Aminoquinolines: Quinolines substituted in any position by one or more amino groups.Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404)Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.Hemolytic Agents: Substances that are toxic to blood in general, including the clotting mechanism; hematotoxins may refer to the hematopoietic system.Antimalarials: Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)Mefloquine: A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.Glucosephosphate Dehydrogenase Deficiency: A disease-producing enzyme deficiency subject to many variants, some of which cause a deficiency of GLUCOSE-6-PHOSPHATE DEHYDROGENASE activity in erythrocytes, leading to hemolytic anemia.Plasmodium: A genus of protozoa that comprise the malaria parasites of mammals. Four species infect humans (although occasional infections with primate malarias may occur). These are PLASMODIUM FALCIPARUM; PLASMODIUM MALARIAE; PLASMODIUM OVALE, and PLASMODIUM VIVAX. Species causing infection in vertebrates other than man include: PLASMODIUM BERGHEI; PLASMODIUM CHABAUDI; P. vinckei, and PLASMODIUM YOELII in rodents; P. brasilianum, PLASMODIUM CYNOMOLGI; and PLASMODIUM KNOWLESI in monkeys; and PLASMODIUM GALLINACEUM in chickens.Plasmodium falciparum: A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.Malaria: A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.Drug Resistance: Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.Drug Evaluation, Preclinical: Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.World War I: Global conflict primarily fought on European continent, that occurred between 1914 and 1918.World War II: Global conflict involving countries of Europe, Africa, Asia, and North America that occurred between 1939 and 1945.American Civil War: 1861-1865 conflict between the Union (Northern states) and the 11 Southern states that seceded and were organized as the Confederate States of America.War: Hostile conflict between organized groups of people.History, 20th Century: Time period from 1901 through 2000 of the common era.Malaria, Falciparum: Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.Halogenation: Covalent attachment of HALOGENS to other compounds.Fluorine: A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as flouride (FLUORIDES) to prevent dental caries.Sulfonamides: A group of compounds that contain the structure SO2NH2.Stereoisomerism: 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)Rhodium: Rhodium. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)Iridium: A metallic element with the atomic symbol Ir, atomic number 77, and atomic weight 192.22.Chloroquinolinols: 8-Hydroxyquinolinols chlorinated on the number 5 and/or 7 carbon atom(s). They are antibacterial, antiprotozoal, and antidiarrheal, especially in amebiasis, and have also been used as antiseborrheics. The compounds are mostly used topically, but have been used also as animal feed additives. They may cause optic and other neuropathies and are most frequently administered in combination with other agents.PyrazinesPhosgene: A highly toxic gas that has been used as a chemical warfare agent. It is an insidious poison as it is not irritating immediately, even when fatal concentrations are inhaled. (From The Merck Index, 11th ed, p7304)Mass Spectrometry: An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.Vacuoles: Any spaces or cavities within a cell. They may function in digestion, storage, secretion, or excretion.Melanoma: A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)Skin Neoplasms: Tumors or cancer of the SKIN.Cell Line, Tumor: A cell line derived from cultured tumor cells.Melanocytes: Mammalian pigment cells that produce MELANINS, pigments found mainly in the EPIDERMIS, but also in the eyes and the hair, by a process called melanogenesis. Coloration can be altered by the number of melanocytes or the amount of pigment produced and stored in the organelles called MELANOSOMES. The large non-mammalian melanin-containing cells are called MELANOPHORES.Melanoma, Experimental: Experimentally induced tumor that produces MELANIN in animals to provide a model for studying human MELANOMA.Artemisinins: A group of SESQUITERPENES and their analogs that contain a peroxide group (PEROXIDES) within an oxepin ring (OXEPINS).Drug Overdose: Accidental or deliberate use of a medication or street drug in excess of normal dosage.Alcohol Drinking: Behaviors associated with the ingesting of alcoholic beverages, including social drinking.Pregnancy: The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.Alcohols: Alkyl compounds containing a hydroxyl group. They are classified according to relation of the carbon atom: primary alcohols, R-CH2OH; secondary alcohols, R2-CHOH; tertiary alcohols, R3-COH. (From Grant & Hackh's Chemical Dictionary, 5th ed)Fraud: Exploitation through misrepresentation of the facts or concealment of the purposes of the exploiter.Medicare Assignment: Concept referring to the standardized fees for services rendered by health care providers, e.g., laboratories and physicians, and reimbursement for those services under Medicare Part B. It includes acceptance by the physician.Insurance, Health, Reimbursement: Payment by a third-party payer in a sum equal to the amount expended by a health care provider or facility for health services rendered to an insured or program beneficiary. (From Facts on File Dictionary of Health Care Management, 1988)Competitive Bidding: Pricing statements presented by more than one party for the purpose of securing a contract.Purchasing, Hospital: Hospital department responsible for the purchasing of supplies and equipment.Chlorine Compounds: Inorganic compounds that contain chlorine as an integral part of the molecule.Contract Services: Outside services provided to an institution under a formal financial agreement.Metals, Heavy: Metals with high specific gravity, typically larger than 5. They have complex spectra, form colored salts and double salts, have a low electrode potential, are mainly amphoteric, yield weak bases and weak acids, and are oxidizing or reducing agents (From Grant & Hackh's Chemical Dictionary, 5th ed)Metals: Electropositive chemical elements characterized by ductility, malleability, luster, and conductance of heat and electricity. They can replace the hydrogen of an acid and form bases with hydroxyl radicals. (Grant & Hackh's Chemical Dictionary, 5th ed)Cadmium: An element with atomic symbol Cd, atomic number 48, and atomic weight 114. It is a metal and ingestion will lead to CADMIUM POISONING.Mercury: A silver metallic element that exists as a liquid at room temperature. It has the atomic symbol Hg (from hydrargyrum, liquid silver), atomic number 80, and atomic weight 200.59. Mercury is used in many industrial applications and its salts have been employed therapeutically as purgatives, antisyphilitics, disinfectants, and astringents. It can be absorbed through the skin and mucous membranes which leads to MERCURY POISONING. Because of its toxicity, the clinical use of mercury and mercurials is diminishing.EthylenediaminesXanthine: A purine base found in most body tissues and fluids, certain plants, and some urinary calculi. It is an intermediate in the degradation of adenosine monophosphate to uric acid, being formed by oxidation of hypoxanthine. The methylated xanthine compounds caffeine, theobromine, and theophylline and their derivatives are used in medicine for their bronchodilator effects. (Dorland, 28th ed)Copper: A heavy metal trace element with the atomic symbol Cu, atomic number 29, and atomic weight 63.55.

