Rainer Netzer

Rainer Netzer
ScieNet

PhD

About

26
Publications
966
Reads
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1,203
Citations
Citations since 2017
0 Research Items
137 Citations
20172018201920202021202220230510152025
20172018201920202021202220230510152025
20172018201920202021202220230510152025
20172018201920202021202220230510152025
Additional affiliations
November 2000 - April 2015
Evotec
Position
  • Senior Vice President

Publications

Publications (26)
Article
A common over-the-counter (OTC) non-opioid antitussive drug, clobutinol, was recently withdrawn from the market due to its potential to induce cardiac arrhythmias by a blockade of the potassium channel coded by the human ether-à-go-go-related gene (hERG). In this study, we investigated the effects of a number of antitussive compounds on the hERG io...
Article
Steroids are known to exert direct and indirect effects on cardiovascular functions, and women have been found to be more susceptible to QT prolongation than men. Although many clinical studies have been performed, the effects of steroids on cardiac repolarization are not yet fully understood. We examined the effects of 17-beta-estradiol (estradiol...
Article
Full-text available
A functional cell-based assay was developed using a generic proprietary assay protocol, based on a membrane-potential sensitive dye, for the identification of small-molecule antagonists against the Kv1.3 potassium ion channel. A high-throughput screen (HTS) was subsequently performed with 20,000 compounds from the Evotec library, preselected using...
Article
Within the past few years, the high-throughput screening (HTS) of compounds targeting cardiac ion channels has been primarily focused on the testing of the HERG channel, which is involved in the termination of cardiac action potential. Interaction of drugs with this channel may induce QT interval prolongation and cardiac arrhythmia. These undesirab...
Article
We present a microfluidic device for the immobilization and electrical measurements, such as patch-clamp or impedance measurements, on individual living cells. Micron-sized hollow SiO2 nozzles are realized in Si wafers using a deep plasma etching process. The micronozzles are integrated with glass wafers containing microfluidic channels and Ag/AgCl...
Article
This paper describes the development of a patch-clamp microsystem for a possible automation of high-throughput drug screening. The system is based on 3-dimensional SiO2 micro-nozzles integrated into a fluidic device. Positioning of living cells by suction is demonstrated. A clear increase of the electrical resistance is observed when a cell is atta...
Article
The late detection of cardiotoxic side effects, such as QT prolongation, induced by compounds of pharmacological interest can dramatically impede drug discovery and development projects, and consequently increase their cost. The launch of new drugs with undetected cardiotoxic side effects could have hazardous consequences and could trigger lethal c...
Article
Untersuchungen zum Wirkmechanismus des neuen Antikonvulsivums Retigabin /Interaktion mit GABAerger und glutamaterger Neurotransmission und mit spannungsabhängigen Ionenkanälen Retigabin (N-(2-Amino-4-(4-fluorobenzylamino)phenyl)carbaminsäure-ethylester, CAS 150812-12-7,D-23129) ist ein neues Antikonvulsivum, das zur Zeit klinisch in der Phase II un...
Article
Retigabine (N-(2-amino-4-(4-fluorobenzylamino)phenyl carbamic acid ethyl ester, CAS 150812-12-7, D-23129) is a novel anticonvulsant currently undergoing phase II clinical trials. The compound was shown to possess broad spectrum and potent anticonvulsant properties both in vitro and in vivo. The mechanism of action of this drug is currently not full...
Article
We have investigated the effects of four fluoroquinolones on the human ether-à-go-go-related gene (HERG) mediated K(+) currents to evaluate their potential to induce QT-prolongation. HERG currents were measured from stably transfected Chinese hamster ovary (CHO) cells by means of the patch-clamp technique. Bath application of sparfloxacin, moxiflox...
Article
A second mammalian gene for the ether-à-go-go (eag) potassium channel has been cloned from the rat, and its predicted protein sequence is 70% identical to that of rat ether-à-go-go1 with a further 10% conservatively replaced residues. The rat eag2 mRNA was predominantly expressed in neural tissue and was not detected in adult skeletal, cardiac, or...
Article
Retigabine (D-23129) is a novel antiepileptic compound with broad spectrum and potent anticonvulsant properties, both in vitro and in vivo. The compound was shown to activate a K(+) current in neuronal cells. The pharmacology of the induced current displays concordance with the published pharmacology of the M-channel, which recently was correlated...
Article
We have cloned and functionally expressed Kv6.2, a new member of the Kv6 subfamily of voltage-gated potassium channel subunits. The human Kv6.2 (KCNF2) gene was mapped at 18q22-18q23. Kv6.2 mRNA is preferentially expressed in rat and human myocard. Rat and human Kv6.2 subunits appear to be unable to form functional Kv channels in a heterologous exp...
Article
Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2 were expressed in Xenopus oocytes in a functionally active form. At all subunit combinations, AWD 131-138 dose-dependently stimulated GABA currents. At 10 microM AWD 1...
Article
Full-text available
High doses of dextromethorphan (20-42 mg/kg/day) were given to four critically ill children with seizures and frequent epileptiform abnormalities in the EEG that were refractory to antiepileptic drugs. Their acute diseases (hypoxia, head trauma and hypoxia, neurodegenerative disease, hypoglycaemia) were thought to be due in part to N-methyl-D-aspar...
Article
Full-text available
The barium current through voltage-dependent calcium channels was recorded from cultured rat cortical neurons with the whole-cell configuration of the patch-clamp technique. The maximal current evoked by depolarising pulses from -80 mV to 0 mV was divided into inactivating and non-inactivating fractions. During the first minutes of whole-cell recor...
Article
Dextromethorphan is a dextrorotary morphinan without affinity for opioid receptors, commonly used as an antitussive medication. During the past 5 years, interest in the compound and its demethylated derivative, dextrorphan, has been revived because additional neuroprotective and antiepileptic properties were found in in vitro studies, animal experi...
Article
The effect of dextromethorphan on several types of cation currents in cultured rat cortical neurons and PC12 cells was studied by using the whole-cell configuration of the patch-clamp technique. The Ba2+ current through L- and N-type Ca2+ channels was blocked with similar potencies (52-71 microM) in both types of cells. The effect was not voltage-d...
Article
(1) The anticonvulsant effects of memantine were examined and compared with those of baclofen in monolayer primary cultures of murine nerve cells using conventional intracellular recordings. (2) Memantine and baclofen (each 10-100 microM) decreased spontaneous synaptic activity when action potential frequencies exceeded 6 Hz. Neurons firing action...

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