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Padsevonil
Padsevonil (, , ; developmental code name UCB-0942) is a synaptic vesicle glycoprotein 2A (SV2A) ligand which is under development for the treatment of epilepsy. It is much more potent than earlier SV2A ligands like levetiracetam and brivaracetam. However, in contrast to its predecessors, padsevonil's chemical structure has been modified such that it is no longer a racetam. In addition, padsevonil also interacts with synaptic vesicle glycoprotein 2B (SV2B) and 2C (SV2C). The drug is being developed by UCB. As of November 2023, it is in phase 2 clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...s. References Anticonvulsants Chloroarenes Experimental drugs Fluoroarenes Ketones Pyrrolidines Synaptic vesicle glycoprotein ligands Trifluoromethyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synaptic Vesicle Glycoprotein 2A
Synaptic vesicle glycoprotein 2A (SV2A) is a transmembrane protein belonging to a family of keratan sulfate proteoglycans, located on the synaptic vesicles of mammalian neuronal and endocrine cells. It's encoded by the ''SV2A'' gene. SV2A is the most widely expressed isoform of the SV2 family (which also includes the SV2B and SV2C proteins) found in all brain regions. The role of the SV2 proteins is not well understood, however they are thought to be involved in regulating vesicular processes. The SV2A protein is a target of the anti-epileptic drugs (anticonvulsants) levetiracetam and brivaracetam but it is not clear how these drug affect SV2A activity. Localisation SV2A is differentially expressed in both inhibitory GABAergic and excitatory glutamatergic terminals however it is not expressed in all synapses as was previously thought. There is a slightly stronger colocalisation between SV2A and GABA than glutamate and the association differs across brain regions and changes w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
