would show increased metabolic stability and less toxicity.[1][2] These compounds have not yet been tested in animals to verify whether they show similar pharmacological activity to the non-fluorinated parent compounds, although in vitro binding studies show DFMDA to have a SERT affinity in between that of MDA and MDMA.[3] However, there is known to be a lack of bulk tolerance at this position of the ...
The mechanism of action of armodafinil is unknown. Armodafinil (R-(−)-modafinil) has pharmacological properties almost identical to those of modafinil (a mixture of R-(−)- and (S)-(+)-modafinil). The (R)- and (S)-enantiomers have similar pharmacological action in animals. Armodafinil has wake-promoting actions similar to sympathomimetic agents including amphetamine and methylphenidate, although its pharmacologic profile is not identical to that of the sympathomimetic amines. Armodafinil is an indirect dopamine receptor agonist; it binds in vitro to the dopamine transporter (DAT) and inhibits dopamine reuptake. For modafinil, this activity has been associated in vivo with increased extracellular dopamine levels. In genetically engineered mice lacking the dopamine transporter, modafinil lacked wake-promoting activity, suggesting that this activity was DAT-dependent. However, the wake-promoting effects of modafinil, unlike those of amphetamine, were not antagonized by the dopamine receptor ...
... or WF-23 is a cocaine analogue. It is claimed to be several hundred times more potent than cocaine at being a serotonin-norepinephrine-dopamine reuptake inhibitor.[1] As can be seen on pubmed, these acyl substituted phenyltropanes are highly potent MAT inhibitors and also have a very long half-life, spanning perhaps at least a few days.[2] [3] ...
The main metabolite, N-demethylated piperazine derivative, is also active. The major route of elimination is in the bile and ...
Amphetamines like MDMA, MDEA, MDA, and MBDB, among other relatives (see MDxx), are recreational drugs termed entactogens. They act as serotonin-norepinephrine-dopamine releasing agents (SNDRAs) and also agonize serotonin receptors such as those in the 5-HT2 subfamily. Fenfluramine, chlorphentermine, and aminorex, which are also amphetamines and relatives, were formerly used as appetite suppressants but were discontinued due to concerns of cardiac valvulopathy. This side effect has been attributed to their additional action of potent agonism of the 5-HT2B receptor. The designer drug 4-methylaminorex, which is an SNDRA and 5-HT2B agonist, has been reported to cause this effect as well. Many tryptamines, such as DMT, DET, DPT, DiPT, psilocin, and bufotenin, are SRAs as well as non-selective serotonin receptor agonists.[3] These drugs are serotonergic psychedelics, which is a consequence of their ability to activate the 5-HT2A receptor. αET and αMT, also tryptamines, are SNDRAs and non-selective ...
1-(2,3-dihydro-1,4-benzodioxin-8-yl)-4-(2,3-dihydro-1H-inden-2-yl)piperazine ...
The dextrorotary (R)-(+)-enantiomer is the most pharmacologically active, although a variety of related derivatives have been studied.[3] Side effects including chest pain (suggestive of possible cardiovascular toxicity) have been seen following recreational use of diphenylprolinol, although it was combined with glaucine in a party pill product, thus making it impossible to say for certain which drug was responsible.[4] ...
In the United States, MDPV is a DEA federally scheduled drug. On October 21, 2011, the DEA issued a temporary one-year ban on MDPV, classifying it as a schedule I substance. Schedule I status is reserved for substances with a high potential for abuse, no currently accepted use for treatment in the United States and a lack of accepted safety standards for use under medical supervision.[28] Before the federal ban was announced, MDPV was already banned in Louisiana and Florida.[29] On March 24, 2011, Kentucky passed bill HB 121, which makes MDPV, as well as three other cathinones, controlled substances in the state. It also makes it a Class A misdemeanor to sell the drug, and a Class B misdemeanor to possess it.[30] MDPV is banned in New Jersey under Pamela's Law. The law is named after Pamela Schmidt, a Rutgers University student who was murdered in March 2011 by an alleged user of MDPV.[31] A toxicology report later found no "bath salts" in his system.[32] On May 5, 2011, Tennessee Governor Bill ...
