Epilepsy|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Epilepsy is a group of neurological conditions consisting of recurrent, usually unprovoked epileptic seizures. Epileptic seizures have recently been defined as "a transient occurrence of signs and/or symptoms due to abnormal, excessive or synchronous neuronal activity in the brain". Epilepsy is one of the most common disorders of the brain, with one in 10 people suffering at least one seizure in their lifetime. There are over 40 different types of epilepsy, each of which presents with its own unique combination of seizure type, typical age of onset, EEG findings, treatment, and prognosis.

Epileptogenesis and Seizures

Epileptogenesis is the mechanism by which an epileptic condition is acquired, the critical step of which is neuronal damage. An initial brain-damaging insult triggers a cascade of molecular and cellular changes that ultimately leads to the occurrence of spontaneous and recurrent seizures. The initial insult does not begin the process, but sets into motion a cascade of changes in gene expression that alters the molecular and cellular constituents of neuronal and glial networks. There is often a long latency period, sometimes decades, between initial insult and the first seizure, and such insults include birth trauma, febrile seizures and encephalitis.

Once epileptogenesis has occurred, there are multiple complex mechanisms that trigger recurrent seizures. Simplistically, seizures arise when there is a disruption in the systems that normally control the balance of glutamatergic excitation and GABAergic inhibition. Disturbances can occur through a vast array of mechanisms. Control of the resting potential of neurons is critical to prevent the excessive discharge that is often associated with seizures. The sodium-potassium ATPase is vital in maintaining the resting potential and blockade or mutation of this ion pump can lead to seizures. In order for a seizure to occur, the activity of a network of neurons, not just a single cell, must be altered. Cell synchronization can be achieved through glutamatergic interconnections, gap channels and GABAergic connections. Many of the changes during epileptogenesis promote cell synchronization, and this represents a mechanism by which seizures become recurrent. Environmental changes can trigger seizures, including circadian changes in hormones, peptides and other neuromodulators, stressful life events and visual stimuli. Normally, changes in the above would not trigger seizures, however, in a brain that has already been altered by epileptogenesis, there is an underlying state of increased excitability and these everyday stimuli can have a proconvulsant effect.

Anticonvulsants

Epilepsy can be controlled pharmacologically with anticonvulsant drugs. The main targets of current anticonvulsants include voltage-gated sodium channels, the GABA inhibitory system (including benzodiazepines) and voltage-gated calcium channels. Due to the diverse mechanisms by which seizures occur, epilepsy is refractory to treatment in a number of causes. There is therefore intense research into the development of novel antiepileptic agents.

Cat. No.	Product Name	CAS No.	Information
H8816	Darigabat	1614245-70-3	Darigabat is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials.
H6592	Padsevonil	1294000-61-5	Padsevonil (UCB-0942, UCB0942) is a potential anti-seizure agent that functions as a pre- and post-synaptic inhibitor.
H6448	JNJ-26489112	871824-55-4	JNJ-26489112 (JNJ26489112) is a broad-spectrum anticonvulsant that displays activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures; exhibits very weak inhibition of human CA-II (IC50=35 μM); inhibits Na+, kainate, and KCNQ2 channels to varying degrees, while moderately potentiating GABA current and inhibiting N-methyl-D-aspartic acid current, its action at several targets appears to be responsible for the observed neurostabilizing effects; shows limited seizure spread and elevated seizure threshold in preclinical animal models.
H6235	Cenobamate	913088-80-9	Cenobamate (YKP-3089, YKP3089) is a potential anti-seizure agent with currently unknown mechanisms of action.
H4796	Lacosamide	175481-36-4	An anticonvulsant compound that enhances the slow inactivation of voltage-gated sodium channels without affecting the fast inactivation of voltage-gated sodium channels; launched for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain.
H4686	PF-04895162		PF-04895162 (ICA-105665, PF 4895162) is an orally available agonist of neuronal Kv7 potassium channel, opens Kv7.2/7.3 and Kv7.3/7.5 potassium channels, also known as KCNQ2/3 and KCNQ3/5 channels; ICA-105665 has demonstrated broad spectrum antiseizure activity in multiple animal models including maximal electroshock, 6 Hz seizures, pentylenetetrazole, and electrical kindling at doses from <1 to 5 mg/kg.
H4599	JNJ-55308942	2166558-11-6	JNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM); exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP; possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo.
H4519	SYM-2206	173952-44-8	An allosteric, non-competitive antagonist of the AMPA receptor with IC50 of 2.8 uM; acts allosterically at the same regulatory site as GYKI 52466 and 53655 and other benzodiazepines but does not bind to the central diazepine binding site; shows selectivity for AMPA relative to kainate receptor sub-types.
H4518	Selurampanel	912574-69-7	Selurampanel (BGG 492) is a selective, orally active and competitive AMPA receptor (AMPAR) antagonist with IC50 of 0.19 uM; displays >100-fold selectivity over NMDA and kainate receptors; demonstrates excellent oral potency against MES-induced generalized tonic-clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy.
H4504	Perampanel	380917-97-5	Perampanel (E2007) is a novel, orally active, noncompetitive AMPA receptor (AMPAR) antagonist with IC50 of 93 nM; inhibits AMPA-induced increases in Ca2+(i) with minimal effect on NMDA-induced Ca2+(i); reduces seizure activity in rodent models of epilepsy.

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