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
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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-(6-bromo-2-pyridyl)piperazine, 97% 1g Alfa Aesar™ 4-Boc-1-(6-bromo-2-pyridyl)piperazine, 97% Bistriphenyl to Boch -Organics
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™ 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. ...
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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.
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RAD51 is a key protein in the homologous recombination (HR) pathway of DNA double-strand break repair, and HR represents a novel target for cancer therapy. Because imatinib (Gleevec) has been reported to reduce RAD51 protein levels, we tested the clonogenic survival for RT112, H1299, PANC1, and PC3 tumor cell lines of varying p53 status and normal GM05757 normal fibroblasts after exposure to single agent imatinib (0-20 micromol/L; 0-72 hours). We also combined imatinib with DNA damaging agents that are toxic to RAD51-deficient cells, including ionizing radiation, gemcitabine, and mitomycin C. We observed decreased nuclear expression and chromatin binding of RAD51 protein following imatinib treatment. Imatinib also resulted in decreased error-free HR as determined by a flow cytometry-based integrated direct repeat-green fusion protein reporter system; this correlated to reduced RAD51 expression. Clonogenic survival experiments revealed increased cell kill for imatinib-treated cells in combination with
RAD51 is a key protein in the homologous recombination (HR) pathway of DNA double-strand break repair, and HR represents a novel target for cancer therapy. Because imatinib (Gleevec) has been reported to reduce RAD51 protein levels, we tested the clonogenic survival for RT112, H1299, PANC1, and PC3 tumor cell lines of varying p53 status and normal GM05757 normal fibroblasts after exposure to single agent imatinib (0-20 micromol/L; 0-72 hours). We also combined imatinib with DNA damaging agents that are toxic to RAD51-deficient cells, including ionizing radiation, gemcitabine, and mitomycin C. We observed decreased nuclear expression and chromatin binding of RAD51 protein following imatinib treatment. Imatinib also resulted in decreased error-free HR as determined by a flow cytometry-based integrated direct repeat-green fusion protein reporter system; this correlated to reduced RAD51 expression. Clonogenic survival experiments revealed increased cell kill for imatinib-treated cells in combination with
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
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Narconon states that other synthetic drugs used in clubs, or which are sold as "Ecstasy", include harmaline; piperazines (e.g ... piperazines (e.g., BZP and TFMPP); PMA/PMMA; mephedrone (generally used outside the US) and MDPV. Though far less common than ...
Alkylation with one equivalent of piperazine gives 1-(4-Chlorobenzhydryl)piperazine [303-26-4] (4). Alkylation of the remaining ... II.1Unsymmetrical 1,4-Disubstituted Piperazines". Journal of the American Chemical Society. 71 (8): 2731-2734. doi:10.1021/ ... "UNSYMMETRICALLY DISUBSTITUTED PIPERAZINES. III. N-METHYL-N'-BENZHYDRYLPIPERAZINES AS HISTAMINE ANTAGONISTS1". The Journal of ...
Piperazines (mCPP, TFMPP, etc.) Tryptamines (5-MeO-DMT, Bufotenin, DMT, Psilocin, etc.) Ro60-0175 Vabicaserin WAY-629 WAY- ... "Behavioral Effects of a Novel Benzofuranyl-Piperazine Serotonin-2C Receptor Agonist Suggest a Potential Therapeutic Application ...
Yohimbine Piperazines: DBL-583 • GBR-12,935 • Nefazodone • Vanoxerine Piperidines: 1-(1-(1-Benzothiophen-2-yl)cyclohexyl) ... Zylofuramine Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine ( ...
Aryl-piperazine derivatives)". Progress in Neuro-Psychopharmacology & Biological Psychiatry. 16 (6): 833-45. doi:10.1016/0278- ...
