Bactericidal cationic quaternary ammonium surfactant used as a topical anti-infective agent. It is an ingredient in medicaments, deodorants, mouthwashes, etc., and is used to disinfect apparatus, etc., in the food processing and pharmaceutical industries, in surgery, and also as a preservative. The compound is toxic orally as a result of neuromuscular blockade.
Portraits as Topic
An independent state in the West Indies. Its capital is Castries. It was probably discovered by Columbus in 1502 and first settled by the English in 1605. Contended for by the French and English in the 17th century, it was regarded as neutral in 1748 but changed hands many times in the wars of the 19th century. It became a self-governing state in association with Great Britain in 1967 and achieved independence in 1979. Columbus named it for the day on which he discovered it, the feast of St. Lucy, a Sicilian virgin martyr. (From Webster's New Geographical Dictionary, 1988, p1051 & Room, Brewer's Dictionary of Names, 1992, p477)
Polymers of silicone that are formed by crosslinking and treatment with amorphous silica to increase strength. They have properties similar to vulcanized natural rubber, in that they stretch under tension, retract rapidly, and fully recover to their original dimensions upon release. They are used in the encapsulation of surgical membranes and implants.
A tube-like invagination of the EPIDERMIS from which the hair shaft develops and into which SEBACEOUS GLANDS open. The hair follicle is lined by a cellular inner and outer root sheath of epidermal origin and is invested with a fibrous sheath derived from the dermis. (Stedman, 26th ed) Follicles of very long hairs extend into the subcutaneous layer of tissue under the SKIN.
Critical and exhaustive investigation or experimentation, having for its aim the discovery of new facts and their correct interpretation, the revision of accepted conclusions, theories, or laws in the light of newly discovered facts, or the practical application of such new or revised conclusions, theories, or laws. (Webster, 3d ed)
Receptor, Serotonin, 5-HT2A
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.
Receptor, Serotonin, 5-HT2C
A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.
Mibefradil (Ro 40-5967) inhibits several Ca2+ and K+ currents in human fusion-competent myoblasts. (1/606)1. The effect of mibefradil (Ro 40-5967), an inhibitor of T-type Ca2+ current (I(Ca)(T)), on myoblast fusion and on several voltage-gated currents expressed by fusion-competent myoblasts was examined. 2. At a concentration of 5 microM, mibefradil decreases myoblast fusion by 57%. At this concentration, the peak amplitudes of I(Ca)(T) and L-type Ca2+ current (I(Ca)(L)) measured in fusion-competent myoblasts are reduced by 95 and 80%, respectively. The IC50 of mibefradil for I(Ca)(T) and I(Ca)(L) are 0.7 and 2 microM, respectively. 3. At low concentrations, mibefradil increased the amplitude of I(Ca)(L) with respect to control. 4. Mibefradil blocked three voltage-gated K+ currents expressed by human fusion-competent myoblasts: a delayed rectifier K+ current, an ether-a-go-go K+ current, and an inward rectifier K+ current, with a respective IC50 of 0.3, 0.7 and 5.6 microM. 5. It is concluded that mibefradil can interfere with myoblast fusion, a mechanism fundamental to muscle growth and repair, and that the interpretation of the effect of mibefradil in a given system should take into account the action of this drug on ionic currents other than Ca2+ currents. (+info)
Developmental regulation of expression of the D3 dopamine receptor in rat nucleus accumbens and islands of Calleja. (2/606)The dopamine D3 receptor (D3R) belongs to the D2 subfamily and is expressed in the rat brain in targets of the mesolimbic dopaminergic system. Little is known about its normal development and control by dopaminergic innervation. We studied developmental expression of D3R in the rat nucleus accumbens (NAC) and islands of Calleja (ISC). At postnatal day (P) 7, D3 binding sites and mRNA were low in both areas. By P14, D3R and mRNA concentrations were close to adult levels in the ISC, whereas, in the NAC, binding increased until 3 months after birth. Cellular concentrations of D3 mRNA in the ISC increased with age in conjunction with a decrease in the number of D3 positive cells. In the NAC, the number of positive cells increased, whereas cellular levels of expression remained unchanged. Neonatal 6-hydroxydopamine lesion caused age-dependent changes in D3R expression. D3 binding sites did not change at P7 or P14, but there was a reduction in the number of D3 mRNA positive neurons accompanied by an increase in cellular levels of D3 mRNA at P14, suggesting that changes occurred in a subset of neurons. Up-regulation of D3 binding sites in NAC and ISC occurred 1 month after the lesion (P35) concomitant with a decrease in cellular levels of D3 mRNA and the number of D3 mRNA positive cells. At 3 months (P90) after the lesion, an increase in D3 mRNA occurred with no change in D3 binding sites. D3R shows region-specific dynamics in receptor/mRNA expression during development and is sensitive to loss of dopamine in early postnatal development. (+info)
Genetic analysis of biodegradation of tetralin by a Sphingomonas strain. (3/606)A strain designated TFA which very efficiently utilizes tetralin has been isolated from the Rhine river. The strain has been identified as Sphingomonas macrogoltabidus, based on 16S rDNA sequence similarity. Genetic analysis of tetralin biodegradation has been performed by insertion mutagenesis and by physical analysis and analysis of complementation between the mutants. The genes involved in tetralin utilization are clustered in a region of 9 kb, comprising at least five genes grouped in two divergently transcribed operons. (+info)
Central hypothyroidism associated with retinoid X receptor-selective ligands. (4/606)BACKGROUND: The occurrence of symptomatic central hypothyroidism (characterized by low serum thyrotropin and thyroxine concentrations) in a patient with cutaneous T-cell lymphoma during therapy with the retinoid X receptor-selective ligand bexarotene led us to hypothesize that such ligands could reversibly suppress thyrotropin production by a thyroid hormone-independent mechanism and thus cause central hypothyroidism. METHODS: We evaluated thyroid function in 27 patients with cutaneous T-cell lymphoma who were enrolled in trials of high-dose oral bexarotene at one institution. In addition, we evaluated the in vitro effect of triiodothyronine, 9-cis-retinoic acid, and the retinoid X receptor-selective ligand LGD346 on the activity of the thyrotropin beta-subunit gene promoter. RESULTS: The mean serum thyrotropin concentration declined from 2.2 mU per liter at base line to 0.05 mU per liter during treatment with bexarotene (P<0.001), and the mean serum free thyroxine concentration declined from 1.0 ng per deciliter (12.9 pmol per liter) at base line to 0.45 ng per deciliter (5.8 pmol per liter) (P<0.001) during treatment. The degree of suppression of thyrotropin secretion tended to be greater in patients treated with higher doses of bexarotene (>300 mg per square meter of body-surface area per day) and in those with a history of treatment with interferon alfa. Nineteen patients had symptoms or signs of hypothyroidism, particularly fatigue and cold intolerance. The symptoms improved after the initiation of thyroxine therapy, and all patients became euthyroid after treatment with bexarotene was stopped. In vitro, LGD346 suppressed the activity of the thyrotropin beta-subunit gene promoter in thyrotrophs by as much as 50 percent, an effect similar to that of triiodothyronine and 9-cis-retinoic acid. CONCLUSIONS: Hypothyroidism may develop in patients with cutaneous T-cell lymphoma who are treated with high-dose bexarotene, most likely because the retinoid X receptor-selective ligand suppresses thyrotropin secretion. (+info)
