The effects of the GABAB (γ-amino butyric acidB) receptor agonist, baclofen and its antagonist, phaclofen on physiologically identified retinal ganglion cells were studied in the optically intact eye of pentobarbitone-anaesthetized cats. These results were compared with the effects of the GABAA...

The influence of γ-aminobutyric acid (GABA) receptor agonists and antagonists on the intracellular concentration of inositol 1,4,5-triphosphate (IP3) was examined in neuronal cultures of embryonic chick tectum. GABA and selective agonists of its receptors were inactive, whereas phaclofen, a GAB...

The present study was performed to determine whether the effects induced by GABAB receptor-acting drugs would be related with the alteration in GABAB receptor expression in the hippocampus using Mongolian gerbil, a genetic epilepsy model. The distribution patterns of both GABAB receptor 1A/B and...

The ability of the GABAB receptor antagonist, phaclofen to alter behavioral effects of ethanol was evaluated by loss of righting reflex (sleep time), motor incoordination (bar holding), spontaneous locomotion (open field activity) and hypothermia. Pretreatment with phaclofen significantly decrea...

Analogues of baclofen, phaclofen and saclofen, incorporating a sulfur atom within the methylene chain, have been tested against responses induced by baclofen for activity at γ-aminobutyric acid-B (GABAB) receptor sites, using a number of preparations including the guinea-pig isolated ileum and ...

The action of phaclofen, the phosphonic acid derivative of baclofen, on baclofen-induced suppression of spinal reflex transmission was tested in anaesthetized rats. Intrathecal (i.th.) injection of phaclofen, 100 nmol, antagonized the depressant effect of baclofen, 2 nmol, on spinal Hoffmann (H)...

Phaclofen, the phosphonic acid derivative of baclofen, reversibly antagonized the depression of the cholinergic twitch response of the guinea pig ileum and distal colon by either baclofen or GABA. When administered microelectrophoretically, phaclofen reversibly blocked the presumed presynaptic r...

Our earlier observation that intrathecal administration of L- and D-baclofen had different effects on sympathetic output regulating arterial pressure and heart rate in the rat prompted the present study which was designed to determine whether intrathecal administration of GABA elicits a phaclofe...

1. Intraperitoneal (ip) injection of (−)-baclofen induced long-lasting antinociceptive and sedative effects in rats.2. Phaclofen, the phosphonic derivative of baclofen, fully antagonized the antinociceptive effect of (−)-baclofen. when injected intracerebroven-tricularly (icv), but not ip, phacl...

Phaclofen, a phosphonic acid analog of baclofen, is a selective, low-affinity (high μM), GABAB receptor antagonist. As one of the first antagonists for this site, phaclofen has been employed extensively for defining the physiological and pharmacological characteristics of this receptor system. ...

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig stria...

The 5-HT1B receptor has attracted significant interest as a potential target for the development of therapeutics for the treatment of affective disorders such as anxiety and depression. Here we present the in vivo characterisation of a novel, selective and orally bioavailable 5-HT1B receptor ant...

The gas chromatographic and mass spectrometric properties of the monohydroxy acids 5-hydroxyeicosatetraenoic acid (5-HETE), 12-hydroxyeicosatetraenoic acid (12-HETE) and 15-hydroxyeicosatetraenoic acid (15-HETE) as their methyl ester trimethylsilyl, methyl ester allyldimethylsilyl and methyl est...

A new type of fluoride ion catalyzed allylation agent, o-bis(allyldimethylsilyl)benzene (1a) and bis(allyldimethylsilyl)methane (1b), can be successfully utilized for various carbonyl substrates. The rate acceleration is ascribable to the shift of equilibrium to complex with Bu4NF by the favorab...

A review on physical and chemical properties, methods of preparation and analysis, as well as pharmacodynamics and pharmacokinetics of amlodipine besylate (3-ethyl 5-methyl (4RS)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate), an app...

This study aimed to perform a pharmacokinetic-pharmacodynamic (PK-PD) target attainment analysis to create a dosing strategy for cefozopran in Japanese adult patients. A total of 145 plasma concentration samples from 32 adult patients were used for a population pharmacokinetic modeling and Monte...

A method for determining the concentration of cefozopran, a cephem anti-microbial agent which has a broad spectrum, in human serum using micellar electrokinetic capillary chromatography (MEKC) by serum direct injection is developed and the validation of the assays of this method is performed. A ...

A simple, rapid and precise HPLC method using ultrafiltration to remove protein was developed to determine total cefozopran concentrations in human peritoneal fluid in the same manner as in human plasma, irrespective of the amount of protein. The recovery of cefozopran after ultrafiltration in p...

Searching for hit compounds within the huge chemical space resembles the attempt to find a needle in a haystack. Cheminformatics-guided selection of few representative molecules of a rationally designed virtual combinatorial library is a powerful tool to confront this challenge, speed up hit ide...

New thiazolopyrimidine and dithiazolopyrimidinone derivatives 2–11 were synthesized and estimated for antimicrobial activity against S. aureus, B. cereus, E. coli, C. albicans, A. fumigatus and A. terreus. The attained results proved that 4, 8a and 11g have significant effectiveness against S. ...