Cations were generally ineffective in stimulating succinate transport in a succinate dehydrogenase mutant of Bacillus subtilis unless accompanied by polyvalent anions; phosphate and sulfate being particularly active. The Km values for the phosphate or sulfate requirement were approx. 3 mM.Biphas...

A study was undertaken to determine if humans excrete both amobarbital N-glucuronides and N-glucosides in urine after an oral dose of amobarbital. Amobarbital N-glucuronides were synthesized and characterized. A reverse phase LC method using post-column pH adjustment and UV detection at 240 nm w...

A study was undertaken to determine if humans excreted barbital N-glucoside as a urinary metabolise following oral administration of barbital. A liquid chromatography method using gradient elution was developed for detecting and quantifying barbital N-glucoside and barbital in urine. Following a...

5-Carbamoyl-2-phenylpyrimidine derivative 2 has been identified as a phosphodiesterase 4 (PDE4) inhibitor with moderate PDE4B inhibitory activity (IC50 = 200 nM). Modification of the carboxylic acid moiety of 2 gave N-neopentylacetamide derivative 10f, which had high in vitro PDE4B inhibitory ac...

Spleen tyrosine kinase (Syk) is a non-receptor-type tyrosine kinase which mediates diverse responses in haematopoietic cells. Therefore, Syk is an attractive therapeutic target, and in a study of Syk inhibitors as potentially new therapeutic agents, we discovered the 4-anilinopyrimidine-5-carbox...

The STAT6 (signal transducers and activators of transcription 6) protein is activated by interleukin (IL)-4 and IL-13, and plays an important role in T-helper cell 2 (Th2) differentiation. STAT6 might therefore be an excellent therapeutic target for various allergic conditions, including asthma ...

In view of inconsistent results reported for 5-hydroxytryptamine1A (5-HT1A) receptor involvement in murine social conflict, this study examined the effects of N1-(bromoacetyl)-N8-[3-(4-indolyloxy)-2-hydroxypropyl]-(Z)-1,8-diamino-p-menthane (pindobind) 5-HT1A, a novel 5-HT1A antagonist, on agoni...

Studies on the behavioural effects of 5-hydroxytryptamine receptor subtype 1A (5-HT1A) antagonists may provide important clues to the precise role of 5-HT1A receptor mechanisms in anxiety. In the first of a series of experiments designed to address this issue, the effects of mixed 5-HT1A and β-...

Serotonin (5-hydroxytryptamine; 5-HT) modulates constituents of the immune system. 5-HT1A receptor antagonists potently suppress lymphocyte function. NK cell activity (NKCA) was measured after exposure of mononuclear cells to the 5-HT1A receptor antagonist pindobind and the 5-HT1C/2 receptor ant...

The purpose of this study was to develop and optimize oral controlled-release formulations for tamsulosin hydrochloride using a combination of two cellulose ester derivatives, hydroxypropyl methylcellulose (HPMC) and hydroxypropyl methylcellulose phthalate (HPMCP), with Surelease® as a coating m...

The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques. Centrifugal granulator and fluidized-bed coater were employed to prepare drug-loaded pellets and to employ two-layered membrane coating respectively. The prepared...

The objective of this study was to prepare tamsulosin hydrochloride-sustained release (TSH-SR) pellets which showed good release stability with frame-controlled method. TSH was added to Eudragit®NE30D and Eudragit®L30D-55 polymers to form drug-loaded inner core. Afterwards, enteric Eudragit®L30D...

In the present study, superparamagnetic graphene oxide-Fe3O4 nanocomposites were successfully prepared by a modified impregnation method (MGOmi) and their application as a sorbent in the magnetic-dispersive solid phase extraction (M-dSPE) mode to the preconcentration and determination of tamsulo...

A new spectrophotometric method for the estimation of tamsulosin hydrochloride in pharmaceutical dosage forms has been developed and validated. The method is based on reaction between drug and bromophenol blue and complex was measured at 421 nm. The slope, intercept and correlation coefficient w...

The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoat®), and an aqueous copolym...

PurposeThe primary aim of this study was to evaluate whether there was clinically significant pharmacokinetic (PK) interaction between finasteride and tamsulosin in healthy Chinese male subjects.

Simple, rapid and accurate new vierordt’s (VI) method or simultaneous equation (SE) method is developed and validated for the simultaneous estimation of dutasteride (DU) and tamsulosin hydrochloride (TA) in pure and pharmaceutical dosage form. The method is based on the measurement of absorbanc...

Novel 1,2-dithiolane/chroman hybrids bearing heterocyclic rings such as 1,2,4- and 1,3,4-oxadiazole, 1,2,3-triazole and tetrazole were designed and synthesized. The neuroprotective activity of the new analogues was tested against oxidative stress-induced cell death of glutamate-challenged HT22 h...

Remote ischemic preconditioning (RIPC) is a cardioprotective strategy against myocardial damage by ischemia-reperfusion. Many in-vivo and ex-vivo animal researches have demonstrated that RIPC decreases significantly the ischemia-reperfusion myocardial damage, by up to 58% in isolated rat heart. ...

Various N-(R)-(+)-(α-methylbenzyl)-(2R,3R)-disubstituted aziridines were prepared by intramolecular cyclization. The regioselective reduction of the ring C(3)-N bond in the presence of (Boc)2O by catalytic hydrogenation with atmospheric pressure of hydrogen provides (D)-phenylalaninol analogues...