Alpha‐1‐acid glycoprotein (AGP) encoded by orosomucoid genes (ORM1 and ORM2) is an acute‐phase response protein and functions as a drug‐binding protein that affects pharmacokinetics (PK)/pharmacodynamics of binding drugs. To explore the effects of genetic variations of ORMs and a role of AGP...
The tosyl ester 2 of tetraethyl 1-acetamido-4-hydroxybutane- 1,1,3,3-tetracarboxylate gave 4-methylene glutammic acid in 90% yield by refluxing with concentrated HC1. Treatment of 2 with NaOEt, then with refluxing concentrated HC1 gave a 54% yield of cis and trans-pyrrolidine-2,4-dicarboxylic ac...
The 1H-1,2,3-triazole-originated derivatives of willardiine were obtained by: (i) construction of the 1H-1,2,3-triazole ring in 1,3-dipolar cycloaddition of the uracil-derived azides and the carboxylate-bearing alkynes or α-acylphosphorus ylide, or (ii) N-alkylation of the uracil derivative wit...
In this communication we describe a simple two-step procedure for the conversion of several steroidal alcohols to their aminopropyl ether derivatives. To demonstrate the usefulness of this procedure we synthesized a second-generation photoaffinity labeling analog of 1α,25-dihydroxyvitamin D3, a...
The photoaffinity labeling of chick intestinal 1α,25-dihydroxyvitamin D3 receptor with 1α,25-dihydroxyvitamin D3-3β-{N-(-4-azido-2-nitro[3,5-3H]phenyl)}glycinate has been determined under a variety of conditions.
3-Azidobenzoates and 3-azidonitrobenzoates of 25-hydroxyvitamin D3 as well as 3-deoxy-3-azido-25-hydroxyvitamin D3 and 3-deoxy-3-azido-1,25-dihydroxyvitamin D3 were prepared as photoaffinity labels for vitamin D serum binding protein and 1,25-dihydroxyvitamin D3 intestinal receptor protein. The ...
We report the synthesis and biological evaluation of new 2-amino-4,5-diarylpyrimidines as selective antagonists at the adenosine A1 receptor. The scaffold they are based upon is a deaza variation of a previously reported collection of 3-amino-5,6-diaryl-1,2,4-triazines, members of which had a su...
Propranolol (0·25%) administered topically to each of six conscious rabbits prevented the initial rise in ocular tension normally seen after topical application of 10·0% adrenaline. Neither 0·25% nor 0·5% propranolol affected the delay in onset of hypotension after 0·5% adrenaline applied t...
Five per cent guanethidine sulphate applied topically twice daily for 7 days to one eye of each of a group of eight rabbits produced a significant miosis and hypotension in the treated eyes. The hypotensive effect of 0·25% (−)-adrenaline bitartrate was augmented in the eyes which had received g...
Adult male Sprague-Dawley rats were administered dopamine (DA) or l-noradrenaline (l-NA) locally into the nucleus accumbens or in the neostriatum. Six minutes following the injections the animals were placed in an open field arena (700×700 mm) and their locomotor activity was recorded every 3 m...
Publisher SummaryThis chapter describes the physical properties and synthesis of levarterenol bitartrate. Rotatory dispersion curves indicate the configuration to be D through its relation to D-mandelic acid and D-lactic acid by their negative Cotton effects. The assignments are confirmed throug...
Electrophysiological studies using reserpinized cats were performed to examine the effects of l-threo-3,4-dihydroxyphenylserine(l-threo-DOPS) on the noradrenergic pathway from the locus coeruleus (LC)_to the spinal trigeminal nucleus (STN). The spike generation of STN relay neurons induced by tr...
l-DOPA-induced dyskinesia is known as involuntary debilitating movement, which limits quality of life in patients suffering from Parkinson's disease. The present study focuses on the role of the neurotransmitter noradrenaline (NA) on dyskinetic movements in comparison to the effect of l-DOP...
SummaryObjectivesNorepinephrine is usually used in emergency situations such as in intensive care units (ICUs) for the restoration of blood pressure. The objective was to study the stability of highly-concentrated solutions of norepinephrine at 0.50 mg/mL and 1.16 mg/mL, diluted in glucose 5% (G...
The aim of the present study was the characterization of the subtypes of inositol 1,4,5-trisphosphate receptors (IP3R) in rat colonic epithelium. A monoclonal antibody against IP3R1 did not stain the colonic epithelial cells. In contrast, IP3R2 and IP3R3 were found within the epithelium; however...
The introduction of a ring of arginine residues near the constriction in the transmembrane β barrel of the staphylococcal α-hemolysin heptamer yielded a pore that could be almost completely blocked by phosphate anions at pH 7.5. Block did not occur with other oxyanions, including nitrate, sulf...
Injection of inositol 1,4,5-trisphosphate (Ins 1,4,5-P3) into Limulus ventral photoreceptors produces excitation similar to that produced by light. One process which might contribute to rapid termination of the responses to Ins 1,4,5-P3 and to light is the hydrolysis of Ins 1,4,5-P3 by an InsP3-...
The reaction of perbenzylated (±)-myo-inositol 1,2-bis- and 1,2,6-tris-phosphites with benzyl bromoacetate, followed by catalytic (PdC) hydrogenolysis affords (±)-myo-inositol 1,2-bis- and 1,2,6-tris(carboxymethylphosphonate). The same procedure is used for the synthesis methyl α-D-mannopyran...
To determine the effects of the aging process on the regulation of phosphoinositide signal transduction pathway, inositol 1,4,5-trisphosphate and inositol 1,4,5-trisphosphate receptor-associated parameters were examined in the striatum of brains removed from young (3 months), adult (12 months) a...
Biomimetic syntheses of enantiomerically pure 3-deoxy-d-muco- and d-myo-inositol-1,4,5 trisphosphate from d-glucose are described. Preliminary biological studies show a dramatic influence of the stereochemistry at C-4 on the binding to IP3 receptor.
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