OV101 is a delta-selective GABAA receptor
agonist that targets the disruption of tonic inhibition, a central physiological process of the brain that is thought to be the underlying cause of Fragile X syndrome and other neurodevelopmental disorders.
OVIOI, a delta (d)-selective GABAA receptor
agonist, is believed to be the first investigational drug to target the disruption of tonic inhibition, a key mechanism that allows the brain to decipher excitatory and inhibitory neurological signals correctly without being overloaded.
Karolinska Development's (KDEV) portfolio company Umecrine Cognition AB, whose novel orally-active GABAA receptor
modulating steroid, GR3027, is in clinical development for hepatic encephalopathy (HE), will present clinical results from its Phase 1 study at The International Liver CongressTM 2017, the annual meeting of the European Association for the Study of the Liver, being held April 19-23, 2017, in Amsterdam, The Netherlands.
The company said the dosing of SAGE-217, which is a novel, internally-developed, next generation oral GABAA receptor
modulator, has been initiated in the first of two movement disorder indications.
Studies have reported the modulation of GABAA receptor
function by flavonoids [51, 52], which can explains that the anti- nociceptive activity of the active extract and its fractions might be due to its modulatory activity of GABAA receptor
, since GABA is an inhibitory pathway which also controls the transmission of nociceptive signals.
antagonism in the extended amygdala decreases ethanol self-administration in rats, European Journal of Pharmacology 283(1-3):151-159, 1995.
Prediction of GABAA receptor
proteins using the concept of Chou's pseudoaminoacid composition and support vector machine.
Even if the majority of studies suggest a direct allosteric modulation of the GABAA receptor
by ethanol, phosphorylation/ dephosphorylation mechanisms also seem to be important in the receptor modulation (Ravindran & Ticku, 2006).
The pressor effect of BMI as well as insignificant response to muscimol injections implies that there should be a tonic release of GABA inhibiting the cardiovascular function via GABAA receptor
Epileptiform activity recordings: Artificial cerebro spinal fluid (ASCF) containing the GABAa receptor
blocker picrotoxin (100 [micro]M) was bath applied and the same was used in electrodes.
As a benzodiazepine, alprazolam exerts its pharmacological actions by binding to the GABAA receptor
in the central nervous system and potentiating its neuroinhibitory effects.
34) Reorganisation of the GABAa receptor
subunits may lead to hypersensitivity of the receptor to neurosteroids.