Search results for "Quinoline"
showing 10 items of 391 documents
Comparative study of the rat uterine smooth muscle relaxant activity of three bisbenzyltetrahydroisoquinolines with tetrandrine
1993
Abstract The relaxant activity of three bisbenzyltetrahydroisoquinolines—obaberine, popisonine and lindoldhamine—was examined in rat isolated uterus and their inhibitory potencies were compared with that of tetrandrine. All alkaloids tested relaxed KCl-depolarized rat uterus and totally or partially inhibited oxytocin-induced rhythmic contractions. The degree of methylation of the free phenolic hydroxy groups and the loss of one diarylether bridge influence the potency of relaxant action of these alkaloids. Only alkaloids with absolute configuration 1R,1′S or 1R1′R acted intracellularly, promoting relaxation of contractile responses induced by oxytocin or vanadate in a Ca2+-free medium.
Inhibition of calcium entry induced by cularines and isocrasifoline in uterine smooth muscle.
1991
Abstract The effects of nifedipine, papaverine and four benzylisoquinoline alkaloids (cularine, cularidine, celtisine and isocrasifoline) were studied in isolated rat uterus in order to clarify the mechanism of their relaxant action. All the compounds tested completely relaxed KCl-induced contractions and totally or partially inhibited oxytocin-induced rhythmic contractions. Only papaverine acted intracellularly, promoting relaxation of contractile responses induced by oxytocin or vanadate in a Ca 2+ -free medium. In spite of the structural relationship between papaverine and the other alkaloids, the mechanism of their relaxant action is not the same. The activities of cularine derivatives …
Selective inhibition of calcium entry induced by benzylisoquinolines in rat smooth muscle.
1992
Abstract The mechanism of relaxant activity of six benzylisoquinolines was examined in order to determine the minimal structural requirements that enable these compounds to have either a non-specific action like papaverine or an inhibitory activity on calcium entry via potential-operated channels. All the alkaloids tested totally or partially relaxed KCl-depolarized rat uterus and inhibited oxytocin-induced rhythmic contractions. Only glaucine and laudanosine inhibited K+-induced uterine contractions more than oxytocin-induced uterine contractions. In Ca+-free medium, sustained contractions induced by oxytocin or vanadate were relaxed by the alkaloids tested except for glaucine and laudanos…
New strategies for medical management of overactive bladder in children.
2011
Purpose of review The medical treatment of children with non-neurogenic overactive bladder syndrome (OAB) is still limited to a small number of drugs approved for use in childhood according to the national regulations of each country. Recent findings Over the last few years, there were several studies on the use of antimuscarinics other than oxybutynin in children, as well as some on the use of extended release oxybutynin and tolterodine and transdermal oxybutynin. It was shown that the combination of two different anticholinergics might be a well tolerated and successful option in children with OAB refractory to monotherapy, as well as administration of a receptor-selective antimuscarinic …
Corticotropin-Releasing Hormone-Mediated Induction of Intracellular Signaling Pathways and Brain-Derived Neurotrophic Factor Expression Is Inhibited …
2005
CRH receptor (CRHR) 1 and the cannabinoid receptor 1 (CB1) are both G protein-coupled receptors. Activation of CRHR1 leadstoincreasesincAMPproductionandphosphorylationof the transcription factor cAMP response element-binding protein (CREB). In contrast, CB1 is negatively coupled to the cAMP signaling cascade. In this study, we analyzed a putative interaction between these two systems focusing on the regulation of the expression of brain-derived neurotrophic factor (BDNF), a CREB-regulated gene. In situ hybridization revealed coexpression of CRHR1 and CB1 receptors in the granular layer of the cerebellum. Therefore, we analyzed the effects of CRH and the CB1 agonist WIN-55,212-2 on BDNF expr…
