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... Direct inhibition of 5-LO, partly through an iron-catalysed redox mechanism, has been achieved with compounds such as benzofurans (L-670,630 and L-650,224), hydroxamates (BWA4C), N-hydroxyurea derivatives (A64077 or zileuton) and indazolinones (ICI 207,968), with good selectivity and potency [49]. I ...
Sudden Sensorineural Hearing Loss Due to Drug Abuse
Sudden Sensorineural Hearing Loss Due to Drug Abuse

... the development of analgesic tolerance and physical dependence.9 Most clinically used opioids for analgesia are either nonselective opioid agonists or selective MOR agonists. The analgesic efficacy of currently used opioid analgesics is limited due to their tendency to cause analgesic tolerance, phy ...
Valsartan to losartan conversion
Valsartan to losartan conversion

... desired brand to find out the drug price. Losartan official prescribing information for healthcare professionals. Includes: indications, dosage, adverse reactions, pharmacology and more. Learn about clinical pharmacology for the drug Cozaar (Losartan Potassium). Valsartan (trade name Diovan) is an a ...
Clinical Indications
Clinical Indications

... They may cause hyperuricemia and precipitate attacks of gout. ...
HERE - INDIGO Biosciences
HERE - INDIGO Biosciences

... The docking analysis was carried out using three TRβ crystal structure with three different ligands; diclofenac (Fig. 2A) could bind to active sites of all three structures, while celecoxib (Fig. 2B) could bind only into active site of 1Q4X PDB entry, as the ligand of this complex ([4-(3-benzyl-4-hy ...
Read more - Jal pharma
Read more - Jal pharma

... • the amount of hederacosid C given in an extract seems to support the concentration of alphahederin in blood (prodrug??) ...
Effects of Antipsychotic Drugs on Extracellular Dopamine Levels in
Effects of Antipsychotic Drugs on Extracellular Dopamine Levels in

... et al., 1997) which may be related to frontal lobe function. Thus, the greater ability of 5-HT2A/D2 receptor antagonists to increase extracellular DA levels in the cortical regions compared with subcortical regions may contribute to their ability to improve negative symptoms (Deutch et al., 1991). T ...
Therapeutic applications of ricin and some alkaloids
Therapeutic applications of ricin and some alkaloids

... acetylcholine receptors. In small concentrations it escalates the activity of these receptors and leads to an increased flow of adrenaline (epinephrine), a stimulating hormone. The release of adrenaline in turn causes an increase in heart rate, blood pressure and respiration, as well as higher gluco ...
Uncoupling between noradrenergic and serotonergic neurons as a
Uncoupling between noradrenergic and serotonergic neurons as a

... related to their blunted locomotor response to D-amphetamine [17]. However, for the highest dose of D-amphetamine tested (6 mg/kg, i.p.), a significant locomotor hyperactivity was observed as well as a weak increase in extracellular DA levels in the nucleus accumbens [18], suggesting that an other l ...
Synta Pharmaceuticals and Madrigal
Synta Pharmaceuticals and Madrigal

... fund several clinical readouts • The transaction has been approved by the boards of directors of both companies and Madrigal shareholders • Expected to close by the end of 3Q 2016, subject to the approval of the stockholders of Synta as well as other customary closing conditions, including satisfact ...
Interactions between endothelin-1 and the renin–angiotensin
Interactions between endothelin-1 and the renin–angiotensin

... 1. Introduction The renin–angiotensin–aldosterone system (RAAS) and the endothelin (ET) system are two of the most potent vasopressor mechanisms identified to date (for a review, see [1–3]). Therefore, it is not surprising that they have been investigated extensively in relation to arterial hyperten ...
Sikh
Sikh

... Mandatory minimum sentence: When convicted of an offense punishable by a mandatory minimum sentence, must serve the minimum sentence or higher. Not eligible for parole. Decriminalization: The state has decriminalized marijuana to some degree. Typically means no prison time or criminal record for fir ...
The Effects of Morphine, Nicotine and Epibatidine on Lymphocyte
The Effects of Morphine, Nicotine and Epibatidine on Lymphocyte

... findings reported with nicotine to those produced by morphine suggest a possible relationship between nicotinic and opioid receptor-mediated immunomodulation. To examine the potential overlap between opioid and nicotinic receptors in a neuroimmunomodulatory pathway, we compared the effects of morphi ...
EFFECTS OF SELECTIVE α4β2 NICOTINIC
EFFECTS OF SELECTIVE α4β2 NICOTINIC