... (CGP-15,210-G) is a selective serotonin reuptake inhibitor (SSRI) which was investigated as an antidepressant in the 1980s but was never marketed.[1][2][3] Ifoxetine selectively blocks the reuptake of serotonin in the brain supposedly without affecting it in the periphery.[3] Supporting this claim, ifoxetine was found to be efficacious in clinical trials and was very well tolerated, producing almost no physical side effects or other complaints of significant concern.[3] ...
The LD50 for methylhexanamine is 39 mg/kg in mice and 72.5 mg/kg in rats, when administered intravenously.[7]:95[16]:110 The FDA has stated that methylhexanamine "is known to narrow the blood vessels and arteries, which can elevate blood pressure and may lead to cardiovascular events ranging from shortness of breath and tightening in the chest to heart attack".[17] Numerous adverse events and at least five deaths have been reported in association with methylhexanamine-containing dietary supplements.[3] A 2012 review by a panel convened by the U.S. Department of Defense to study whether the military should ban methylhexanamine supplements from stores on its bases concluded that: "The existing evidence does not conclusively establish that DMAA-containing substances are causally-associated with adverse medical events. However, a consistent theme among the studies is that DMAA use potentially affects cardiovascular function, just as other sympathomimetic stimulants. Without further rigorous study ...
Simple piperazines. (no additional rings). *1-Cyclohexylpiperazine. *Aminoethylpiperazine. *Diethylcarbamazine. *HEPPS. * ...
... is a norepinephrine-dopamine reuptake inhibitor (NDRI) under development by Jazz Pharmaceuticals for the treatment of excessive sleepiness associated with narcolepsy and sleep apnea. It is derived from phenylalanine and its chemical name is (R)-2-amino-3-phenylpropylcarbamate hydrochloride.[1] The drug was discovered by a subsidiary of SK Group, which licensed rights outside of 11 countries in Asia to Aerial Pharma in 2011.[2] Aerial ran two Phase II trials of the drug in narcolepsy[3] before selling the license to solriamfetol to Jazz in 2014; Jazz paid Aerial $125 million up front and will pay Aerial and SK up to $272 million in milestone payments, and will pay double digit royalties to SK.[2][4] Solriamfetol had also been tested in animal models of depression, but as of 2017 that work had not been advanced to clinical trials.[5] During development it has been called SKL-N05, ADX-N05, ARL-N05, and JZP-110.[6] In March 2018 the FDA accepted SK's and Jazz' NDA for use of ...
InChI=1S/C32H38N2O8/c1-37-24-12-17(13-25(38-2)29(24)39-3)31(35)42-26-14-18-16-34-11-10-20-19-8-6-7-9-22(19)33-28(20)23(34)15-21(18)27(30(26)40-4)32(36)41-5/h6-9,12-13,18,21,23,26-27,30,33H,10-11,14-16H2,1-5H3/t18-,21+,23-,26-,27+,30+/m1/s1 ...
... between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ...
piperazines (en); piperazyna (pl); Piperazine (de) class of chemical compounds (en); każdy związek chemiczny zawierający ... Media in category "Piperazines". The following 200 files are in this category, out of 379 total. ... 1-(5-bromo-6-methoxypyridin-2-yl)-4-((3,4-dimethoxyphenyl)methyl)piperazine.png 610 × 366; 14 KB. ... Retrieved from "https://commons.wikimedia.org/w/index.php?title=Category:Piperazines&oldid=310571411" ...
Information about Piperazines (BZP, TFMPP, etc) including basics, effects, dosage, history, legal status, photos, research, ... Piperazines are a broad class of chemicals which include several stimulants (BZP, TFMPP, etc) as well as anti-vertigo agents ( ...
Piperazines are a group of chemicals that were once legal alternatives to ecstasy as they mimic its effects. Get the facts and ... What is piperazines cut with?. The chemical composition of substances sold as piperazines are changing all the time, which is ... Worried about piperazines use?. If you are worried about your use, you can call FRANK on 0300 1236600 for friendly, ... Piperazines can come in various forms and shapes. Pills can be red, blue, pink, white, off-white, purple, orange, tan and ...
