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.
Pipecolic acids are a group of amino acids that are produced during the breakdown of certain proteins and are involved in various metabolic processes in the body.
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)
Diphenylacetic acids are a class of organic compounds that have been used in the medical field as anti-inflammatory and analgesic agents.
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)
Pyrrolidines are a class of organic compounds containing a five-membered ring with four carbon atoms and one nitrogen atom, which are used in various medical applications such as as analgesics, anti-inflammatory agents, and muscle relaxants.
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)
Piperidones are a class of organic compounds that are used in the medical field as anti-inflammatory and anti-allergic agents.
Dioxolanes are a class of cyclic ethers with a six-membered ring containing two oxygen atoms, used in various medical applications such as as antiseptics and anesthetics.
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.
Dioxoles are a class of heterocyclic compounds containing an oxygen atom and two carbon atoms in a six-membered ring.
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.
Piperazines are a class of psychoactive drugs that act as anticholinergics, antispasmodics, and central nervous system stimulants, and are sometimes used in the treatment of various medical conditions.
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.
Guanine is a nitrogenous base found in DNA and RNA that plays a crucial role in the genetic code and regulation of gene expression.
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)

Piperidines are a class of organic compounds that contain a six-membered ring with nitrogen atoms at positions 1 and 4. They are commonly used in the pharmaceutical industry as a building block for the synthesis of a wide range of drugs, including analgesics, anti-inflammatory agents, and antihistamines. Piperidines are also found in natural products, such as alkaloids, and have been used in traditional medicine for their various therapeutic effects. In the medical field, piperidines are often used as a starting point for the development of new drugs, as they can be easily modified to produce a wide range of pharmacological activities.

Receptors, Phencyclidine (PCP) are a type of neurotransmitter receptor found in the brain that are activated by the drug phencyclidine (PCP). PCP is a synthetic compound that was originally developed as an anesthetic, but it was later found to have powerful hallucinogenic effects. It works by binding to and activating N-methyl-D-aspartate (NMDA) receptors, which are involved in a variety of brain functions, including learning, memory, and mood regulation. The activation of these receptors by PCP leads to a range of effects, including altered perception, mood changes, and impaired motor coordination. PCP is a potent and dangerous drug, and its use can lead to serious health problems and addiction.

Pipecolic acids are a group of compounds that are produced by the breakdown of certain amino acids in the body. They are found in small amounts in many foods, including meat, fish, and dairy products, and are also produced by the gut bacteria in the digestive system. In the medical field, pipecolic acids are sometimes used as a diagnostic tool to help identify certain medical conditions. For example, elevated levels of pipecolic acids in the blood or urine may be a sign of a genetic disorder called maple syrup urine disease, which is caused by a deficiency in an enzyme that is needed to break down certain amino acids. Pipecolic acids may also have potential therapeutic applications. Some studies have suggested that they may have anti-inflammatory and neuroprotective effects, and they are being investigated as a potential treatment for a variety of conditions, including Alzheimer's disease, Parkinson's disease, and multiple sclerosis. However, more research is needed to fully understand the potential benefits and risks of using pipecolic acids as a treatment.

Receptors, sigma (σ receptors) are a type of G protein-coupled receptors (GPCRs) that are found in the central nervous system and other tissues. They are activated by a variety of endogenous and exogenous ligands, including certain drugs and neurotransmitters. σ receptors are thought to play a role in a number of physiological processes, including pain perception, mood regulation, and the regulation of stress responses. They are also believed to be involved in the development of certain neurological disorders, such as schizophrenia and addiction. There are two main subtypes of σ receptors: σ1 receptors and σ2 receptors. σ1 receptors are found primarily in the brain and are thought to play a role in modulating the effects of other neurotransmitters, such as dopamine and serotonin. σ2 receptors are found throughout the body and are thought to play a role in regulating cell growth and survival. In the medical field, σ receptors are being studied as potential targets for the development of new drugs for the treatment of a variety of conditions, including pain, anxiety, and addiction.

Phencyclidine (PCP) is a synthetic drug that was originally developed as an anesthetic in the 1950s. However, it was later found to have potent hallucinogenic and dissociative effects, leading to its use as a recreational drug. In the medical field, PCP is not currently used as an anesthetic or for any other medical purpose. Instead, it is primarily used in research settings to study the effects of hallucinogens on the brain and behavior. It is also sometimes used in veterinary medicine to anesthetize animals. However, due to its potential for abuse and serious side effects, PCP is a controlled substance and its use is tightly regulated by law.

Diphenylacetic acids are a class of organic compounds that contain a diphenylacetic acid moiety. They are commonly used as intermediates in the synthesis of various pharmaceuticals and other chemicals. In the medical field, diphenylacetic acids have been studied for their potential therapeutic effects on a variety of conditions, including inflammation, pain, and anxiety. Some specific examples of diphenylacetic acids that have been studied in the medical field include: * Dexamethasone diphenylacetic acid (DDA): a synthetic glucocorticoid that has been used to treat a variety of inflammatory conditions, including rheumatoid arthritis and asthma. * Betamethasone diphenylacetic acid (BDA): a synthetic glucocorticoid that has been used to treat a variety of inflammatory conditions, including dermatitis and allergic conjunctivitis. * Prednisolone diphenylacetic acid (PDA): a synthetic glucocorticoid that has been used to treat a variety of inflammatory conditions, including asthma and dermatitis. It is important to note that diphenylacetic acids are not currently used as a standalone treatment for any medical condition, but rather as a component in the synthesis of other pharmaceuticals.

In the medical field, heterocyclic compounds, bridged-ring refer to a class of organic compounds that contain at least one heteroatom (such as nitrogen, oxygen, or sulfur) in the ring structure. These heteroatoms are connected to the carbon atoms of the ring through single or double bonds, and the resulting ring structure is referred to as a bridged-ring heterocycle. Bridged-ring heterocycles are important in the medical field because they often exhibit unique chemical and biological properties that make them useful as drugs or drug candidates. For example, many antibiotics, anti-inflammatory drugs, and anti-cancer drugs contain bridged-ring heterocycles as key structural features. The synthesis and modification of bridged-ring heterocycles is an active area of research in medicinal chemistry, as scientists seek to develop new drugs with improved efficacy and reduced side effects.

Imino sugars are a class of organic compounds that contain a nitrogen atom bonded to two carbon atoms. They are also known as azasugars or azahexitols. In the medical field, imino sugars have been studied for their potential use as antiviral agents, particularly against HIV and hepatitis C virus. They work by inhibiting the activity of enzymes that are essential for the replication of these viruses. Some imino sugars have also been shown to have antifungal and antibacterial properties.