Substituted piperazine Rotzinger S, Bourin M, Akimoto Y, Coutts RT, Baker GB (August 1999). "Metabolism of some "second"- and " ... "1-(3-chlorophenyl) piperazine (mCPP) - Expert peer review on pre-review report" (PDF). Retrieved 2021-01-12.{{cite web}}: CS1 ... Rajkumar R, Pandey DK, Mahesh R, Radha R (April 2009). "1-(m-Chlorophenyl)piperazine induces depressogenic-like behaviour in ... Elliott S (2011). "Current awareness of piperazines: pharmacology and toxicology". Drug Test Anal. 3 (7-8): 430-8. doi:10.1002/ ...
"Indanyl piperazines as melatonergic MT2 selective agents". Bioorganic & Medicinal Chemistry Letters. 13 (6): 1199-202. doi: ...
Cignarella G, Occelli E, Cristiani G, Paduano L, Testa E (November 1963). "Bicyclic Homologs of Piperazine. VI.1Synthesis and ... Cignarella G, Occelli E, Testa E (May 1965). "Bicyclic Homologs of Piperazine. VII.1Synthesis and Analgesic Activity of 3- ... "Computer-aided structure-affinity relationships in a set of piperazine and 3,8-diazabicyclo[3.2.1]octane derivatives binding to ...
... (Attentil, Vigilor) is a psychoactive drug of the piperazine chemical class which was developed in Italy in 1983. It ... Gardini, G. P.; Palla, G.; Scapini, G.; Cesaroni, M. R. (2006). "Convenient Synthesis of N-Benzyl-N′-acyl-piperazines". ... PTC alkylation of piperazine (1) with 2 equivalents of piperonyl chloride [25054-53-9] (2) in the presence of cetrimonium ... Substituted piperazine Befuraline Piberaline Missale C, Pasinetti G, Govoni S, Spano PF, Trabucchi M (February 1983). "[ ...
"New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ"". Journal of ...
Simmler LD, Rickli A, Schramm Y, Hoener MC, Liechti ME (March 2014). "Pharmacological profiles of aminoindanes, piperazines, ...
1994). "Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse ... Piperazines, Aminopyridines, All stub articles, Antiinfective agent stubs). ... of the pyridylpiperazine moiety starts by aromatic displacement of chlorine from 2-chloro-3-nitropyridine by piperazine to give ...
Nozaki M, Niwa M, Imai E, Hori M, Fujimura H (1983). "(1,2-Diphenylethyl) piperazines as potent opiate-like analgesics; the ... Nakamura H, Shimizu M (May 1976). "Comparative study of 1-cyclohexyl-4-(1,2-diphenylethyl)-piperazine and its enantiomorphs on ... It is chemically a 1-substituted-4-(1,2-diphenylethyl)piperazine derivative, which is structurally unrelated to most other ... 2. Structure-activity relationships of 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines". Journal of Medicinal Chemistry. 21 (12 ...
Piperazine is the drug of choice. Continuous medication in feed with hygromycin B is also widely employed. Piperazine may be ... 1-3. Pavlícek J, Dyková I (1976). "Tetramisol, piperazine, and metrifonate treatment of experimental invasion by Ascaridia ... piperazine is quite ineffective for young chickens, while tetramisole is 89-100% effective for chicken of different ages. More ...
Such medications include piperazine and pyrantel. These are frequently combined with the drug praziquantel which appears to ...
Piperazine and salts of piperazine are classified as Prescription Only Medicines in the UK. Any products containing salts of ... BZP is not a salt of piperazine, but mislabelling of BZP products as containing "piperazine blend" resulted in some ... BZP is a piperazine derivative which comes as either the hydrochloride salt or a free base. The hydrochloride salt is a white ... Deaths from piperazine derivatives are extremely rare, but there has been at least one death apparently due to BZP alone. Its ...
Piperazine Catalytic method for the conjoint manufacture of N-aminoethylpiperazine Safety MSDS Data Safety data sheet Data ... Aminoethylpiperazine is a derivative of piperazine. This ethyleneamine contains three nitrogen atoms; one primary, one ... Piperazines, Ethyleneamines, All stub articles, Amine stubs). ...