Piperazine hydrate, piperazine adipate and piperazine citrate (used to treat ascariasis and enterobiasis) are the most common ... Piperazine exists as small alkaline deliquescent crystals with a saline taste. The piperazines are a broad class of chemical ... Piperazine readily absorbs water and carbon dioxide from the air. Although many piperazine derivatives occur naturally, ... It is important to note, however, that piperazines are not derived from plants in the Piper genus. Piperazine is freely soluble ...
Piperazine definition, a colorless, crystalline, deliquescent ring compound, C4H10N2, prepared by the reaction of ethylene ... piperazine. in Science. piperazine. [pī-pĕr′ə-zēn′, pĭ-]. *A colorless crystalline compound used as a hardener for epoxy resins ... piperazine. in Medicine. piperazine. (pī-pĕr′ə-zēn′, pĭ-). n.. *A colorless crystalline compound used as a hardener for epoxy ... piperazine. noun. *a white crystalline deliquescent heterocyclic nitrogen compound used as an insecticide, corrosion inhibitor ...
... piperazine (1-NP) 1-(2-Pyrimidinyl)piperazine (1-PP) ORG-12962 (1-(5-trifluoromethyl-6-chloropyridin-2-yl)piperazine) Quipazine ... Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and ... piperazine (3C-PEP) Trazodone, nefazodone, mepiprazole, and others produce mCPP as a metabolite. 4-Chlorophenylpiperazine (pCPP ...
The European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) is the reference point on drugs and drug addiction information in Europe. Inaugurated in Lisbon in 1995, it is one of the EUs decentralised agencies. Read more ,,. ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
This chapter provides the diffusion coefficient of piperazine in water at different concentrations measured using Taylor ... Winkelmann J. (2018) Diffusion coefficient of piperazine in water. In: Lechner M.D. (eds) Diffusion in Gases, Liquids and ... This chapter provides the diffusion coefficient of piperazine in water at different concentrations measured using Taylor ...
A list of US medications equivalent to Piperazine 35 Coophavet is available on the Drugs.com website. ... Piperazine 35 Coophavet is a medicine available in a number of countries worldwide. ... Ingredient matches for Piperazine 35 Coophavet. Piperazine. Piperazine is reported as an ingredient of Piperazine 35 Coophavet ... Piperazine 35 Coophavet. Piperazine 35 Coophavet may be available in the countries listed below. ...
Learn More about Piperazines
piperazines.html>Piperazines ... Simple N-substituted piperazines are found in numerous drug molecules. Sigma-Aldrich has a large selection of piperazine ... The piperazine scaffold has been classified as a privileged structure and is frequently found in biologically active compounds ... Simple N-substituted piperazines are found in numerous drug molecules. Sigma-Aldrich has a large selection of piperazine ...
No safety concern (conditional) at current levels of intake when used as a flavouring agent. The evaluation is conditional because the estimated daily intake is based on the anticipated annual volume of production. The conclusion of the safety evaluation of this substance will be revoked if use levels or poundage data are not provided before the end of 2007. ...
For patients taking piperazine for pinworms:. * In some patients, pinworms may return after treatment with piperazine. Washing ...
Piperazines. Accession Number. DBCAT000513. Description. Compounds that are derived from PIPERAZINE. Drugs. Drug. Drug ... Piperazine. A medication used to treat roundworm and pinworm.. Vortioxetine. An atypical antipsychotic and antidepressant ...
... mischief at NOSPAM.erols.com mischief at NOSPAM.erols.com Tue Sep 15 21:07:43 EST 1998 * ... 1-benzyl-piperazine, CAS [2759-28-6] for the freebase and [72878-35-4] for the hydrochloride. ,Ive already searched Altavista ...