Alkaloids are a diverse group of naturally occurring organic compounds that are derived from plants and have a basic or alkaline nature. They are often found in the leaves, seeds, bark, and roots of plants and are known for their bitter taste and pharmacological properties. In the medical field, alkaloids have been used for centuries as traditional remedies for a variety of ailments, including pain relief, fever reduction, and digestive disorders. Many alkaloids have also been isolated and synthesized for use in modern medicine, particularly in the treatment of cancer, infections, and neurological disorders. Some well-known examples of alkaloids include caffeine, nicotine, morphine, codeine, and quinine. These compounds have a wide range of effects on the body, including stimulating the central nervous system, reducing pain and inflammation, and affecting heart rate and blood pressure. However, it is important to note that many alkaloids can also be toxic in high doses and can cause side effects such as nausea, vomiting, and dizziness. Therefore, the use of alkaloids in medicine is typically closely monitored and regulated by healthcare professionals.

Organosilicon compounds are chemical compounds that contain a carbon-silicon bond. They are commonly used in a variety of medical applications, including as anticoagulants, anti-inflammatory agents, and as components of silicone-based medical devices. One example of an organosilicon compound used in medicine is heparin, which is a naturally occurring anticoagulant. Heparin is often used to prevent blood clots in patients who are at risk of developing deep vein thrombosis or pulmonary embolism. Another example is silastic, a silicone-based material that is used in medical devices such as catheters, implants, and prosthetic devices. Organosilicon compounds can also be used in the treatment of certain medical conditions. For example, some organosilicon compounds have been shown to have anti-inflammatory properties and may be useful in the treatment of conditions such as rheumatoid arthritis. Additionally, some organosilicon compounds have been shown to have antiviral properties and may be useful in the treatment of viral infections. Overall, organosilicon compounds have a wide range of potential medical applications and are an important area of research in the field of medicine.

Lobeline is a naturally occurring alkaloid found in the plant Lobelia inflata, also known as Indian tobacco or pukeweed. It has been used in traditional medicine for its bronchodilatory and anti-inflammatory effects, and has been studied for its potential therapeutic uses in the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). In the medical field, lobeline is sometimes used as a bronchodilator, which helps to relax and widen the airways in the lungs, making it easier to breathe. It is also sometimes used as an anti-inflammatory agent to reduce inflammation in the airways and lungs. However, it is important to note that lobeline is not currently approved for use as a medical treatment by regulatory agencies such as the US Food and Drug Administration (FDA). Its use in medicine is limited and primarily involves research studies and clinical trials.

Haloperidol is a medication that is used to treat various mental health conditions, including schizophrenia, bipolar disorder, and severe anxiety. It is a type of antipsychotic medication that works by blocking the action of dopamine in the brain, which can help to reduce symptoms such as hallucinations, delusions, and disordered thinking. Haloperidol is typically administered orally, although it can also be given intramuscularly or intravenously in certain situations. It is available in both immediate-release and extended-release formulations, and the dosage and frequency of administration will depend on the specific condition being treated and the individual patient's response to the medication. While haloperidol can be effective in managing symptoms of mental illness, it can also have side effects, including drowsiness, dizziness, constipation, dry mouth, and tremors. In some cases, haloperidol can also cause more serious side effects, such as tardive dyskinesia, a movement disorder that can cause involuntary movements of the face, tongue, and limbs. As with any medication, it is important to carefully weigh the potential benefits and risks of haloperidol before starting treatment.

Pyrrolidines are a class of organic compounds that contain a five-membered ring with four carbon atoms and one nitrogen atom. They are commonly used in the medical field as pharmaceuticals, as well as in the synthesis of other drugs and chemicals. One example of a pyrrolidine used in medicine is metoclopramide, which is used to treat nausea and vomiting. Another example is pyrilamine, which is used to treat allergies and hay fever. Pyrrolidines can also be used as chiral auxiliaries in organic synthesis, which allows for the synthesis of enantiomerically pure compounds. This is important in the pharmaceutical industry, as many drugs are effective only when administered in a specific enantiomer. Overall, pyrrolidines are a versatile class of compounds with a wide range of applications in the medical field.

Heterocyclic compounds are organic compounds that contain at least one carbon atom and one heteroatom (such as nitrogen, oxygen, sulfur, or phosphorus) in their ring structure. In the medical field, heterocyclic compounds are often used as pharmaceuticals or as intermediates in the synthesis of pharmaceuticals. Some examples of heterocyclic compounds used in medicine include: - Pyrimidines: These are a class of heterocyclic compounds that contain a six-membered ring with two nitrogen atoms. Pyrimidines are found in many important biological molecules, including DNA and RNA. They are also used in the treatment of various medical conditions, such as cancer, viral infections, and gout. - Purines: These are another class of heterocyclic compounds that contain a six-membered ring with two nitrogen atoms. Purines are also found in DNA and RNA, and they are used in the treatment of conditions such as gout and psoriasis. - Quinolines: These are heterocyclic compounds that contain a six-membered ring with one nitrogen atom and one oxygen atom. Quinolines are used in the treatment of various medical conditions, including malaria, tuberculosis, and leprosy. Overall, heterocyclic compounds play an important role in the development of new drugs and therapies in the medical field.

Amino alcohols are a class of organic compounds that contain both an amino group (-NH2) and an alcohol group (-OH) attached to the same carbon atom. They are commonly found in nature and have a wide range of biological activities, including antimicrobial, antiviral, and anticancer properties. In the medical field, amino alcohols are used as drugs and as intermediates in the synthesis of other drugs. For example, the amino alcohol chloroquine is used to treat malaria, while the amino alcohol amantadine is used to treat influenza. Other amino alcohols, such as proline and hydroxyproline, are important components of collagen, a protein that is essential for the structure and function of connective tissue in the body. Amino alcohols can also be used as precursors for the synthesis of other compounds, such as amino acids and peptides. They are also used in the production of detergents, surfactants, and other industrial chemicals.

The Muscarinic M1 receptor is a type of protein receptor found in the cells of various organs and tissues in the body. It is a subtype of the muscarinic acetylcholine receptor family, which is activated by the neurotransmitter acetylcholine. The M1 receptor is primarily located in the central nervous system, where it plays a role in regulating various functions such as cognition, mood, and movement. It is also found in the heart, smooth muscle, and glands, where it regulates processes such as heart rate, muscle contraction, and glandular secretion. Activation of the M1 receptor can produce a range of effects, depending on the tissue and organ in which it is located. For example, activation of the M1 receptor in the heart can cause the heart to beat faster and stronger, while activation in the smooth muscle of the airways can cause bronchodilation, or widening of the airways. In the medical field, the M1 receptor is an important target for the development of drugs used to treat a variety of conditions, including asthma, Alzheimer's disease, and Parkinson's disease.

