Losigamone
Encyclopedia
Losigamone is an investigational drug for the treatment of epilepsy
. It has been studied as an add-on treatment for partial seizures. Phase III clinical trial
s were conducted around the year 2000.
s are inconsistent: it increases GABA-induced chloride influx in spinal cord
neuron cultures, but has no significant influence on GABAergic inhibitory postsynaptic potential
s in hippocampal slices. Interaction with potassium
and sodium channels has been proposed. Results from both in vitro
and in vivo
experiments confirm that the pharmacological activity profiles of the two losigamone enantiomer
s are not identical and suggest further that excitatory amino acid-mediated processes are involved in the mode of action of (+)-losigamone (the compound shown in the image) whereas (–)-losigamone does not possess such properties.
Epilepsy
Epilepsy is a common chronic neurological disorder characterized by seizures. These seizures are transient signs and/or symptoms of abnormal, excessive or hypersynchronous neuronal activity in the brain.About 50 million people worldwide have epilepsy, and nearly two out of every three new cases...
. It has been studied as an add-on treatment for partial seizures. Phase III clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s were conducted around the year 2000.
Mechanism of action
The mechanism of action is not known. Data regarding the interaction of losigamone with GABA receptorGABA receptor
The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid , the chief inhibitory neurotransmitter in the vertebrate central nervous system...
s are inconsistent: it increases GABA-induced chloride influx in spinal cord
Spinal cord
The spinal cord is a long, thin, tubular bundle of nervous tissue and support cells that extends from the brain . The brain and spinal cord together make up the central nervous system...
neuron cultures, but has no significant influence on GABAergic inhibitory postsynaptic potential
Postsynaptic potential
Postsynaptic potentials are changes in the membrane potential of the postsynaptic terminal of a chemical synapse. Postsynaptic potentials are graded potentials, and should not be confused with action potentials although their function is to initiate or inhibit action potentials...
s in hippocampal slices. Interaction with potassium
Potassium channel
In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. They form potassium-selective pores that span cell membranes...
and sodium channels has been proposed. Results from both in vitro
In vitro
In vitro refers to studies in experimental biology that are conducted using components of an organism that have been isolated from their usual biological context in order to permit a more detailed or more convenient analysis than can be done with whole organisms. Colloquially, these experiments...
and in vivo
In vivo
In vivo is experimentation using a whole, living organism as opposed to a partial or dead organism, or an in vitro controlled environment. Animal testing and clinical trials are two forms of in vivo research...
experiments confirm that the pharmacological activity profiles of the two losigamone enantiomer
Enantiomer
In chemistry, an enantiomer is one of two stereoisomers that are mirror images of each other that are non-superposable , much as one's left and right hands are the same except for opposite orientation. It can be clearly understood if you try to place your hands one over the other without...
s are not identical and suggest further that excitatory amino acid-mediated processes are involved in the mode of action of (+)-losigamone (the compound shown in the image) whereas (–)-losigamone does not possess such properties.