Estradiol modulates vascular response to melatonin in rat caudal artery. (5/606)The purpose of this study was to determine whether estrogen modulates the function of vascular melatonin receptors. We used the rat caudal artery and found that the contractile effects of melatonin were influenced by the estrous cycle, ovariectomy, and estrogen replacement. In arterial ring segments isolated from female rats, melatonin potentiated, in a concentration-dependent manner, contractions produced either by adrenergic nerve stimulation or by phenylephrine. Constrictor responses to melatonin were smaller in arteries from female rats in proestrus compared with other stages of the estrous cycle and after ovariectomy. Administration of 17beta-estradiol to ovariectomized female rats also resulted in decreased constriction of isolated arteries to melatonin; however, in vitro addition of 17beta-estradiol (10(-7) M) had no effect. In the caudal artery, melatonin appears to act on two receptor subtypes that mediate contraction and relaxation, respectively. The selective melatonin MT2-receptor antagonist 4-phenyl-2-propionamidotetraline (4P-PDOT) enhanced constrictor responses to melatonin in arterial segments from intact female rats, consistent with the inhibition of MT2 receptor-mediated relaxation. In contrast, 4P-PDOT had no significant effect in arteries from ovariectomized female rats. However, when estradiol was replaced in vivo, the effect of 4P-PDOT on melatonin responses was restored. Thus circulating estradiol appears to enhance MT2 melatonin-receptor function in the thermoregulatory caudal artery of the female rat resulting in increased vasodilatation in response to melatonin. (+info)
Metabolic interactions between mibefradil and HMG-CoA reductase inhibitors: an in vitro investigation with human liver preparations. (6/606)AIMS: To determine the effects of mibefradil on the nletabolism in human liver microsomal preparations of the HMG-CoA reductase inhibitors simvastatin, lovastatin, atorvastatin, cerivastatin and fluvastatin. METHODS: Metabolism of the above five statins (0.5, 5 or 10 microM), as well as of specific CYP3A4/5 and CYP2C8/9 marker substrates, was examined in human liver microsomal preparations in the presence and absence of mibefradil (0.1-50 microM). RESULTS: Mibefradil inhibited, in a concentration-dependent fashion, the metabolism of the four statins (simvastatin, lovastatin, atorvastatin and cerivastatin) known to be substrates for CYP3A. The potency of inhibition was such that the IC50 values (<1 microM) for inhibition of all of the CYP3A substrates fell within the therapeutic plasma concentrations of mibefradil, and was comparable with that of ketoconazole. However, the inhibition by mibefradil, unlike that of ketoconazole, was at least in part mechanism-based. Based on the kinetics of its inhibition of hepatic testosterone 6beta-hydroxylase activity, mibefradil was judged to be a powerful mechanism-based inhibitor of CYP3A4/5, with values for Kinactivation, Ki and partition ratio (moles of mibefradil metabolized per moles of enzyme inactivated) of 0.4 min(-1), 2.3 microM and 1.7, respectively. In contrast to the results with substrates of CYP3A, metabolism of fluvastatin, a substrate of CYP2C8/9, and the hydroxylation of tolbutamide, a functional probe for CYP2C8/9, were not inhibited by mibefradil. CONCLUSION: Mibefradil, at therapeutically relevant concentrations, strongly suppressed the metabolism in human liver microsomes of simvastatin, lovastatin, atorvastatin and cerivastatin through its inhibitory effects on CYP3A4/5, while the effects of mibefradil on fluvastatin, a substrate for CYP2C8/9, were minimal in this system. Since mibefradil is a potent mechanism-based inhibitor of CYP3A4/5, it is anticipated that clinically significant drug-drug interactions will likely ensue when mibefradil is coadministered with agents which are cleared primarily by CYP3A-mediated pathways. (+info)
Morphological transformation induced by activation of the mitogen-activated protein kinase pathway requires suppression of the T-type Ca2+ channel. (7/606)Transformation of fibroblasts by various oncogenes, including ras, mos, and src accompanies with characteristic morphological changes from flat to round (or spindle) shapes. Such morphological change is believed to play an important role in establishing malignant characteristics of cancer cells. Activation of the mitogen-activated protein kinase (MAPK) pathway is a converging downstream event of transforming activities of many oncogene products commonly found in human cancers. Intracellular calcium is known to regulate cellular morphology. In fibroblasts, Ca2+ influx is primarily controlled by two types of Ca2+ channels (T- and L-types). Here, we report that the T-type current was specifically inhibited in cells expressing oncogenically activated Ras as well as gain-of-function mutant MEK (MAPK/extracellular signal-regulated kinase (ERK) kinase, a direct activator of MAPK), whereas treatment of ras-transformed cells with a MEK-specific inhibitor restored T-type Ca2+ channel activity. Using a T-type Ca2+ channel antagonist, we further found that suppression of the T-type Ca2+ channel by the activated MAPK pathway is a prerequisite event for the induction and/or maintenance of transformation-associated morphological changes. (+info)
Combination of calcium channel blockers and beta-adrenoceptor blockers for patients with exercise-induced angina pectoris: a double-blind parallel-group comparison of different classes of calcium channel blockers. Netherlands Working Group on Cardiovascular Research (WCN). (8/606)AIMS: The combination of calcium channel blockers and beta-adrenoceptor blockers is more effective for the treatment of exercise-induced angina pectoris than beta-adrenoceptor blocker monotherapy. As ischaemia in exercise-induced angina is preceded by increase in heart rate, calcium channel blockers with negative chronotropic properties may perform better for this purpose than nonchronotropic compounds. METHODS: A 335 patient double-blind parallel-group study comparing 14 day treatment with amlodipine 5 and 10 mg, with diltiazem 200 and 300 mg, and mibefradil 50 and 100 mg added to baseline beta-adrenoceptor blocker treatment was performed. Exercise testing (ETT) was performed by bicycle ergometry. RESULTS: Although none of the calcium channel blockers improved duration of exercise or amount of workload, all significantly delayed onset of 1 mm ST-segment depression on ETT (P<0.001 for any treatment vs baseline). In addition, mibefradil, both low and high dose treatment, produced the longest delays (low dose: different from diltiazem and amlodipine by 24.1 and 29.8 s, respectively, P<0. 003 and <0.001; high dose: different from diltiazem and amlodipine by 33.7 and 37.0 s, respectively, P<0.001 and <0.001). These effects were linearly correlated with the reduction in rate pressure product (RPP). Serious symptoms of dizziness occurred significantly more frequently on mibefradil (P<0.05), and 19 patients on mibefradil withdrew from trial. CONCLUSIONS: Calcium channel blockers with negative chronotropic properties provide greater delay of ischaemia in patients with exercise-induced angina, but the concomitant risk of intolerable dizziness attenuates this benefit. (+info)
Global Market Report of 1,1,4,4,6-Pentamethyl-1,2,3,4-tetrahydronaphthalene (CAS 6683-48-3)
Global Market Report of 1,1,4,4,6-Pentamethyl-1,2,3,4-tetrahydronaphthalene (CAS 6683-48-3) aims at providing comprehensive data on 1,1,4,4,6-Pentamethyl-1,2,3,4-tetrahydronaphthalene globally and regionally (Europe, Asia, North America, Latin America etc.). It captures 1,1,4,4,6-Pentamethyl-1,2,3,4-tetrahydronaphthalene market trends, pays close attention to 1,1,4,4,6-Pentamethyl-1,2,3,4-tetrahydronaphthalene manufacturers and consumers ...