... is a piperazine calcium channel blocker. It is a coronary vasodilator with some antiarrhythmic action. Lidoflazine ... piperazine [5631-35-6]. Acylation of 2,6-xylidine (4) with chloroacetyl chloride (5) gives N-chloroacetyl-2,6-xylidine [1131-01 ... Piperazines, HERG blocker, Calcium channel blockers, Acetanilides, Fluoroarenes, Janssen Pharmaceutica, Belgian inventions, All ...
It is made from 4-methyl-piperazine. Diethylcarbamazine was discovered in 1947 by Yellapragada Subbarow. It is on the World ... Piperazines, Ureas, Wikipedia medicine articles ready to translate, World Health Organization essential medicines). ...
Substituted piperazine "www.emcdda.europa.eu" (PDF).[dead link] Fuller RW, Snoddy HD (July 1980). "Comparative effects of p- ... It has been encountered in illicit capsules as a recreational drug similarly to other piperazines like mCPP. Scientific ... chloroamphetamine and 1-(p-chlorophenyl)piperazine on 5-hydroxyindole concentration in rat brain". Research Communications in ...
MCI3434 acting on piperazine-2-tert-butylcarboxamide". European Journal of Biochemistry. 271 (8): 1580-90. CiteSeerX 10.1.1.547 ... R)-amidase (EC 3.5.1.100, R-stereospecific amidase, R-amidase) is an enzyme with systematic name (R)-piperazine-2-carboxamide ... This enzyme catalyses the following chemical reaction (1) (R)-piperazine-2-carboxamide + H2O ⇌ {\displaystyle \ ... rightleftharpoons } (R)-piperazine-2-carboxylic acid + NH3 (2) beta-alaninamide + H2O ⇌ {\displaystyle \rightleftharpoons } ...
Unlike the related piperazine compound meta-chlorophenylpiperazine (mCPP), TFMPP has insignificant affinity for the 5-HT3 ... Yarosh HL, Katz EB, Coop A, Fantegrossi WE (November 2007). "MDMA-like behavioral effects of N-substituted piperazines in the ... Baumann MH, Clark RD, Budzynski AG, Partilla JS, Blough BE, Rothman RB (March 2005). "N-substituted piperazines abused by ... Antrafenine CPD-1 Substituted piperazine "Ustawa z dnia 15 kwietnia 2011 r. o zmianie ustawy o przeciwdziałaniu narkomanii ( Dz ...
Piperazine is present in prazosin, terazosin and doxazosin which seems to contribute to the non-selective inhibition of alpha-1 ... 2. Role of the piperazine ring on .alpha.-blocking activity". Journal of Medicinal Chemistry. 36 (6): 690-698. doi:10.1021/ ...
1-(2-Pyridinyl)piperazine is a chemical compound and piperazine derivative. Some derivatives of this substance are known to act ... Piperazines, 2-Pyridyl compounds, All stub articles, Organic compound stubs). ... "Synthesis and Pharmacological Study of New Piperazine Derivatives. I. Benzylpiperazines". Journal of Medicinal Chemistry. 6 (5 ... as potent and selective α2-adrenergic receptor antagonists, such as 1-(3-fluoro-2-pyridinyl)piperazine. A few ...
August 2001). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element ... The changes that were made on the left hand side of the lead compound and the addition of a methyl group on the piperazine ... October 2001). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]- ... May 2004). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4 ...
... is an antiparkinsonian agent and piperazine derivative which acts as a D2 and D3 receptor agonist. It also has α2-adrenergic ... "Synthesis and vasodilator activity of new piperazine derivatives". Journal of Medicinal Chemistry. 11 (6): 1151-1155. doi: ...
Erowid Experience Vaults: Piperazines - pFPP - Refreshing Enhancement - 62575 Erowid Experience Vaults: Piperazines - pFPP - A ... Antia U, Tingle MD, Russell BR (July 2009). "Metabolic interactions with piperazine-based 'party pill' drugs". The Journal of ... para-Fluorophenylpiperazine (pFPP, 4-FPP, 4-Fluorophenylpiperazine; Fluoperazine, Flipiperazine) is a piperazine derivative ... Substituted piperazine "Ustawa z dnia 15 kwietnia 2011 r. o zmianie ustawy o przeciwdziałaniu narkomanii ( Dz.U. 2011 nr 105 ...