Monoacylglycerol lipases (MAGLs) are a group of enzymes that play a crucial role in the metabolism of endocannabinoids, which are signaling molecules that bind to cannabinoid receptors in the brain and body. MAGLs are responsible for breaking down 2-arachidonoylglycerol (2-AG), the most abundant endocannabinoid in the body, into arachidonic acid and glycerol. In the medical field, MAGLs have gained attention as potential therapeutic targets for a variety of conditions, including chronic pain, inflammation, and neurodegenerative diseases. By inhibiting MAGL activity, it is possible to increase the levels of 2-AG in the body, which may have therapeutic benefits. However, it is important to note that the use of MAGL inhibitors is still in the experimental stage and more research is needed to fully understand their potential therapeutic effects and potential side effects.

Receptors, Neurotransmitter are proteins found on the surface of neurons that bind to specific neurotransmitters, such as dopamine, serotonin, or glutamate. These receptors are responsible for transmitting signals across the synapse, the gap between neurons, and play a crucial role in regulating various physiological processes, including mood, memory, and movement. Dysfunction of neurotransmitter receptors has been implicated in a variety of neurological and psychiatric disorders, including depression, anxiety, and schizophrenia.

In the medical field, alkenes are a type of organic compound that contain at least one carbon-carbon double bond. They are unsaturated hydrocarbons, which means they have fewer hydrogen atoms than the maximum possible number for their molecular formula. Alkenes are commonly used in the production of various medical products, including drugs, plastics, and synthetic rubber. They are also used as solvents in some medical procedures and as components in medical devices. One example of an alkene used in medicine is propylene glycol, which is a common ingredient in many medications and medical devices. It is used as a solvent, a preservative, and a stabilizer. Another example is ethylene oxide, which is used as a sterilizing agent for medical equipment and as a precursor for the production of various medical products. Overall, alkenes play an important role in the medical field and are used in a variety of applications to improve patient care and medical technology.

Piperidones are a class of organic compounds that contain a six-membered ring with a nitrogen atom and an oxygen atom. They are commonly used in the medical field as pharmaceuticals, particularly as anti-inflammatory agents and analgesics. Some examples of piperidones include piroxicam, a nonsteroidal anti-inflammatory drug (NSAID) used to treat arthritis and other inflammatory conditions, and etoricoxib, another NSAID used to treat pain and inflammation. Piperidones can also be used as intermediates in the synthesis of other drugs.

Dioxolanes are a class of cyclic ethers that contain two oxygen atoms and one carbon atom in their ring structure. They are commonly used as solvents in various chemical reactions and as intermediates in the synthesis of other compounds. In the medical field, dioxolanes have been studied for their potential use as antiviral agents, particularly against HIV. Some dioxolanes have also been shown to have anti-inflammatory and analgesic properties, and are being investigated as potential treatments for various conditions such as pain and inflammation. However, more research is needed to fully understand the potential therapeutic applications of dioxolanes in medicine.

N-Methylaspartate (NMA) is a chemical compound that is found in the human body. It is a non-essential amino acid that is structurally similar to aspartate, another amino acid that is important for the proper functioning of the nervous system. NMA is thought to play a role in the regulation of neurotransmitter release and has been implicated in a number of neurological disorders, including epilepsy, Alzheimer's disease, and multiple sclerosis. In the medical field, NMA is often used as a research tool to study the function of the nervous system and to develop new treatments for neurological disorders.

Phenazocine is a synthetic opioid analgesic that is used to relieve moderate to severe pain. It is a derivative of pethidine (meperidine) and has similar effects, but with a longer duration of action and a lower potential for respiratory depression. Phenazocine is typically administered intravenously or intramuscularly and is used in a variety of medical settings, including surgery, trauma, and chronic pain management. It is also sometimes used as a substitute for morphine in patients who are allergic to that drug. Phenazocine can cause side effects such as nausea, vomiting, dizziness, and constipation, and it may also be habit-forming with prolonged use.

Benzylidene compounds are a class of organic compounds that contain a benzene ring with a double bond between two carbon atoms that are bonded to a hydrogen atom and an alkyl group. These compounds are often used in the medical field as intermediates in the synthesis of various drugs and other chemical compounds. They are also used as dyes, pigments, and as stabilizers in the production of plastics and other materials. Some examples of benzylidene compounds include benzaldehyde, benzyl acetate, and benzylamine.

Pepstatins are a class of synthetic peptides that are used as inhibitors of aspartic proteases, a type of protease enzyme that cleaves proteins at aspartic acid residues. These proteases are involved in a variety of biological processes, including digestion, blood clotting, and the immune response. Pepstatins are often used in research to study the function of aspartic proteases and to develop new drugs for the treatment of diseases that are caused by the overactivity of these enzymes. They are also used as diagnostic tools to detect the presence of certain diseases, such as cancer and viral infections.

Cadaverine is a chemical compound that is produced by the breakdown of proteins in dead tissue. It is a diamine, which means it has two amine groups (-NH2) attached to a carbon atom. Cadaverine is one of the primary products of putrefaction, the process by which dead tissue decomposes. In the medical field, cadaverine is sometimes used as a diagnostic tool to help identify the cause of death. For example, high levels of cadaverine in the blood or other bodily fluids may indicate that the person died from a traumatic injury, such as a blow to the head. Cadaverine is also used in some laboratory tests to detect the presence of bacteria or other microorganisms that can cause infections. In addition to its use in forensic science and laboratory testing, cadaverine has a number of other applications. It is used as a preservative in some foods, such as sausages and canned meats, to help prevent the growth of bacteria and other microorganisms. It is also used in the production of some dyes and other chemicals.

Benzodioxoles are a class of organic compounds that contain a six-membered ring with two oxygen atoms and one nitrogen atom. They are also known as dibenzodioxoles or dibenzodioxolanes. In the medical field, benzodioxoles are used as a class of drugs that have a wide range of pharmacological activities. Some examples of benzodioxoles that are used in medicine include: 1. Diazepam: A benzodiazepine that is used to treat anxiety, insomnia, and muscle spasms. 2. Lorazepam: Another benzodiazepine that is used to treat anxiety, insomnia, and seizures. 3. Alprazolam: A benzodiazepine that is used to treat anxiety and panic disorder. 4. Clonazepam: A benzodiazepine that is used to treat epilepsy, anxiety, and panic disorder. 5. Triazolam: A benzodiazepine that is used to treat insomnia. Benzodioxoles are also used as intermediates in the synthesis of other drugs, such as anticonvulsants, anesthetics, and antidepressants.