... bottom dwelling and an increase of the total distance travelled. The similar behaviours elicited by nicotine and cytisine further support the idea that nicotine’s effects are mediated, at least in part, by the  nAChR (Bencan and Levin, 2008), and also show that the selective activation of this r ...
Characterization of the Analgesic and Anti
Characterization of the Analgesic and Anti

... [3H](R,S)-ketorolac (100 nmol; 0.495 mCi/mmol) by i.c.v. injection. At 0, 5, 20, 35, 60, and 180 min after injection, the rats were anesthetized with CO2/O2 (60:40%); blood was withdrawn into a heparinized syringe and a plasma fraction was obtained by centrifugation of the blood at 2600g for 5 min i ...
THC on learning in adolescent and adult rats
THC on learning in adolescent and adult rats

... In Experiment 3, 20 male adolescent and 20 male adult rats were used to assess the long-lasting effects of chronic THC treatment on spatial learning. The rats were given i.p. injections of either the control vehicle solution (n = 10 in each age group) or 5.0 mg/kg THC (n = 10 in each age group) once ...
File
File

... these, 63.8% were under age 18. In the last half of 2003, marijuana was the third most commonly abused drug mentioned in drug-related hospital emergency department (ED) visits in the continental United States, at 12.6%, following cocaine (20%) and alcohol (48.7%). Marijuana use is widespread among a ...
The use of cannabis for medical purposes
The use of cannabis for medical purposes

... affinity for CB1 and CB2 receptors but acts as an indirect antagonist of cannabinoid agonists.9 Recently it was found to be an antagonist at the putative new cannabinoid receptor, GPR55, in the caudate nucleus and putamen.10 CBD has also been shown to act as a 5-HT1A receptor agonist, an action whic ...
Pharmacokinetic–pharmacodynamic modelling of the hypothermic
Pharmacokinetic–pharmacodynamic modelling of the hypothermic

... control in an indirect physiological response model (Dayneka et al., 1993) and is able to characterise quantitatively the effect of 5-HT1A receptor agonists in vivo. In this model, the set-point for maintenance of body temperature is attenuated by 5-HT1A receptor agonist via a sigmoidal transducer f ...
the pharmacokinetics of a thiazole benzenesulfonamide
the pharmacokinetics of a thiazole benzenesulfonamide

... the stimulation of lipolysis (Arch et al., 1984). In brown adipose tissue, ␤3-adrenergic receptor activation leads to up-regulation of UCP1, a mitochondrial uncoupling protein, which uncouples oxidative phosphorylation from fatty acid ␤-oxidation, resulting in an increase in energy expenditure (Lowe ...
INSILICO DRUG DESIGN AND MOLECULAR DOCKING STUDIES OF SOME NOVEL
INSILICO DRUG DESIGN AND MOLECULAR DOCKING STUDIES OF SOME NOVEL

... abnormal over growth of tissues. Benzothiazole is an important class of heterocyclic compound which possess interesting biological activities like anti-tumor, anti-microbial, anti-tubercular, anti-malarial, anti-convulsant, anthelmintic, analgesic and anti-inflammatory activity. The drugs containing ...
Università degli Studi di Milano
Università degli Studi di Milano

... increased while IL-10 production was lower, indicating a switch towards a pro-inflammatory phenotype of the macrophage. These effects on cytokines are at transcriptional level since we observed similar result by measuring IL-10, IL-1β and TNF-α mRNA with RT-PCR. In adult animals evaluated 47 days af ...
Effects of psilocybin on hippocampal neurogenesis and extinction of
Effects of psilocybin on hippocampal neurogenesis and extinction of

... James Haley VA Medical Center, Tampa, FL 33613, USA C. L. Kirstein  Department of Psychology, University of South Florida, Tampa, FL 33620, USA ...
Dopamine Agonists and the Risk of Cardiac
Dopamine Agonists and the Risk of Cardiac

... • Underdiagnosing the incidence of asymptomatic cases could have occurred, since it was not based on echocardiographic monitoring of all patients in the cohort, thus underestimating the true risks associated with pergolide and cabergoline. ...
The Marijuana Detection Window
The Marijuana Detection Window

... to be excreted in urine in sufficient quantities to produce a positive drug test (by standard screening and confirmation testing). ...
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Cannabinoid receptor antagonist



The discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor antagonist, rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been shown to decrease food intake and regulate body-weight gain. The prevalence of obesity worldwide is increasing dramatically and has a great impact on public health. The lack of efficient and well-tolerated drugs to cure obesity has led to an increased interest in research and development of cannabinoid antagonists. Cannabidiol, a naturally occurring cannabinoid, is a non-competitive CB1/2 antagonist.
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