A family of hexahydropyridines.
Specific sites or molecular structures on cell membranes or in cells with which phencyclidine reacts or to which it binds to elicit the specific response of the cell to phencyclidine. Studies have demonstrated the presence of multiple receptor sites for PCP. These are the PCP/sigma site, which binds both PCP and psychotomimetic opiates but not certain antipsychotics, and the PCP site, which selectively binds PCP analogs.
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.
A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.
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)
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms.
Sugars in which the OXYGEN is replaced by a NITROGEN atom. This substitution prevents normal METABOLISM resulting in inhibition of GLYCOSIDASES and GLYCOSYLTRANSFERASES.
The creation of an amine. It can be produced by the addition of an amino group to an organic compound or reduction of a nitro group.
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 nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
Organic compounds that contain silicon as an integral part of the molecule.
An alkaloid that has actions similar to NICOTINE on nicotinic cholinergic receptors but is less potent. It has been proposed for a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation.
A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
The geographic designation for states bordering on or located in the Pacific Ocean. The states so designated are Alaska, California, Hawaii, Oregon, and Washington. (U.S. Geologic Survey telephone communication)
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 class of organic compounds containing two ring structures, one of which is made up of more than one kind of atom, usually carbon plus another atom. The heterocycle may be either aromatic or nonaromatic.
Compounds possessing both a hydroxyl (-OH) and an amino group (-NH2).
A specific subtype of muscarinic receptor that has a high affinity for the drug PIRENZEPINE. It is found in the peripheral GANGLIA where it signals a variety of physiological functions such as GASTRIC ACID secretion and BRONCHOCONSTRICTION. This subtype of muscarinic receptor is also found in neuronal tissues including the CEREBRAL CORTEX and HIPPOCAMPUS where it mediates the process of MEMORY and LEARNING.
A plant species of the genus PINUS that contains isocupressic acid.
An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
The characteristic three-dimensional shape of a molecule.
An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Compounds containing the PhCH= radical.
N-acylated oligopeptides isolated from culture filtrates of Actinomycetes, which act specifically to inhibit acid proteases such as pepsin and renin.
A foul-smelling diamine formed by bacterial decarboxylation of lysine.
Compounds based on benzene fused to oxole. They can be formed from methylated CATECHOLS such as EUGENOL.
Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
The relationship between the dose of an administered drug and the response of the organism to the drug.
One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
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.
The univalent radical OH. Hydroxyl radical is a potent oxidizing agent.
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)
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).
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)
Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
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.
Delivery of drugs into an artery.
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.
One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
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.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
The first branch of the SUBCLAVIAN ARTERY with distribution to muscles of the NECK; VERTEBRAE; SPINAL CORD; CEREBELLUM; and interior of the CEREBRUM.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
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.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
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.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
The rate dynamics in chemical or physical systems.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
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.
A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).
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.
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 sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A sub-subclass of endopeptidases that depend on an ASPARTIC ACID residue for their activity.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Injections made into a vein for therapeutic or experimental purposes.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The physical activity of a human or an animal as a behavioral phenomenon.

Inhibition of in vitro enteric neuronal development by endothelin-3: mediation by endothelin B receptors. (1/5317)

The terminal colon is aganglionic in mice lacking endothelin-3 or its receptor, endothelin B. To analyze the effects of endothelin-3/endothelin B on the differentiation of enteric neurons, E11-13 mouse gut was dissociated, and positive and negative immunoselection with antibodies to p75(NTR )were used to isolate neural crest- and non-crest-derived cells. mRNA encoding endothelin B was present in both the crest-and non-crest-derived cells, but that encoding preproendothelin-3 was detected only in the non-crest-derived population. The crest- and non-crest-derived cells were exposed in vitro to endothelin-3, IRL 1620 (an endothelin B agonist), and/or BQ 788 (an endothelin B antagonist). Neurons and glia developed only in cultures of crest-derived cells, and did so even when endothelin-3 was absent and BQ 788 was present. Endothelin-3 inhibited neuronal development, an effect that was mimicked by IRL 1620 and blocked by BQ 788. Endothelin-3 failed to stimulate the incorporation of [3H]thymidine or bromodeoxyuridine. Smooth muscle development in non-crest-derived cell cultures was promoted by endothelin-3 and inhibited by BQ 788. In contrast, transcription of laminin alpha1, a smooth muscle-derived promoter of neuronal development, was inhibited by endothelin-3, but promoted by BQ 788. Neurons did not develop in explants of the terminal bowel of E12 ls/ls (endothelin-3-deficient) mice, but could be induced to do so by endothelin-3 if a source of neural precursors was present. We suggest that endothelin-3/endothelin B normally prevents the premature differentiation of crest-derived precursors migrating to and within the fetal bowel, enabling the precursor population to persist long enough to finish colonizing the bowel.  (+info)

Role of endothelin in the increased vascular tone of patients with essential hypertension. (2/5317)

We investigated the possible role of endothelin in the increased vasoconstrictor tone of hypertensive patients using antagonists of endothelin receptors. Forearm blood flow (FBF) responses (strain-gauge plethysmography) to intraarterial infusion of blockers of endothelin-A (ETA) (BQ-123) and endothelin-B (ETB) (BQ-788) receptors, separately and in combination, were measured in hypertensive patients and normotensive control subjects. In healthy subjects, BQ-123 alone or in combination with BQ-788 did not significantly modify FBF (P=0.78 and P=0.63, respectively). In hypertensive patients, in contrast, BQ-123 increased FBF by 33+/-7% (P<0.001 versus baseline), and the combination of BQ-123 and BQ-788 resulted in a greater vasodilator response (63+/-12%; P=0.006 versus BQ-123 alone in the same subjects). BQ-788 produced a divergent vasoactive effect in the two groups, with a decrease of FBF (17+/-5%; P=0.004 versus baseline) in control subjects and transient vasodilation (15+/-7% after 20 minutes) in hypertensive patients (P<0.001, hypertensives versus controls). The vasoconstrictor response to endothelin-1 was slightly higher (P=0.04) in hypertensive patients (46+/-4%) than in control subjects (32+/-4%). Our data indicate that patients with essential hypertension have increased vascular endothelin activity, which may be of pathophysiological relevance to their increased vascular tone. In these patients, nonselective ETA and ETB blockade seems to produce a greater vasodilator effect than selective ETA blockade.  (+info)

Comparison of functional antagonism between isoproterenol and M2 muscarinic receptors in guinea pig ileum and trachea. (3/5317)

The ability of the M2 muscarinic receptor to mediate an inhibition of the relaxant effects of forskolin and isoproterenol was investigated in guinea pig ileum and trachea. In some experiments, trachea was first treated with 4-diphenylacetoxy-N-methylpiperidine (4-DAMP) mustard to inactivate M3 receptors. The contractile response to oxotremorine-M was measured subsequently in the presence of both histamine (10 microM) and isoproterenol (10 nM). Under these conditions, [[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5, 11-dihydro-6H-pyrido[2,3b]-[1,4]benzodiazepine-6-one (AF-DX 116) antagonized the contractile response to oxotremorine-M in a manner consistent with an M3 mechanism. However, when the same experiment was repeated using forskolin (4 microM) instead of isoproterenol, the response to oxotremorine-M exhibited greater potency and was antagonized by AF-DX 116 in a manner consistent with an M2 mechanism. We also measured the effects of pertussis toxin treatment on the ability of isoproterenol to inhibit the contraction elicited by a single concentration of either histamine (0.3 microM) or oxotremorine-M (40 nM) in both the ileum and trachea. Pertussis toxin treatment had no significant effect on the potency of isoproterenol for inhibiting histamine-induced contractions in the ileum and trachea. In contrast, pertussis toxin treatment enhanced the relaxant potency of isoproterenol against oxotremorine-M-induced contractions in the ileum but not in the trachea. Also, pertussis toxin treatment enhanced the relaxant potency of forskolin against oxotremorine-M-induced contractions in the ileum and trachea. We investigated the relaxant potency of isoproterenol when very low, equi-effective (i.e., 20-34% of maximal response) concentrations of either histamine or oxotremorine-M were used to elicit contraction. Under these conditions, isoproterenol exhibited greater relaxant potency against histamine in the ileum but exhibited similar relaxant potencies against histamine and oxotremorine-M in the trachea. Following 4-DAMP mustard treatment, a low concentration of oxotremorine-M (10 nM) had no contractile effect in either the ileum or trachea. Nevertheless, in 4-DAMP mustard-treated tissue, oxotremorine-M (10 nM) reduced the relaxant potency of isoproterenol against histamine-induced contractions in the ileum, but not in the trachea. We conclude that in the trachea the M2 receptor mediates an inhibition of the relaxant effects of forskolin, but not isoproterenol, and the decreased relaxant potency of isoproterenol against contractions elicited by a muscarinic agonist relative to histamine is not due to activation of M2 receptors but rather to the greater contractile stimulus mediated by the M3 receptor compared with the H1 histamine receptor.  (+info)

Intestinal prokinesia by two esters of 4-amino-5-chloro-2- methoxybenzoic acid: involvement of 5-hydroxytryptamine-4 receptors and dissociation from cardiac effects in vivo. (4/5317)