Substituted piperazine Befuraline Fipexide Tekes K, Tóthfalusi L, Malomvölgyi B, Hermán F, Magyar K (1987). "Studies on the ... Piberaline (EGYT-475; Trelibet) is a psychoactive drug and member of the piperazine chemical class which was developed in the ... Younes, S (2000). "Synthesis and structure-activity relationships of novel arylalkyl 4-benzyl piperazine derivatives as σ site ... Piperazines, Carboxamides, 2-Pyridyl compounds, Serotonin-norepinephrine-dopamine releasing agents, All stub articles, ...
New Conjugated Systems Derived from Piperazine-2,5-dione. Molecules 2000, 5, 629-636 Cara E. Humphrey, Markus Furegati, Kurt ...
Blier P, Curet O, Chaput Y, de Montigny C (July 1991). "Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. ... piperazine (1-PP). Tandospirone has also been known as metanopirone. The Noreximide [6319-06-8] precursor also has dual uses to ... piperazine". Journal of Clinical Psychopharmacology. 12 (5): 341-345. doi:10.1097/00004714-199210000-00009. PMID 1362206. S2CID ...
OSHA had no limit for piperazine dihydrochloride. The ACGIH recommends a TLV-TWA limit of 5 mg/m3. The proposed PEL was an 8- ... Piperazine dihydrochloride is a solid.. Piperazine dihydrochloride is a water-soluble solid with low systemic toxicity and mild ... In the final rule, OSHA is establishing a limit of 5 mg/m3 as an 8-hour TWA for piperazine dihydrochloride. The Agency ... Previously, OSHA had no limit for piperazine dihydrochloride. The ACGIH recommends a TLV-TWA limit of 5 mg/m3. The proposed PEL ...
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... Molecular Formula: C14H28N2O2S ...
... piperazine; CAS No.: 70931-28-1; Linear Formula: C11H15FN2; Empirical Formula: C11H15FN2; find related products, papers, ...
Resources relating to Synthesis of Homochiral 2-(2-Arylethyl) piperazines ...
... piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention ... Piperazine salts as d3/d2 antagonists PL08750834T PL2155696T3 (en) 2007-05-11. 2008-05-13. Piperazine salts as d3/d2 ... Piperazine salts as d3/d2 antagonists HRP20170918TT HRP20170918T1 (en) 2007-05-11. 2017-06-16. Piperazine salts as d3/d2 ... EP2155696A2 - Piperazine salts as d3/d2 antagonists - Google Patents. Piperazine salts as d3/d2 antagonists Info. Publication ...
This page contains information on the chemical Piperazine, 1-(diphenylmethyl)-4-methyl-, hydrochloride including: 39 synonyms/ ... Piperazine, 1- (diphenylmethyl)-4-methyl-*Piperazine, 1- (diphenylmethyl)-4-methyl-, monohydrochloride*Piperazine, 1-( ... Piperazine, 1-(diphenylmethyl)-4-methyl-, hydrochloride. Identifications. *CAS Number: 303-25-3*Synonyms/Related:*(.+-.)-1- ... Piperazine, 1-(diphenylmethyl)-4-methyl-, hydrochloride*Reis-fit*Valoid*Wellcome*Wellcome preparation 47-83*Wellcome prepn 47- ...
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Wondering if anyone knows the breakdown dosage for Piperazine 52 powder. This is what the container says: Chickens and turkeys ... Wondering if anyone knows the breakdown dosage for Piperazine 52 powder.. This is what the container says:. Chickens and ...
... Molecular Formula: C21H27ClN2 ...
Maes RA Piperazine-like compounds: a new group of designer drugs-of-abuse on the European market Forensic Sci Int 2001 121(1-2 ... piperazine pMeOPP and 1-[3-trifluoromethylphenyl]-piperazine TFMPP were studied. BZP was not detected by the AxSYM FPIA ... 1-Aryl-piperazine compounds are, depending on their substituents, selective for certain serotonin receptors and together with ... "Piperazine-like compounds: a new group of designer drugs-of-abuse on the European market". ...