Dioxoles are a class of organic compounds that contain a six-membered ring with two oxygen atoms and two double bonds. They are also known as furan derivatives. In the medical field, dioxoles have been studied for their potential therapeutic properties, including anti-inflammatory, anti-cancer, and anti-viral effects. Some dioxoles have also been used as analgesics and anti-emetics. However, it is important to note that dioxoles can also be toxic and have been associated with adverse effects, such as liver damage and developmental toxicity. Therefore, their use in medicine is carefully regulated and monitored.

Receptors, Opioid are specialized proteins found on the surface of cells in the body that bind to opioid drugs, such as morphine, heroin, and oxycodone. These receptors are part of the body's natural pain-relieving system and are involved in regulating pain, mood, and reward. When opioid drugs bind to these receptors, they can produce a range of effects, including pain relief, sedation, and euphoria. However, long-term use of opioid drugs can lead to dependence and addiction, as the body becomes accustomed to the presence of the drug and requires more of it to achieve the same effect.

Piperazines are a class of organic compounds that contain a six-membered ring with two nitrogen atoms. They are commonly used in the medical field as drugs and are known for their anticholinergic, antispasmodic, and sedative properties. Some examples of piperazine-based drugs include antihistamines, antipsychotics, and antidiarrheals. Piperazines can also be used as intermediates in the synthesis of other drugs.

Papaverine is a medication that is used to treat a variety of medical conditions, including erectile dysfunction, Raynaud's disease, and glaucoma. It is a vasodilator, which means that it helps to widen blood vessels and improve blood flow. Papaverine is usually administered intravenously or intramuscularly, and it can cause side effects such as headache, nausea, and dizziness. It is important to note that papaverine should only be used under the supervision of a healthcare professional.

Receptors, N-Methyl-D-Aspartate (NMDA) are a type of ionotropic glutamate receptor found in the central nervous system. They are named after the agonist N-methyl-D-aspartate (NMDA), which binds to and activates these receptors. NMDA receptors are important for a variety of physiological processes, including learning and memory, synaptic plasticity, and neuroprotection. They are also involved in various neurological and psychiatric disorders, such as schizophrenia, depression, and addiction. NMDA receptors are heteromeric complexes composed of two subunits, NR1 and NR2, which can be differentially expressed in various brain regions and cell types. The NR2 subunit determines the pharmacological properties and functional profile of the receptor, while the NR1 subunit is essential for receptor function. Activation of NMDA receptors requires the binding of both glutamate and a co-agonist, such as glycine or d-serine, as well as the depolarization of the postsynaptic membrane. This leads to the opening of a cation-permeable channel that allows the influx of calcium ions, which can trigger various intracellular signaling pathways and modulate gene expression. In summary, NMDA receptors are a type of glutamate receptor that play a crucial role in various physiological and pathological processes in the central nervous system.

Dizocilpine maleate, also known as dizocilpine or dizocilpine dibromide, is a drug that belongs to a class of compounds called N-methyl-D-aspartate (NMDA) receptor antagonists. It is used in scientific research to study the effects of NMDA receptor antagonists on the brain and nervous system. In the medical field, dizocilpine maleate has been studied for its potential therapeutic effects in a variety of neurological and psychiatric conditions, including Parkinson's disease, Huntington's disease, and schizophrenia. However, it has not been approved for use in humans by regulatory agencies such as the US Food and Drug Administration (FDA) due to concerns about its safety and efficacy. Dizocilpine maleate is a potent and selective NMDA receptor antagonist that blocks the action of glutamate, a neurotransmitter that plays a key role in learning, memory, and other cognitive functions. It is believed that by blocking NMDA receptors, dizocilpine maleate can reduce the overactivity of neurons in the brain that is thought to contribute to the symptoms of certain neurological and psychiatric conditions. However, dizocilpine maleate has also been associated with a range of side effects, including cognitive impairment, psychosis, and motor dysfunction. As a result, its use in humans is limited and is typically only conducted in controlled clinical trials under the supervision of a qualified healthcare professional.

Receptors, Muscarinic are a type of cell surface receptors that are activated by the neurotransmitter acetylcholine. They are found in various tissues throughout the body, including the heart, lungs, digestive system, and central nervous system. There are five subtypes of muscarinic receptors, designated M1 through M5, each with different properties and functions. Activation of muscarinic receptors can produce a wide range of effects, including contraction of smooth muscle, stimulation of glandular secretion, and modulation of neurotransmitter release. In the medical field, muscarinic receptors are important targets for the treatment of various conditions, including asthma, irritable bowel syndrome, and certain types of heart disease. Drugs that interact with muscarinic receptors are often referred to as muscarinic agonists or antagonists, depending on whether they stimulate or block the activity of the receptors.

The serotonin 5-HT2A receptor is a protein found on the surface of certain cells in the brain and body. It is a type of serotonin receptor, which are proteins that bind to and respond to the neurotransmitter serotonin. Serotonin is a chemical messenger that plays a role in regulating a wide range of functions, including mood, appetite, and sleep. The 5-HT2A receptor is involved in a number of physiological processes, including the regulation of mood, cognition, and motor function. It is also thought to play a role in the development of certain mental health conditions, such as schizophrenia and depression. In the medical field, the 5-HT2A receptor is the target of several drugs, including hallucinogens like LSD and psilocybin. These drugs are thought to produce their psychoactive effects by binding to and activating the 5-HT2A receptor, leading to changes in perception, mood, and consciousness. The 5-HT2A receptor is also the target of some medications used to treat mental health conditions, such as schizophrenia and depression.

In the medical field, the hydroxyl radical is a highly reactive molecule that is formed when water molecules are broken down by ionizing radiation or by the presence of certain chemicals. It is also known as the hydroxyl radical or the hydroxyl radical. The hydroxyl radical is a highly reactive molecule that can damage cells and DNA, leading to a variety of health problems. It is also a powerful oxidizing agent that can cause oxidative stress, which is thought to play a role in the development of many diseases, including cancer, cardiovascular disease, and neurodegenerative diseases. In the medical field, the hydroxyl radical is often studied as a potential therapeutic target for the treatment of these diseases. For example, researchers are exploring the use of antioxidants to neutralize the effects of the hydroxyl radical and prevent oxidative stress.

