Related to our research on structural modifications of pentalongin, the active principle of the medicinal plant Pentas longiflora Oliv., a new synthesis of N-protected 1,2-dihydrobenz[g]isoquinoline-5,10-diones and their 4-methyl derivatives, which represent a new class of compounds, is reported...
A strategy for the preparation of 4,4-disubstituted-3-amino-2-azetidinones, which are useful intermediates for the synthesis of analogues of monosulfactam Tigemonam, was developed. It employs D-serine as chiral starting material and involves, as key steps, the diastereoselective addition of orga...
We prepared 5-HT1A receptor ligands (S)-N-{[1-(2-phenylethyl)pyrrolidin-2-yl]methyl}-3-[11C]methylthiobenzamide ([11C](S)-PPMMB) (Ki = 4.3 nM) and the less active [11C](R)-PPMMB (Ki = 160 nM) by reduction of the disulfide dimer and subsequent [11C]methylation of demethyl (S)- and (R)-PPMMB, resp...
Cycloaddition between (+) or (−)-menthone-derived nitrones and N-benzyl-3-pyrroline afforded enantiopure spiro-fused heterocycles. The reaction occurred enantio- and diastereo-selectively on the less hindered side of the nitrone, the 3-pyrroline N-benzyl group being oriented outwards, thus contr...
Reaction of 3-alkylsulfanyl-2-arylazo-3-(pyrrolidin-1-yl)acrylonitriles with maleimides, dimethyl maleate and dimethylacetylene dicarboxylate were carried out to give octahydro-pyrrolo[3,4-a]pyrrolizin-4-ylidenes, hexahydro-pyrrolizines and 6,7-dihydro-5H-pyrrolizines. The formation of the synth...
Oxidative polymerization of 2,6-dimethylphenol yields the polyphenylene oxide which is manufactured commercially on a large scale. Most of this polymer is sold as a homogeneous blend with polystyrene or as a heterogeneous blend with nylon. Polymers have also been synthesized from 2,6-diarylpheno...
This chapter describes the reactions of direct enantioselective carbon–X bond formation based on electrophilic reactions via the functionalization of C–H bonds or sp2 carbon with electrophilic X donors. The X atoms treated here are F, Br, Cl, I, S, and Se. Both stoichiometric and catalytic str...
AimsThe current study was conducted to evaluate, by the noninvasive positron emission tomography (PET), the binding of antimuscarinic agents used to treat overactive bladder (OAB) to muscarinic receptors in rat brain.
A selective stability-indicating ultra-performance liquid chromatographic (UPLC) method was developed for the quantitative determination of darifenacin hydrobromide (DFN) and its related compounds in API and pharmaceutical dosages. The chromatographic separation was achieved on an Acquity UPLC B...
Objectives: To evaluate the efficacy, tolerability and safety of darifenacin, a once-daily M3 selective receptor antagonist (M3 SRA), in patients with overactive bladder (OAB).Methods: This multicentre, double-blind, placebo-controlled, parallel-group study enrolled 561 patients (19−88 years; 85...
Objectives:To evaluate the effects of darifenacin, an M3 selective receptor antagonist, compared with oxybutynin, on ambulatory urodynamics, salivary flow, heart rate and visual nearpoint in patients with overactive bladder (OAB).
ObjectivePrevious studies have revealed that intravesical and systemic administration of oxybutinin suppress pelvic afferent nerves. This study evaluates the efficacy of a selective M3 antimuscarinic, darifenacin, on bladder afferent activity.
Aim:To evaluate the efficacy, tolerability and safety of darifenacin, an M3 selective receptor antagonist, in the subgroup of older patients from a pooled analysis of three phase III, multicentre, randomized, double-blind clinical trials in patients with overactive bladder (OAB).
A novel muscarinic receptor antagonist, darifenacin, inhibited specific binding of [N-methyl-3H]scopolamine ([3H]NMS) in the mouse bladder, submaxillary gland and heart in a concentration-dependent manner. The inhibitory effect was most potent in the submaxillary gland, followed by the bladder a...
ObjectivesTo investigate the effects of darifenacin controlled-release (CR) and oxybutynin extended-release (ER) on cognitive function (particularly memory) in older subjects.
ABSTRACTPurpose:We assessed the effect of darifenacin, an M3 selective receptor antagonist, on the warning time associated with urinary urgency.
ABSTRACTPurpose:Overactive bladder is common in the elderly population, which is susceptible to cognitive disorders and drug induced cognitive impairment. Existing overactive bladder treatments may cause adverse events, such as cognitive impairment, due to antagonism of the M1 receptor in the ce...
Darifenacin is a selective muscarinic M3 receptor antagonist …
A highly selective, sensitive, and rapid high-performance liquid chromatography (HPLC) method has been developed and validated for the quantification of darifenacin in mouse plasma. Bisoprolol was used as an internal standard (IS). Darifenacin and the IS were extracted using the deproteinisation...
Isoflurane and carbon dioxide (CO2) gas are used for rodent euthanasia. This study compared mouse aversion to isoflurane versus gradual-fill CO2 gas, and compared two methods of isoflurane delivery: vaporizer and drop. Mouse acclimation to a light–dark apparatus was used to create a light avers...
About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia
Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog
©2008 LookChem.com,License: ICP
NO.:Zhejiang16009103
complaints:service@lookchem.com Desktop View