Central nervous system-mediated hyperglycemic effects of NIK-247, a cholinesterase inhibitor, and MKC-231, a choline uptake enhancer, in rats. (1/943)

We investigated the effects of intracerebroventricular administration of NIK-247 (9-amino-2,3,5,6,7,8-hexahydro-1H-cyclo-penta(b)-quinoline monohydrate hydrochloride; a cholinesterase inhibitor) or MKC-231 (2-(2-oxypyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofur o[2,3-b]quinolin-4-yl) acetoamide; a choline uptake enhancer) on plasma glucose level in comparison with that of neostigmine administration in rats. The extents of NIK-247- and MKC-231-induced hyperglycemia were considerably less than that by neostigmine, suggesting that the potencies of the drugs to produce the peripheral hyperglycemia may be pharmacologically negligible.  (+info)

The immune response modifier imiquimod requires STAT-1 for induction of interferon, interferon-stimulated genes, and interleukin-6. (2/943)

Imiquimod is an oral inducer of interferon (IFN) and several other proinflammatory cytokines and has been successfully used topically as an antiviral agent for the treatment of genital warts. We have investigated the molecular mechanisms by which imiquimod induces the expression of IFNs, IFN-stimulated genes (ISGs), and proinflammatory cytokines in vivo, using mice deficient in various components of the IFN signaling system. Mice deficient in the transcription factor interferon regulatory factor 1 (IRF-1) or in the serine/threonine protein kinase PKR responded normally to imiquimod, producing high levels of circulating IFN and induction of several ISGs. On the other hand, when mice deficient in STAT-1 were treated, a 32-fold reduction in the level of circulating IFN was observed, together with a lack of induction of 2-5 oligo adenylate synthetase (2-5 OAS) and IRF-1 genes. Interestingly, there was also a lack of induction of interleukin-6 (IL-6) gene expression, although tumor necrosis factor was induced and readily detected in serum. In mice deficient in the type I IFN receptor, imiquimod induced levels of IFN similar to those in control mice, but again, neither 2-5 OAS, IRF-1, nor IL-6 genes were induced in mutant mice. Our results suggest that STAT-1 plays a critical role in the mechanism of gene activation by imiquimod. Moreover, induction of IL-6 gene expression appears to be dependent on components of the IFN signaling cascade.  (+info)

