epilepsy

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Clidinium bromide (Ro 2-3773) , a synthetic anticholinergic agent, has been shown in experimental and clinical researchers to have a pronounced antisecretory and antispasmodic effect on the gastrointestinal tract. It can inhibit muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve cramps or stomach spasms or abdominal due to colicky abdominal diverticulitis, pain, and irritable bowel syndrome.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Divalproex Sodium (Valproate semisodium) binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor, Comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through the inhibition of voltage-sensitive sodium channels.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural compound derived from the roots and rhizomes of Notopterygium incisum.

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) is a potent anticholinergic agent and also have NMDA antagonist properties.

Soticlestat (OV935) is a potent, selective and orally active cholesterol 24-hydroxylase (CYP46A1) inhibitor. It has the potential for epilepsy syndromes research.

TTA-A2 is a selective T-type calcium channel antagonist as a potent anticonvulsant that the Cav3.1 isoform plays a prominent role in mediating. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own).

Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.

Gamibetal (4-Amino-3-hydroxybutyric Acid) is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues. Also used in the preparation of HIV-1 inhibitors derived from Betulinic Acid (B330250).

ML 297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML 297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters.

Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) is the pharmacologically active metabolite of oxcarbazepine, a drug indicated for the treatment of partial seizures and bipolar disorders.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

(S)-(+)-Niguldipine hydrochloride is a selective α1A-AR antagonist used in the study of depression and epilepsy.

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.

Milenperone (R 34009) is a novel anti-invasive compound designed to control behavioral disorders in patients with epilepsy and alcoholism.

ELB-139 is a GABAA receptor agonist that can be used to study depression and epilepsy.

ZTZ240 is a KCNQ2 channel activator used in the study of epilepsy.

E6801 is a novel selective 5-HT6 receptor agonist with a wide range of biological activities.E6801 can be used in the study of dementia, Parkinson's disease, depression, obesity epilepsy, anxiety, and many other diseases.

Elpetrigine (GW273293) is a potential sodium channel blocker with antiepileptic activity that can be used to study epilepsy.