In five fasting, conscious dogs, we compared the prokinetic action of two selective 5-hydroxytryptamine-4 (5-HT4) receptor agonists with low affinity for 5-HT3 receptors ML10302 (2-piperidinoethyl 4-amino-5-chloro-2-methoxybenzoate) and SR59768 (2-[(3S)-3-hydroxypiperidino]ethyl 4-amino-5-chloro-2-methoxybenzoate) in the duodenum and jejunum, using cisapride as a reference compound. Heart rate and rate-corrected QT (QTc) also were monitored to assess whether or not the cardiac effects of cisapride are shared by other 5-HT4 receptor agonists. Both ML10302 and SR59768 dose-dependently stimulated spike activity in the duodenum with similar potencies (dose range, 3-300 nmol/kg i.v.; ED50 values: 24 and 23 nmol/kg i.v., respectively), mimicking the effect of cisapride (30-3000 nmol/kg i.v.). The maximal effect was achieved with the dose of 100 nmol/kg i.v. for both compounds. Similar findings were obtained in the jejunum. Atropine and GR125487 (1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl-methyl 5-fluoro-2-methoxy-1H-indole-3-carboxylate, selective 5-HT4 receptor antagonist), at doses having no effect per se, antagonized intestinal prokinesia by maximal doses of ML10302 and SR59768. Neither ML10302 nor SR59768 had any effect on heart rate or QTc at any of the doses tested, whereas cisapride, at the highest dose (3000 nmol/kg), induced tachycardia and lengthened the QTC (p <.01). In conclusion, ML10302 and SR59768 share with cisapride a similar prokinetic action in the canine duodenum and jejunum in vivo. This effect is mediated by pathways involving activation of 5-HT4 and muscarinic receptors. Unlike cisapride, which induces tachycardia and prolongs the QTc by a mechanism probably unrelated to 5-HT4 receptor activation, ML10302 and SR59768 are devoid of cardiac effects in this model.  (+info)

Development of muscarinic analgesics derived from epibatidine: role of the M4 receptor subtype. (5/5317)

Epibatidine, a neurotoxin isolated from the skin of Epipedobates tricolor, is an efficacious antinociceptive agent with a potency 200 times that of morphine. The toxicity of epibatidine, because of its nonspecificity for both peripheral and central nicotinic receptors, precludes its development as an analgesic. During the synthesis of epibatidine analogs we developed potent antinociceptive agents, typified by CMI-936 and CMI-1145, whose antinociception, unlike that of epibatidine, is mediated via muscarinic receptors. Subsequently, we used specific muscarinic toxins and antagonists to delineate the muscarinic receptor subtype involved in the antinociception evoked by these agents. Thus, the antinociception produced by CMI-936 and CMI-1145 is inhibited substantially by 1) intrathecal injection of the specific muscarinic M4 toxin, muscarinic toxin-3; 2) intrathecally administered pertussis toxin, which inhibits the G proteins coupled to M2 and M4 receptors; and 3) s.c. injection of the M2/M4 muscarinic antagonist himbacine. These results demonstrate that the antinociception elicited by these epibatidine analogs is mediated via muscarinic M4 receptors located in the spinal cord. Compounds that specifically target the M4 receptor therefore may be of substantial value as alternative analgesics to the opiates.  (+info)

The central cannabinoid receptor (CB1) mediates inhibition of nitric oxide production by rat microglial cells. (6/5317)

Upon activation, brain microglial cells release proinflammatory mediators, such as nitric oxide (NO), which may play an important role in the central nervous system antibacterial, antiviral, and antitumor activities. However, excessive release of NO has been postulated to elicit immune-mediated neurodegenerative inflammatory processes and to cause brain injury. In the present study, the effect of cannabinoids on the release of NO from endotoxin/cytokine-activated rat cortical microglial cells was evaluated. A drug dose-dependent (0.1 microM-8 microM) inhibition of NO release from rat microglial cells was exerted by the cannabinoid receptor high-affinity binding enantiomer (-)-CP55940. In contrast, a minimal inhibitory effect was exerted by the lower affinity binding paired enantiomer (+)-CP56667. Pretreatment of microglial cells with the Galphai/Galphao protein inactivator pertussis toxin, cyclic AMP reconstitution with the cell-permeable analog dibutyryl-cAMP, or treatment of cells with the Galphas activator cholera toxin, resulted in reversal of the (-)-CP55940-mediated inhibition of NO release. A similar reversal in (-)-CP55940-mediated inhibition of NO release was effected when microglial cells were pretreated with the central cannabinoid receptor (CB1) selective antagonist SR141716A. Mutagenic reverse transcription-polymerase chain reaction, Western immunoblot assay using a CB1 receptor amine terminal domain-specific antibody, and cellular colocalization of CB1 and the microglial marker Griffonia simplicifolia isolectin B4 confirmed the expression of the CB1 receptor in rat microglial cells. Collectively, these results indicate a functional linkage between the CB1 receptor and cannabinoid-mediated inhibition of NO production by rat microglial cells.  (+info)

Cannabinoid suppression of noxious heat-evoked activity in wide dynamic range neurons in the lumbar dorsal horn of the rat. (7/5317)

The effects of cannabinoid agonists on noxious heat-evoked firing of 62 spinal wide dynamic range (WDR) neurons were examined in urethan-anesthetized rats (1 cell/animal). Noxious thermal stimulation was applied with a Peltier device to the receptive fields in the ipsilateral hindpaw of isolated WDR neurons. To assess the site of action, cannabinoids were administered systemically in intact and spinally transected rats and intraventricularly. Both the aminoalkylindole cannabinoid WIN55,212-2 (125 microg/kg iv) and the bicyclic cannabinoid CP55,940 (125 microg/kg iv) suppressed noxious heat-evoked activity. Responses evoked by mild pressure in nonnociceptive neurons were not altered by CP55,940 (125 microg/kg iv), consistent with previous observations with another cannabinoid agonist, WIN55,212-2. The cannabinoid induced-suppression of noxious heat-evoked activity was blocked by pretreatment with SR141716A (1 mg/kg iv), a competitive antagonist for central cannabinoid CB1 receptors. By contrast, intravenous administration of either vehicle or the receptor-inactive enantiomer WIN55,212-3 (125 microg/kg) failed to alter noxious heat-evoked activity. The suppression of noxious heat-evoked activity induced by WIN55,212-2 in the lumbar dorsal horn of intact animals was markedly attenuated in spinal rats. Moreover, intraventricular administration of WIN55,212-2 suppressed noxious heat-evoked activity in spinal WDR neurons. By contrast, both vehicle and enantiomer were inactive. These findings suggest that cannabinoids selectively modulate the activity of nociceptive neurons in the spinal dorsal horn by actions at CB1 receptors. This modulation represents a suppression of pain neurotransmission because the inhibitory effects are selective for pain-sensitive neurons and are observed with different modalities of noxious stimulation. The data also provide converging lines of evidence for a role for descending antinociceptive mechanisms in cannabinoid modulation of spinal nociceptive processing.  (+info)

Nitric oxide limits the eicosanoid-dependent bronchoconstriction and hypotension induced by endothelin-1 in the guinea-pig. (8/5317)

1. This study attempts to investigate if endogenous nitric oxide (NO) can modulate the eicosanoid-releasing properties of intravenously administered endothelin-1 (ET-1) in the pulmonary and circulatory systems in the guinea-pig. 2. The nitric oxide synthase blocker N(omega)-nitro-L-arginine methyl ester (L-NAME; 300 microM; 30 min infusion) potentiated, in an L-arginine sensitive fashion, the release of thromboxane A2 (TxA2) stimulated by ET-1, the selective ET(B) receptor agonist IRL 1620 (Suc-[Glu9,Ala11,15]-ET-1(8-21)) or bradykinin (BK) (5, 50 and 50 nM, respectively, 3 min infusion) in guinea-pig isolated and perfused lungs. 3. In anaesthetized and ventilated guinea-pigs intravenous injection of ET-1 (0.1-1.0 nmol kg(-1)), IRL 1620 (0.2-1.6 nmol kg(-1)), BK (1.0-10.0 nmol kg(-1)) or U 46619 (0.2-5.7 nmol kg(-1)) each induced dose-dependent increases in pulmonary insufflation pressure (PIP). Pretreatment with L-NAME (5 mg kg(-1)) did not change basal PIP, but increased, in L-arginine sensitive manner, the magnitude of the PIP increases (in both amplitude and duration) triggered by each of the peptides (at 0.25, 0.4 and 1.0 nmol kg(-1), respectively), without modifying bronchoconstriction caused by U 46619 (0.57 nmol kg(-1)). 4. The increases in PIP induced by ET-1, IRL 1620 (0.25 and 0.4 nmol kg(-1), respectively) or U 46619 (0.57 nmol kg(-1)) were accompanied by rapid and transient increases of mean arterial blood pressure (MAP). Pretreatment with L-NAME (5 mg kg(-1); i.v. raised basal MAP persistently and, under this condition, subsequent administration of ET-1 or IRL 1620, but not of U-46619, induced hypotensive responses which were prevented by pretreatment with the cyclo-oxygenase inhibitor indomethacin. 5. Thus, endogenous NO appears to modulate ET-1-induced bronchoconstriction and pressor effects in the guinea-pig by limiting the peptide's ability to induce, possibly via ET(B) receptors, the release of TxA2 in the lungs and of vasodilatory prostanoids in the systemic circulation. Furthermore, it would seem that these eicosanoid-dependent actions of ET-1 in the pulmonary system and on systemic arterial resistance in this species are physiologically dissociated.  (+info)