DGIST Scholar: Effect of bexarotene on differentiation of glioblastoma multiforme compared with ATRA
Glioblastoma multiforme (GBM) is the most aggressive malignant brain tumor. Since differentiation can attenuate or halt the growth of tumor cells, an image-based phenotypic screening was performed to find out drugs inducing morphological differentiation of GBMs. Bexarotene, a selective retinoid X receptor agonist, showed strong inhibition of neurospheroidal colony formation and migration of cultured primary GBM cells. Bexarotene treatment reduced nestin expression, while significantly increasing glial fibrillary acidic protein (GFAP) expression. The effect of bexarotene on gene expression profile was compared with the activity of all-trans retinoic acid (ATRA), a well-known differentiation inducer. Both drugs largely altered the gene expression pattern into a tumor-ameliorating direction. These drugs increased the gene expression levels of Kruppel-like factor 9 (KLF9), regulator of G-protein signaling 4 (RGS4), growth differentiation factor 15 (GDF15), angiopoietin-like protein 4 (ANGPTL4), and ...
The effects of the dopamine agonist rotigotine on hemispatial neglect following stroke. - Wellcome Centre for Integrative...
Hemispatial neglect following right-hemisphere stroke is a common and disabling disorder, for which there is currently no effective pharmacological treatment. Dopamine agonists have been shown to play a role in selective attention and working memory, two core cognitive components of neglect. Here, we investigated whether the dopamine agonist rotigotine would have a beneficial effect on hemispatial neglect in stroke patients. A double-blind, randomized, placebo-controlled ABA design was used, in which each patient was assessed for 20 testing sessions, in three phases: pretreatment (Phase A1), on transdermal rotigotine for 7-11 days (Phase B) and post-treatment (Phase A2), with the exact duration of each phase randomized within limits. Outcome measures included performance on cancellation (visual search), line bisection, visual working memory, selective attention and sustained attention tasks, as well as measures of motor control. Sixteen right-hemisphere stroke patients were recruited, all of whom
RXR-Selective retinoid, Bexarotene (Targretin) upregulates IL2R expression and enhances sensitivity of B-chronic lymphocytic...
RXR-Selective retinoid, Bexarotene (Targretin) upregulates IL2R expression and enhances sensitivity of B-chronic lymphocytic leukemia (CLL) cells to Denileukin diftitox (ONTAK). RXR-Selective retinoid, Bexarotene (Targretin) upregulates IL2R expression and enhances sensitivity of B-chronic lymphocytic leukemia (CLL) cells to Denileukin diftitox (ONTAK). 2001; 91(11a, Suppl. ):150a ...
Bexarotene Reduces Blood-Brain Barrier Permeability in Cerebral Ischemia-Reperfusion Injured Rats
Background Matrix metalloproteinase-9 (MMP-9) over-expression disrupts the blood-brain barrier (BBB) in the ischemic brain. The retinoid X receptor agonist bexarotene suppresses MMP-9 expression in endothelial cells and displays neuroprotective effects. Therefore, we hypothesized that bexarotene may have a beneficial effect on I/R-induced BBB dysfunction. Methods A total of 180 rats were randomized into three groups (n = 60 each): (i) a sham-operation group, (ii) a cerebral ischemia-reperfusion (I/R) group, and (iii) an I/R+bexarotene group. Brain water content was measured by the dry wet weight method. BBB permeability was analyzed by Evans Blue staining and the magnetic resonance imaging contrast agent Omniscan. MMP-9 mRNA expression, protein expression, and activity were assessed by reverse transcription polymerase chain reaction, Western blotting, and gelatin zymography, respectively. Apolipoprotein E (apoE), claudin-5, and occludin expression were analyzed by Western blotting. Results After 24
The RXR Agonist Bexarotene Improves Cholesterol Homeostasis and Inhibits Atherosclerosis Progression in a Mouse Model of Mixed...
In the present report, we show that bexarotene, a rexinoid used in humans, inhibits atherogenesis in the apoE2-KI mouse. Bexarotene treatment induces effects both on systemic plasma lipid parameters and on macrophage lipid homeostasis. Bexarotene likely exerts atheroprotection in apoE2-KI mice by lowering circulating atherogenic cholesterol-containing lipoproteins. Interestingly, the pronounced effect of bexarotene treatment on plasma cholesterol concentrations coincides with a decrease in intestinal cholesterol absorption, which is associated with a reduced intestinal gene expression of NPC1L1 and CD13. Indeed, NPCL1 has been recently identified as a target of the hypocholesterolemic drug ezetimibe through regulating intestinal cholesterol absorption.14-18 Thus, inhibiting NPC1L1 activity by ezetimibe in apoE-KO mice14 or gene expression by bexarotene in apoE2-KI mice leads to a decreased susceptibility to atherosclerosis. CD13 has been identified as a molecule potentially implicated in ...
1-phenyl-3-dimethylamino-6-chloro-7-hydroxy-1,2,3,4-tetrahydronaphthalene Summary Report | CureHunter
1-phenyl-3-dimethylamino-6-chloro-7-hydroxy-1,2,3,4-tetrahydronaphthalene: RN refers to (trans)-isomer; a phenylaminotetralin; structure given in first source
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2-CHLORO-1-(5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)ETHANONE (CAS 5803-67-8) Market Research Report 2018
2-CHLORO-1-(5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)ETHANONE (CAS 5803-67-8) Market Research Report 2018 aims at providing comprehensive data on 2-chloro-1-(5,6,7,8-tetrahydronaphthalen-2-yl)ethanone
A Phase I Study of Bexarotene, a Retinoic X Receptor Agonist, in Non-M3 Acute Myeloid Leukemia | Clinical Cancer Research
This phase I study has defined a clinically active and tolerable dose of bexarotene for patients with non-M3 AML. Importantly, we identified no severe DLTs in this population. In addition, we identified laboratory and clinical evidence of differentiation of non-M3 myeloid leukemic cells in response to retinoid X receptor activation as well as evidence of clinical response in chemotherapy refractory non-M3 AML. The findings establish retinoid X receptor agonists as a novel class of therapeutic agents for the treatment of non-M3 AML.. This trial has identified 300 mg/m2 as the maximum patient tolerable dose for bexarotene in patients with AML. Our study was originally done in a phase I format to identify AML-specific side effects of bexarotene that might reduce the standard treatment dose. In previous phase I and II studies in patient with cutaneous T-cell lymphoma and solid tumors, bexarotene was tested up to 600 mg/m2 and found to be safe but difficult to tolerate (9, 15). In addition, in a ...