Find manufacturers and suppliers for 1-Benzyl-3-phenyl-piperazine, 5368-32-1. Synonyms: N4-Benzyl-2-phenylpiperazine; 1-benzyl- ... N4-Benzyl-2-phenylpiperazine; 1-benzyl-3-phenylpiperazine; piperazine, 3-phenyl-1-(phenylmethyl)- ...
The Prophylactic and Curative Activity of 1-Maleinyl-4-(3′-Chloro-4′-Methyl-Phenyl)-Piperazine (Hoechst S 688) in Experimental ... Oral regimens of the compound 1-maleinyl-4-(3′-chloro-4′-methyl-phenyl)-piperazine (Hoechst S 688) were found to have a strong ... The Prophylactic and Curative Activity of 1-Maleinyl-4-(3′-Chloro-4′-Methyl-Phenyl)-Piperazine (Hoechst S 688) in Experimental ...
1-[(2-Chlorophenyl)phenylmethyl]piperazine is a novel compound derived from the previously reported N-type calcium channel ...
Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U- ... Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U- ...
3-(4-Boc-Piperazine-1-carbonyl)phenyl]boronic acid pinacol ester 883738-41-8 from AK Scientific, in San Francisco, California ... 3-(4-Boc-Piperazine-1-carbonyl)phenyl]boronic acid pinacol ester. , 98%. Add to Favorites ...
... thien-4-yl-piperazine hydrochloride CAS 913614-18-3 Brexpiprazole intermediate ...
Piperazine. 384 Karen June 23, 2003 at 15:57. (last edited September 6, 2020 at 15:30. ) ...
Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma‑1 Receptor Antagonists ... where piperidine is replaced by piperazine. We identified the putative protein−ligand interactions responsible for their high ...
We also provide custom synthesis and GMP manufacturing services.where to buy Piperazines ... where to buy Piperazines, Chemenu is research-based manufacturer of pharmaceutical intermediates and fine chemicals offering ... Piperazines. Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite ... The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines ...
N-(3-Trifluoromethylphenyl)piperazine. 15532-75-9. Please Enquire. N-[2-Nitro-4-(trifluoromethyl)phenyl]piperazine. 58315-38-1 ... 1-(4-Fluoro-2-nitrophenyl)piperazine. 243128-46-3. Please Enquire. 1-[3-Chloro-5-(trifluoromethyl)-2-pyridinyl]piperazine. ... 3-(4-Methyl-piperazine-1-carbonyl)-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid. 436811-00-6. Please Enquire. ... 1-(Toluene-4-sulfonyl)-piperazine. 27106-51-0. Please Enquire. 1-Cyclohex-3-enylmethyl-piperazinetrifluoroacetate. 436099-82-0 ...
Sethi AS, Jain AM, Chawla V. Piperazine toxicity. Report of a case. Indian Journal of Pediatrics. 1968 May; 35(244): 237-8. ...
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Piperazine Citrate) for Horses, Cattle, Cows, Lamb, Sheep, Dogs, Cats ... Usage and dosage for Piperazine. Piperazine may be administered with drinking water : Cows, horses,sheeps: 6 g / 10 kg b.w ... Indications of Piperazine. For prevention and treatment of intestinal roundworms (oxyures, small oesophagostomes, strongylides ...
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Moghadam, E. S., Al-Sadi, A. M., Talebi, M., Amanlou, M., Shongwe, M., Amini, M., & Abdel-Jalil, R. (2022). Piperazine-based ... Moghadam, ES, Al-Sadi, AM, Talebi, M, Amanlou, M, Shongwe, M, Amini, M & Abdel-Jalil, R 2022, Piperazine-based Semicarbazone ... Piperazine-based Semicarbazone Derivatives as Potent Urease Inhibitors: Design, Synthesis, and Bioactivity Screening. Letters ... Piperazine-based Semicarbazone Derivatives as Potent Urease Inhibitors : Design, Synthesis, and Bioactivity Screening. In: ...