Nitric oxide inhibits L-type Ca2+ current in glomus cells of the rabbit carotid body via a cGMP-independent mechanism. (3/943)

Previous studies have shown that nitric oxide (NO) inhibits carotid body sensory activity. To begin to understand the cellular mechanisms associated with the actions of NO in the carotid body, we monitored the effects of NO donors on the macroscopic Ca2+ current in glomus cells isolated from rabbit carotid bodies. Experiments were performed on freshly dissociated glomus cells from adult rabbit carotid bodies using the whole cell configuration of the patch-clamp technique. The NO donors sodium nitroprusside (SNP; 600 microM, n = 7) and spermine nitric oxide (SNO; 100 microM, n = 7) inhibited the Ca2+ current in glomus cells in a voltage-independent manner. These effects of NO donors were rapid in onset and peaked within 1 or 2 min. In contrast, the outward K+ current was unaffected by SNP (600 microM, n = 6), indicating that the inhibition by SNP was not a nonspecific membrane effect. 2-(4-carboxyphenyl)-4,4,5, 5-tetramethyl-imidazoline-1-oxyl-3-oxide (carboxy-PTIO; 500 microM), an NO scavenger, prevented inhibition of the Ca2+ current by SNP (n = 7), whereas neither superoxide dismutase (SOD; 2,000 U/ml, n = 4), a superoxide scavenger, nor sodium hydrosulfite (SHS; 1 mM, n = 7), a reducing agent, prevented inhibition of the Ca2+ current by SNP. However, SNP inhibition of the Ca2+ current was reversible in the presence of either SOD or SHS. These results suggest that NO itself inhibits Ca2+ current in a reversible manner and that subsequent formation of peroxynitrites results in irreversible inhibition. SNP inhibition of the Ca2+ current was not affected by 30 microM LY 83, 583 (n = 7) nor was it mimicked by 600 microM 8-bromoguanosine 3':5'-cyclic monophosphate (8-Br-cGMP; n = 6), suggesting that the effects of NO on the Ca2+ current are mediated, in part, via a cGMP-independent mechanism. N-ethylmaleimide (NEM; 2.5 mM, n = 6) prevented the inhibition of the Ca2+ current by SNP, indicating that SNP is acting via a modification of sulfhydryl groups on Ca2+ channel proteins. Norepinephrine (NE; 10 microM) further inhibited the Ca2+ current in the presence of NEM (n = 7), implying that NEM did not nonspecifically eliminate Ca2+ current modulation. Nisoldipine, an L-type Ca2+ channel blocker (2 microM, n = 6), prevented the inhibition of Ca2+ current by SNP, whereas omega-conotoxin GVIA, an N-type Ca2+ channel blocker (1 microM, n = 9), did not prevent the inhibition of Ca2+ current by SNP. These results demonstrate that NO inhibits L-type Ca2+ channels in adult rabbit glomus cells, in part, due to a modification of calcium channel proteins. The inhibition might provide one plausible mechanism for efferent inhibition of carotid body activity by NO.  (+info)

Possible novel mechanism for bitter taste mediated through cGMP. (4/943)

Taste is the least understood among sensory systems, and bitter taste mechanisms pose a special challenge because they are elicited by a large variety of compounds. We studied bitter taste signal transduction with the quench-flow method and monitored the rapid kinetics of the second messenger guanosine 3',5'-cyclic monophosphate (cGMP) production and degradation in mouse taste tissue. In response to the bitter stimulants, caffeine and theophylline but not strychnine or denatonium cGMP levels demonstrated a rapid and transient increase that peaked at 50 ms and gradually declined throughout the following 4.5 s. The theophylline- and caffeine-induced effect was rapid, transient, concentration dependent and gustatory tissue-specific. The effect could be partially suppressed in the presence of the soluble guanylyl cyclase (GC) inhibitor 10 microM ODQ and 30 microM methylene blue but not 50 microM LY 83583 and boosted by nitric oxide donors 25 microM NOR-3 or 100 microM sodium nitroprusside. The proposed mechanism for this novel cGMP-mediated bitter taste signal transduction is cGMP production partially by the soluble GC and caffeine-induced inhibition of one or several phosphodiesterases.  (+info)