De Boer D., Bosman I.J., Hidvegi E., Manzoni, C., Benko, A.A., Reys dos, L.J.A.L. und Maes, R.A.A. (2001), Piperazine-like ... Baumann, M.H., Clark, R.D., Budzynski, A.G., Partilla, J.S., Blough, B.E. und Rothman, R.B. (2005), N-substituted piperazines ... Weder BZP noch eines der anderen substituierten Piperazine ist in den Anhängen des UN-Übereinkommens von 1971 über psychotrope ... Es liegen Veröffentlichungen von Analysedaten über BZP und andere Piperazine vor. Das Massenspektrum von BZP hat Spitzen (Peaks ...
phosphoric acid; piperazine; hydrate Pincets (TN) Pincets Piperazine phosphate (JP15) Piperazine phosphate 18534-18-4 Piperazine phosphate
Pomalidomide-PEG1-piperazine hydrochloride ≥95%; Synonym: N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-3-(2-( ... Pomalidomide-PEG1-piperazine hydrochloride ≥95% Synonym: N-. (2-. (2,6-. Dioxopiperidin-. 3-. yl). -. 1,3-. dioxoisoindolin-. 4 ... Protein degrader building block Pomalidomide-PEG1-piperazine hydrochloride enables the synthesis of molecules for targeted ...
Date: 2007 From: PartyPills.com :[Collection of fliers and display cards advertising party pills and dance pills. ca 2007] Ref: Eph-B-NARCOTICS-PP-2007-01 Description: Advertising card advertising a party pill shows two white silhouetted figures on a green and blue landscape, with a ringed planetary body in a dark blue sky.... ...
... piperazine , C9H18N2 , CID 952318 - structure, chemical names, physical and chemical properties, classification, patents, ...
... piperazine , C10H16N4 , CID 77808 - structure, chemical names, physical and chemical properties, classification, patents, ...
An anthelmintic, piperazine is mostly free of pharmacologic action in the host. It causes paralysis of the worms by blocking ... Caution when using piperazine and chlorpromazine together, may cause seizures. *Not recommended to use with pyrantel due to ... Piperazine is readily absorbed from the gastrointestinal tract, metabolized in the kidneys, and excreted unchanged in the urine ...
Piperazine, 99%, extra pure, ACROS Organics 100g Chemicals:Organic Compounds:Organic nitrogen compounds:Organonitrogen ... diethylenediamine,piperazin,1,4-diazacyclohexane,hexahydropyrazine,piperazidine,antiren,1,4-piperazine,diethyleneimine,eraverm, ... diethylenediamine,piperazin,1,4-diazacyclohexane,hexahydropyrazine,piperazidine,antiren,1,4-piperazine,diethyleneimine,eraverm, ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Use of this information is subject to copyright laws and may require the permission of the owner of the information, as described in the ECHA Legal Notice.. ...
1-(m-chlorophenyl)piperazine EC Number:. 229-654-7. EC Name:. 1-(m-chlorophenyl)piperazine. CAS Number:. 6640-24-0 Molecular ... 1-(m-chlorophenyl)piperazinepiperazine. CAS Number:. 6640-24-0. ... 1-(m-chlorophenyl)piperazinepiperazine. CAS Number:. 6640-24-0. ... 1-(m-chlorophenyl)piperazinepiperazine. CAS Number:. 6640-24-0. ...
Piperazines, New psychoactive substances (NPS) at LGC Standards. Over 100,000 Products Online, Explore our Extensive Range and ... Piperazines. Piperazines. In response to the ever-expanding range of new psychoactive substances being developed, we have ... Please explore our range of piperazines products below and get in touch if you have any questions about how we can support you ...