4-(2-Chlorophenoxy)piperidine hydrochloride 849107-20-6 route of synthesis, 4-(2-Chlorophenoxy)piperidine hydrochloride chemical synthesis methods, 4-(2-Chlorophenoxy)piperidine hydrochloride synthetic routes ect.
TY - JOUR. T1 - [2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists. T2 - Bioorganic and Medicinal Chemistry Letters. AU - Duan,Maosheng. AU - Aquino,Christopher. AU - Ferris,Robert. AU - Kazmierski,Wieslaw M.. AU - Kenakin,Terry. AU - Koble,Cecilia. AU - Wheelan,Pat. AU - Watson,Chris. AU - Youngman,Michael. PY - 2009/3/15. Y1 - 2009/3/15. N2 - Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives exhibited potent inhibition against HIV-1infection. The pharmacokinetic properties of the lead compounds 11a, 14a, 15b, and 16b have been evaluated in vivo.. AB - Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives exhibited potent inhibition against HIV-1infection. The pharmacokinetic properties of the lead compounds 11a, 14a, 15b, and 16b have been evaluated in vivo.. KW - ...
(1-methylpiperidin-4-yl)methanol 20691-89-8 MSDS report, (1-methylpiperidin-4-yl)methanol MSDS safety technical specifications search, (1-methylpiperidin-4-yl)methanol safety information specifications ect.
Read about the chemical and physical properties of (S)-2-(2-methylpiperidin-1-yl)-4-(piperidin-1-yl)pyrido[2,3-d]pyrimidine. Get (S)-2-(2-methylpiperidin-1-yl)-4-(piperidin-1-yl)pyrido[2,3-d]pyrimidine molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
4-Spiro-[1-thiophthalane]piperidine hydrochloride/AFI191673071 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
4-(Bromomethyl)piperidine hydrochloride/ACM1159825225 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
Background: Recent studies have shown that remifentanil increases the risk of aspiration and induces subjective swallowing difficulties. The mechanisms are not completely understood. Here, we investigated whether remifentanil impairs esophageal motility and hypothesized that this is one possible underlying mechanism. Naloxone was used to evaluate whether the effects of remifentanil are mediated through opioid receptors. We also examined subjective swallowing difficulties and the influence of metoclopramide on remifentanil-induced effects.. Methods: Fourteen healthy volunteers participated in a double-blind, randomized, cross-over trial at the University Hospital in orebro, Sweden. They were studied on two different occasions, during which they were randomly assigned to receive either naloxone given as a bolus of 6g/kg followed by an infusion of 0.1g/kg/min, or saline 5min before target-controlled infusions of remifentanil at three target-site concentrations: 1, 2, and 3 ng/ml. On both occasions, ...
Export Data And Price Of N Methyl 4 Chloro Piperidine , www.eximpulse.com Eximpulse Services is the place where you can find the recent and updated Trade intelligence report of N Methyl 4 Chloro Piperidine 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 N Methyl 4 Chloro Piperidine Export data. You can find previous two days N Methyl 4 Chloro Piperidine Export data on Eximpulse Services. N Methyl 4 Chloro Piperidine 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 N Methyl 4 Chloro Piperidine 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 ...
In connection with on-going studies of spiro-pyrrolidine derivatives (Girgis et al. 2012; Moustafa et al. 2012), the title compound, (I), was synthesised and characterised crystallographically. These compounds have biological activity and the structure of the skeltal structure is well established (Kumar et al. 2008).. There are two spiro links in the molecule, Fig. 1, i) where the piperidine and pyrrolidine rings are connected at C1, and ii) where the pyrrolidine ring and indole residue are connected at C6. The phenyl-methyl-idene functional group is connected to the piperidine ring at position C4 while the pyrrolidine-bound aryl ring is attached at C8. The conformation about the C4═C11 double bond is E. The sum of the angles around the piperidine-N1 atom is approximately 333° confirming its sp3 character. The piperidine ring adopts a half-chair conformation where the C2 atom lies 0.713 (3) Å out of the plane of the remaining five atoms (r.m.s. deviation = 0.086 Å). The C6 and C8 atoms ...
Treatment of chronic pain is a major clinical challenge since chronic pain is frequent and leads to deterioration of quality of life. An injury or wound can lead to long term changes in the nervous system that make the skin more sensitive at and near the injury; this is termed hyperalgesia and occurs through long term depotentiation (LTP), i.e., a change in the synaptic interaction between neurons.. Opioids are the gold standard for the symptomatic therapy of moderate to severe pain. Now, in animal studies the investigators have discovered previously unrecognized effects of opioids.. UV-B irradaition of the skin of the thigh is an established model of priamary and secondary hyperalgeisa in humans. The investigators want to test the influence of remifentanil, an ultra-short acting opioid, on hyperalgesia observed after UV-B irradiation in human volunteers in a double blind cross-over prospective active placebo controlled clinical trial, at a dose corresponding to 0.7 µg kg-1 min-1. ...
N,N-Diethyl-6-[[4-(4-fluorophenyl)-1-methylpiperidin-4-yl]methoxymethyl]-4-(trifluoromethyl)pyridin-2-amine | C24H31F4N3O | CID 24799366 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
N-(3-Iodophenyl)-1-methylpiperidin-3-amine | C12H17IN2 | CID 81716446 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Chemical structure of 1-[2-(1-methylpiperidin-4-yl)ethyl]-5-(propan-2-yl)-1H-imidazole-2-thiol. See its properties and synonyms.
Learn more about 5-4-methylpiperidin-1-yl-methyl-1h-tetrazol-1-yl-acetic-acid. We enable science by offering product choice, services, process excellence and our people make it happen.
Learn more about 2-1-methylpiperidin-4-yl-ethyl-amine-dihydrochloride. We enable science by offering product choice, services, process excellence and our people make it happen.
Although agonists with the choline motif such as choline, QN-O, and QN-OH can selectively activate α7 receptors, the potency of these drugs is typically at least 10-fold lower than related agonists that lack the oxygen group (e.g., ETMA and QN). In the case of the QN compounds, there was also decreased efficacy in the α7-selective compounds using the choline motif. The choline motif is also present in four other inactive compounds closely related to α7 agonists (gray in Fig. 1), N-methyl-3-piperidinol, N,N-dimethyl-3-piperidinol, 1-(2-hydroxyethyl)piperidine, and 1-(2-hydroxyethyl)pyrrolidine (data not shown). In the case of N-methyl-3-piperidinol and N,N-dimethyl-3-piperidinol, the hydroxyl group resides in a piperidine ring with a chair-like conformation. Though structurally similar to QN-OH, this latter compound places the six-membered piperidine ring in a boat-like conformation because of the bridgehead. This alters and locks the orientation of the hydroxyl group, which could reasonably ...
The ATD interface that accommodates the linker region is conserved between GluN2A and GluN2B (Fig. 2) and is made up of residues from both the GluN1 (Tyr109, Gly112, Phe113, Ile133, and Leu135) and GluN2B R1 domains (Glu106, Ala107, and Gln110). This portion of the binding pocket apparently can accommodate a wide range of chemical moieties (Tamiz et al., 1998; Mony et al., 2009a; Hansen et al., 2010a). The linkers between the A and B rings of GluN2B-selective modulators are chemically diverse and include alkyl chains, aryl chains, amides, amines, ethers, piperidine rings, or piperazine rings. In general, the optimal linker length is often between 9 and 11 Å (Chenard et al., 1991; Marinelli et al., 2007; Tahirovic et al., 2008; Mosley et al., 2009). The piperidine ring of Ro 25-6981 and ifenprodil, with a pKa of 9.05 (Kobayashi et al., 2006), is protonated under physiological pH and forms a hydrogen bond with the oxygen of Gln110 (Karakas et al., 2011). Mutation of GluN2B Gln110 to Ala reduced ...
We know that if nitrogen is part of an aromatic ring, however, its basicity decreases markedly. So in pyridine nitrogen is part of an aromatic ring hence its basicity is much more less than piperidine. The difference between the two lies in the fact that the nitrogen lone pair occupies an sp3- hybridized orbital in piperidine versus an sp2-hybridized one in pyridine. As we have noted on several occasions, electrons in orbitals with more s character are more strongly held than those with less s character. For this reason, nitrogen holds on to its unshared pair more strongly in pyridine than in piperidine and is less basic ...
As part of a comprehensive program to discover α9α10 nicotinic acetylcholine receptor antagonists, the title compounds C30H36N2, (I), and C36H48N2, (II), were synthesized by coupling 4,4′-bis(3-bromoprop-1-yn-1-yl)-1,1′-biphenyl with 4-methylpiperidine and 2,2,6,6-tetramethylpiperidine, respectively, in acetonitrile at room temperature. In compound (I), the biphenyl system has a twisted conformation with a dihedral angle of 26.57 (6)° between the two phenyl rings of the biphenyl moiety, while in compound (II), the biphenyl moiety sits on a crystallographic inversion centre so the two phenyl rings are exactly coplanar. The terminal piperidine rings in both compound (I) and compound (II) are in the chair conformation. In compound (I), the dihedral angles about the ethynyl groups between the planes of the phenyl rings and the piperidine ring N atoms are 37.16 (16) and 14.20 (17)°. In compound (II), the corresponding dihedral angles are both 61.48 (17)°. There are no noteworthy ...