A pyrroloquinazoline derivative with anti-inflammatory and analgesic activity by dual inhibition of cyclo-oxygenase-2 and 5-lipoxygenase
2002
Abstract In a previous study, we reported a new pyrroloquinazoline derivative, 3-(4′-acetoxy-3′,5′-dimethoxy)benzylidene-1,2-dihydropyrrolo[2,1- b ]quinazoline-9-one (PQ), which inhibited human purified 5-lipoxygenase activity and prostaglandin E 2 release in lipopolysaccharide-stimulated RAW 264.7 cells. In the present work, we show that PQ inhibits cyclo-oxygenase-2 activity in intact cell assays (human monocytes) and purified enzyme preparations (ovine isoenzymes) without affecting cyclo-oxygenase-1 activity. This behaviour was confirmed in vivo by using the zymosan-injected mouse air pouch model, where PQ caused a marked reduction in cell migration and leukotriene B 4 levels at 4 h, as …
Preparation of tungstophosphoric acid/cerium-doped NH2-UiO-66 Z-scheme photocatalyst: a new candidate for green photo-oxidation of dibenzothiophene a…
2021
International audience; The goal of this study was to introduce an effective visible-light induced photocatalytic system with a good ability for photocatalytic oxidative desulfurization (PODS) and denitrogenation (PODN) using molecular oxygen (O2) as an oxidant. In this regard, tungestophosphoric acid (PW12) was supported onto cerium-doped NH2-UiO-66 (PW12/Ce-NUiO-66) and employed for the photo-oxidation of dibenzothiophene (DBT) and quinoline (Qu). Herein, using cerium (Ce) as a “mediator” facilitated the separation of charge carriers, while NH2-UiO-66 remarkably enhanced the surface area with plentiful adsorption sites and shifted the adsorption edge of PW12to the visible region. The sum …
Combined Spectroscopic and TD-DFT Analysis to Elucidate Substituent and Acidochromic Effects in Organic Dyes: A Case Study on Amino- versus Nitro-Sub…
2020
Made available in DSpace on 2020-12-12T01:33:30Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-01-01 A combined spectroscopic and TD-DFT case study was performed, to identify a robust method to calculate the complex near UV/Vis absorption spectra of various amino- vs. nitro-substituted 2,4-diphenylquinolines, which vary strongly under neutral and successively acidic conditions. For this, different DFT functionals were tested for geometry optimization and the TD part to calculate the neutral and different protonated species in a fast screening approach, i. e. using single point calculations in an implicit solvent. Offset-corrected M06HF, hitherto only applied to polymers, was identif…
Tenapanor for the treatment of irritable bowel syndrome with constipation.
2020
Introduction: Irritable bowel syndrome with constipation is associated with higher rates of functional impairment, as compared to other subtypes of the syndrome. Conventional laxative-based pharmacologic therapy of IBS-C, which is mostly symptom-based, is often unsatisfactory. Tenapanor represents a first-in-class orally available inhibitor of NHE3, which is minimally absorbed in the GI tract, what constitutes a significant therapeutic benefit, as it may act on the drug target. Areas covered: Aim of this article is to sum up the evidences about pharmacodynamics and pharmacokinetics of tenapanor, focusing on animal models and in vitro studies, but also discuss clinical trials on tenapanor's …
The Synthesis of Quinoline‐based Tin Complexes with Pendant Schiff Bases
2019
Whilst pursuing the synthetic utility of quinoline‐based tin complexes, Me2Sn(Quin‐NO2)2 (1) and Ph2Sn(Quin‐NO2)2 (2) (Quin‐NO2 = 5‐nitroquinolino‐8‐oate) were synthesized bearing coordinatively inert nitro groups. Conventional reduction methodologies successfully converted 1 to Me2Sn(Quin‐NH2)2 (3) and 2 to Ph2Sn(Quin‐NH2)2 (4) (Quin‐NH2 = 5‐aminoquinolino‐8‐oate). The synthetically useful amine groups proved difficult to exploit in the presence of the central tin atom, however, a complete Schiff base functionalized Sn complex of the dimethyltin pro‐ligand Me2Sn(Quin‐py)2 (6) was successfully synthesized from 5‐[(pyridin‐2‐ylmethylene)amino]quinolin‐8‐ol (HQuin‐py; 5) in good yield via an …