Search results for "Quinuclidine"
showing 10 items of 16 documents
Evidence for the presence of functional protease activated receptor 4 (PAR4) in the rat colon
2004
Background and aims: Protease activated receptors (PARs) have been postulated to play a role during intestinal inflammation. The presence and role played by PAR4 in gastrointestinal functions have not been fully clarified. The aims of this study were: (i) to examine expression of PAR4 in rat proximal colon; (ii) to determine the mechanical effects induced by PAR4 activation in longitudinal muscle; and (iii) to characterise the underlying mechanisms. Methods: PAR4 expression was determined by reverse transcription-polymerase chain reaction (RT-PCR) and immunohistochemistry. Mechanical activity was recorded as changes in isometric tension. Results: A PCR product corresponding to the predicted…
Role of solvent and base in the silanization reaction of silicas for reversed-phase high-performance liquid chromatography
1984
Reversed-phase packings were synthesized by reaction of n-alkyldimethylchloro- and trifluoroacetoxysilanes with silicas of 15 and 25 nm pore size, employing tetrahydrofuran, N,N-dimethylformamide, benzene, diethyl ether, dichloromethane and acetonitrile as solvents and triethylamine, pyridine, triazole, quinuclidine, 2,4- and 2,6-lutidine and imidazole as bases. With dichloromethane as solvent and 2,6- lutidine as base, n-alkyldimethyltrifluoroacetoxysilanes did not yield n-alkyl ligand densities higher than those obtained with n-alkyldimethylchlorosilanes under identical conditions. With a given base and given n-alkyldimethylchlorosilane the solvent type was found to exert a noticeable inf…
Altered tachykinergic influence on gastric mechanical activity in mdx mice
2006
Abstract This study investigated whether alterationsin gastric activity in dystrophic mdx mouse can beattributed to dysfunctions of tachykinins. Endolumi-nal pressure was recorded and the expression ofneuronal nitric oxide synthase (nNOS), NK1 and NK2neurokinin receptors was investigated by immunoh-istochemistry. SR48968, NK2 receptor antagonist, butnot SR140333, NK1 receptor antagonist, decreased thetone only in mdx gastric preparations. In the presenceof N x -nitro- L -arginine methyl ester ( L -NAME), inhib-itor of NOS, SR48968 reduced the tone also in normalstomach. [Sar 9 , Met(O 2 ) 11 ]-SP, agonist of NK1 recep-tors, caused tetrodotoxin-sensitive relaxations, antag-onized by SR140333…
One shot NEPA plus dexamethasone to prevent multiple-day chemotherapy in sarcoma patients
2019
Purpose: Chemotherapy-induced nausea and vomiting (CINV) is one of the most feared and disturbing adverse events of cancer treatment associated with decreased adherence to effective chemotherapy regimens. For high-risk soft tissue sarcoma patients, receiving multiple-day chemotherapy (MD-CT), antiemetic guidelines recommend a combination of an NK 1 receptor antagonist (NK 1 -RA), a 5-HT 3 receptor antagonist (5HT 3 -RA), and dexamethasone on each day of the antineoplastic treatment. NEPA is the first oral fixed-dose combination of a highly selective NK 1 -RA, netupitant, and second-generation 5HT 3 -RA, palonosetron. So far, no data has been published in literature about the efficacy of a s…
Single-dose Palonosetron for prevention of chemotherapy-induced nausea and vomiting in patients with aggressive non-Hodgkin's lymphoma receiving mode…
2011
PURPOSE: The control of nausea and vomiting induced by chemotherapy is paramount for overall treatment success in cancer patients. Antiemetic therapy during chemotherapy in lymphoma patients generally consists of anti-serotoninergic drugs and dexamethasone. The aim of this trial was to evaluate the efficacy of a single dose of palonosetron, a second-generation serotonin type 3 (5-HT(3)) receptor antagonist, in patients with aggressive non-Hodgkin's lymphoma receiving moderately emetogenic chemotherapy (MEC) containing steroids. METHODS: Patients received a single intravenous bolus of palonosetron (0.25 mg) before administration of chemotherapy. Complete response (CR) defined as no vomiting …
A Comparison of the Efficacy and Tolerability of Solifenacin Succinate and Extended Release Tolterodine at Treating Overactive Bladder Syndrome: Resu…
2005
Abstract Objective: To compare two new generation antimuscarinics at their recommended doses for treatment of overactive bladder syndrome (OAB). Methods: A prospective, double blind, double-dummy, two-arm, parallel-group, 12-week study was conducted to compare the efficacy and safety of solifenacin 5 or 10mg and tolterodine extended release (ER) 4mg once daily in OAB patients. After 4 weeks of treatment patients had the option to request a dose increase but were dummied throughout as approved product labelling only allowed an increase for those on solifenacin. Results: Solifenacin, with a flexible dosing regimen, showed greater efficacy to tolterodine in decreasing urgency episodes, inconti…
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands
2001
In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine series afforded the most promising compounds in terms of both receptor affinity and M2-subtype selectivity.
Molecular aggregates of quinuclidine and chlorophyll a
1991
A slightly polar molecule quinuclidine seems to form weakly bound aggregates in concentrated water solutions. Molecular dynamics simulation of a 6 mol water solution indicates clustering of quinuclidine molecules into an almost spherical structure with polar ends of the molecules pointing towards the solvent. Experimental evidence of aggregation was obtained by observing a small but obvious red shift of the o'' a absorption and a dramatic shortening of the fluorescence lifetime of the c n transition of concentrated solutions. The observed self-quenching is interpreted in terms of Frster model for energy transfer in the cluster. It is estimated that excitation may migrate on the cluster surf…
CCDC 2079430: Experimental Crystal Structure Determination
2021
Related Article: Jas S. Ward, Antonio Frontera, Kari Rissanen|2021|Dalton Trans.|50|8297|doi:10.1039/D1DT01437D
CCDC 2079431: Experimental Crystal Structure Determination
2021
Related Article: Jas S. Ward, Antonio Frontera, Kari Rissanen|2021|Dalton Trans.|50|8297|doi:10.1039/D1DT01437D