Treatment of experimental leishmaniasis with the immunomodulators imiquimod and S-28463: efficacy and mode of action. (5/943)

There is a need for new, effective, and less toxic treatments for leishmaniasis, an infectious disease caused by Leishmania protozoa and is a major cause of suffering and morbidity in much of the developing world. Imiquimod, an immune-response modifier, has recently been approved by the Food and Drug Administration for the treatment of genital warts caused by human papillomaviruses. Imiquimod initiates a local immune reaction, including the stimulation of macrophages, resulting in resolution of human papillomavirus infection and regression of the viral lesion. Since imiquimod activates a number of immune cells, including macrophages, which are the only host cells of Leishmania species, an investigation was done to determine whether it induces leishmanicidal properties in infected macrophages in vitro and in vivo in a mouse model. Imiquimod and a related compound, S-28463, effectively stimulated leishmanicidal activity in macrophages; moreover, imiquimod stimulated signal transduction associated with inducing nitric oxide synthesis in macrophages.  (+info)

Protection against hydrogen peroxide cytotoxicity in rat-1 fibroblasts provided by the oncoprotein Bcl-2: maintenance of calcium homoeostasis is secondary to the effect of Bcl-2 on cellular glutathione. (6/943)

The oncoprotein Bcl-2 protects cells against apoptosis, but the exact molecular mechanism that underlies this function has not yet been identified. Studying H2O2-induced cell injury in Rat-1 fibroblast cells, we observed that Bcl-2 had a protective effect against the increase in cytosolic calcium concentration and subsequent cell death. Furthermore, overexpression of Bcl-2 resulted in an alteration of cellular glutathione status: the total amount of cellular glutathione was increased by about 60% and the redox potential of the cellular glutathione pool was maintained in a more reduced state during H2O2 exposure compared with non-Bcl-2-expressing controls. In our cytotoxicity model, disruption of cellular glutathione homoeostasis closely correlated with the pathological elevation of cytosolic calcium concentration. Stabilization of the glutathione pool by Bcl-2, N-acetylcysteine or glucose delayed the cytosolic calcium increase and subsequent cell death, whereas depletion of glutathione by dl-buthionine-(S, R)-sulphoximine, sensitized Bcl-2-transfected cells towards cytosolic calcium increase and cell death. We therefore suggest that the protection exerted by Bcl-2 against H2O2-induced cytosolic calcium elevation and subsequent cell death is secondary to its effect on the cellular glutathione metabolism.  (+info)

Nitric oxide stimulates cGMP production and mimics synaptic responses in metacerebral neurons of Aplysia. (7/943)

Nitric oxide (NO) acts as a neurotransmitter and neuromodulator in the nervous systems of many vertebrates and invertebrates. We investigated the mechanism of NO action at an identified synapse between a mechanoafferent neuron, C2, and the serotonergic metacerebral cell (MCC) in the cerebral ganglion of the mollusc Aplysia californica. Stimulation of C2 produces a decreasing conductance, very slow EPSP in the MCC. C2 is thought to use histamine and NO as cotransmitters at this synapse, because both agents mimic the membrane responses. Now we provide evidence that treatment with NO donors stimulates soluble guanylyl cyclase (sGC) in the MCC, and as a result cGMP increases. S-Nitrosocysteine (SNC, an NO donor) and 8-bromo-cGMP (8-Br-cGMP) both induced the membrane depolarization and increase in input resistance that are characteristic of the very slow EPSP. Two inhibitors of sGC, 6-anilino-5,8-quinolinequinone (LY83583) and 1H-[1,2,4]oxadiazolo[4, 3-a]quinoxaline-1-one (ODQ), suppressed both the very slow EPSP and the membrane responses to SNC but not the histamine membrane responses. NO-induced cGMP production was determined in the MCC using cGMP immunocytochemistry (cGMP-IR). In the presence of 3-isobutyl-1-methylxanthine (IBMX), 10 microM SNC was sufficient to induce cGMP-IR, and the staining intensity increased as the SNC dose was increased. This cGMP-IR was suppressed by ODQ in a dose-dependent manner and completely blocked by 10 microM ODQ. Histamine did not induce cGMP-IR. The results suggest that NO stimulates sGC-dependent cGMP synthesis in the MCC and that cGMP mediates the membrane responses. The cotransmitter histamine induces essentially the same membrane responses but seems to use a separate and distinct second messenger pathway.  (+info)