Fentanyl is a synthetic opioid pain medication that is approximately 100 times more potent than morphine. It is used to treat severe pain, such as that caused by cancer or after surgery. Fentanyl is available in a variety of forms, including tablets, lozenges, patches, and injections. It is also sometimes used in combination with other medications, such as hydromorphone or oxycodone, to increase their effectiveness. Fentanyl can be highly addictive and can cause respiratory depression, which can be life-threatening. It is important to use fentanyl only under the guidance of a healthcare professional and to follow their instructions carefully.

2-Amino-5-phosphonovalerate (APV) is a chemical compound that is used in the medical field as a drug. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, which means that it blocks the action of NMDA receptors in the brain. NMDA receptors are a type of ion channel that are involved in a variety of brain functions, including learning, memory, and mood regulation. By blocking NMDA receptors, APV can have a range of effects on the brain, including reducing seizures, improving mood, and reducing anxiety. APV is sometimes used as a treatment for conditions such as epilepsy, depression, and anxiety disorders. It is also being studied as a potential treatment for other neurological and psychiatric conditions.

Aspartic acid is an amino acid that is naturally occurring in the human body. It is a non-essential amino acid, meaning that it can be synthesized by the body from other compounds and does not need to be obtained through the diet. Aspartic acid is found in high concentrations in the brain and spinal cord, and it plays a role in various physiological processes, including the production of neurotransmitters and the regulation of acid-base balance in the body. In the medical field, aspartic acid is sometimes used as a diagnostic tool to measure the function of the liver and kidneys, as well as to monitor the progression of certain diseases, such as cancer and HIV. It is also used as a dietary supplement in some cases.

Guanine is a nitrogenous base that is found in DNA and RNA. It is one of the four nitrogenous bases that make up the genetic code, along with adenine, cytosine, and thymine (in DNA) or uracil (in RNA). Guanine is a purine base, which means it has a double ring structure consisting of a six-membered pyrimidine ring fused to a five-membered imidazole ring. It is one of the two purine bases found in DNA and RNA, the other being adenine. Guanine plays a critical role in the structure and function of DNA and RNA, as it forms hydrogen bonds with cytosine in DNA and with uracil in RNA, which helps to stabilize the double helix structure of these molecules.

DNA, or deoxyribonucleic acid, is a molecule that carries genetic information in living organisms. It is composed of four types of nitrogen-containing molecules called nucleotides, which are arranged in a specific sequence to form the genetic code. In the medical field, DNA is often studied as a tool for understanding and diagnosing genetic disorders. Genetic disorders are caused by changes in the DNA sequence that can affect the function of genes, leading to a variety of health problems. By analyzing DNA, doctors and researchers can identify specific genetic mutations that may be responsible for a particular disorder, and develop targeted treatments or therapies to address the underlying cause of the condition. DNA is also used in forensic science to identify individuals based on their unique genetic fingerprint. This is because each person's DNA sequence is unique, and can be used to distinguish one individual from another. DNA analysis is also used in criminal investigations to help solve crimes by linking DNA evidence to suspects or victims.

Receptors, AMPA are a type of ionotropic glutamate receptor that are widely expressed in the central nervous system. They are named after the neurotransmitter AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid), which is a major excitatory neurotransmitter in the brain. AMPA receptors are important for fast synaptic transmission, as they are rapidly activated by glutamate and can mediate strong postsynaptic currents. They are also involved in a variety of physiological processes, including learning and memory, and have been implicated in several neurological and psychiatric disorders, such as schizophrenia and depression. AMPA receptors are composed of four subunits, each of which contains an ion channel that opens in response to binding of glutamate. There are several different subunit combinations that can form AMPA receptors, which can affect their properties and distribution in the brain.

Aspartic acid endopeptidases are a class of enzymes that cleave peptide bonds in proteins, specifically at the carboxyl side of aspartic acid residues. These enzymes are involved in various physiological processes, including digestion, blood clotting, and the regulation of hormone levels. In the medical field, aspartic acid endopeptidases are often studied for their potential therapeutic applications, such as in the treatment of cancer, neurodegenerative diseases, and infections. They are also used as research tools to study protein structure and function, and to develop new drugs and diagnostic tests.

Acetylcholine is a neurotransmitter that plays a crucial role in the transmission of signals between neurons in the nervous system. It is synthesized from the amino acid choline and is stored in vesicles within nerve cells. When an electrical signal reaches the end of a nerve cell, it triggers the release of acetylcholine into the synaptic cleft, the small gap between the nerve cell and the next cell it communicates with. Acetylcholine then binds to receptors on the surface of the receiving cell, causing a change in its electrical activity. Acetylcholine is involved in a wide range of bodily functions, including muscle movement, memory, and learning. It is also important for the regulation of the autonomic nervous system, which controls involuntary bodily functions such as heart rate and digestion. In the medical field, acetylcholine is used as a diagnostic tool to study the function of the nervous system, particularly in conditions such as Alzheimer's disease and myasthenia gravis. It is also used as a therapeutic agent in the treatment of certain conditions, such as glaucoma and myasthenia gravis, by increasing the activity of the affected nerves.

Amino acids are organic compounds that are the building blocks of proteins. They are composed of an amino group (-NH2), a carboxyl group (-COOH), and a side chain (R group) that varies in size and structure. There are 20 different amino acids that are commonly found in proteins, each with a unique side chain that gives it distinct chemical and physical properties. In the medical field, amino acids are important for a variety of functions, including the synthesis of proteins, enzymes, and hormones. They are also involved in energy metabolism and the maintenance of healthy tissues. Deficiencies in certain amino acids can lead to a range of health problems, including muscle wasting, anemia, and neurological disorders. In some cases, amino acids may be prescribed as supplements to help treat these conditions or to support overall health and wellness.

Pyridines are a class of heterocyclic aromatic compounds that contain a six-membered ring with one nitrogen atom and five carbon atoms. They are commonly used in the medical field as precursors for the synthesis of various drugs and as ligands in metal complexes that have potential therapeutic applications. Some examples of drugs that contain pyridine rings include the antihistamine loratadine, the antipsychotic drug chlorpromazine, and the anti-inflammatory drug ibuprofen. Pyridines are also used as chelating agents to remove heavy metals from the body, and as corrosion inhibitors in the manufacturing of metal products.