U11U22U33U12U13U23N10.062 (3)0.052 (3)0.0307 (18)?0.009 (2)?0.0069 (18)0.0009 (18)C20.048 (3)0.051 (3)0.047 (3)0.001 (2)0.002 (2)?0.001 (2)C30.049 (3)0.044 (3)0.038 (2)?0.002 (2)?0.001 (2)0.002 (2)C40.049 (3)0.041 (3)0.037 (2)?0.006 (2)?0.002 (2)0.0023 (19)C50.053 (3)0.033 (2)0.032 (2)?0.003 (2)0.0015 (19)?0.0006 (19)N60.046 (2)0.052 (2)0.0373 (19)0.0060 (19)0.0052 (17)?0.0011 (17)C70.056 (3)0.050 (3)0.037 (2)0.002 (2)0.005 (2)?0.000 (2)N80.059 (3)0.048 (2)0.0340 (18)?0.004 (2)0.0029 (19)?0.0006 (16)C90.052 (3)0.039 (3)0.032 (2)?0.004 (2)0.001 (2)0.0042 (19)N100.041 (2)0.047 (2)0.0304 (17)0.0066 (18)0.0005 (15)?0.0002 (16)C110.046 (3)0.051 (3)0.038 (2)0.006 (2)0.003 (2)0.001 (2)C120.044 (3)0.043 (3)0.037 (2)0.005 (2)?0.003 (2)0.001 (2)C130.048 (3)0.047 (3)0.031 (2)0.008 (2)?0.0015 (19)?0.001 (2)N140.050 (2)0.037 (2)0.0333 (17)0.0038 (19)?0.0005 (16)?0.0040 (16)C150.055 (3)0.038 (3)0.039 (2)?0.000 (2)?0.003 (2)?0.005 (2)C160.059 (3)0.042 (3)0.041 (2)?0.001 (2)?0.002 (2)0.002 (2)C170.046 (3)0.042 ...
1-(quinoxalin-6-ylcarbonyl)piperidine: modulates AMPA receptor desensitization ; an analog of 1-(1,3-benzodioxol-5-ylcarbonyl)piperidine
연구 방법 : 이전 연구에서 140명의 환자들을 무작위로2군으로 나누었다. 두 군 모두 2단계의 중심 효과처 목표 농도 증가를 이용하여 remifentanil을 투여받았는데, 한 군은 1.0에서 4.0ng/ml로, 한 군은 2.0에서 4.0ng/ml로 증가시켰다. 이 연구 결과를 바탕으로 본 연구에서는 3단계의 목표농도주입을 시행하였고(1.0에서 2.0, 그리고 4.0ng/ml), 처음부터 4.0ng/ml로 즉시 목표농도주입을 시작한 군과 비교하기 위해 새로운 140명의 환자를 무작위로 두 군으로 나누어 연구를 진행하였다. 기침이 발생했을 경우를 기록하였고, 그 정도를 약함(1-2), 중간(3-4), 심함(5회 이상)으로 분류하여 기록하였다 ...
This trial is entitled "An Open Label Phase I Study of Gemcitabine/Oxaliplatin (GEMOX) and Vandetanib (ZACTIMA; ZD6474) Combination in Patients With
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1-(3-Chloro-2-methylphenyl)piperidine. CAS Number: 1020253-08-0. Catalog Number: AA0006AI. MDL Number: MFCD09972164. Molecular Formula: C12H16ClN. Molecular Weight: 209.7151. AA Blocks.
1-Azepanyl(4-piperidinyl)methanone, ≥97%, Maybridge 10g 1-Azepanyl(4-piperidinyl)methanone, ≥97%, Maybridge Arb to Az -Organics
59594-17-1 - WKQOHUCQOIKTFF-UHFFFAOYSA-N - Piperidine, 1-(4-fluorobenzoyl)-2-(2-(4-(4-fluorophenyl)-1-piperazinyl)ethyl)-, dihydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Functionalized piperidines are found to constitute a very important core in numerous natural products (Desai et al., 1992; Pinder, 1992), synthetic pharmaceuticals (Breman et al., 2001; Watson et al., 2000), and a wide variety of biologically active compounds. In particular, 1,4-disubstituted piperidine scaffolds find useful applications as established drugs (Targum et al., 1995; Schotte et al.,1996), and they exhibit a wide range of pharmacological activities including antibacterial (Zhou et al., 2007), antimalarial (Misra et al., 2009), anticonvulsant, anti-inflammatory (Bin et al., 2001), and enzyme inhibitory activity (Agrawal & Somani, 2009; Dekus et al., 2007). Moreover a large number of compounds bearing piperidine scaffold have entered into preclinical and clinical trials over the last few years (Kamei et al., 2005). Hence, investigation of the structural features of biologically relevant piperidine derivatives is demanding. In continuation of our structural studies of densely ...
63867-66-3 - ODJHQMBSMIPWOW-UHFFFAOYSA-N - Piperidine, 1-butyl-4-chloro-4-phenyl-, hydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Health,...Alimta Zactima extend survival but cure remains out of reach studies...SATURDAY May 30 (HealthDay News) -- Certain drugs offer incremental y...Thats the conclusion of studies presented Saturday at the annual meet...Lung cancer remains Americas leading cancer killer and significant...,Drug,Trials,Show,Modest,Gains,Against,Lung,Cancer,medicine,medical news today,latest medical news,medical newsletters,current medical news,latest medicine news
Detail záznamu - Influence of pyridine versus piperidine ligands on the chemical, DNA binding and cytotoxic properties of light activated trans,trans,trans-[Pt(N3)2(OH)2(NH3)(L)] - Detail záznamu - Knihovna Akademie věd České republiky
Piperidines are the most prevalent heterocyclic core found in medicines. Yet, while these structures often contain chiral substituents, there are no robust meth
TY - JOUR. T1 - Remifentanil protects myocardium through activation of anti-apoptotic pathways of survival in ischemia-reperfused rat heart. AU - Kim, H. S.. AU - Cho, J. E.. AU - Hong, S. W.. AU - Kim, S. O.. AU - Shim, J. K.. AU - Kwak, Y. L.. PY - 2010. Y1 - 2010. N2 - Remifentanil is a commonly used opioid in anesthesia with cardioprotective effect in ischemia-reperfused (I/R) heart. We evaluated the influence of remifentanil on myocardial infarct size and expressions of proteins involved in apoptosis in I/R rat heart following various time protocols of remifentanil administration. Artificially ventilated anesthetized Sprague-Dawley rats were subjected to a 30 min of left anterior descending coronary artery occlusion followed by 2 h of reperfusion. Rats were randomly assigned to one of five groups; Sham, I/R only, remifentanil preconditioning, postconditioning and continuous infusion group. Myocardial infarct size, the phosphorylation of ERK1/2, Bcl2, Bax and cytochrome c and the expression ...
Evidence from behavioral and self-reported data suggests that the patients beliefs and expectations can shape both therapeutic and adverse effects of any given drug. We investigated how divergent expectancies alter the analgesic efficacy of a potent opioid in healthy volunteers by using brain imaging. The effect of a fixed concentration of the μ-opioid agonist remifentanil on constant heat pain was assessed under three experimental conditions using a within-subject design: with no expectation of analgesia, with expectancy of a positive analgesic effect, and with negative expectancy of analgesia (that is, expectation of hyperalgesia or exacerbation of pain). We used functional magnetic resonance imaging to record brain activity to corroborate the effects of expectations on the analgesic efficacy of the opioid and to elucidate the underlying neural mechanisms. Positive treatment expectancy substantially enhanced (doubled) the analgesic benefit of remifentanil. In contrast, negative treatment expectancy
BackgroundHigh-dose remifentanil (1â€5 µg kgâˆ1 minâˆ1), commonly used for cardiac surgery, has been associated with muscle rigidity, hypotension, bradycardia, and reduced cardiac output. The aim of this study was to determine an optimal lower remifentanil dose, which should be accompanied by fewer adverse events, that still effectively suppresses haemodynamic responses to typical stressful stimuli (i.e. intubation, skin incision, and sternotomy).MethodsTotal i.v. anaesthesia consisted of a target-controlled propofol (2 µg mlâˆ1) and a remifentanil infusion. Forty patients were allocated to receive either a constant infusion of remifentanil at 0.1 µg kgâˆ1 minâˆ1 or up-titrations to 0.2, 0.3, or 0.4 µg kgâˆ1 minâˆ1, respectively, 5 min before each stimulus. Subsequently, changes in heart rate and mean arterial blood pressure were recorded for 8 min. Increases exceeding 20% of baseline were considered to be of clinical relevance. Patients who exhibited these ...
Remifentanil is a potent ultrashort-acting opioid, with rapid onset and offset of drug effect. It allows rapid anesthetic emergence even after a prolonged infusion, and decreases the at-risk time during extubation. In addition, cough suppression of remifentanil enables smooth extubation with reduced complications. However, the infusion of remifentanil suppresses the emergence cough effectively in clinical practice, whereas it still delays the awakening from anesthesia, resulting in prolonged emergence time. Reduced Ce of remifentanil during emergence would decrease the adverse events that are associated with remifentanil infusion ...
Background & Objectives: One of the most common ways in intubation without muscle relaxant is using propofol and remifentanil. The common practice is injection of remifentanil and then propofol. This occasionally produces severe hemodynamic changes. The aim of this study is to inject propofol followed by remifentanil for evaluating the ...
Author: Sarwat Jahan, Shamim Akhtar, Arfa Kamil, Nousheen Mushtaq, Zafar Saied Saify and Muhammad Arif. Publishing Date: 2016. E-ISSN: 1011-601X. Volume: 29 Issue: 1. ABSTRACT:. Piperidine is the most significant scaffold which reveals therapeutic potential because of its conformationally flexible nature. During the course of present investigations synthetic quaternary salts of alkyl piperidine with various phenacyl bromides were explored for their possible analgesic activity. Compounds I analogs (1a-1f) and compound II analogs (IIa-IIf) showed varying degree of analgesic activity when compared with pethidine as standard and its duration by tail immersion method.. KEYWORDS: Alkyl piperidine derivatives, analgesic activity, SAR.. Full Text ...
2085 Mantle cell lymphoma (MCL) is an aggressive non-Hodgkins lymphoma carrying poor prognosis. The disease is characterized by the t(11;14) (q13;q32) chromosomal translocation and overexpression of cyclin D1, which drives cellular proliferation by stimulating the activity of cyclin-dependent kinases (cdks) 4 and 6. Overexpression of anti-apoptotic proteins, most notably Mcl-1, is an additional hallmark of MCL cells. The pan-cyclin-dependent kinase inhibitor flavopiridol has demonstrated responses in MCL patients, even when suboptimal schedules have been employed. Flavopiridol most potently inhibits cdk9, with Ki 3 nM, and its effects on cellular transcription are expected to compromise Mcl-1 expression. Preclinical studies of flavopiridol in Z138-C, NCEB-1, Granta 519, and JVM-2 MCL cell lines were performed to elucidate mechanisms of cell death. Z138-C cells were the most sensitive with IC50 around 100nM. Growth of Granta 519 was compromised above 200nM drug, while NCEB-1 and JVM-2, which ...