Histochemically reactive zinc in plaques of the Swedish mutant beta-amyloid precursor protein transgenic mice. (8/943)

Endogenous metals such as zinc may contribute to beta-amyloid (Abeta) aggregation and hence the plaque formation. In the present study, we examined brains of four Swedish mutant amyloid precursor protein (APP) transgenic mice at 12 months of age for histochemically reactive zinc in the plaques. Here, we report that all the Congo red (+) mature plaques contained chelatable zinc, as demonstrated by staining with the zinc-specific fluorescent dye 6-methoxy-8-quinolyl-para-toluenesulfonamide (TSQ). On the other hand, Congo red (-) preamyloid Abeta deposits were not stained with TSQ. Interestingly, although cerebellum contained similar degree of preamyloid Abeta deposits as cerebral cortex, it was completely devoid of Congo red- or TSQ-stained mature plaques. Although zinc from plaques was only slowly and partially removed by a specific zinc remover, dithizone, treatment of brain sections with heparinase-III, which degrades heparan sulfate proteoglycan (HSPG), another major constituent of plaques, greatly fastened the zinc removal with dithizone. The present study has demonstrated the presence of histochemically reactive zinc in plaques, but not preamyloid Abeta deposits, of the Swedish mutant APP transgenic mice. Because preamyloid Abeta deposits fail to develop into congophilic plaques in cerebellum where synaptic vesicle zinc is deficient, the synaptic zinc may be a necessary element in the plaque formation. In holding zinc inside plaques, HSPG may contribute in addition to Abeta.  (+info)

