Essay Example on Gabather AB is a Swedish Biotech Company

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INTRODUCTION Gabather AB is a Swedish Biotech Company dedicated for development of novel drug candidates for the treatment of Central nervous system CNS disorders It focuses on four different areas including anti depressants anti psychotics anxiolytics and analgesics It mainly focuses on the potential candidates that interact with Gamma amino butyric acid GABA It has developed a highly potent novel lead compound GT 002 by focusing on the area of antipsychotics that is known to target and bind with GABAA receptor and cause a behavioural effect 12 1 1 GABA Gamma Aminobutyric Acid GABA is an amino acid of the central nervous system CNS The chemical formula of GABA is C4H9NO2 1 It is the most potent depressive neuro amine in mammalian brain tissues It is synthesised from glutamate a human brain cortex excitatory neurotransmitter by glutamate decarboxylase enzyme 2 4 Whereas GABA is the main inhibitory neurotransmitter in human brain and activates many receptor subtypes in mammalian central nervous system It mainly targets the ionotropic transmembrane GABAA receptor thereby inhibiting the neurotransmission 

The effect of GABA is modulated by the modulators of GABAA receptor by binding to the allosteric sites which are the common drug targets 3 The Chemical formula of Gamma amino butyric acid GABA The GABA is one of the key neurotransmitters involved in the anxiolytic action of many drugs used to treat anxiety disorders by counterbalancing the action of glutamate excitatory neurotransmitter Novel GABAergic agents such as tiagabine modulate the overall effect of GABA system and thereby used in the treatment of anxiety disorders 5 Anxiety disorders are usually due to mixture of feelings such as worry and fear



They are a group of mental illness due to anxiety which is a frequent negative emotional state characterised by feelings of worry fear accompanied by cognitive somatic and behavioural manifestations 6 1 2 GABA RECEPTORS The postsynaptic GABA receptors are classified as GABAA GABAB and GABAC receptors which are identified pharmacologically or electro physiologically in all the brain regions GABAA receptor is the important molecular target for the action of several drugs in the brain GABAA and GABAC receptors are ionotropic and are a part of Cl channel macromolecular complex which upon activation of neurotransmitters results in an augmented Cl conductance GABAB receptors are always inhibitory metabotropic and are coupled to G proteins which upon activation the intracellular levels of second messengers will increase 7 1 3 GABAA RECEPTOR GABAA receptors are a ligand gated ion channels responsible for the inhibitory effects of GABA This receptor consists of 6 different alpha subunits 3 different beta subunits 3 different gamma subunits Various combinations of these subunits confer various pharmacological properties among various receptors Upon stimulation GABAA receptors results in increased permeability to Cl raising the postsynaptic membrane threshold potential inhibitory 3 GABAA receptor showing its subunits Crystal structure of GABAA receptor in humans The current project mainly focused upon GABAA receptor as it is the target for various GABA modulatory substances such as benzodiazepines BZ which are widely used in the treatment of anxiety disorders Benzodiazepines are the class of psychoactive drugs with a combination of benzene diazepine ring and enhance the effect of GABA at the GABAA receptor resulting in sedative hypnotic anxiolytic properties This project characterized the binding of the lead compound GT 002 as well as benzodiazepine BZ antagonist 



Flumazenil to GABAA receptor in porcine brain tissue samples through validation of a radioligand binding assay using the pharmaceutical excipient Labrasol The binding of GT 002 and flumazenil to GABAA receptor originating from porcine brain tissue will be characterized using radioligand binding assays Both the lead GT 002 and validating compound flumazenil has been tritium labelled 3H GT 002 and 3H FLU to perform radioligand binding assay 1 4 RADIOLIGAND BINDING ASSAY It is basically used to measure the receptor ligand binding interactions using radioactive labelling of the ligand This technique mainly focuses upon measuring of the radioactive decay for detection of radio isotopic labelled ligand interaction to a specific receptor The assays could be either homogeneous doesn't need separation of free fraction of ligand prior to measurement of receptor ligand binding or heterogenous requires separation of free fraction of ligands before measuring the receptor ligand binding 8 The heterogenous radioligand binding filtration assay is being performed in this project In this assay as discussed above a free ligand is separated from bound fraction through a filtration step There are 4 major experiments for a basic radio ligand assay including saturation tissue binding kinetic and displacement 9 The current project focus upon comparative evaluation among the lead compound GT 002 and validating compound flumazenil to determine the receptor ligand binding 1 5 DISPLACEMENT STUDIES The displacement experiments are focused upon the competition between labrasol and a radioactively labelled ligand GT 002 FLU to a certain receptor GABA Because of these assays displacement graphs with curves can be constructed when the radioactively labelled ligand and receptor concentration are kept constant 10



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