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R Haseneder

Publications and source records attributed to R Haseneder.

8 recordsLinked to original sources
PubMed2004

Alpha-thujone reduces 5-HT3 receptor activity by an effect on the agonist-reduced desensitization.

The convulsant effects of alpha-thujone, the psychotropic component of absinthe, were attributed to inhibitory actions at the GABAA receptor. Here, we investigated for the first time the 5-HT3 receptor as a potential site of the psychotropic actions of alpha-thujone. This cation permeable ligand-gated ion channel shows considerable homology to the GABAA receptor. We previously demonstrated that in homomeric assemblies of cloned human 5-HT,A receptor subunits. the endogenous agonist 5-HT induced desensitization via channel blockade. When the 5-HT3 B receptor subunit was co-expressed, the resulting heteromeric assemblies desensitized independent from channel blockade. In the present study, patch-clamp experiments revealed an inhibitory action of alpha-thujone on both homomeric and heteromeric 5-HT3 receptors. This inhibitory action was mediated via channel blockade. However, it was not alpha-thujone itself which blocked the channel. The present experiments suggested that, in homomeric receptors, alpha-thujone enhanced the inherent channel-blocking potency of the natural ligand. 5-HT. In heteromeric receptors, alpha-thujonerecruited an additional channel-blocking component of the agonist. By means of kinetic modeling, we simulated possible mechanisms by which alpha-thuljone decreased the 5-HT-induced responses. It is suggested that alpha-thujone reduced 5-HT3 receptor activity by an effect on mechanisms involved in receptor desensitization, which depend on receptor subunit composition. It remains to be shown if this inhibitory action on serotonergic responses contributes to behavioral effects of alpha-thujone.

Bicyclic Monoterpenes↗
PubMed2003

Co-expression of the 5-HT3B serotonin receptor subunit alters the biophysics of the 5-HT3 receptor.

Homomeric complexes of 5-HT(3A) receptor subunits form a ligand-gated ion channel. This assembly does not fully reproduce the biophysical and pharmacological properties of native 5-HT(3) receptors which might contain the recently cloned 5-HT(3B) receptor subunit. In the present study, heteromeric assemblies containing human 5-HT(3A) and 5-HT(3B) subunits were expressed in HEK 293 cells to detail the functional diversity of 5-HT(3) receptors. We designed patch-clamp experiments with homomeric (5-HT(3A)) and heteromeric (5-HT(3AB)) receptors to emphasize the kinetics of channel activation and desensitization. Co-expression of the 5-HT(3B) receptor subunit reduced the sensitivity for 5-HT (5-HT(3A) receptor: EC(50) 3 micro M, Hill coefficient 1.8; 5-HT(3AB) receptor: EC(50) 25 micro M, Hill coefficient 0.9) and markedly altered receptor desensitization. Kinetic modeling suggested that homomeric receptors, but not heteromeric receptors, desensitize via an agonist-induced open-channel block. Furthermore, heteromeric 5-HT(3AB) receptor assemblies recovered much faster from desensitization than homomeric 5-HT(3A) receptor assemblies. Unexpectedly, the specific 5-HT(3) receptor agonist mCPBG induced an open-channel block at both homomeric and heteromeric receptors. Because receptor desensitization and resensitization massively affect amplitude, duration, and frequency of synaptic signaling, these findings are evidence in favor of a pivotal role of subunit composition of 5-HT(3) receptors in serotonergic transmission.

Adaptation, Physiological↗
PubMed2002

The application of membrane filtration for the removal of ammonium ions from potable water.

It is well recognized that soluble ammonia and nitrite in drinking water has chronic effects on humans. Ammonia has potential environmental health hazards, particularly to young children. European Union Standards limit the concentration of ammonia to 0.5 mg/l in drinking water. In Eskisehir (Turkey) drinking and tap water are supplied from a water treatment plant, consisting mainly of screening, sedimentation, filtration and sterilization units and having a capacity of 80.000 m3/d. Depend on the industrial and climatic effects the observed high ammonium concentration in treated water causes undesirable effects of water quality. Therefore, people in Eskisehir do not want to use tap water for drinking. The aim of the study was to evaluate the performance of membrane processes, i.e. Nanofiltration and reverse osmosis to the removal of ammonium and Ca ions from plant effluent and recommend one of them for a subsequent pilot plant application.

Climate↗
PubMed2001

Isoflurane slows inactivation kinetics of rat recombinant alpha1beta2gamma2L GABA(A) receptors: enhancement of GABAergic transmission despite an open-channel block.

Recombinant alpha1beta2gamma2L gamma-aminobutyric acid (A) receptor (GABA(A)R) channels expressed in human embryonic kidney (HEK293) cells were used for patch-clamp experiments. The currents activated by brief pulses of GABA (10(-4) M) applied with a device for fast solution exchange to cells clamped in the whole-cell configuration mimicked GABA(A)R-mediated inhibitory postsynaptic currents. Isoflurane (ISO) at clinically relevant concentrations (0.6 mM) decreased the amplitude and prolonged the decay of the GABA-evoked response. To further detail the mechanism underlying the prolonged decay time, we made simulations based on these measurements. These simulations suggest that ISO slows the rate of GABA unbinding from the receptor. Under these conditions, ISO increases the GABA-induced charge transfer and, thus, could enhance GABAergic inhibition despite the concomitant open-channel block causing the decrease in the current amplitude.