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Chloroquine (CQ), a 4-aminoquinoline, accumulates in acidic digestive vacuoles of the malaria parasite, preventing conversion of toxic haematin to beta-haematin. We examine how bis 4-aminoquinoline piperaquine (PQ) and its hydroxy-modification (OH-PQ) retain potency on chloroquine-resistant (CQ-R) Plasmodium falciparum. For CQ, PQ, OH-PQ and 4 and 5, representing halves of PQ, beta-haematin inhibitory activity (BHIA) was assayed, while potency was determined in CQ-sensitive (CQ-S) and CQ-R P. falciparum. From measured pK(a)s and the pH-modulated distribution of base between water and lipid (logD), the vacuolar accumulation ratio (VAR) of charged drug from plasma water (pH 7.4) into vacuolar water (pH 4.8) and lipid accumulation ratio (LAR) were calculated. All agents were active in BHIA. In CQ-S, PQ, OH-PQ and CQ were equally potent while 4 and 5 were 100 times less potent. CQ with two basic centres has a VAR of 143,482, while 4 and 5, with two basic centres of lower pK(a)s have VARs of 1287 and ...
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Information about using Aldara cream to treat three different skin conditions: genital warts, small superficial skin cancers and actinic keratoses.
Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of ,= 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo pr...olonged ...
IMIQUIMOD, 1 INDICATIONS AND USAGE Aldara Cream is indicated for the topical treatment of: •Clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses (AKs) on the face or scalp in immunocompetent
This treatment is highly effective for the precancerous actinic keratoses, especially when used to treat in cases with numerous lesions. It is about 80% effective in the treatment of superficial skin cancers. It is 50-80% effective in the treatment of very superficial skin cancers.. It is more unpredictable than Efudix and reactions may be severe and can lead to ulceration and scarring. It may be associated with a "flu like" illness (especially when large areas area treated). It is for these reasons, that SPSSCC will typically recommend Efudix instead of Aldara.. ...
Treatment: ALDARA from your local pharmacy. 1.Apply 3 times per week (such as Monday, Wednesday, and Friday) for no longer than 16 weeks. 2. Apply the cream from one Aldara packet to the treatment area, and rub in the cream until it disappears. 3. Do not cover the treated skin areas with any type of plastic bandaging, and avoid nylon underwear. 4. You may wear cotton gauze or underwear over the treated area. 5. Use the medicine before going to bed and leave it on for 6 to 10 hours. Then wash off the medicine with water and a mild soap.. 6. When treating genital warts around the vagina, avoid getting the cream on the more sensitive inner layers of vaginal tissue. This could result in vaginal swelling or irritation and painful urination.. 7. Aldara is not a cure for molluscum or genital warts and it may not keep you from spreading this condition to others through vaginal, anal, or oral sex. You may develop new lesions during treatment with Aldara. ...
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Zyclara: Imiquimod cream belongs to a group of medications called immune response modifiers. It works by stimulating the bodys defenses to fight certain types of skin conditions. Imiquimod cream is used to treat actinic keratosis (AK) on the face or balding scalp in adults. AK is a skin condition that could turn into skin cancer (symptoms include rough, red, scaly patches or lesions, or crusts) that is caused by chronic sun exposure.
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Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
The cyclization of 3-N(4- and 5-benzimidazolyl and benztriazolyl)amino-2-cyano- and 2-ethoxycarbonyl-2-propenoate esters Ia, b-IVa, b under the conditions of the Gould-Jacobs reaction leads to angularly ring-fused substituted imidazo or triazolo[4,5-f] (V, VI) and [4,5-h] (VII, VIII) quinolines, respectively. The esters Vb-VIIIb have been transformed into the corresponding chloroderivatives Vc-VIIIc. 3-N(5-Benzimidazolyl and 5-benztriazolyl)amino-2-cyano-2-propenenitriles are cyclized in the presence of aluminium(III) chloride to give the aminoquinolines Vd, VId. The structure of the products has been characterized by their 1H, 13C NMR, IR, and UV spectra.. ...
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Imiquimod is a medication successfully used in the treatment of skin diseases. In addition to its known mechanism of action, it also triggers other processes in the body. Scientists at the Technical University of Munich (TUM) have succeeded in explaining the molecular fundamentals of these additional effects. The results also shine a new light on other known molecular processes which could indicate an approach to the treatment of inflammatory illnesses.
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Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
J-113,397 LY-2940094 SB-612,111 Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (2000). "4-Aminoquinolines: novel ...
... and aminoquinoline structures!) (Error! the last step must involve As2O5, not As2O3 as an oxidant in Skraup reaction!): An ...
... is a 4-aminoquinoline compound related to chloroquine. Amodiaquine was first made in 1948. It is on the World ...
... is a member of the drug class 4-aminoquinoline. It works against the asexual form of malaria inside the red blood ...
2ohl: X-ray crystal structure of beta secretase complexed with 2-aminoquinoline ...