Dual efficacy of delta opioid receptor-selective ligands for ethanol drinking and anxiety<...
TY - JOUR. T1 - Dual efficacy of delta opioid receptor-selective ligands for ethanol drinking and anxiety. AU - Van Rijn, Richard M.. AU - Brissett, Daniela I.. AU - Whistler, Jennifer. PY - 2010/1/1. Y1 - 2010/1/1. N2 - Alcoholism and anxiety disorders have a huge impact on society and afflict 17.6 million and 40 million people in the United States, respectively. A strong comorbidity exists between alcoholism and anxiety disorders. Indeed, alcohol withdrawal-induced anxiety is a primary contributing factor for relapse, and anxiolytics are a common adjuvant therapy prescribed for treatment-seeking alcoholics. It is thought that the use of alcohol to self-medicate and relieve anxiety contributes to the development of addiction. Treatment for anxiety disorders and alcoholism exist but are not universally effective. The delta opioid receptor (DOR) plays a role in both alcohol consumption and anxiety, making it a very interesting clinical target. Two pharmacologically distinct DORs have been ...
CAS 170638-05-8 (R)-7-Methoxy-2-aminotetraline hydrochloride - BOC Sciences
Boc Sciences offers cas 170638-05-8 (R)-7-Methoxy-2-aminotetraline hydrochloride in bulk,please inquire us to get a quote for 170638-05-8 (R)-7-Methoxy-2-aminotetraline hydrochloride.
2S)-7-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine hydrochloride, in stock
MolPort offers (2S)-7-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine hydrochloride for your scientific research needs. It is also know by registry numbers ZINC000002567334. This compound is available from 1 suppliers, including Axon Medchem.
6-Chloro-1,2,3,4-tetrahydronaphthalen-2-amine | C10H12ClN - PubChem
6-Chloro-1,2,3,4-tetrahydronaphthalen-2-amine | C10H12ClN | CID 16244336 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Bexarotene QuickView - Correlation Engine
Bexarotene is a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs). Bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy. Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models ...
Patent US5856490 - Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and ... - Google Patents
Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
Targretin® (bexarotene) gel 1% - Drug label and information - Rx Drugs Info
Targretin® gel was evaluated for the treatment of patients with early stage (Stage IA-IIA) CTCL in one multicenter, open-label, clinical trial as well as in a Phase I-II program (dose-seeking trials with different response criteria than the multicenter trial). These clinical studies enrolled a total of 117 patients.. In the multicenter, open-label clinical trial, Targretin® gel was evaluated for the treatment of patients with early stage CTCL who were refractory to, intolerant to, or reached a response plateau for at least six months on at least two prior therapies. The study was conducted in the U.S., Canada, Europe, and Australia and enrolled a total of 50 patients; 46% of these patients were male, 80% were Caucasian, and the median age was 64 years (range 13 to 85).. Targretin® gel was also evaluated for the treatment of patients with CTCL in a U.S. Phase I-II program involving patients with early stage CTCL. This program enrolled a total of 67 patients; 55% of these patients were male, ...
5,6-dimethoxy-2-aminotetraline hydrochloride | Building block | CAS [21489-75-8] - [21489-50-9] | Axon 1042 | Axon Ligand™ with...
5,6-dimethoxy-2-aminotetraline hydrochloride | Building block | CAS [21489-75-8] - [21489-50-9] | Axon 1042 | Axon Ligand™ with >98% purity available from supplier Axon Medchem, prime source of life science reagents for your research
Targretin (Bexarotene): Side Effects, Interactions, Warning, Dosage & Uses
Learn about Targretin (Bexarotene) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
Bexarotenes Effects Vary by ApoE Genotype, Amyloid Pathology | ALZFORUM
The lymphoma drug bexarotene, under cross-examination as an Alzheimers therapeutic, dramatically lowers soluble Aβ in mice in some studies but not others. A paper in the September 12 Journal of Biological Chemistry offers an explanation for the discrepancy. Researchers led by Mary Jo LaDu at the University of Illinois at Chicago reported that bexarotene squelched soluble Aβ only in mice that expressed human apolipoprotein E4 (ApoE4), a major Alzheimers risk factor, and only in brain regions with extensive amyloid deposits. The authors attribute this to the drugs ability to stimulate the packing of lipids onto ApoE4. This variant normally hooks less lipid than the other isoforms do, and may clear Aβ ineffectively as a result. In mice carrying human ApoE3, or in brain regions with little amyloid accumulation, bexarotene treatment provided no benefit.. For ApoE4 carriers who have high Aβ levels, increasing ApoE lipidation may be a promising therapeutic strategy, first author Leon Tai told ...
Bexarotene and GM-CSF in Treating Patients With Myelodysplastic Syndrome or Acute Myeloid Leukemia - Full Text View -...
OUTLINE: Patients receive oral bexarotene and sargramostim (GM-CSF) subcutaneously on days 1-28. Treatment repeats every 28 days for up to 6 courses in the absence of disease progression or unacceptable toxicity.. Blood and bone marrow samples are collected at baseline and after 1 or 2 courses of study therapy. Samples are examined by flow cytometry for laboratory studies, including biological markers, and by fluorescent in situ hybridization (FISH) for cytogenetic changes.. After completion of study treatment, patients are followed periodically for 6 months.. PROJECTED ACCRUAL: A total of 18 patients will be accrued for this study. ...
1S)-1,2,3,4-tetrahydronaphthalen-1-amine - Registration Dossier - ECHA
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
1S)-1,2,3,4-tetrahydronaphthalen-1-amine - Registration Dossier - ECHA
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Once-Weekly Subcutaneous Delivery of Polymer-Linked Rotigotine (SER-214) Provides Continuous Plasma Levels in Parkinsons...
2020 International Parkinson and Movement Disorder Society Background: Extensive scientific and clinical evidence indicates that continuous delivery of a dopaminergic agent is associated with significant reduction in motor complications compared with intermittent oral dosing with the same agent. There has been an intensive effort to develop a method of providing continuous plasma levels of a dopaminergic agent that avoids the need for surgical therapy or an infusion system. Studies in MPTP-treated monkeys demonstrate that once-weekly injections of polymer-linked rotigotine provide continuous plasma levels and antiparkinsonian benefits. Methods: We performed a multicenter open-label, multiple-ascending-dose-ranging cohort study to evaluate the safety, tolerability, and pharmacokinetics of polymer-linked rotigotine in PD patients. Results: A total of 19 patients were evaluated in 4 cohorts in doses of 20 50, 100, and 200 mg of polymer-linked rotigotine, administered subcutaneously once weekly. The ...