Get 2-(R)-4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide ... piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide. ... 2-(R)-4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide. ... 2-(R)-4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide Properties. ...
Buy high quality Palbociclib Piperazine N-Oxide from SynZeal Research PVT LTD. CAS 2174002-29-8,463.5,C24H29N7O3 ... This page contains information about Palbociclib Piperazine N-Oxide. ...
  • Previously, OSHA had no limit for piperazine dihydrochloride. (cdc.gov)
  • Piperazine dihydrochloride is a solid. (cdc.gov)
  • In the final rule, OSHA is establishing a limit of 5 mg/m 3 as an 8-hour TWA for piperazine dihydrochloride. (cdc.gov)
  • We value your input so if you have suggestions regarding new applications for (S)-(-)-PIPERAZINE-2-CARBOXYLIC ACID DIHYDROCHLORIDE email us and we will include your contribution on the website. (discofinechem.com)
  • Oral regimens of the compound 1-maleinyl-4-(3′-chloro-4′-methyl-phenyl)-piperazine (Hoechst S 688) were found to have a strong chemotherapeutic effect on mature infections of Schistosoma mansoni (Puerto Rican) in white mice and monkeys. (ajtmh.org)
  • Methods: A series of piperazine-based semicarbazone derivatives 5a-o were synthesized and isolated, and their structures were elucidated by 1 H-NMR and 13 C-NMR spectroscopic techniques besides MS and elemental analysis. (elsevier.com)
  • Based on the recommendation of the EACD, the New Zealand government has passed legislation which placed BZP, along with the other piperazine derivatives TFMPP, mCPP, pFPP, MeOPP and MBZP, into Class C of the New Zealand Misuse of Drugs Act 1975. (wikipedia.org)
  • Antihistamines : H1-antagonists with classical structure :Piperazines derivatives - Synthesis and Drug Profile - i. (pharmacy180.com)
  • The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. (chemenu.com)
  • Piperazines are a broad class of chemical compounds used widely in human and veterinary medicines. (knowthescore.info)
  • 3-Trifluoromethylphenylpiperazine ( TFMPP ) is a recreational drug of the piperazine chemical class . (wikipedia.org)
  • studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity. (chemenu.com)
  • Because this development may have consequences for the interpretation of future clinical and forensic toxicological case studies, some analytical aspects of 1-benzyl-piperazine BZP, 1-[4-methoxyphenyl]-piperazine pMeOPP and 1-[3-trifluoromethylphenyl]-piperazine TFMPP were studied. (erowid.org)
  • [4] Unlike the related piperazine compound meta -chlorophenylpiperazine (mCPP), TFMPP has insignificant affinity for the 5-HT 3 receptor (IC 50 = 2,373 nM). (wikipedia.org)
  • Studies into other related piperazine drugs such as mCPP suggest that certain side effects such as anxiety , headache and nausea are common to all drugs of this class, and pills containing TFMPP are reported by users to produce comparatively more severe hangover effects than those containing only BZP. (wikipedia.org)
  • "Piperazine-like compounds: a new group of designer drugs-of-abuse on the European market" Forensic Sci Int . 2001 Sep 22;121(1-2):47-56. (erowid.org)
  • 1-Aryl-piperazine compounds are, depending on their substituents, selective for certain serotonin receptors and together with their easy availability and their so-called legal status, this group of psychoactive compounds are potential designer drugs-of-abuse. (erowid.org)
  • It is most likely a critical structural element for dual H3/σ1 receptor activity as can be seen by comparing the data for compounds 4 and 5 (hH3R Ki = 3.17 and 7.70 nM, σ1R Ki = 1531 and 3.64 nM, respectively), where piperidine is replaced by piperazine. (ugr.es)