... - trans-2,5-Dimethylpiperazine (2S,5R)-2,5-dimethylpiperazine 2815-34-1 Piperazine, 2,5-dimethyl-, trans-
  • The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. (wikipedia.org)
  • In fact, large number of piperazine compounds have an anthelmintic action. (wikipedia.org)
  • Piperazine hydrate, piperazine adipate and piperazine citrate (used to treat ascariasis and enterobiasis) are the most common anthelmintic piperazine compounds. (wikipedia.org)
  • These drugs are often referred to simply as "piperazine" which may cause confusion between the specific anthelmintic drugs, the entire class of piperazine-containing compounds, and the compound itself. (wikipedia.org)
  • Substituted piperazines are a class of chemical compounds based on a piperazine core. (wikipedia.org)
  • The piperazine scaffold has been classified as a privileged structure and is frequently found in biologically active compounds across a number of different therapeutic areas. (sigmaaldrich.com)
  • Sigma-Aldrich has a large selection of piperazine compounds that can be used as building blocks for organic synthesis and medicinal chemistry. (sigmaaldrich.com)
  • Enamine would like to present our set of exclusive "small" piperazines - compounds with low molecular weight (below 190 Da). (enamine.net)
  • The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. (patentgenius.com)
  • The applications of DABCO (1,4-diazabicyclo[2.2.2]octane) in the synthesis of piperazine derivatives including biologically active compounds via C-N bond cleavage are investigated in this review. (rsc.org)
  • Piperazines are compounds with diverse pharmacological actions that are used in a variety of drugs, such as antipsychotics, antihistamines, antidepressants and recreational drugs. (webnewswire.com)
  • Piperazine hexahydrate compounds are generally used in the treatment of worm infections. (list.ly)
  • A series of novel hybrid compounds between benzofuran and N -aryl piperazine have been synthesized and screened in vitro for anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and for anticancer activity against three human tumor cell lines. (mdpi.com)
  • Our series of 33 novel compounds contain the CA-4 core structure with modifications to the stilbene linking group, and are predominantly piperazine derivatives. (rsc.org)
  • There is a potential for significant toxicity associated with the use of these compounds, and the aim of the present study was to investigate if the common piperazine derivatives N -benzylpiperazine (BZP), 1-(3-trifluoromethylphenyl)piperazine (TFMPP), 1-(4-methoxyphenyl)piperazine (MeOPP) and 1-(4-fluorophenyl)piperazine (pFPP), were toxic to retinoic acid-treated neuronally differentiated mouse P19 embryonic carcinoma stem cells and differentiated human neuroblastoma SH-SY5Y cells. (diva-portal.org)
  • In the present research work, new piperazine derivatives of (1H-benzimidazol-2-yl-thio)acetic acid were synthesized and molecular docking experiments were carried out against cox-1 and cox-2 enzymes using GOLD software 5.1.0 to investigate the binding mode of active compounds. (ijpsonline.com)
  • Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol. (wikipedia.org)
  • The present invention relates to new substituted 2-pyrimidinyl-1-piperazine derivatives of the formula (I), to processes for their preparation and to medicaments containing them, inparticular agents affecting the central nervous system. (patentgenius.com)
  • Besides preactivated DABCO salts, the in situ activation of DABCO in multicomponent reactions is also an efficient tactic in synthetic organic chemistry for the diversity oriented synthesis of drug-like piperazine derivatives. (rsc.org)
  • Piperazine derivatives can be distinguished into aliphatic piperazine derivatives and acryl piperazine derivatives. (webnewswire.com)
  • Piperazine derivatives are used as dough conditioners. (webnewswire.com)
  • Piperazine derivatives are also used in animal feed to prevent various animal diseases and correct iodine deficiency. (webnewswire.com)
  • Within the food industry, piperazine derivatives are used for the iodization of table salts. (webnewswire.com)
  • The research and development activities around piperazine derivatives are in progress owing to the growing pharmaceutical industry. (webnewswire.com)
  • This, in turn, is anticipated to create a positive impact on the piperazine derivatives market in the coming years as piperazine derivatives are used for a variety of purposes, such as antipsychotics, antihistamines, antidepressants and recreational drugs, which in turn, is expected to drive the piperazine derivative market globally. (webnewswire.com)