An Open-Label Extension Trial to Assess the Safety of Long-Term Treatment of Rotigotine in Early-Stage Parkinson's Disease...
Rotigotine trans-dermal patches, once daily:. 10 cm2 (2 mg/24 hours); 20 cm2 (4 mg/24 hours); 30 cm2 (6 mg/24 hours); 40 cm2 (8 mg/24 hours); 50 cm2 (10 mg/24 hours); 60 cm2 (12 mg/24 hours); 70 cm2 (14 mg/24 hours); 80 cm2 (16 mg/24 hours);. Optimal dosing:. During the first year: The maximum Rotigotine dose allowed is 8 mg/24 hours.. After the first year: allowed dose increase of rotigotine up to a maximum of 16 mg/24 hours. ...
52 patients were randomised 1:1 to receive six months of bexarotene or placebo. Two placebo patients withdrew before receiving study drug and one bexarotene patient withdrew consent during the trial. All bexarotene patients experienced adverse effects, notably central hypothyroidism (26 [100%]) and hypertriglyceridaemia (24 [92%, mean maximum of 6.79 mmol/L ,SD 4.4]; as well as rash (13 [50%]) and neutropenia (10 [38%]). Two discontinued placebo because of adverse events and five discontinued bexarotene because of rash , neutropenia, triglyceridaemia and mood disturbance. The primary efficacy outcome was negative (mean submedian lesion MTR change was 0.25pu in the bexarotene group versus 0.09pu in the placebo group, p=0.54), but in an exploratory, lesion-level analysis, though treatment difference in submedian lesions was too small to achieve significance, it was statistically significantly greater than in supermedian lesions (p=0·007). This suggests that bexarotene has a biological effect ...
The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice | Cancer Prevention...
Figure 2. Rexinoids inhibit nitric oxide production and COX-2 expression, but increase ABCA1 expression. A, RAW264.7 cells were treated with 15 to 1,000 nmol/L of rexinoids or 1 to 50 nmol/L of the triterpenoid CDDO-Im for 1 hour and then stimulated with 1 ng/mL LPS for 24 hours. NO released into media was measured by the Griess reaction. *, P , 0.05 vs. stimulated control cells. B, RAW264.7 cells were treated with rexinoids or CDDO-Im and stimulated with LPS (1 ng/mL) for 24 hours to measure COX-2 expression or treated with drugs alone for 24 hours and then stimulated with TNFα (10 ng/mL) for 15 minutes to assess IκBα degradation by Western blotting (C). D, RAW264.7 cells were treated with the compounds for 24 hours, and protein expression of ABCA1 was evaluated by Western blotting. ...
Ionene(6CI); 1,1,6-Trimethyl-1,2,3,4-tetrahydronaphthalene; 1,1,6-Trimethyltetralin;1,2,3,4-Tetrahydro-1,1,6-trimethylnaphthalene; a- ...
AAN: Rotigotine Eases Non-Motor Parkinsons Symptoms | Medpage Today
TORONTO -- Non-motor symptoms of Parkinsons disease -- often overlooked by clinicians -- can be alleviated by treatment with the dopamine-agonist transdermal rotigotine (Neupro) patch, researchers sa
Gemcitabine and Bexarotene in Treating Patients With Progressive or Refractory Stage IB, Stage II, Stage III, or Stage IV...
RATIONALE: Drugs used in chemotherapy, such as gemcitabine and bexarotene, work in different ways to stop the growth of cancer cells, either by killing
Get information on Bexarotene capsules including uses, dosage details, medication side-effects and drug interaction facts from Cleveland Clinics health library.
PB28 - Википедија, слободна енциклопедија
Berardi F, Abate C, Ferorelli S, Uricchio V, Colabufo NA, Niso M, Perrone R (2009). „Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). Journal of Medicinal Chemistry. 52 (23): 7817-28. PMID 19842660. doi:10.1021/jm9007505 ...
Is Rotigotine Neupro safe when allergic to sulfates and suffering from AFIB?
Question - Is Rotigotine Neupro safe when allergic to sulfates and suffering from AFIB?. Ask a Doctor about uses, dosages and side-effects of Bactrim, Ask a Cardiologist
CiNii Articles - Matsuura Tomomi
Orally-Administered Caspase Inhibitor PF-03491390 Is Retained in the Liver for Prolonged Periods With Low Systemic Exposure, Exerting a Hepatoprotective Effect Against α-Fas-Induced Liver Injury in a Mouse Model （2007 ...
ebelactone A | Semantic Scholar
Known as: 2-Oxetanone, 4-(8-hydroxy-1,3,5,7,9-pentamethyl-6-oxo-3-undecenyl)-3-methyl-, (3S-(3alpha,4beta(1R*,3E,5S*,7R*,8S*,9S*)))- ...
Enhanced Efficacy of Combinations of Retinoic Acid- and Retinoid X Receptor-selective Retinoids and α-Interferon in Inhibition...
Retinoic acid receptors and retinoid X receptors form heterodimers, bind to retinoic acid response elements, and transactivate the transcription of retinoid-responsive genes. Two synthetic retinoids [4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthracenyl)benzoic acid (TTAB) and 6-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-2-naphthalenecarboxylic acid (TTNN)], which preferentially bind retinoic acid receptors, inhibited the proliferation of cervical carcinoma ME180 cells by 50% at 0.2 nm and 0.2 µm, respectively. In contrast, two other retinoids [2-(4-carboxyphenyl)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1,3-dithiane (SR11203) and 4-(2-methyl-1-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)propenyl)benzoic acid (SR11217)], which preferentially bind retinoic X receptors, inhibited growth by only 12 and 18% at 1 µm, respectively. The combination of suboptimal concentrations of TTAB (0.1 nm) or TTNN (10 nm) with each of the retinoic X receptor-selective ...
Receptor specificity of retinoid-induced epidermal hyperplasia: effect of RXR-selective agonists and correlation with topical...
Retinoid induction of epidermal hyperplasia was investigated in hairless mice with synthetic ligands for the retinoic acid (RAR) and retinoid X (RXR) nuclear receptors. Induction of hyperplasia by all-trans retinoic acid and the RAR-specific retinoids TTNPB, tazarotene and AGN 190121 varied over a wide range (ED50 = 0.2-100 nmol/animal in three daily applications). Potency of induction was not directly correlated to receptor-binding affinity, but specificity of action could be demonstrated by inhibition with the high-affinity antagonist of the RARs, AGN 193109. Although RAR is functionally complexed with RXR in vivo, RXR-selective compounds have only weak potency in induction of hyperplasia. The ED50 value of the RXR-selective AGN 191701 was 600 nmol/animal compared with an ED50 value of 0.2 nmol for the structurally similar RAR-selective TTNPB. SR11237 and SR11217, also RXR-selective, each have an ED50 value of ,1000 nmol. Unlike RAR-specific retinoids, RXR-selective retinoids cause only very ...