Anesthetics, Inhalation↗
PubMed2001

Photochemical oxidation of p-chlorophenol by UV/H2O2 and photo-Fenton process. A comparative study.

In this study, photochemical advanced oxidation processes (AOPs) utilizing the combinations of UV/H2O2 and the photo-Fenton reaction (UV + classical Fenton reaction) were investigated in lab-scale experiments for the degradation of p-chlorophenol. The study showed that the photo-Fenton process, (a mixture of hydrogen peroxide and ferrous or ferric ion), was the most effective treatment process under acidic conditions and produced a higher rate of degradation of p-chlorophenol at a very short radiation time. It accelerated the oxidation rate by 5-9 times the rate for the UV/H2O2 process. The reaction was found to follow the first order, the reaction was influenced by the pH, the input concentration of H2O2 and the amount of the iron catalyst and the type of iron salt. The experimental results showed that the optimum conditions were obtained at a pH value of 3, with 0.03 mol/l H2O2, and 1 mmol/l Fe(II) for the UV/H2O2/Fe(II) system and 0.01 mol/l H2O2 and, 0.4 mmol/l Fe(III) for the UV/H2O2/Fe(III) system. The reactions were accompanied by the generation of Cl- which reached its maximum value at a short reaction time when using the photo-Fenton process. Finally a rough comparison of the specific energy consumption shows that photo-Fenton process reduced the energy consumption by at least 73 to 83% compared with the UV/H2O2 process.

Chlorophenols↗
PubMed2001

Coadministered nitrous oxide enhances the effect of isoflurane on GABAergic transmission by an increase in open-channel block.

Clinically relevant concentrations of isoflurane (ISO) and nitrous oxide (N2O) enhance chloride currents induced by activating gamma-aminobutyric acid(A) receptors (GABA(A)R). Channel blocking by ISO overcomes the enhancing effect at higher concentrations. In this study, the effect of coadministered ISO and N2O on responses evoked by GABA in transfected human embryonic kidney 293 cells carrying alpha1beta2gamma2L GABA(A)R was investigated. Patch-clamp recordings from these cells were performed in the whole cell mode. A piezo-driven "liquid filament" drug application system was used to apply solutions of GABA, ISO, and N2O. Increasing the concentration of ISO in steps from 0.15 to 1.2 mM resulted in a bell-shaped concentration-response curve for GABA-induced currents. The maximum increase in current (1.51 +/- 0.14-fold) was seen at 0.45 mM ISO (about 1 minimum alveolar concentration, EC50). N2O (29.2 mM) increased GABA-evoked currents 1.54 +/- 0.10-fold. The enhancing effects of ISO and N2O on the GABAergic response were not additive. However, a transient current, associated with the rapid withdrawal of ISO from the receptor, was markedly increased by N2O. Such rebound currents probably reflect the transition from a "channel-blocked" to a "reopened" state. An open-channel block at ligand-gated receptors can prolong postsynaptic currents. Thus, we conclude that coadministered N2O could increase the enhancing effect of ISO on the GABAergic transmission by an increase in open-channel block at the GABA(A)R.

Anesthetics, Inhalation↗
PubMed2000

Nitrous oxide and xenon increase the efficacy of GABA at recombinant mammalian GABA(A) receptors.

We investigated the interactions between recombinant gamma-aminobutyric acid receptor complex (GABA(A)R) and nitrous oxide (N(2)O) or xenon (Xe). Human embryonic kidney cells (HEK 293) were transfected with rat cDNA for alpha(1)beta(2)gamma(2L) or for alpha(1)beta(2) recombinant GABA(A)R subunits. Patch clamp techniques were used in the whole-cell mode to evaluate the effect of N(2)O and Xe on GABA-induced currents. A piezo-driven "liquid filament switch" was used for fast application. Both N(2)O (100%, 29.2 mM) and Xe (100%, 3.9 mM) reversibly increased GABA-induced currents through the alpha(1)ss(2)gamma(2L) and the alpha(1)beta(2) GABA(A)R channels. The potentiating effect of N(2)O or Xe on peak currents was prominent at small GABA concentrations (10(-7) to 10(-5) M). The addition of N(2)O or Xe increased the efficacy of GABA (10(-7) to 10(-3) M). Both N(2)O and Xe significantly decreased the risetime((10%-90%)) of the currents elicited by small GABA concentrations. At the concentrations used, neither N(2)O nor Xe had an intrinsic effect. We conclude that, similar to other anesthetics, both N(2)O and Xe increase the efficacy of GABA at the GABA(A)R and enhance inhibitory GABAergic synaptic transmission.

Anesthetics, Inhalation↗