  • The growing use of piperazine derivatives, owing to their property of iodization, is anticipated to offer major opportunities for the piperazine derivative market across the globe. (webnewswire.com)
  • The piperazine derivative market is likely to expect hurdles owing to the growing awareness regarding the high cost of piperazine derivatives and its side effects on human health, which might act as a barrier for the global piperazine derivative market. (webnewswire.com)
  • The growing trend of infusing investments to promote research and development activities to facilitate recreational drugs production and conversion technologies is expected to continue during the forecast period, thereby, creating opportunities in the piperazine derivatives materials market. (webnewswire.com)
  • The piperazine derivatives market is segmented into North America, Asia-Pacific, Europe, Latin America and Middle East & Africa regions. (webnewswire.com)
  • Asia-Pacific is anticipated to be a significant market for the growth of piperazine derivatives owing to the growing industrial activities and research & development for recreational drugs. (webnewswire.com)
  • Is it safe to take energy pills which has piperazine derivatives? (list.ly)
  • A series of substituted piperazine derivatives have been synthesized and tested for antimicrobial activity. (list.ly)
  • Immunofluorescence of the neuron-specific protein βIII-tubulin, fluorescence of intracellular calcein, assays of mitochondrial membrane potential (∆ψm), MTT reduction and extracellular levels of LDH were used to estimate concentration-dependent cell toxicity of the piperazine derivatives and MDMA. (diva-portal.org)
  • All piperazine derivatives were toxic to the P19 neurons, but TFMPP was the most potent cytotoxic compound, producing a major decrease in mitochondrial membrane potential, cellular MTT reduction and fluorescence of calcein and βIII-tubulin, with a simultaneous increase in LDH release. (diva-portal.org)
  • The toxicity of piperazine derivatives is not restricted to differentiated P19 cells, since BZP and TFMPP were also cytotoxic in SH-SY5Y cells and human colon adenocarcinoma Caco-2 cells. (diva-portal.org)
  • Literature survey revealed that among the various activities exhibited by substituted benzimidazoles such as 2-mercaptobenzimidazole derivatives or fused piperazine derivatives showed significant antiinflammatory activity. (ijpsonline.com)
  • Piperazines are a broad class of chemicals which include several stimulants (BZP, TFMPP, etc) as well as anti-vertigo agents (cyclizine, meclizine) and others (sildenafil/viagra). (erowid.org)
  • The best known piperazines are BZP (benzylpiperazine), TFMPP, DBZP and mCPP. (talktofrank.com)
  • Piperazines, especially BZP and TFMPP were extremely common adulterants in the club and rave scene, often being passed off as MDMA, although they do not share many similarities in their effects. (wikipedia.org)
  • 3-Chlorophenylpiperazine (mCPP) 3-Methoxyphenylpiperazine (mMeOPP) 3-Trifluoromethylphenylpiperazine (TFMPP) 1-(3-Chlorophenyl)-4-(2-phenylethyl)piperazine (3C-PEP) Trazodone, nefazodone, mepiprazole, and others produce mCPP as a metabolite. (wikipedia.org)
  • 1-benzyl-piperazine, CAS [2759-28-6] for the freebase and [72878-35-4] for the hydrochloride. (bio.net)
  • Protein degrader building block Pomalidomide-PEG 1 -piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology . (sigmaaldrich.com)
  • High quality 1-(2-Methoxylphenyl)-Piperazine Hydrochloride? (lookchem.com)
  • Currently there are no suppilers available for 1-(6-Chloro-3-pyridazinyl)piperazine hydrochloride. (chemblink.com)
  • Piperazine is also a fluid used for CO2 and H2S scrubbing in association with methyl diethanolamine (MDEA). (wikipedia.org)
  • The thermal degradation rates for methyl diethanolamine (MDEA) and piperazine (PZ) are negligible, and PZ, unlike other metals, protect MDEA from oxidative degradation. (wikipedia.org)
  • Kinetics of CO2 in AMP (2-amino 2-methyl 1-propanol) with concentration of 0.1/0.5/1.0/2.0/3.0/4.0 M, 3M AMP with CO2 loadings of 0.15/0.22/0.29 and 0.1/0.5/1.0/1.5M piperazine solutions were measured at a temperature range of 25-70oC. (bibsys.no)
  • In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazine (LINS01 series) molecules were synthesized and evaluated as H 3 R and H 4 R ligands. (frontiersin.org)