  • Some piperazine compounds act as effective worming agents for pets and farm animals. (knowthescore.info)
  • Wondering if anyone knows the breakdown dosage for Piperazine 52 powder. (backyardchickens.com)
  • DISTRIBUTOR FOR PHARMA / AGRO CHEMICALS, GACL Aluminium Chloride Granular Powder, Benzyl Methyl Piperazine. (needsinfo.com)
  • Research Chemicals Manufacturer of 1,4-(Diacryloyl)Piperazine Extrapure, 1,3,5-Tribromobenzene Pure, 1-Amino-2-Naphthol-4-Sulphonic Acid Extrapure AR,1-Naphthylacetonitirile 4 Chlorobenzhydrol. (needsinfo.com)
  • Impinger sampling with 1-(2- methoxyphenyl)piperazine (MOPIP) in toluene and solid sorbent sampling with a TR coated XAD-2 resin were compared with impinger sampling with TR in dimethyl-sulfoxide (DMSO). (cdc.gov)
  • Collection is carried out by passing sampled air through toluene containing l-(2-methoxyphenyl)-piperazine to derivatize the HDI. (cdc.gov)
  • Another derivatization agent used was 1-(2-pyridyl)piperazine either in a toluene solution (Ellwood et al. (cdc.gov)
  • Aminoethylpiperazine is a derivative of piperazine. (researchreporthub.com)
  • A benzofuran, indole, and piperazine derivative that functions as a SEROTONIN UPTAKE INHIBITOR and partial SEROTONIN 5-HT1 RECEPTOR AGONIST. (bvsalud.org)
  • The 1-(2-methoxyphenyl)- piperazine used as a derivatization reagent in the NIOSH methods was also used on a sorbent (Schmidtke and Seifert 1990) and inert supports (Huynh et al. (cdc.gov)
  • Available Ready Stocks Mono ethylene glycol (MEG), Propylene glycol (PG), Diethylene glycol Methyl Piperazine. (needsinfo.com)
  • 1-[(2-Chlorophenyl)phenylmethyl]piperazine is a novel compound derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one). (trc-canada.com)
  • Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. (chemenu.com)
  • The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group . (mdwiki.org)
  • MANUFACTURERS & EXPORTER OF 2-Methyl 5-Nitro Aniline Acrylic Acid Adipic Acid Alpha Methyl Piperazine. (needsinfo.com)
  • Manufacturing Pharma Raw Materials, 1,2-Di Methoxy Ethane (Monoglyme) 1,4-Dioxane 2,4-Dichlorobenzyl chloride 2-Methyl Methyl Piperazine. (needsinfo.com)
  • Importer & Dealer for Pharma, Pigment Raw Materials & Industrial Chemicals, Acrylic Methyl Piperazine. (needsinfo.com)
  • Piperazine citrate is used as a second-line treatment for treating roundworm infections caused by Ascaris lumbricoides and pinworm infections caused by Enterobius vermicularis (oxyuris). (medindia.net)
  • Diethylcarbamazine and piperazine citrate stops th. (curezone.com)
  • Piperazine citrate is a anti-parasitic. (curezone.com)
  • 1-[bis(4-fluorophenyl)methyl]piperazine (OR) 4,4′-Difluorobenzhydrylpiperazine. (mumglobal.com)
  • Description 1-(3-Trifluoromethylphenyl)-piperazine.HCl (TFMPP.HCl) Product reference number PPZ-971-HC Full chemical name N-(3-Trifluoromethylphenyl)-piperazine.hydrochloride Formula C11H13F3N2.HCl Molecular weight 266.69 Chemical abstract number 16015-69-3 Supplied as hydrochloride s. (lipomed-usa.com)
  • We are supplier of N-(2-Hydroxyethyl)piperazine CAS:103-76-4,We offer custom synthesis of various chemical compounds like 2-(1-Piperazinyl)ethanol CAS:103-76-4 and custom manufacturing of 4-(2-hydroxyethyl)-piperazine, please feel free to contact us for your demand of 2-(1-Piperazinyl)ethanol,suppose you are looking for 1-(2-Hydroxyethyl)piperazine factory, producer or manufacturer. (dearchem.com)