SIMONI, Ricardo Francisco; PEREIRA, Antônio Márcio Sanfim Arantes; BOREGA, Renato dos Santos and SIMOES, Daniel Caldeira Pereira. Remifentanil versus Sufentanil em infusão contínua em intervenções cirúrgicas videolaparoscópicas: estudo comparativo. Rev. Bras. Anestesiol. [online]. 2008, vol.58, n.3, pp.193-201. ISSN 0034-7094. http://dx.doi.org/10.1590/S0034-70942008000300001.. JUSTIFICATIVA E OBJETIVOS: A infusão contínua (IC) de remifentanil na técnica de anestesia venosa total é prática comum. Já o sufentanil em IC para cirurgias de curta/média duração tem sido pouco utilizado. O objetivo desse estudo foi comparar duas técnicas de anestesia venosa total, utilizando remifentanil ou sufentanil em IC, quanto ao comportamento anestésico no intra-operatório e às características da recuperação anestésica em pacientes submetidos à videolaparoscopia. MÉTODO: Participaram desse estudo 60 pacientes divididos em 2 grupos iguais (GR e GS). O GR foi induzido com remifentanil IC ...
TY - JOUR. T1 - Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program. AU - Pang, Yuan-Ping. AU - Kozikowski, Alan P.. PY - 1994/12. Y1 - 1994/12. N2 - In the preceding paper we reported on a docking study with the SYSDOC program for predicting the binding sites of huperzine A in acetylcholinesterase (AChE) [Pang, Y.-P. and Kozikowski, A.P., J. Comput.-Aided Mol. Design, 8 (1994) 669]. Here we present a prediction of the binding sites of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (E2020) in AChE by the same method. E2020 is one of the most potent and selective reversible inhibitors of AChE, and this molecule has puzzled researchers, partly due to its flexible structure, in understanding how it binds to AChE. Based on the results of docking 1320 different conformers of E2020 into 69 different conformers of AChE and on the pharmacological data reported for E2020 and its ...
This trial will investigate the efficacy and tolerability of vandetanib [Zactima] in prostate cancer patients undergoing intermittent androgen deprivation
Derivatives of p-alkyl-carbonyl-phenoxy-alkyl- and carboxy-phenoxy-alkyl-carboxylic acids complying to the general formula: R-C-O-CH-(CH2)n-C-Y PARALLEL PARALLEL XRO where R represents -H, NH2; (-CH3C2H5, C3H7, or the omega halogen derivatives of these groups); C6H5; -OH, -OCH3, OC2H5, NHOH or R1 N ANGLE R2 where R1 and R2 can be linear radicals such as -CH3 or -CH2-CH3 or can be a ring such as that of piperidine, methyl-2-piperidine, piperazine, morpholine, pyrrolidine, methyl-4-piperidine, N-phenyl-piperazine, N-p-methoxy-phenyl-piperazine, N-methyl-4-piperazine, N-p-chlorophenyl-piperazine or hexamethyleneimine or ethylamino-ethyl-amine; X represents =O or =N-O-H; R-C- represents -C 3BOND N; n is 0, 1, 2 or 3 normal or iso when R is -H and N IS 1, 2, 3 WHEN R is -C6H5; R represents -H or C6H5; and Y represents -OH -OCH3; -OC2H5; NHOH or R1 N ANGLE R2 where R1 and R2 can be linear radicals such as -CH3 or -CH2-CH3 or can be represented by a ring such as that of piperidine, methyl-2-piperidine,
chemBlink provides information about CAS # 105813-40-9, trans-(-)-3-[(1,3-Benzodioxol-5-yloxy)methyl]-4-phenyl-1-(phenylmethyl)piperidine, molecular formula: C26H27NO3.
Epidural analgesia remains the gold standard during labour, but is contraindicated in several clinical settings due to increased risk of serious complications. There are few effective alternatives to epidural analgesia. However, there is an increasing interest for the use of remifentanil as a labour analgesic. In this focused review, we describe the effect, dose and safety of remifentanil for the mother and fetus/neonate. Remifentanil appears to have a potential as labour analgesic. Careful monitoring of the parturient and the newborn is advised ...
CAS: NA | Risperidone Piperidine Impurity | Buy and find out price, stock availability of high quality R&D product with data and CoA from SynThink
Lookchem Provide Cas No.84255-31-2 Basic information: Properties,Safety Data,Sds and Other Datebase. We also Provide Trading Suppliers & Manufacture for 84255-31-2 N-[[5-(dimethylamino)-1-naphthyl]sulphonyl]-DL-leucine, compound with piperidine (1:1).
New piperidine derivatives of 1,3-pyrimidine and 1,3,5-triazine are used as stabilizers for organic materials, especially for polymers.
sir pyridine piperidine morpholline pyrrole among these strength of basic order explain with proper explanations 63gd9rll -Chemistry - TopperLearning.com
Semantic Scholar extracted view of [Studies on the toxicology of barbiturates from the tetrahydro-pyridine and piperidine group]. by Otto Pribilla
Conclusion. The administration of intravenous remifentanil makes easer the pick-up of oocytes because women had no pain during the procedure. In this way, it was possible to recover more oocytes and to verify that the drug doesnt interfere with the exitus of the techniques For these reasons we decided to continue in using intravenous infusion of remifentanil for the retrieval of oocytes.. ...
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|p|Crenolanib (CP-868596) is a potent, specific, and orally available inhibitor of PDGFRα, PDGFRβ and FLT3 with inhibitor-binding constant (Kd) of 3.2, 2.1, and 0.74 nM, respectively [1].|/p||p|It has been shown that crenolanib is more potent than quizart
2VTH: Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
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Purpose: To elucidate any differences in the exposure-response of alvocidib (flavopiridol) given by 1-hour bolus or a hybrid schedule (30-minute bolus followed by a 4-hour infusion) using a flavopiridol/cytosine arabinoside/mitoxantrone sequential protocol (FLAM) in patients with acute leukemia. The hybrid schedule was devised to be pharmacologically superior in chronic leukemia based on unbound exposure.. Experimental Design: Data from 129 patients in three FLAM studies were used for pharmacokinetic/pharmacodynamic modeling. Newly diagnosed (62%) or relapsed/refractory (38%) patients were treated by bolus (43%) or hybrid schedule (57%). Total and unbound flavopiridol concentrations were fit using nonlinear mixed-effect population pharmacokinetic methodologies. Exposure-response relationships using unbound flavopiridol AUC were explored using recursive partitioning.. Results: Flavopiridol pharmacokinetic parameters were estimated using a two-compartment model. No pharmacokinetic covariates were ...
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
This invention relates to a process for the preparation of compounds of the formula: wherein R1 is C1-C6alkyl and the C1-C6alkyl moiety is straight or branched.
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The chemistry of copper is extremely rich because it can easily access Cu0, CuI, CuII, and CuIII oxidation states allowing it to… Expand ...
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A process for preparing a compound of formula I wherein R 1 and R 2 are independently selected from the group consisting of hydrogen, lower alkyl and halogen
2-(o-Acylaminophenethyl)piperidines". Journal of Medicinal Chemistry. 16 (9): 1015-20. doi:10.1021/jm00267a012. PMID 4745503. v ...
Lee, J.; Ziering, A.; Heineman, S. D.; Berger, L. (1947). "Piperidine Derivatives. Part II. 2-Phenyl- and 2-Phenylalkyl- ... Piperidines". Journal of Organic Chemistry. 12 (6): 885-893. doi:10.1021/jo01170a021. PMID 18919741. Vinken, P. J.; Bruyn, G. W ...
US1851832, 29 March 1932 Marvel, C. S.; Lazier, W. A. (1929). "Benzoyl Piperidine". Organic Syntheses. 9: 16. doi:10.15227/ ... piperidine". Organic Syntheses. 69: 44. doi:10.15227/orgsyn.069.0044. El-Samragy, Yehia (2004). "Chemical and Technical ...
Structural analogs of desmethylprodine with different N-substituents than a methyl group on the piperidine have been ... Ziering A, Lee J (November 1947). "Piperidine derivatives; 1,3-dialkyl-4-aryl-4-acyloxypiperidines". The Journal of Organic ...
Tricyclic and piperidine: pimethixene, cyproheptadine. *Acyclic: gilutensin. Alkyl(amine)s[edit]. *Acyclic: (3- ...
Piperidines. *1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine. *2-Benzylpiperidine. *2-Methyl-3-phenylpiperidine ...
TCAs were the first medications that had dual mechanism of action. The mechanism of action of tricyclic secondary amine antidepressants is only partly understood. TCAs have dual inhibition effects on norepinephrine reuptake transporters and serotonin reuptake transporters. Increased norepinephrine and serotonin concentrations are obtained by inhibiting both of these transporter proteins. TCAs have substantially more affinity for norepinephrine reuptake proteins than the SSRIs. This is because of a formation of secondary amine TCA metabolites.[24][25] In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of norepinephrine in or near the synaptic clefts. Actions of imipramine-like tricyclic antidepressants have complex, secondary adaptions to their initial and sustained actions as inhibitors of norepinephrine transport and variable blockade of serotonin transport. Norepinephrine interacts with postsynaptic α and β adrenergic ...
N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate. *2β-Propanoyl-3β-(2-naphthyl)-tropane (WF-23) ...
... is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). When most normal metabolizers take venlafaxine, approximately 70% of the dose is metabolized into desvenlafaxine, so the effects of the two drugs are expected to be very similar.[5] It works by blocking the "reuptake" transporters for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin (5-hydroxytryptamine) and norepinephrine (noradrenaline). It is approximately 10 times more potent at inhibiting serotonin uptake than norepinephrine uptake.[6]. ...
... was discovered by scientists at Angelini, who also discovered trazodone.[15] Its development names have included ST-1191 and McN-A-2673-11.[16][1] The INN etoperidone was proposed in 1976 and recommended in 1977.[17][18] The drug was given brand names in Spain (Centren (Esteve) and Depraser (Lepori)) and Italy (Staff (Sigma Tau))[1] and was also given the brand names Axiomin and Etonin,[16] but it is not entirely clear if it was actually marketed; the Pharmaceutical Manufacturing Encyclopedia provides no dates for commercial introduction.[19] According to Micromedex's Index Nominum: International Drug Directory, etoperidone was indeed previously marketed in Spain and Italy.[1] ...