The cytochrome P-450 enzyme system is a group of enzymes that are responsible for the metabolism of a wide variety of drugs, toxins, and other substances in the body. These enzymes are found in the liver, lungs, and other organs, and they play a critical role in the detoxification of harmful substances and the elimination of drugs from the body. The cytochrome P-450 enzymes are classified into several families, each of which is responsible for the metabolism of specific types of compounds. For example, the CYP3A family is responsible for the metabolism of a wide variety of drugs, including many commonly prescribed medications. The CYP2D6 family is responsible for the metabolism of some antidepressants, antipsychotics, and other drugs. The activity of the cytochrome P-450 enzyme system can be affected by a variety of factors, including genetic variations, age, sex, and the presence of other medications. In some cases, these factors can lead to differences in the metabolism of drugs, which can affect their effectiveness and the risk of side effects. Overall, the cytochrome P-450 enzyme system plays a critical role in the metabolism of drugs and other substances in the body, and understanding its function is important for the safe and effective use of medications.

... is widely used to convert ketones to enamines. Enamines derived from piperidine are substrates in the Stork enamine ... Piperidine and its derivatives are ubiquitous building blocks in pharmaceuticals and fine chemicals. The piperidine structure ... Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair ... pKa value of piperidinium (protonated piperidine), corresponding to a pKb value of 2.78 for piperidine. Anvisa (2023-03-31). " ...
... 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, ...
Other names in common use include piperidine piperoyltransferase, and piperoyl-CoA:piperidine N-piperoyltransferase. Geisler JG ... piperidine Thus, the two substrates of this enzyme are (E,E)-piperoyl-CoA and piperidine, whereas its two products are CoA and ... In enzymology, a piperidine N-piperoyltransferase (EC 2.3.1.145) is an enzyme that catalyzes the chemical reaction (E,E)- ... The systematic name of this enzyme class is (E,E)-piperoyl-CoA:piperidine N-piperoyltransferase. ...
1-Benzyl-4-[2-(diphenyl​methoxy)​ethyl]​piperidine is a stimulant of the piperidine class which acts as a potent and selective ... "Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine ( ...
... is a drug developed by a team led by Alan Kozikowski, which acts as a potent ... The rearranged structural isomer 2-[1-(4-chlorophenyl)butyl]piperidine is also a potent inhibitor of dopamine reuptake. 4- ... Fluoropethidine Allylprodine JZ-IV-10 N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate WY-46824 US 6180648, Kozikowski AP, ... "Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the ...
N,O-Dimethyl-4β-(2-naphthyl)piperidine-3β-carboxylate (DMNPC) is a piperidine based stimulant drug which is synthesised from ... March 2000). "Further SAR Studies of Piperidine-Based Analogues of Cocaine. 2. Potent Dopamine and Serotonin Reuptake ... piperidine Naphthylamphetamine Naphyrone List of cocaine analogues Tamiz AP, Zhang J, Flippen-Anderson JL, Zhang M, Johnson KM ...
Dimethocaine Procaine Tetracaine Hermans B, Verhoeven H, Janssen P (September 1970). "4-substituted piperidines. V. Local ... Piperidines, Diethylamino compounds, Ethanolamines, All stub articles, Nervous system drug stubs). ...
2-(o-Acylaminophenethyl)piperidines". Journal of Medicinal Chemistry. 16 (9): 1015-20. doi:10.1021/jm00267a012. PMID 4745503. v ... Piperidines, Sodium channel blockers, Withdrawn drugs, All stub articles, Cardiovascular system drug stubs). ...
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 ...
Klioze SS, Bauer VJ, Geyer HM (April 1977). "Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central ... Puri SK, Mantione CR, Petko W, Ellis DB (1979). "Spiroisobenzofuran Piperidine Derivatives. Interaction with Pre- and Post- ... Piperidines, Isobenzofurans, Spiro compounds, All stub articles, Nervous system drug stubs). ...
"PIPERIDINE DERIVATIVES IV. SUBSTITUTED PIPERIDINE-ALKYL BENZOATES AND PARA-AMINOBENZOATES". Journal of the American Chemical ... Piperidines, Benzoate esters, All stub articles, Nervous system drug stubs). ...
... a piperidine derivative. Brand names include Tolson, Mydocalm, Biocalm, Mydeton, Miderizone, Mydoflex, Myolax, ...
Vardanyan R (2017). Piperidine-Based Drug Discovery. Elsevier. ISBN 9780128134283. Consolidated List of Products - Whose ... Piperidines, Butyramides, All stub articles, Gastrointestinal system drug stubs). ...
ISBN 978-0-8155-1856-3. Vardanyan RS (2017). "Chapter 5: 4-Substituted and 1,4-Disubstituted Piperidines". Piperidine-based ...
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 ...
piperidine-brasofensine U.S. Patent 6,376,673 piperidine-tesofensine U.S. Patent 20,060,094,759 Ritalin, Meperidine, sertraline ... 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 ...
"Material Safety Data Sheet: Piperidine". Fisher. 29 October 2007. "Diamorphine (PIM 261F, French)". www.inchem.org. Archived ...
It can be viewed as a derivative of piperidine. 4-Piperidone is used as an intermediate in the manufacture of chemicals and ... "Recent advances in the synthesis of piperidones and piperidines". Tetrahedron. 59 (17): 2953-2989. doi:10.1016/s0040-4020(03) ...
5: Piperidine alkaloids of poison hemlock (Conium maculatum) in: Cheeke, Peter R., ed., Toxicants of Plant Origin: Alkaloids, ... Denić, Marija; Blagojević, Polina; Radulović, Niko (2013). "Synthetic approaches to coniine and other 2-alkyl piperidines". ... piperidine-2-carboxylic acid) and some of its derivatives under varying conditions, that it must belong to the D-series of ... in this case a piperidine). In this way, starting from (S)-alcohol an (S)-enantiomer of Coniine is obtained and vice versa. ...
3F-PCP (C17H24FN). 1-(1-(3-fluorophenyl)cyclohexyl)piperidine. National Forensic Laboratory, Slovenia "Amendment of Minister ...