... is an 8-aminoquinoline drug used for the treatment of malaria. It is closely related to primaquine. Pamaquine was the ... 1 August 2004). "Short report: The activity of pamaquine, an 8-aminoquinoline drug, against sporozoite-induced infections of ...
"Formation of derivatives of dioxindole from esters of mesoxalic acid and aromatic amines or amino quinolines". Compt. Rend. 156 ...
Shinkai, H; Ito, T; Iida, T; Kitao, Y; Yamada, H; Uchida, I (2000). „4-Aminoquinolines: novel nociceptin antagonists with ...
... is an analog of pamaquine which was the first drug of the 8-aminoquinoline class; tafenoquine is another such drug. ...
Two doses of the 8-aminoquinoline plasmoquine were given weekly to workers and their families in two camps. The prevalences of ... For example, the widespread use of 8-aminoquinolines in areas where Glucose-6-phosphate dehydrogenase deficiency is common ...
His PhD dissertation focused on the preparation and properties of 5-aminoquinoline-6-carboxylic acid and related compounds. ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
Most were 8-aminoquinoline compounds, analogs of pamaquine, an existing alternative to quinine that was unfavorable due to its ... primarily from the 8-aminoquinoline group of compounds. The study marked the first human test of the antimalarial drug ...
Later when synthetic derivatives of quinine were introduced, chloroquine phosphate, a 4-aminoquinoline was found to be less ...
... is an 8-aminoquinoline drug manufactured by GlaxoSmithKline that is being investigated as a potential treatment for ...
... the first synthetic antimalarial compound-Atabrin and this was followed by Resochin and Sontochin derived from 4-aminoquinoline ...
... aminoquinolines MeSH D03.438.810.050.060 --- amodiaquine MeSH D03.438.810.050.180 --- chloroquine MeSH D03.438.810.050.180.350 ...
8-Aminoquinoline is a form of aminoquinoline with an amine at the 8-position of quinoline. ... The 8-aminoquinoline family of drugs contains three members, primaquine, tafenoquine and pamaquine[1] and are used in the ... The 8-aminoquinoline drugs must not be given to patients with G6PD deficiency, because they cause potentially fatal haemolysis ... "Short report: The activity of pamaquine, an 8-aminoquinoline drug, against sporozoite-induced infections of Plasmodium vivax ( ...
Depending upon the location of the amino group, they can be divided into: 4-Aminoquinoline 8-Aminoquinoline. ... Aminoquinolines are derivatives of quinoline, most notable for their roles as antimalarial drugs. ...
4-Aminoquinoline is a form of aminoquinoline with the amino group at the 4-position of the quinoline. A variety of derivatives ... Bourne SA, De Villiers K, Egan TJ (2006). "Three 4-aminoquinolines of antimalarial interest". Acta Crystallogr C. 62 (Pt 2): ... Amodiaquine Chloroquine Hydroxychloroquine Bray PG, Hawley SR, Ward SA (1996). "4-Aminoquinoline resistance of Plasmodium ... of 4-aminoquinoline are antimalarial agents useful in treating erythrocytic plasmodial infections. Examples include amodiaquine ...
3-Aminoquinoline 0.98; CAS No.: 580-17-6; Synonyms: 3-AQ; 3-Quinolinamine; Linear Formula: C9H8N2; Empirical Formula: C9H8N2; ... 3-Aminoquinoline was used:. • in liquid matrix for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) for ...
5-Aminoquinoline 99.0 %, TCI America 5G Chemicals:Organic Compounds:Organoheterocyclic compounds:Quinolines and derivatives: ... 5-aminoquinoline,5-quinolinamine,quinoline, 5-amino,5-quinolylamine,quinolin-5-ylamine,unii-yyj34z13sh,5-amino-quinoline,ccris ... 5-aminoquinoline,5-quinolinamine,quinoline, 5-amino,5-quinolylamine,quinolin-5-ylamine,unii-yyj34z13sh,5-amino-quinoline,ccris ...
EN) 2-AMINO-QUINOLINE DERIVATIVES. (FR) DÉRIVÉS DE 2-AMINO-QUINOLÉINE. Abstract: (EN) Described herein are 2-amino-quinoline ... in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.. (FR) Linvention ...
Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in ... There was considerable discussion of Plasmodium falciparum resistance to the 4-aminoquinolines and to mefloquine. The ... A Role for 8-Aminoquinolines in Falciparum Malaria? * Author(s): * Publisher: The American Society of Tropical Medicine and ... Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in ...
We developed a copper-catalyzed 5-position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives. The reaction ... 5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives Y. Kuninobu, M. Nishi and M. Kanai, Org. Biomol. ... On the other hand, the trifluoromethylation of 8-aminoquinolines was also promoted by other Lewis acids as well as a copper ... These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. ...
... amino]quinoline-4-carboxamide
RE: The tariff classification of 8-Aminoquinoline (CAS 578-66-5) from China and Tricyclic Olefin from Italy.. Dear Mr. von ... In your letter dated February 4, 1999, you requested a tariff classification ruling for 8-Aminoquinoline which you have stated ... The applicable subheading for 8-Aminoquinoline will be 2933.40.7000, Harmonized Tariff Schedule of the United States (HTS), ...
It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which ... It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which ... Title : Method for Inducing Protection in Animal Against Cyanide Poisoning Using 8-Aminoquinolines. ...
... amino]quinoline-4-carboxamide
S. Ray, B. Madrid, P. Catz et al., "Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive ... Exploring QSAR for Antimalarial Activities and Drug Distribution within Blood of a Series of 4-Aminoquinoline Drugs Using ... "Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities," Bioorganic and Medicinal ... "Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug ...