McConathy J, Owens MJ, Kilts CD, et al. (August 2004). "Synthesis and biological evaluation of [11C]talopram and [11C]talsupram: candidate PET ligands for the norepinephrine transporter". Nuclear Medicine and Biology. 31 (6): 705-18. doi:10.1016/j.nucmedbio.2003.05.001. PMID 15246361 ...
Piperidines. *1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine. *2-Benzylpiperidine. *2-Methyl-3-phenylpiperidine ...
Piperidines. *1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine. *2-Benzylpiperidine. *2-Methyl-3-phenylpiperidine ...
Piperidines. *Selective serotonin reuptake inhibitors. *Nervous system drug stubs. Hidden categories: *CS1: long volume value ...
InChI=1S/C32H38N2O8/c1-37-24-12-17(13-25(38-2)29(24)39-3)31(35)42-26-14-18-16-34-11-10-20-19-8-6-7-9-22(19)33-28(20)23(34)15-21(18)27(30(26)40-4)32(36)41-5/h6-9,12-13,18,21,23,26-27,30,33H,10-11,14-16H2,1-5H3/t18-,21+,23-,26-,27+,30+/m1/s1 ...
Piperidines *Donepezil. *Tacrine, also known as tetrahydroaminoacridine (THA'). *Edrophonium. *Huperzine A[17][18] ...
... (DOV-220,075) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) discovered at American Cyanamid as an analgesic drug candidate, and licensed to DOV Pharmaceutical in 1998 after American Cyanamid was acquired by Wyeth.[1][2][3] In January 2007, Dov licensed the rights to bicifadine to XTL Biopharmaceuticals after bicifadine failed in a Phase III clinical trial for chronic lower back pain.[4][5][6] XTL ran a PhaseIIb clinical trial for pain caused by diabetic neuropathy, which failed in 2008;[7] XTL terminated the agreement in 2010.[8] In 2010 Dov was acquired by Euthymics Bioscience which intended to continue development of other candidates from Dov's portfolio.[9] Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs.[10] While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has ...
Starr KR, Price GW, Watson JM, Atkinson PJ, Arban R, Melotto S, Dawson LA, Hagan JJ, Upton N, Duxon MS (2007). "SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test". Neuropsychopharmacology. 32 (10): 2163-2172. doi:10.1038/sj.npp.1301341. PMID 17356576 ...
Piperidines. *Serotonin reuptake inhibitors. Hidden categories: *Chemical pages without DrugBank identifier. *Articles without ...
Randomized, double blind, placebo-controlled trials have confirmed the efficacy of dapoxetine for the treatment of PE.[8] Different dosage has different impacts on different types of PE. Dapoxetine 60 mg significantly improves the mean intravaginal ejaculation latency time (IELT) compared to that of dapoxetine 30 mg in men with lifelong PE, but there is no difference in men with acquired PE.[9] Dapoxetine, given 1-3 hours before sexual episode, prolongs IELT and increases the sense of control and sexual satisfaction in men of 18 to 64 years of age with PE. Since PE is associated with personal distress and interrelationship difficulty, dapoxetine provides help for men with PE to overcome this condition.[10] With no drug approved specifically for treatment for PE in the US and some other countries, other SSRIs such as fluoxetine, paroxetine, sertraline, fluvoxamine, and citalopram have been used off-label to treat PE. Waldinger's meta-analysis shows that the use of these conventional ...
Piperidines. *1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine. *2-Benzylpiperidine. *2-Methyl-3-phenylpiperidine ...
... , sold under the brand name Azafen or Azaphen, is an antidepressant approved in Russia for the treatment of depression.[1][2][3][4] It was introduced in the late 1960s and is still used today.[5][6] Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin.[7][8] In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity.[4] Other properties such as anticholinergic or antiadrenergic actions are less clear but are likely.[citation needed] ...
... is effective for prevention of shivering during surgery or recovery from surgery.[5][6] Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial,[7] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[8][9] The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine,[10][11][12] or oxycodone,[13] while Nefopam tends to produce fewer side effects, does not produce respiratory depression,[14] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[12][15] Nefopam is also used to treat severe hiccups.[16] ...
3S,4R)-3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine ...
Piperidines. *1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine. *2-Benzylpiperidine. *2-Methyl-3-phenylpiperidine ...
... a piperidine derivative. Brand names include Mydocalm, Biocalm, Mydeton, Miderizone, Mydoflex, Myolax, Myoxan and ...
Vardanyan R (2017). Piperidine-Based Drug Discovery. Elsevier. ISBN 9780128134283. Consolidated List of Products - Whose ...
Cyrille Guimard, who had won the first part of stage eight, tested positive for piperidine after stage thirteen. Three other ... cyclists tested positive:Claude Tollet, for amphetamine; Daniel Ducreux, for piperidine; Carlos Melero, for piperidine. There ...
List of cocaine analogues 1-Methyl-3-propyl-4-(p-chlorophenyl)piperidine N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate JZ ... Å distant from the 3α-substituted piperidine ring. Noticeably, high potency at the DAT of dimeric piperidine-based esters and ... "Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ... This model was successfully used for the design of a novel piperidine-based DAT inhibitor, that is economically affordable to ...
"Material Safety Data Sheet: Piperidine". Fisher. 29 October 2007. "Diamorphine (PIM 261F, French)". www.inchem.org. Archived ...
Natural occurrence of piperidine and derivatives[edit]. Piperidine itself has been obtained from black pepper,[11][12] from ... Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair ... Piperidine is used as a solvent and as a base. The same is true for certain derivatives: N-formylpiperidine is a polar aprotic ... 4] the name comes from the genus name Piper, which is the Latin word for pepper.[5] Although piperidine is a common organic ...
Media in categorie "Piperidines". Deze categorie bevat de volgende 200 bestanden, van in totaal 514. ... 4-(4-Chloro-phenyl)-3-(3-methyl-(1,2,4)oxadiazol-5-yl)-piperidine.png 225 × 223; 5 kB. ... Overgenomen van "https://commons.wikimedia.org/w/index.php?title=Category:Piperidines&oldid=270215866" ... 4-(4-iodo-1H-pyrazol-1-yl)piperidine.svg 146 × 57; 11 kB. ...
... is a azacycloalkane (CHEBI:37949) piperidine (CHEBI:18049) is a piperidines (CHEBI:26151) piperidine ( ... piperidine (CHEBI:18049) has role base (CHEBI:22695) piperidine (CHEBI:18049) has role catalyst (CHEBI:35223) piperidine (CHEBI ... piperidine (CHEBI:18049). N-[(Z)-dodec-2-enoyl]piperidine (CHEBI:87155) has functional parent piperidine (CHEBI:18049). ... piperidine (CHEBI:18049) has role non-polar solvent (CHEBI:48355) piperidine (CHEBI:18049) has role plant metabolite (CHEBI: ...
Burrows, G.H.; King, L.A., Jr., The free energy change that accompanies hydrogenation of pyridine to piperidine, J. Am. Chem. ... Hales, J.L.; Herington, E.F.G., Equilibrium between pyridine and piperidine, Trans. Faraday Soc., 1957, 53, 616-622. [all data ... Gan, T.-H.; Peel, J.B., Photoelectron spectroscopic studies of piperidine and its N-halo derivatives, Aust. J. Chem., 1979, 32 ... Hossenlopp, I.A.; Archer, D.G., Enthalpies of vaporization of piperidine and 1,2-dimethylbenzene; gas-phase isobaric heat ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Process for piperidine derivatives. US5644061 *. May 1, 1995. Jul 1, 1997. Merrell Pharmaceuticals Inc.. Process for piperidine ... Process for piperidine derivatives. US5654433 *. May 3, 1995. Aug 5, 1997. Merrell Pharmaceuticals Inc.. Process for piperidine ... Process for production of piperidine derivatives. US7022880. Aug 13, 2004. Apr 4, 2006. Amr Technology , Inc.. Piperidine ... When in the procedure of Example 1(B) an appropriate amount of 4-(diphenylmethylene)piperidine or 4-(diphenylmethyl)piperidine ...
New piperidine derivatives of 1,3-pyrimidine and 1,3,5-triazine are used as stabilizers for organic materials, especially for ... are the same or different piperidine residue of formula IIA. More preferably, residues D, D" and D" are the same piperidine ... Piperidine stabilizers for polymers. US3887516 *. 20 Oct 1972. 3 Jun 1975. American Cyanamid Co. Hindered tris (meta- ... Z" and Z" are the same or different and each is a piperidine group of formula II as hereinbefore defined, a halogen atom, a ...
... which are chemically derived from piperidine. Alkaloids with a piperidine building block are widespread and are usually further ... The piperidine alkaloids also include the sedum alkaloids (e.g. sedamine), pelletierine, the lobelia alkaloids (e.g. lobeline ... The most important representative of piperidine alkaloids is piperine, which is responsible for the pungent taste of pepper. ... Piperidine alkaloids are naturally occurring chemical compounds from the group of alkaloids, ...
Piperidines explanation free. What is Piperidines? Meaning of Piperidines medical term. What does Piperidines mean? ... Looking for online definition of Piperidines in the Medical Dictionary? ... piperidine. (redirected from Piperidines). Also found in: Dictionary, Encyclopedia. pi·per·i·dine. (pī-peri-dēn), 1. a ... Piperidines , definition of Piperidines by Medical dictionary https://medical-dictionary.thefreedictionary.com/Piperidines ...
Piperidine derivatives. US4285957. Oct 14, 1980. Aug 25, 1981. Richardson-Merrell Inc.. 1-Piperidine-alkanol derivatives, ... The piperidine derivative of formula (I) is used according to the present invention as a histamine H1-receptor antagonist and ... The novel process for preparing the piperidine derivatives of formula (I) is set forth in Scheme A. in Scheme A, R1, and R2 are ... The piperidine derivative of formula (I) can be administered according to the present invention in any form or mode which makes ...
Trifluoro(piperidine)boron. Regulatory process names 1 IUPAC names 3 Other identifiers 5 ...
... piperidines , C35H33NO2 , CID 94053 - structure, chemical names, physical and chemical properties, classification, patents, ...
... piperidine-1-carbothioamide