Purpose: Pralatrexate is a folic acid analogue metabolic inhibitor similar to methotrexate, which has shown tolerability and efficacy with an overall response rate of 45% in a phase I dose deescalation study of patients with relapsed/refractory cutaneous T-cell lymphoma (CTCL).. Experimental Design: The object of this phase I/II open-label, multicenter clinical trial was to determine the MTD and recommended dose of pralatrexate plus oral bexarotene in 34 patients with relapsed/refractory CTCL who had failed prior systemic therapies. Pralatrexate was administered by intravenous push at 15 mg/m2 given weekly 3 weeks out of 4 weeks with daily oral bexarotene (150 or 300 mg/m2), levothyroxine, atorvastatin, folate, and with B12 every 2 months.. Results: At the MTD of 15 mg/m2 bexarotene and 15 mg/m2 pralatrexate, the response rate was 60% [4 complete responses (CR), 14 partial responses (PR)], the maximum observed response duration was 28.9+ months, and duration of response for 4 CRs ranged from 9.0 ...
Ligand Expands License with Sermonix to Include Worldwide Rights for Oral Lasofoxifene :: Ligand Pharmaceuticals Incorporated ...
SAN DIEGO--(BUSINESS WIRE)-- Ligand Pharmaceuticals Incorporated (NASDAQ: LGND) announces that it has expanded its license with Sermonix Pharmaceuticals to include worldwide rights to develop and commercialize oral lasofoxifene. Ligand originally licensed the U.S. rights to oral lasofoxifene to Sermonix in February of 2015, and has now expanded the agreement to include the rest of the world. Sermonix is focused on breast and ovarian cancer treatment with oral lasofoxifene, particularly an indication in the treatment of advanced Estrogen Receptor positive (ER+) endocrine-resistant breast cancer. Lasofoxifene is an asset with a rich heritage originating at Ligand and with a substantial set of global clinical data. This agreement with Sermonix represents an expansion of our relationship and enables further development of oral lasofoxifene on a worldwide basis, said John Higgins, Chief Executive Officer of Ligand Pharmaceuticals. This amendment includes an upfront payment, additional commercial ...
PatientsLikeMe | Bexarotene report for patients like you
Bexarotene: Find the most comprehensive real-world treatment information on Bexarotene at PatientsLikeMe. 1 patients with fibromyalgia, multiple sclerosis, major depressive disorder, generalized anxiety disorder, diabetes type 2, post-traumatic stress disorder, systemic lupus erythematosus, bipolar disorder, Parkinsons disease, panic disorder, rheumatoid arthritis, high blood pressure (hypertension), myalgic encephalomyelitis/chronic fatigue syndrome, persistent depressive disorder (dysthymia), amyotrophic lateral sclerosis, epilepsy, migraine, hypothyroidism, osteoarthritis, traumatic brain injury, bipolar II disorder, attention deficit/hyperactivity disorder, asthma, social anxiety disorder, high cholesterol (hypercholesterolemia), irritable bowel syndrome, idiopathic pulmonary fibrosis, gastroesophageal reflux disease, bipolar I disorder or psoriasis currently take Bexarotene.
Pesquisa | Portal Regional da BVS
BACKGROUND: There are limited effective drugs that can reach the brain to target brain tumors, in particular glioblastoma, which is one of the most difficult cancers to be cured from. Because the overexpression of the sigma-2 receptor is frequently reported in glioma clinical samples and associated with poor prognosis and malignancy, we herein studied the anti-tumor effect of the sigma-2 receptor agonist PB221 (4-cyclohexyl-1-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperidine) on an anaplastic astrocytoma tumor model based on previous encouraging results in pancreatic cancer and neuroblastoma SK-N-SH cells. METHODS: The expression of the sigma-2 receptor, transmembrane protein 97 (TMEM97), in ALTS1C1 and UN-KC6141 cell lines was measured by RT-PCR and quantitative RT-PCR. The binding of sigma-2 receptor fluorescent ligands PB385 (6-[5-[3-(4-cyclohexylpiperazin-1-yl)propyl]-5,6,7,8-tetrahydronaphthalen-5-yloxy]-N-(7-nitro-2,1,3-benzoxadiazol-4-yl)hexanamine) and NO1 ...
Could Bexarotene Treat Parkinsons Disease? | ALZFORUM
A drug currently under investigation as an Alzheimers treatment may show promise for Parkinsons disease as well, suggests a paper in the October 11 ACS Chemical Neuroscience. Bexarotene, an approved cancer drug, made headlines in 2012 when researchers claimed it cleared Aβ plaques and improved cognition in mice modeling AD (see ARF related news story). Subsequent attempts to independently reproduce these original findings have met with mixed success (see ARF related news story). Now a new group joins the fray, reporting that bexarotene protects dopaminergic neurons and improves movement in models of Parkinsons. Whats more, the drug seems to work differently than AD researchers had envisaged. Scientists led by Ethan Burstein of Acadia Pharmaceuticals in San Diego, California, report that the drug activates a nuclear hormone receptor called Nurr1, known to promote growth and survival of dopamine neurons. Curiously, much lower doses are needed for these effects than are typically used for ...
Investigators Present Targretin Lung Cancer Data From SPIRIT I & II Trials
Ligand Pharmaceuticals has reported results of two pivotal Phase III studies of Targretin (bexarotene) capsules in front-line combination therapy with standard chemotherapy to treat advanced non-small cell lung cancer (NSCLC).
Growth factor-antagonized rexinoid apoptosis involves permissive PPARgamma/RXR heterodimers to activate the intrinsic death...
Growth factor (GF) deprivation and/or blocking of cognate signaling can induce apoptosis and is the basis of several cancer treatment paradigms. We observed that RXR agonists (rexinoids) induce apoptosis of tumor cells when GF support is abrogated. This rexinoid apoptosis involves activation of both iNOS and eNOS by RXR-PPARgamma and results in production of apoptogenic NO. IGF/EGF-induced IGF receptor 1-mediated MAP kinase blocks rexinoid apoptosis by RXR phosphorylation. Combining rexinoids with the MAPK inhibitor U0126 induced apoptosis in human cancer cells in vitro and ex vivo and blocked xenograft growth in vivo. Our results suggest a regulatory mechanism in which GF signaling antagonizes RXR-PPARgamma-mediated default apoptosis to sustain cell life.
A Phase II Study of Oral Tamibarotene in Acute Promyelocytic Leukemia Patients Who Have Received Prior Therapy with ATRA and...
The goal of this clinical research study is to find out if tamibarotene can help to control APL. The safety of this treatment will also be studied.