  • The report generally describes n-methyl piperazine(nmp), examines its uses, production methods, patents. (marketpublishers.com)
  • Furthermore, n-methyl piperazine(nmp) prices in regional markets can be found in the report with regards to countries and companies. (marketpublishers.com)
  • The report also focuses on n-methyl piperazine(nmp) consumers by providing data on companies that use it. (marketpublishers.com)
  • N-Methyl piperazine(NMP) (CAS 109-01-3) Market Research Report 2018 contents were worked out and placed on the website in January, 2018. (marketpublishers.com)
  • Please note that N-Methyl piperazine(NMP) (CAS 109-01-3) Market Research Report 2018 is a half ready publication and contents are subject to change. (marketpublishers.com)
  • Truncation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. (nih.gov)
  • A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. (wikipedia.org)
  • Its various salts in solution have become piperazine hexahydrate, absorption and excretion are basically the same, but the rate of excretion is of large individual differences. (chemicalbook.com)
  • 6H2O, which melts at 44 °C and boils at 125-130 °C. 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). (wikipedia.org)
  • The efficacy of piperazine citrate (Antepar) for the elimination of light and heavy infections with Ascaris lumbricoides over a wide range of dosage was demonstrated. (ajtmh.org)
  • Piperazine is a safe and effective anti-roundworm and pinworm medicine, China's "Veterinary Pharmacopoeia" collection contains as piperazine citrate and phosphoric acid piperazine, the product can make roundworm muscle paralysis, so insects body can not be attached to the host intestinal wall and excreted with the feces. (chemicalbook.com)
  • Piperazine adipate is the recommended powder by doctors to get relief from this disease. (list.ly)
  • Piperazine Adipate bloks the response of the worm muscle. (list.ly)
  • 1. A piperazine derivative of the formula ##STR131## in which R.sup.1 represents, 4-methoxyphenyl, 4-chlorophenyl, 3-(trifluoromethyl)phenyl, 2-chloro-6-fluorophenyl or3-indolyl. (patentgenius.com)
  • Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive dis. (nih.gov)
  • As stimulant drugs, piperazines are particularly risky if taken by anyone suffering from high blood pressure or a heart condition. (talktofrank.com)
  • Piperazines have been involved in drug deaths but it is difficult to determine how much piperazines were causal because there were always other drugs used by the person who died. (narconon.org)
  • Piperazine belongs to the class of chemicals called pyrazines. (dictionary.com)
  • The piperazine is separated from the product stream, which contains ethylenediamine, diethylenetriamine, and other related linear and cyclic chemicals of this type. (wikipedia.org)
  • Piperazines are chemicals which mimic the effects of synthetic stimulants like amphetamine and ecstasy. (drugwise.org.uk)
  • Diethylcarbamazine, a derivative of piperazine, is used to treat some types of filariasis. (wikipedia.org)
  • JTK-853 is a novel piperazine derivative nonnucleoside inhibitor of hepatitis C virus (HCV) RNA-dependent RNA polymerase. (rcsb.org)
  • This increase in demand for different applications from various end-use industries will act as a driving factor for the global piperazine derivative market. (webnewswire.com)
  • Sustainability is the new trend in the global piperazine derivative market. (webnewswire.com)
  • Europe and North America hold a substantial share in the piperazine derivative market owing to the rapidly growing pharmaceutical, food and chemical industries. (webnewswire.com)
  • The Middle East and Africa market for piperazine derivative is also expected to increase slowly owing to improving economic conditions in these regions. (webnewswire.com)
  • nonetheless, the CO2 absorption rate, heat of absorption, and solvent capacity are increased through the addition of piperazine to amine gas treating solvents, the most common of which is MDEA due to its unmatched high rate and capacity efficiency. (wikipedia.org)
  • This entails all parts of the streams, but also during formulation and transport of the solvent.In this work the extended UNIQUAC thermodynamic model is presented with the addition of piperazine (PZ or PIPH2) in combination with the potassium ion of mixtures with CO2 in equilibration with KOH-KHCO3-K2CO3. (dtu.dk)