P4S stands for Piperidine-4-Sulphonate (brain research). P4S is defined as Piperidine-4-Sulphonate (brain research) very rarely ... S.v. "P4S." Retrieved August 18 2019 from https://www.acronymfinder.com/Piperidine_4_Sulphonate-(brain-research)-(P4S).html ... n.d.) Acronym Finder. (2019). Retrieved August 18 2019 from https://www.acronymfinder.com/Piperidine_4_Sulphonate-(brain- ... a href=https://www.acronymfinder.com/Piperidine_4_Sulphonate-(brain-research)-(P4S).html,P4S,/a,. ...
Reacts violently with dicyanofurazan, N-nitrosoacetanilide and 1-perchloryl-piperidine, causing explosion hazard.. OCCUPATIONAL ...
... piperidine , C18H27N , CID 611739 - structure, chemical names, physical and chemical properties, classification, patents, ...
2-(2,2-dicyclohexylethyl)piperidine Regulatory process names 2 Other identifiers 1 ...
Cadmium bis(piperidine-1-carbodithioate) Regulatory process names 3 CAS names 1 IUPAC names 2 Other identifiers 2 ...
... piperidine hydrochloride; CAS Number: 1378304-65-4; Linear Formula: C6H14CLNO2S; find AChemBlock-ADV390216990 MSDS, related ...
A series of arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines was synthesized to develop new α1- ... Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro- ... Arylsulfonamide derivatives of pyrrolidines and piperidines; Benign prostatic hyperplasia; LCAP flexible biomimetic; ...
The present invention is directed to certain novel compounds identified as substituted piperidines, pyrrolidines and hexahydro- ... SPIRO PIPERIDINES AND HOMOLOGS WHICH PROMOTE RELEASE OF GROWTH HORMONE. WO1994019367A1. 1994-09-01. SPIRO PIPERIDINES AND ... The piperidine 27 can be elaborated to GH secretagogues of Formula I by using chemistry detailed in Schemes 1-8. The piperidine ... As depicted in Scheme 14 the piperidine 26 may also serve as a key intermediate for the synthesis of a variety of piperidines ...
3-boc-amino piperidine, 3-n-boc-amino piperidine, 3-tert-butoxycarbonylamino piperidine, 3-aminopiperidine, 3-boc protected, ... 3-boc-amino piperidine, 3-n-boc-amino piperidine, 3-tert-butoxycarbonylamino piperidine, 3-aminopiperidine, 3-boc protected, ...
... 968-85-4 piperidine-4-carbonitrile
... piperidine hydrochloride; CAS Number: 333954-89-5; find Apollo Scientific Ltd-APO455826972 MSDS, related peer-reviewed papers, ...
Piperidines are the most prevalent heterocyclic core found in medicines. Yet, while these structures often contain chiral ... Piperidines are the most prevalent heterocyclic core found in medicines. Yet, while these structures often contain chiral ... Chiral Piperidines from Acyclic Amines Via Enantioselective, Radical-Mediated δ C-H Cyanation. Chem ... Zhang, Zuxiao and Zhang, Xin and Nagib, David A., Chiral Piperidines from Acyclic Amines Via Enantioselective, Radical-Mediated ...
4-3-fluorobenzyl piperidine hydrochloride, 4-3-fluorophenyl methyl piperidine hydrochloride, 4-3-fluoro-benzyl-piperidine ... 4-3-fluorobenzyl piperidine hydrochloride, 4-3-fluorophenyl methyl piperidine hydrochloride, 4-3-fluoro-benzyl-piperidine ...
Precautionary Statements: P261-P280a-P305+P351+P338-P304+P340-P405-P501a Avoid breathing dust/fume/gas/mist/vapours/spray. Wear protective gloves and eye/face protection. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations. ...
  • This invention relates to novel substituted piperidine derivatives. (google.com)
  • Piperidine and its derivatives are ubiquitous building blocks in pharmaceuticals and fine chemicals. (wikipedia.org)
  • New piperidine derivatives of 1,3-pyrimidine and 1,3,5-triazine are used as stabilizers for organic materials, especially for polymers. (google.com.au)
  • The inhibition of enzyme was done (in triplicates) in 96 well plate format and response were obtained on a Perkin Elmer LS55 Fluorescence spectrometer with an excitation and emission wavelengths of 336 and 490 nm, respectively and analgesic activity of synthesized derivatives of 4-(4'-Bromophenyl)-4-hydroxy piperidine was conducted by Eddy's hot plate method in albino mice by providing standard colony conditions using Pethidine as standard drug. (thefreedictionary.com)
  • The dimensional pharmacological and biological characteristics have drawn the attraction of researchers towards Piperidine to work on it's antimalarial response and for this purpose different strong piperidine derivatives were developed and were targeted against Plasmodium falciparum, responsible for producing severe life- threatening malaria [2-5]. (thefreedictionary.com)
  • Several p-substituted phenacyl piperazine and piperidine derivatives were prepared and proved for good analgesic activity [35]. (thefreedictionary.com)
  • Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity. (nih.gov)
  • A series of arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines was synthesized to develop new α 1 -adrenoceptor antagonists with uroselective profile. (nih.gov)
  • Piperidine derivatives are used as medicinal preparations, especially as local anesthetics and spasmolytics. (thefreedictionary.com)
  • Catalytic asymmetric synthesis of piperidine derivatives through the [4 + 2] annulation of imines with allenes. (semanticscholar.org)
  • Catalytic asymmetric hydrogenation of N-iminopyridinium ylides: expedient approach to enantioenriched substituted piperidine derivatives. (semanticscholar.org)
  • Conformational analysis using Molecular Dynamics Simulation of sulfo carboxamide derivatives confirms a twofold increased stability when compared with sulphonyl derivatives of piperidine. (biomedcentral.com)
  • In silico analysis of these piperidine based Sulfo carboxamide derivates show a better competitive inhibition than existing sulphonyl derivatives of carboxyl amine. (biomedcentral.com)
  • Further in vivo tests are required to analyze the effective concentration for constructing effective derivatives of carboxamide based piperidine as potential antagonists of CCR5 in future. (biomedcentral.com)
  • Background: Herein, a new chitosan-supported ytterbium nano-catalyst has been prepared and used in a mild, efficient, and expeditious method for the synthesis of substituted piperidine derivatives via threecomponent condensation of substituted anilines, formaldehyde and different cyclic/acyclic active methylene compounds at room temperature. (eurekaselect.com)
  • Eisai's Aricept (donepezil hydrochloride) is a piperidine derivative that acts centrally as a reversible AChEI. (thefreedictionary.com)
  • [5] Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids . (wikipedia.org)
  • The piperidine structural motif is present in numerous natural alkaloids . (wikipedia.org)
  • Piperidine alkaloids are naturally occurring chemical compounds from the group of alkaloids, which are chemically derived from piperidine. (wikipedia.org)
  • Alkaloids with a piperidine building block are widespread and are usually further subdivided according to their occurrence and biogenetic origin. (wikipedia.org)
  • The most important representative of piperidine alkaloids is piperine, which is responsible for the pungent taste of pepper. (wikipedia.org)
  • The piperidine alkaloids also include the sedum alkaloids (e.g. sedamine), pelletierine, the lobelia alkaloids (e.g. lobeline), the conium alkaloids (such as coniine) and the pinus alkaloids. (wikipedia.org)
  • 2. One of a class of alkaloids containing a piperidine (1) moiety. (thefreedictionary.com)
  • Effects of piperidine and piperideine alkaloids from the venom of red imported fire ants, Solenopsis invicta Buren, on Pythium ultimum Trow growth in vitro and the application of piperideine alkaloids to control cucumber damping-off in the greenhouse. (thefreedictionary.com)
  • michiganensis In vitro and the application of piperidine alkaloids to manage symptom development of bacterial canker on tomato in the greenhouse. (thefreedictionary.com)
  • The poison hemlock plant (Conium maculatum) contains several toxic piperidine alkaloids, primarily coniine, and has been used since antiquity as an intentional poison--most notably by the Athenians to execute Socrates. (thefreedictionary.com)
  • However, a synergistic action of piperidine alkaloids has been suggested to be responsible for neurotoxic damage observed in animals. (scielo.br)
  • found that the toxic activity observed in mice is chemically related to piperidine alkaloids such as juliprosopine present in the pods of this Leguminosae. (scielo.br)
  • A flash chromatography system with a silica gel cartridge was further developed to isolate and purify the piperidine and piperideine alkaloids (Li et al. (thefreedictionary.com)
  • In most cases, the structures are derived from two main chemical frames: the piperidine alkaloid and N-isobutylamide alkaloids. (thefreedictionary.com)
  • CAS:124443-68-1Synonyms: tert-Butyl methyl piperidine-1,4-dicarboxy. (chemnet.com)
  • Here we present a prediction of the binding sites of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (E2020) in AChE by the same method. (elsevier.com)
  • Pang, Y-P & Kozikowski, AP 1994, ' Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program ', Journal of Computer-Aided Molecular Design , vol. 8, no. 6, pp. 683-693. (elsevier.com)
  • Kozikowski, Alan P. / Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program . (elsevier.com)
  • Piperidine is also commonly used as a base for the deprotection of Fmoc-amino acids used in solid-phase peptide synthesis. (wikipedia.org)
  • Yet, while these structures often contain chiral substituents, there are no robust methods for the synthesis of enantioenriched, substituted piperidines. (ssrn.com)
  • The key spirocycle forming step involves the oxidative rearrangement of cyclic tertiary furfuryl alcohols and amines for the synthesis of spirocyclic pyrans and piperidines, respectively. (gla.ac.uk)
  • Synthesis of pharmaceutically active compounds containing a disubstituted piperidine framework. (semanticscholar.org)