The suggestion by Körner and Dewar was later confirmed in an experiment where pyridine was reduced to piperidine with sodium in ... The hydrogenation of pyridine to piperidine releases 193.8 kJ·mol−1, which is slightly less than the energy of the ... Ladenburg, A. (1884). "Synthese des Piperidins und seiner Homologen" [Synthesis of piperidine and its homologues]. Berichte der ... ISBN 81-224-1212-2. Ladenburg, A. (1884). "Synthese des Piperidins" [Synthesis of piperidine]. Berichte der Deutschen ...
Klumpp, D. A., Garza, M., Jones, A., Mendoza, S. (1 September 1999). "Synthesis of Aryl-Substituted Piperidines by Superacid ...
... has a bicyclic scaffold consisting of two condensed piperidines. The unsubstituted bispidine backbone can assume ...
... are chemical compounds with a phenyl moiety directly attached to piperidine. There are a variety of ... v t e (Piperidines, All stub articles, Heterocyclic compound stubs). ...
3Cl-PCP (C17H24ClN). 1‐[1‐(3‐chlorophenyl)cyclohexyl]piperidine" (PDF). National Forensic Laboratory. Slovenia. "Amendment of ...
Of these three piperidines, desoxypipradrol has the longest elimination half-life, as it is a highly lipophilic molecule ... Tripod J, Sury E, Hoffmann K (June 1954). "[Analeptic effect of a new piperidine derivative]". Experientia. 10 (6): 261-2. doi: ... Bellucci G (June 1955). "[(2-Diphenylmethyl-piperidine hydrochloride and the methyl ester of 2-chloro-2-phenyl-2-(2-piperidyl)- ... 2-Diphenyl-Methyl-Piperidine Ferris RM, Tang FL (September 1979). "Comparison of the effects of the isomers of amphetamine, ...
Calcium hypochlorite converts piperidine to N-chloropiperidine. Chlorine can be the nucleus of oxyanions with oxidation states ...
... is a piperidine alkaloid that was first isolated from the plant Lythrum anceps. It contains a 17-membered ... Pinder, A. R (1992). "Azetidine, pyrrole, pyrrolidine, piperidine, and pyridine alkaloids". Natural Product Reports. 9 (5): 491 ... Piperidine alkaloids, Cyclophanes, Methoxy compounds, Alcohols, Phenols, Heterocyclic compounds with 4 rings, All stub articles ...
... Molecular Formula: C14H18N4O4 ...
3,4-2H2)Piperidine *Molecular FormulaC5H9D2N ... Piperidine [ACD/IUPAC Name] (3,4-2. H2. )Pipéridine [French] [ ...
Dual Piperidine-Based Histamine H and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.. ... Dual Piperidine-Based Histamine H and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. ... In a series of 16 new ligands, mainly based on the piperidine core, we selected three lead structures (, , and ) for further ... we first focused on an in-depth analysis of the protonation states of piperazine and piperidine derivatives in the studied ...
2R)-2-[(2-fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4-piperidine]-1-yl)propanamide , ...
Piperidines. Piperidine derivatives include PCP and ketamine. PCP was developed in the late 1950s as a dissociative anesthetic/ ...
WGP offers broad capabilities, competitive pricing, exceptional quality and outstanding service to each and every customer.. ...
Piperidine, L-Glutamic Acid, Triethoxymethylsilane offered by Triveni Interchem Private Limited (Group Of Triveni Chemicals), ... Piperidine 110-89-4 is Liquid. It is know as Piperidine .It is use as Pharmaceutical Industry. Storage: Keep container tightly ...
Piperidine. Pyridine. Indazole. Furan. Quinoline. Indole. Oxazole. Thiophene. Other heterocyclic. Senior halogenated ...
1-N-Boc-4-(Phenylamino)piperidine CAS 125541-22-2. Rated 0 out of 5 ...
Piperidine derivatives for the treatment of obesity Butlin, R. J.; Caulkett, P. W. R.; Leach, A.; Newcombe, N. J.; ODonnell, C ... Piperidine derivatives for the treatment of obesity Butlin, R. J.; Caulkett, P. W. R.; Leach, A.; Newcombe, N. J.; ODonnell, C ... Piperidine derivatives for the treatment of obesity. Chloe Atkinson2017-11-07T15:50:43+00:00 ...
... piperidine;_x000D_ (R)-1-Boc-3-(Hydroxymethyl)piperidine;_x000D_ (R)-1-Boc-3-(hyroxymethyl)piperidine;_x000D_ tert-butyl (3R)-3 ... hydroxymethyl)piperidine-1-carboxylate;_x000D_ (R)-tert-Butyl 3-(hydroxymethyl)piperidine-1-carboxylate; Formula. ... R)-1-BOC-3-(hydroxymethyl)piperidine. For more information please contact us at [email protected] or Inquire with a ... R)-(-)-1-Boc-3-(hydroxymethyl)piperidine;_x000D_ R-(-)-1-Boc-3-(hydroxymethyl) ...
... piperidine, including NMR, HPLC, LC-MS, UPLC & more. ... piperidine (200 mg, 0.96 mmol) and pyridine (253 mg, 3.2 mmol) ... 4-(3-chlorobenzyl)-N-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)piperidine-1-carboxamide [ No CAS ] ... piperidine- 1-carboxamide (93.7 mg, 0.26 mmol, 33%) as a brown solid.1H NMR (500 MHz, Dimethylsulfoxide-d6) 8.14 (s, 1H), 7.75- ...
3-Piperidine carboxylic acid. CAS number: 60252-41-7. Groups: All Chemicals. Information: IUPAC Name: (+/-)-3-Piperidine ... PIPERIDINE-3-CARBOXYLIC ACID. PIPERIDINE-3-CARBOXYLIC ACID. RARECHEM AK HD C011. RARECHEM AK PQ 0322. (R,S)-NIPECOTIC ACID. ...
... piperidine IUPAC Name 1-[(E)-but-1-enyl]piperidine InChI InChI=1S/C9H17N/c1-2-3-7-10-8-5-4-6-9-10/h3,7H,2,4-6,8-9H2,1H3/b7-3+ ... ","requires_shipping":true,"taxable":true,"featured_image":null,"available":true,"name":"((E)-1-But-1-enyl)piperidine, \u003e95 ...
... piperidine hydrochloride. 1159825-25-8 MSDS,ROS,1159825-25-8 MOA,COA,SPECS,pecifications,1H-NMR,GHS,CAT #31852 ... For more information, please view Spec of 4-(3-bromophenyl)piperidine hydrochloride 1159825-25-8.pdf. ...
... piperidine 125541-22-2 Melting point 136-137 Boiling point 400.6±38.0 °C(Predicted) density 1.107±0.06 g/cm3(Predicted) storage ... 1-N-Boc-4-(Phenylamino)piperidine 125541-22-2 Melting point 136-137 Boiling point 400.6±38.0 °C(Predicted) density 1.107±0.06 g ... piperidine,br /, 71368-80-4    Bromazolam,br /, 119276-01-6    Protonitazene,br /, 14680-51-4& ...
... piperidine hydrochloride AldrichCPR; Linear Formula: C16H26ClNO; find -PH012346 MSDS, related peer-reviewed papers, technical ...
... *Posted:April 22, 2022 ... Factory Price 1-N-Boc-4-(Phenylamino)piperidine CAS 125541-22-2. Price On Call ...