  • This response is rapidly blocked by dilute solutions of piperazine. (ajtmh.org)
  • A straightforward procedure is described for the synthesis of piperazines from amines and 1,2‐diols. (dtu.dk)
  • H. S. Patel, H. D. Desai, and H. J. Mistry, "Synthesis and Antimicrobial Activity of Some New Piperazine Derivaties Containing Aryl Sulfonyloxy Group," E-Journal of Chemistry , vol. 1, no. 2, pp. 93-98, 2004. (hindawi.com)
  • Piperazine Anhydrous use in corrosion inhibitor. (indiamart.com)
  • Piperazine Anhydrous use in anthelmintic. (indiamart.com)
  • Piperazine Anhydrous use in insecticide, accelerator for curing polychloroprene. (indiamart.com)
  • An anthelmintic, piperazine is mostly free of pharmacologic action in the host. (ratguide.com)
  • the pH of a 10% aqueous solution of piperazine is 10.8-11.8. (wikipedia.org)
  • n-benzyl piperazine manufacturers and suppliers with contacts and product range are mentioned in the study. (marketpublishers.com)
  • 1-(Methylsulfonyl)piperazine is employed as a intermediate for pharmaceutical and chemical research. (alfa.com)
  • Piperazine-based CCR5 antagonists as HIV-1 inhibitors. (nih.gov)
  • Various salts of piperazine ( more stable than piperazine) belong to low toxicity, efficient drive roundworm medicine, in addition to roundworms, also having impact on Oesophagostomum, pointed filaria , it has been widely used in veterinary clinic. (chemicalbook.com)
  • Simple N -substituted piperazines are found in numerous drug molecules. (sigmaaldrich.com)
  • We provide independent and unbiased information on manufacturers, prices, production news and consumers for the global and regional (North America, Asia and Europe) market of Piperazine-2-carboxylic acid dihydrochloride. (reportsnreports.com)
  • Research and Markets has announced the addition of the 'Global Market Report On Piperazine, 1-Acetyl-4-(Hydroxy-Nno-Azoxy)- (9Ci) 2016' report to their offering. (prnewswire.co.uk)
  • Deerfield, FL -- ( SBWIRE ) -- 05/17/2016 -- Global 1,4-Dimethyl-piperazine Industry 2016 Market Research Report was a professional and depth research report on Global 1,4-Dimethyl-piperazine industry that you would know the world's major regional market conditions of 1,4-Dimethyl-piperazine industry, the main region including North American, Europe and Asia etc, and the main country including United States ,Germany ,Japan and China etc. (sbwire.com)
  • The chemical composition of substances sold as piperazines are changing all the time, which is why you can never be sure of what you're getting and how it could affect you. (talktofrank.com)
  • Piperazines were originally named because of their chemical similarity with piperidine, part of the structure of piperine in the black pepper plant (Piper nigrum). (wikipedia.org)
  • The stimulant effects of piperazines are similar to MDMA ( ecstasy ) but dose for dose they are not as potent. (talktofrank.com)
  • Despite the use of some piperazines as tranquilizers, BZP is a stimulant. (narconon.org)
  • i want to define aMDEA in promax, when i use MDEA as amine, every thing is ok, but when i enter MDEA and piperazine in component list, the flowsheet doesnt run, could someone help me? (cheresources.com)
  • Amine blends that are activated by concentrated piperazine are used extensively in commercial CO2 removal for carbon capture and storage (CCS) because piperazine advantageously allows for protection from significant thermal and oxidative degradation at typical coal flue gas conditions. (wikipedia.org)
  • Piperazine is an amine which is used both as an activator or promoter, but also as active component in CO2 capture solvents. (dtu.dk)
  • Piperazine readily absorbs water and carbon dioxide from the air. (wikipedia.org)
  • Piperazine is freely soluble in water and ethylene glycol, but insoluble in diethyl ether. (wikipedia.org)
  • Piperazines are also sold as an off-white powder, in capsules and as a liquid. (talktofrank.com)
  • Immersion of motile specimens of Ascaris lumbricoides in piperazine solutions gradually results in paralysis of the worms. (ajtmh.org)
  • This evidence indicates that piperazine produces paralysis of Ascaris by blocking the neuromuscular junction. (ajtmh.org)
  • This observation can account for the therapeutic effectiveness of piperazine against Ascaris. (ajtmh.org)
  • Mixing piperazines with alcohol can be particularly dangerous - the effects of these two substances interact, and you may also be less in control, making use much riskier. (talktofrank.com)