  • Aim & Scope: The synthesis of highly substituted piperidine from the one-pot reaction between aromatic aldehydes, anilines and β-ketoesters in the presence of tartaric acid as a catalyst has been investigated in both methanol and ethanol media at ambient temperature. (eurekaselect.com)
  • Methanol was optimized as a desirable solvent in the synthesis of piperidine, nevertheless, ethanol in a kinetic investigation had none effect on the enhancement of the reaction rate than methanol. (eurekaselect.com)
  • Synthesis routes of novel piperidine-containing acetylenes are presented. (diva-portal.org)
  • 2R,6R)-rel-tert-Butyl 4-(hydroxymethyl)-2,6-dimethyl-d6-piperidine-1-carboxylate is the labeled analogue of (2R,6R)-rel-tert-Butyl 4-(hydroxymethyl)-2,6-dimethylpiperidine-1-carboxylate (B809310), a reactant in the synthesis of piperidinylmethyl (thiazolyl)phenylcarbamates as M3 muscarinic acetylcholine receptor antagonists. (trc-canada.com)
  • These sites appear to exist predominantly within the kappa receptor since the selectivity arises from a 530-fold loss of affinity of 8 for the mu receptor and an 18-fold increase in affinity for the kappa receptor relative to the mu-selective ligand, (+)-N-[trans-4-phenyl-2-butenyl]-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine (5a). (nih.gov)
  • I. 4-alkyl-4-(m-hydroxy-phenyl)-piperidines. (aspetjournals.org)
  • The 4-(m-OH-phenyl)piperidines are a flexible fragment of the morphine/benzomorphan fused-ring opioids. (aspetjournals.org)
  • The 4-t-butyl compounds are, in fact, the first simple mono-alkyl-substituted 4-phenyl-piperidines predicted to definitely exist in a phenyl axial conformation, as confirmed by X-ray analysis. (aspetjournals.org)
  • In search of other opioids with good analgesic potency and fewer incidence of side effects mainly respiratory depression, a phenyl piperidine derivative fentanyl and thienyl analogue of fentanyl-Sufentanil and many more were discovered and studied. (thefreedictionary.com)
  • Fentanyl, a Phenyl piperidine derivative, is a short-acting and potent synthetic narcotic. (thefreedictionary.com)
  • The present invention is directed to certain novel compounds identified as substituted piperidines, pyrrolidines and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R 1 , R 4 , R 5 , A, X, Y and n are as defined herein. (freepatentsonline.com)
  • The compounds were biased toward opioid receptor antagonist activity by incorporating (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine (a potent, nonselective opioid pure antagonist) as one of the monomers. (nih.gov)
  • Screening of these compounds in competitive binding experiments with the kappa opioid receptor selective ligand [3H]U69,593 led to the discovery of a novel kappa opioid receptor selective ligand, N-¿(2'S)-[3-(4-hydroxyphenyl)propanamido]-3'-methylbutyl¿-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine (8, RTI-5989-29). (nih.gov)
  • Piperidine derivative compounds are used as intermediate to make crystal derivative of aromatic nitrogen compounds containing nuclear halogen atoms. (chemicalland21.com)
  • Conclusion: Our findings suggest that compounds bearing spiro-piperidine scaffold, synthesized using reusable nano-catalyst, could be effective biological agents. (eurekaselect.com)
  • Being an alkaloid and secondary metabolite piperidine has also proved active against mosquito larva. (thefreedictionary.com)
  • Piperidine was first obtained from piperine, an alkaloid found in black pepper. (thefreedictionary.com)
  • Gardner DR, Panter KE(1994) Ammodendrine and related piperidine alkaloid levels in the blood plasma of cattle, sheep and goats fed Lupinus formosus. (thefreedictionary.com)
  • Despite being miscible with water, piperidine is a relatively apolar solvent (similar to benzene and considerably less polar than pyridine, chloroform, or ethyl acetate. (ebi.ac.uk)
  • Reaction of 1 with ethyl cyanoacetate in the presence of catalytic amount of piperidine furnished the chromene derivative (12), while its reaction with ethyl cyanoacetate in the presence of ammonium acetate gave the quinoline derivative (13). (thefreedictionary.com)
  • CAS:142851-03-4Synonyms: Ethyl 1-(tert-butoxycarbonyl)-4-piperidine. (chemnet.com)
  • Piperidine, hexahydropyridine, is a family of heterocyclic organic compound derived from p yridine through hydrogenation. (chemicalland21.com)
  • They are used to determine the strain enthalpies of the cyclic amines A-G. The N-alkylated piperidine rings have been found to be about strainless. (ovid.com)
  • The photochemistry and photophysics of piperidine- and steroid- separated bichromophoric systems containing an aroyl azide as the electron acceptor and secondary aromatic amines as the electron donors was examined. (illinois.edu)
  • The Knoevenagel condensation is generally carried out in the presence of weak organic bases such as aliphatic amines, ethylenediamine and piperidine or their corresponding ammonium salts, Lewis bases and acids including Zn[Cl. (thefreedictionary.com)
  • Piperidines are the most prevalent heterocyclic core found in medicines. (ssrn.com)
  • Notable examples of spirocyclic piperidine-containing biologically active natural products are halichlorine, pinnaic acid and tauropinnaic acid. (gla.ac.uk)
  • This method had been employed for the addition of both azido [52, 62, 63] and alkyne functionalities to the BODIPY core in reactions catalyzed by acetic acid and piperidine (Figure 29). (thefreedictionary.com)
  • The broad scope and utility of this catalytic method for enantioselective δ C-C formation by an N-centered radical relay is presented, as well as the conversion of the resulting enantioenriched d amino nitriles to a family of chiral piperidines. (ssrn.com)
  • Enamine's EurJOC paper on the scalable and regioselective preparation of all isomeric (cyclo)alkyl piperidines and the corresponding amino alcohols was featured on the cover of the issue. (enamine.net)
  • This paper presents the results of an optimization study on biaryl piperidine and 4-amino-2-biarylurea MCH1 receptor antagonists, which was accomplished by using quantitative-structure activity relationships (QSARs), classification and virtual screening techniques. (springer.com)
  • Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol . (wikipedia.org)
  • Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: C5H5N + 3 H2 → C5H10NH Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. (wikipedia.org)
  • The Pipe and Kim research groups devised a way to strongly link long polymer chains of a plastic called polyacrylic acid (PAA) with short strands of another called polyacryloyl piperidine (PAP). (thefreedictionary.com)
  • Piperidine is an organic compound with the molecular formula (CH 2 ) 5 NH. (wikipedia.org)
  • Piperidine is an organic compound with the molecular formula (CH2)5NH. (wikipedia.org)
  • 3. A compound of claim 2 wherein Z" and Z'" are each independently a halogen atom or a piperidine group of formula II. (google.com.au)
  • In the title compound, C18H24N6OH2O, the piperidine ring adopts a chair conformation with an NCCC torsion angle of 39. (immune-source.com)
  • We provide independent and unbiased information on manufacturers, prices, production news and consumers for the global and regional (North America, Asia and Europe) market of tert-butyl4-(2-aminophenoxy)piperidine-1-carboxylate. (reportsnreports.com)
  • Finally, the annulation reaction between 2-alkoxy-1,1-cyclobutane diesters and imines or aldehydes gave access to highly functionalized piperidines and tetrahydropyrans, respectively. (oatd.org)
  • piperidine may participate in [http://en.wikipedia.org/wiki/Hydrogenation_of_carbon-nitrogen_double_bonds hydrogenation of C=N double bounds] where the N-substituted chiral imine may be converted to a enamine, the tautomeric form of a imine. (openwetware.org)
  • The bicyclic dihydropyridine products are in some cases unstable, but may be isolated after hydrogenation as fused bicyclic piperidines. (beilstein-journals.org)
  • In this stage, 4-t-butyl-2-(N-piperdinomethyl)cyclohexanone was produced from 4- t-butyl-cyclohexanone, piperidine and paraformaldehyde according to reference one. (thefreedictionary.com)
  • Piperidine is used as a solvent and as a base . (wikipedia.org)
  • 13C NMR: (CDCl3, ppm) 47.27.2, 25.2[citation needed] 1H NMR: (CDCl3, ppm) 2.79, 2.19, 1.51[citation needed] Piperidine is used as a solvent and as a base. (wikipedia.org)
  • Results: The preparation of Yb/chitosan nano-catalyst was verified and the catalyst was found effective towards substituted piperidine formations with the catalyst reusability. (eurekaselect.com)
  • Piperidine is a widely used secondary amine . (wikipedia.org)
  • Silia Bond ® Piperidine (Si-PIP) is a general purpose tertiary amine base to scavenge acids, thereby avoiding salt elimination problems. (silicycle.com)
  • Enamines derived from piperidine are substrates in the Stork enamine alkylation reaction. (wikipedia.org)
  • Upon treatment with calcium hypochlorite, piperidine converts to N-chloropiperidine, a chloramine with the formula C5H10NCl. (wikipedia.org)
  • [20] Enamines derived from piperidine can be used in the Stork enamine alkylation reaction. (wikipedia.org)
  • The work described herein details the development of a methodology capable of accessing both spirocyclic pyran and spirocyclic piperidine core structures from a common cyclic tertiary furfuryl alcohol intermediate. (gla.ac.uk)
  • Spirocyclic piperidines and spirocyclic pyrans are prevalent throughout nature, often appearing in natural products which exhibit exciting biological activities. (gla.ac.uk)
  • It captures n-methylbenzyl-piperidine hcl market trends, pays close attention to n-methylbenzyl-piperidine hcl manufacturers and names suppliers. (marketpublishers.com)
  • The report includes n-methylbenzyl-piperidine hcl description, covers its application areas, manufacturing methods, patents. (marketpublishers.com)
  • The report includes 4-(4-morpholinyl)-piperidine dihydrochloride description, covers its application areas, manufacturing methods, patents. (marketpublishers.com)