... piperidine, HCl. CAS Number: 1004618-89-6. Catalog Number: AA0001YI. MDL Number: MFCD08436156. Molecular Formula: C11H14ClF2N. ... Tags:1004618-89-6 Molecular Formula,1004618-89-6 MDL,1004618-89-6 SMILES,1004618-89-6 4-(3,5-Difluorophenyl)piperidine, HCl ...
Handan Tongyi New Material Technology Co., Ltd. Professional export of high-quality chemical raw materials, resin chemical industry, and copper wire, aluminum ingot and other metals ...
Piperidines / pharmacology * RNA, Messenger / metabolism * Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors ...
Asymmetric synthesis of piperidines and octahydroindolizines using a one-pot ring-closure/N-debenzylation procedure ... Asymmetric synthesis of piperidines and octahydroindolizines using a one-pot ring-closure/N-debenzylation procedure ...
... piperidine-1-carboxylate CAS Number 288573-56-8 Molekhule Weight 294.364 Density N/A Ho belisa ... Lebitso: tert-butyl 4-(4-fluoroanilino)piperidine-1-carboxylate. Synonym :Mantsoe a tšoanang le a mang ...
1-Phenethyl-4-(N-phenylpropionamido)piperidine. N-Phenethyl-4-(N-propionylanilino)piperidine. 1-Phenethyl-4-( ... phenylpropionylamino) piperidine. 1-Phenethyl-4-N-propionylanilinopiperidine. N-(1-Phenethyl-4-piperidyl)propionanilide. ...
... hydroxyethyl isobutyl piperidine carboxylate; Kothrin, 20% deltamethrin (Bayer Crop Science, Monheim am Rhein, Germany). ...
Fentanyl immediate precursor chemical, 4-anilino-N-phenethyl-4-piperidine (ANPP).. h2. Norfentanyl (N-phenyl-N-(piperidin-4-yl ... Some trade or other names: 1-[1-(2-thienyl)-cyclohexyl]-piperidine, 2-thienyl analog of phencyclidine, TPCP, TCP. ... any substitution on the piperidine ring, any substitution on or replacement of the propanamide group, any substitution on the ...
4.2.2.2 2-(Hydroxymethyl)piperidine. 4.2.2.3 Amberlite XAD-2 non-ionic polymeric adsorbent, 20 to 60 mesh, Aldrich Chemical XAD ... The acrolein sampling tubes contain XAD-2 adsorbent coated with 2-(hydroxymethyl)piperidine (2-HMP) which reacts with acrolein ... 3.2.4 Amberlite XAD-2 adsorbent coated with 2-(hydroxymethyl-piperidine (2-HMP), 10% by weight (Section 4). ... piperidine. The samples are desorbed with toluene and then analyzed by gas chromatography using a nitrogen selective detector. ...
Buy (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride hemihydrate,tech.,97%,10g online ... 3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride hemihydrate,tech.,97%,10g ... 3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride hemihydrate,tech.,97%,10g is used in ... Shop All (3s,4r)-3-((Benzo[D][1,3]Dioxol-5-Yloxy)Methyl)-4-(4-Fluorophenyl)Piperidine Hydrochloride Hemihydrate,Tech. products ...
Concurrent N-H and alpha-C-H bond activations of pyrrolidine and piperidine under ambient conditions by 18e tungsten allyl ... Concurrent N-H and alpha-C-H bond activations of pyrrolidine and piperidine under ambient conditions by 18e tungsten allyl ... Concurrent N-H and alpha-C-H bond activations of pyrrolidine and piperidine under ambient conditions by 18e tungsten allyl ...
  • 1-N-Boc-4-(Phenylamino)piperidine 125541-22-2 Melting point 136-137 Boiling point 400.6±38.0 °C(Predicted) density 1.107±0.06 g/cm3(Predicted) storage temp. (croozi.com)
  • For more information, please view Spec of 4-(3-bromophenyl)piperidine hydrochloride 1159825-25-8.pdf . (capotchem.com)
  • 3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride hemihydrate,tech.,97%,10g is typically sold in 1x1 Gram, 1x250 Milligram, 1x100mg Milligram, 1x5g Gram, and 1x10g Gram quantities and has a chemical weight of 749.668. (chemdirect.com)
  • Therefore, we first focused on an in-depth analysis of the protonation states of piperazine and piperidine derivatives in the studied compounds. (iasp-pain.org)
  • Part 3: Tropenyl and homotropenyl-piperidine urea derivatives. (bvsalud.org)
  • However, we kept in mind that within the previous series, a pair of closely related compounds, and , differing only in the piperazine/piperidine moiety in the structural core showed a significantly different affinity at sigma-1 receptors (σRs). (iasp-pain.org)
  • History or evidence of allergy or hypersensitivity to Fexofenadine, Loratadine, Levocetirizine, Cetirizine, Hydroxyzine or any piperidine derivative drugs or any of the excipients of this product. (who.int)
  • The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide γ-secretase inhibitors is reported. (nih.gov)
  • Piperidine is a staple component for the synthesis of complex drugs and chemicals. (psychonautwiki.org)
  • 3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride,tech.,97%,250mg has the molecular formula C19H21ClFNO3, and its chemical weight is 365.8264. (chemdirect.com)
  • Piperidine with 99% purity and above is the purest form of piperidine available. (researchandmarkets.com)
  • The pharmaceutical end-use industry is boosting the demand for piperidine with 99% purity. (researchandmarkets.com)
  • Substituted piperidines refers to a class of compounds which can produce stimulant , analgesic or dissociative effects. (psychonautwiki.org)
  • Piperidines include compounds which can produce a variety of pharmacological effects. (psychonautwiki.org)
  • The growth of the piperidine market is attributed to its high demand as solvents, base and catalyst in pharmaceutical, agrochemical and other industries. (researchandmarkets.com)
  • High affinity phenyl-piperidine P2Y 14 R antagonist 1 (PPTN) was modified with piperidine bridging moieties to probe receptor affinity and hydrophobicity. (nih.gov)
  • The piperidine market comprises major manufacturers, Jubilant Ingrevia Limited (India), Vertellus (US), KOEI Chemical Co. Ltd. (Japan), and BASF (Germany). (researchandmarkets.com)
  • 1-(3-Chloro-4-methylphenyl)piperidine is a useful research chemical. (cymitquimica.com)
  • The study includes an in-depth competitive analysis of these key players in the piperidine market, with their company profiles, and key market strategies. (researchandmarkets.com)