Rexinoid Developed by NuRx Pharmaceuticals Shows Promise in Prevention, Treatment of Lung, Breast Cancer, Paper in Clinical...
... IRVINE Calif. March 26 /- NuRx Pharmaceut...In addition the paper showed that NRX4204 caused marked tumorregress...Entitled A New Rexinoid NRX4204 Prevents Carcinogenesis in Both Lun... This study demonstrates that NRX4204 is exceptionally potent and not...,Rexinoid,Developed,by,NuRx,Pharmaceuticals,Shows,Promise,in,Prevention,,Treatment,of,Lung,,Breast,Cancer,,Paper,in,Clinical,Cancer,Research,Reports,medicine,advanced medical technology,medical laboratory technology,medical device technology,latest medical technology,Health
BLOG - Page 39 of 39 - BrainStromBrainStrom | Power of Science | Page 39
improvement of insulin action in skeletal muscle compared with stimulation of PPARg alone. Stimulating RXR alone may be ineffective or produce variable effects such as reduced food intake, reduced body weight gain, increased expression of uncoupling proteins, and increased expression of the p85a subunit of PI3K. Each of these effects could facilitate insulin action, but they may depend on structural components of the RXR agonist that do not actually bind to the RXR ligand-binding site of the RXR receptor. Thus, binding of an RXR agonist to the RXR may be accompanied by interactions of the agonist with other regions of the receptor, and this will alter the profile of genes transcribed. Thus, there is a potential for selective RXR agonists and dual PPARg-RXR agonists. Mineral enhancers of insulin action Several mineral supplements, notably magnesium and chromium, will improve insulin action in patients who are deficient in these minerals. The roles of these minerals in insulin signaling and energy ...
Where can i buy the homeopathic for bexarotene - Venapro Herbal Hemorrhoids Treatment - Jan 22, 2018
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Bexarotene Capsules 75 Mg | Canadian Pharcharmy Online
Bexarotene - Glossed over is the fact that the amount of earnings on which Social Security taxes are payable would have to rise from the would be taxed at the full Social Security rate.
JCI - Loss of SPARC-mediated VEGFR-1 suppression after injury reveals a novel antiangiogenic activity of VEGF-A
Historically, VEGFR-1 was assigned a role as a nonsignaling decoy receptor because of the low activity and embryonic dispensability of its tyrosine kinase function. More recently, its role has become more interesting because VEGFR-1 signaling has been reported both to promote (6, 7) and suppress (8) VEGF-A-driven angiogenesis. We report not only that PlGF-1 inhibits inflammatory CNV, extending the scope of VEGFR-1 function, but also what we believe is the unprecedented observation that VEGF-A itself can suppress angiogenesis. Multiple lines of evidence emerging from genetic ablation, antibody neutralization, and receptor-selective ligand activation all strongly support the thesis that the antiangiogenic action of VEGF-A is mediated by VEGFR-1. Previously, VEGF-A has been reported to reduce VEGF-E-induced VEGFR-2 tyrosine kinase phosphorylation in capillary endothelial cells in vitro, raising the provocative hypothesis that VEGF-A could limit its own angiogenic activity through VEGFR-1 (29). We ...
Alzheimers Disease New Treatments |IYTHEALTH.com
Inflammation is another crucial Alzheimers brain problem. Both beta-amyloid plaques and tau tangles cause an immune response in the brain. Microglia are cells that serve as the first kind of immune defense in the brain. While microglia help clear beta-amyloid in the brain, they might end up being overactive in the existence of beta-amyloid and produce compounds that damage close-by cells. Existing drug in research that targets inflammation: CSP-1103. CSP-1103 is a microglial modulator that aims to reduce inflammation in the brain. At AAIC 2013, researchers provided the results of a 90-week trial where people who had mild cognitive problems (MCI) were offered CSP-1103. Preliminary research studies proved to that CSP-1103 avoided beta-amyloid from being deposited on nerve cells and forming plaques. It also minimized problems with thinking and memory (cognition). The cognitive tests of individuals who had gotten involved for at least 64 weeks proved to statistically considerable enhancements in ...
The |i|Neupro|/i| (NU-pro, rotigotine) patch will be back for Parkinsons disease, and its now also approved for restless legs...
The Neupro (NU-pro, rotigotine) patch will be back for Parkinsons disease, and its now also approved for restless legs syndrome.... Learn more with Pharmacists Letter.
Doktor Liliy Koval
Although a read in 2012 suggested a cancer antidepressant could annul the thinking and remembrance problems associated with Alzheimers disease, three groups of researchers now approximately they have been unable to identical those findings. The teams said their exploration could have serious implications for patient safety since the soporific involved in the study, bexarotene (Targretin), has genuine side effects, such as major blood-lipid abnormalities, pancreatitis, headaches, fatigue, force gain, depression, nausea, vomiting, constipation and rash vitorun men. Anecdotally, we have all heard that physicians are treating their Alzheimers patients with bexarotene, a cancer dope with unsmiling marginal effects, said bone up co-author Robert Vassar, a professor of apartment and molecular biology at Northwestern University Feinberg School of Medicine, in Chicago ...
Pfizer Receives FDA Complete Response Letter for Lasofoxifene
Fablyn (lasofoxifene tartrate) is a new drug in development for the treatment of osteoporosis in postmenopausal women. Fablyn information includes news, clinical trial results and side effects.
WikiGenes - Targret - 4-[1-(3,5,5,8,8-pentamethyl-6,7...
The worlds first wiki where authorship really matters. Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts.
Retinoid and Rexinoid Signaling - Methods and Protocols | Swapan Ray | Springer
This volume explores synthetic procedures for producing receptor-specific retinoids and rexinoids, molecular biology methods, and new technologies to demonstrate the therapeutic activities of molecules. Chapters discuss lentiviral delivery of shRNA constructs and RAR signaling.
2016 Grant Recipient David Linehan, MD - Pancreatic Cancer Action Network
A prominent characteristic of pancreatic tumors is a dense and complex stroma, which is made up of various types of cells that surround and infiltrate the tumor. Immune and inflammatory cells are prevalent within the stroma, and these cells help hide the tumor from the immune system, blocking its ability to recognize and attack the cancer cells.. Dr. Linehans 2015 Translational Research Grant focused on blocking the activity of a protein called CCR2 that is involved in the stromal cells ability to be recruited to the tumor and to block the immune system. In May 2016, Dr. Linehan published a study in the prestigious journal Lancet Oncology that describes encouraging results from a phase 1b clinical trial of the CCR2 inhibitor (PF-04136309, from Pzifer) in pancreatic cancer patients with locally advanced disease (their tumor has begun to spread within the pancreas and surrounding blood vessels, but hasnt metastasized to other organs yet).. Based on promising results from this early-phase ...
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Selective glucocorticoid receptor modulator
... tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) ...
4-tetrahydronaphthalenes". Bioorg. Med. Chem. 14 (19): 6640-58. doi:10.1016/j.bmc.2006.05.077. PMID 16782354. Nguyen T, Shapiro ...