  • Li, WR & Yang, JH 2002, ' Solid-phase synthesis of unsaturated 3-substituted piperazine-2,5-diones ', Journal of Combinatorial Chemistry , vol. 4, no. 2, pp. 106-108. (ncu.edu.tw)
  • Synthesis and Characterization of a Series of 1-Aryl-4-[aryldiazenyl]- piperazines. (benthamopen.com)
  • 1. Design, synthesis and biological evaluation of rhein-piperazine-dithiocarbamate hybrids as potential anticancer agents. (nih.gov)
  • 2. Design, Synthesis, and Biological Evaluation of Artemisinin-Piperazine-Phosphoramide Mustard Hybrids as Potential Anticancer Agents. (nih.gov)
  • Here we tested a variety of 1,4-disubstituted aromatic piperidines/piperazines (1,4-DAPs) with different subtype selectivities and functional properties against a panel of D4 receptor mutations in the aromatic microdomain to ascertain whether these ligands recognize this common site. (aspetjournals.org)
  • Buy 73874-95-0, 4-N-BOC-AminopiperidinePyrans, Piperidines&Piperazines Product on Hanhong Pharmaceutical Technology (Hubei)Co., Ltd. (hanhong-hh.net)
  • 1-[2-(2-Hydroxyethoxy)ethyl]piperazine is used in the preparation of pharmaceutical compounds. (suryaremedies.in)
  • 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)
  • Contains an E3 ligase ligand with alkyl linker and a terminal piperazine moiety. (tenovapharma.com)
  • Despite the use of some piperazines as tranquilizers, BZP is a stimulant. (narconon.org)
  • Due to their stimulant properties piperazines are often sold as MDMA. (adf.org.au)
  • 1-(m-chlorophenyl)piperazine (mCPP) dissociates in vivo serotonin rele. (erowid.org)
  • Vistaril, a drug with the generic name of Hydroxyzine, is an antihistamine under diphenylmethane and piperazine drug class. (drug.education)
  • Our offered Piperazine Adipate Powder is tested on various quality parameters and can be availed at highly competitive price by us. (adanipharmachem.com)
  • S)-PIPERAZINE-1,3-DICARBOXYLIC ACID 1-BENZYL ESTER Anbieter Lieferant Produzent Hersteller Vertrieb Händler. (chemicalbook.com)
  • The 1-(2-methoxyphenyl)- piperazine used as a derivatization reagent in the NIOSH methods was also used on a sorbent (Schmidtke and Seifert 1990) and inert supports (Huynh et al. (cdc.gov)
  • Genetic Toxicity Evaluation of Piperazine in Salmonella/E.coli Mutagenicity Test or Ames Test. (nih.gov)
  • Beschreibung 1-(4-Chlorophenyl)-piperazine.HCl (pCPP.HCl) Product reference number PPZ-1097-HC Full chemical name 1-(para-Chlorophenyl)piperazine.monohydrochloride Formula C10H13N2Cl.HCl Molecular weight 233.14 Chemical abstract number 1307. (lipomed-shop.com)
  • If you know of a relevant reference for Lenalidomide 5'-piperazine-4-methylpiperidine, please let us know . (tocris.com)
  • Currently there are no citations for Lenalidomide 5'-piperazine-4-methylpiperidine. (tocris.com)
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  • Have you used Lenalidomide 5'-piperazine-4-methylpiperidine? (tocris.com)
  • Our 1-[2-(2-Hydroxyethoxy)ethyl]piperazine is offered in various customized packaging for our clients. (suryaremedies.in)
  • https://pubchem.ncbi.nlm.nih.gov/compound/N-(2-Hydroxyethyl)piperazine. (vibratist.com)
  • Both chemisorption and physisorption are suggested as mechanism in which the chemisorption is based on an acid-base reaction between H2S and amine, epoxy, hydroxyl functional groups on the surface of RGO-N-(piperazine), GO, and RGO. (swan.ac.uk)
  • tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially piperazine (another antiworm medication), and vitamins. (medlineplus.gov)
  • 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 is a drug with wide margin of safety, occasionally an animal may show nausea, vomiting, or muscular tremors. (nih.gov)