This is the first report of 4-aminoquinoline drug resistance in P. falciparum malaria in a country north of Colombia in the ... 4-aminoquinoline drugs. The cure rate was only 22%. Failures were represented by relapses, persistence of the parasitemia, or ... Plasmodium Falciparum Malaria in Panama Resistant to 4-Aminoquinoline Drugs * * Martin D. Young, Carl M. Johnson ... This is the first report of 4-aminoquinoline drug resistance in P. falciparum malaria in a country north of Colombia in the ...
Graves, P.M.; Gelband, H.; Garner, P. Primaquine or other 8-aminoquinoline for reducing P. falciparum transmission. Cochrane ...
Buy 6-Chloro-8-aminoquinoline (CAS 5470-75-7), a derivative used in the preparation fungitoxic analogs, from Santa Cruz. MF: ... 6-Chloro-8-aminoquinoline A derivative used in the preparation fungitoxic analogs *Home. ... 6-Chloro-8-aminoquinoline (CAS 5470-75-7) *bvseo_sdk, java_sdk, bvseo-3.2.0 ... 6-Chloro-8-aminoquinoline is a di-substituted quinoline derivative used in the preparation fungitoxic analogs. ...
A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. ... C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions ... C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions Y. ... A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. ...
Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria. July 29, ... Home » Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria ... Widespread drug-resistant Plasmodium falciparum strains have challenged the pivotal role played by 4- aminoquinolines, ...
In Vivo and In Vitro Efficacy of Amodiaquine againstPlasmodium falciparumin an Area of Continued Use of 4-Aminoquinolines in ... or second-line treatment in areas with similar patterns of 4-aminoquinoline resistance should be reassessed. ...
8-aminoquinoline (m-CPAQ) was synthesized. Palladium(Ⅱ) reacts with m-CPAQ to form a violet-blue ternary complex in the ... A new reagent 5-(3-carboxylphenylazo)-8-aminoquinoline (m-CPAQ) was synthesized. Palladium(Ⅱ) reacts with m-CPAQ to form a ... Spectrophotometric Determination of Palladium(Ⅱ) with 5-(3-Carboxylphenylazo)-8-Aminoquinoline. Huang Zhangjie, Shen Tao, Xu ... 8-aminoquinoline-5-azo)-8-hydroxy-3, 6-naphthalenedisulfonic acid with copper[J];Metallurgical Analysis;2002-02. ...
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... Novel 6-acylamino-2-aminoquinoline melanin-concentrating hormone 1 receptor (MCH1R) antagonists were identified by sequential ...
Multivariate Modeling of Cytochrome P450 Enzymes for 4- Aminoquinoline Antimalarial Analogues using Genetic- Algorithms ... by chloroquine and a new series of 4-aminoquinoline derivatives in order to obtain a set of predictive in-silico models using ...
The synthesis and characterization of N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide (L), an aminoquinoline ... The synthesis and characterization of N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide (L), an aminoquinoline ... A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of ... an aminoquinoline - pyrazinamide hybrid, and the complexes (N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide)( ...
Aminoquinoline based highly sensitive fluorescent sensor for lead(II) and aluminum(III) and its application in live cell ... A method for aminoquinoline-directed, cobalt-promoted dimerization of benzamides has been developed. Reactions proceed in ... An operationally simple and general method for copper-catalyzed, aminoquinoline-assisted amination of β-C(sp(2))-H bonds of… ... A method for cobalt-catalyzed, aminoquinoline-directed ortho-functionalization of sp2 C-H bonds with alkenes has been developed ...
  • 400 mu M). Through detailed structure-activity study, we have identified 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines (5 and 10) as biofilm formation inhibitors with 50% biofilm inhibition at 69 mu M and 63 mu M in S. marcescens and P. aeruginosa, respectively. (ac.rs)
  • 2-Aminoquinolines showed promise as bioavailable nNOS inhibitors but suffered from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. (rcsb.org)
  • AbstractPurpose of ReviewTo review the current status of 8-aminoquinolines in the prophylaxis of malaria among travelers, in light of the recent approval of tafenoquine.Recent FindingsPrimaquine continues to provide excellent primary prophylaxis against allPlasmodium species. (medworm.com)
  • P. B. Madrid, A. P. Liou, J. L. DeRisi, and R. K. Guy, "Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum ," Journal of Medicinal Chemistry , vol. 49, no. 15, pp. 4535-4543, 2006. (hindawi.com)
  • Our data show that 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines present the promising scaffolds for developing antivirulence and anti-biofilm formation agents against multidrug-resistant bacterial species. (ac.rs)
  • 8-Aminoquinolines are an important class of antiparasitic agents, with broad utility and excellent efficacy, but also limitations due to hematological toxicities, primarily methemoglobinemia and hemolysis. (elsevier.com)
  • The 8-aminoquinoline drugs must not be given to patients with G6PD deficiency , because they cause potentially fatal haemolysis in these patients. (wikipedia.org)
  • Safety of 8-aminoquinolines given to people with G6PD deficiency: protocol for systematic review of prospective studies. (lstmed.ac.uk)
  • It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which are administered orally. (dtic.mil)
  • These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. (rsc.org)