4-tetrahydronaphthalenes". Bioorganic & Medicinal Chemistry. 14 (19): 6640-58. doi:10.1016/j.bmc.2006.05.077. PMID 16782354. ...
4-tetrahydronaphthalenes". Bioorg. Med. Chem. 14 (19): 6640-58. doi:10.1016/j.bmc.2006.05.077. PMID 16782354. Appl H, Holzammer ...
4-tetrahydronaphthalenes". Bioorg. Med. Chem. 14 (19): 6640-58. doi:10.1016/j.bmc.2006.05.077. PMID 16782354. Stanton T, Bolden ...
List of selective estrogen receptor modulators
... tetrahydronaphthalenes (lasofoxifene, nafoxidine), and benzopyrans (acolbifene, ormeloxifene, levormeloxifene). Pinkerton, ...
4-tetrahydronaphthalenes Friedrich Mühlthau, Thorsten Bach Synthesis 2005: 3428-3436 doi:10.1055/s-2005-918482 High Facial ...
List of MeSH codes (D04)
... tetrahydronaphthalenes MeSH D04.615.638.960.400 - 8-hydroxy-2-(di-n-propylamino)tetralin MeSH D04.615.638.960.492 - levobunolol ...
Tetrahydronaphthalenes Diagnostic Use | Keywords | Survey Research Center
OBJECTIVE: To explore the neurochemical basis of REM sleep behavior disorder (RBD) in multiple-system atrophy (MSA). METHODS: In 13 patients with probable MSA, nocturnal, laboratory-based polysomnography was used to rate the severity of REM atonia loss by the percentage of REM sleep with tonically increased electromyographic (EMG) activity and the percentage of REM sleep with phasic EMG bursts. PET with (+)-[11C]dihydrotetrabenazine ([11C]DTBZ) was employed to measure the density of striatal monoaminergic terminals and SPECT with (-)-5-[123I]iodobenzovesamicol ([123I]IBVM) to measure the density of 123I]IBVM. RESULTS: Age and gender distributions were similar in patient and normal control groups. The MSA subjects showed decreased mean [11C]DTBZ binding in the striatum (p , 0.0001) and decreased [123I]IBVM binding in the thalamus (p , 0.001). Moreover, in the MSA group, striatal [11C]DTBZ binding was inversely correlated with the severity of REM atonia loss (p = 0.003). Thalamic [123I]IBVM ...
RCSB PDB - EVP Ligand Summary Page
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex assemblies. As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
Molecules | Free Full-Text | Synthesis and Anticancer Activity of Some Novel Tetralin-6-yl-pyrazoline, 2-Thioxopyrimidine, 2...
The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo
Life-threatening interaction of mibefradil and beta-blockers with dihydropyridine calcium channel blockers
MEDLINE - Resultado p gina 1
Yr Athro Thomas Wirth - Pobl - Prifysgol Caerdydd
TNO Repository search for: subject:'Retinoic acid'
Patent US3385831 - Textile fibers of polyethylene terephthalate/hexahydroterephthalate copolyester - Google Patents
Selective glucocorticoid receptor modulator - Wikipedia
BJOC - Multicomponent reactions II
EP0874800B1 - Indane dimer compounds with smooth muscle relaxing and/or mast cell stabilising and/or antiinflammatory activity ...
Browsing Pharmacognosy (Theses and Dissertations) by Title
Nicholas Oberlies , NC DOCKS (North Carolina Digital Online Collection of Knowledge and Scholarship)
Amitriptyline - Wikipedia
MPI-INF D3 Publications, generated: 1:16, 17 December 2017
MPI-INF D3 Publications - 1. Author,Editor - 2. by Group - 1. by Names of First Author,Editor, MPI-INF D3 Publications -...
US20090306026A1 - Pharmaceutical Formulations and Uses Thereof in the Treatment of Female Sexual Dysfunction - Google...
WikiGenes - TH - tyrosine hydroxylase
relapsed mycosis fungoides drug therapy 2000:2010[pubdate] *count=100 - BioMedLib™ search engine
mycosis fungoides stage ii drug therapy 2000:2010[pubdate] *count=100 - BioMedLib™ search engine
Tetrahydronaphthalenes / therapeutic use. *[MeSH-minor] Adult. Age Factors. Aged. Aged, 80 and over. Cohort Studies. Female. ... Tetrahydronaphthalenes / administration & dosage. *[MeSH-minor] Adult. Aged. Aged, 80 and over. Female. Gels. Humans. Male. ... Tetrahydronaphthalenes / therapeutic use. *[MeSH-minor] Algorithms. Dermatitis, Exfoliative / complications. Dermatitis, ... Chemical-registry-number] 0 / Anticarcinogenic Agents; 0 / Gels; 0 / Tetrahydronaphthalenes; A61RXM4375 / bexarotene ...
Patent WO2005110353A1 - Personal care compositions and methods for regulating mammalian hair growth ... - Google Patentsuche
Scott E Denmark - Research Output - University of Illinois at Urbana-Champaign
Arylmagnesium Bromide Additions to 1-Tetralone-2-acetic Acid Followed by Catalytic Hydrogenolysis: Stereochemical Consequences ...
promethazine | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY
The Curious Wavefunction: A simple substitution to possibly avoid phenol elimination
The Curious Wavefunction: 2007
Characterization of the dopamine-responsive adenylate cyclase of bovine parathyroid cells and its relationship to parathyroid...
TY - JOUR. T1 - Characterization of the dopamine-responsive adenylate cyclase of bovine parathyroid cells and its relationship to parathyroid hormone secretion. AU - Attie, M. F.. AU - Brown, E. M.. AU - Gardner, D. G.. AU - Spiegel, A. M.. AU - Aurbach, G. D.. PY - 1980/12. Y1 - 1980/12. N2 - To investigate further the mechanism of dopamine (DA)-stimulated parathyroid hormone (PTH) secretion, we have identified and studied DA-sensitive adenylate cyclase in a particulate preparation of osmotically lysed dispersed bovine parathyroid cells. Adenylate cyclase was responsive to DA at concentrations as low as 0.3 μM, and the maximal stimulation in the presence of GTP was 2- to 4-fold that of activity with GTP alone. (-)Propranolol (1 μM) abolished the stimulation by (-)isoproterenol but did not inhibit the DA-stimulated adenylate cyclase, whereas a-flupenthixol (1 μM) inhibited DA stimulation but not that of (-)isoproterenol. The dopaminergic agonists epinine and BJ-dihydroxy-l, 2, 3, ...
- Novel ligands for the human histamine H1 receptor: synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1,2,3,4-tetrahydronaphthalenes. (guidetopharmacology.org)
- Bidentate Lewis Acid Catalyzed Domino Diels-Alder Reaction of Phthalazine for the Synthesis of Bridged Oligocyclic Tetrahydronaphthalenes. (unibas.ch)