9 results about "Antiepileptic Agents" patented technology

A genetically-modified rat having a PKHD1L1 gene with a point or other mutation and a construction method thereof are disclosed. A CRISPR / Cas9 system knocks the PKHD1L1 gene into a rat source, and a codon changes from TTA to TCA to construct the mutant PKHD1L1 gene. The genetically-modified rat can be applied to epilepsy pathogenesis studies and design and testing of new anti-epileptic drugs. Methods for detecting abnormal cortical excitability and detecting an epileptic phenotype of an animal can use the genetically-modified rat. A somatosensory evoked potential is used to detect whether the genetically-modified rat has an abnormal cortical excitability phenotype, so as to confirm whether the rat can be a successful model for testing anti-epileptic drugs. The method can detect abnormal cortical excitability and verify the effectiveness of anti-epileptic drugs or treatments.

This invention discloses a glutamate-responsive nanoliposome, its preparation method, and its application in antiepileptic treatment. The glutamate-responsive nanoliposome comprises liposomes, glutamate oxidase, DSPE-TK-mPEG, and an antiepileptic drug. The glutamate oxidase is encapsulated in the hydrophilic region at the center of the liposome, the antiepileptic drug is loaded in the hydrophobic region of the liposome bilayer, and DSPE-TK-mPEG is modified onto the liposome bilayer membrane. The preparation method includes: first preparing a lipid solution, adding an antiepileptic drug solution and glutamate oxidase, and obtaining drug-loaded nanoliposomes through repeated extrusion. The glutamate-responsive drug-releasing nanoliposomes of this invention can significantly improve the stability and bioavailability of antiepileptic drugs, overcoming the shortcomings of traditional antiepileptic drugs in the treatment process. By optimizing the preparation of liposomes, a good drug delivery platform for antiepileptic drugs is provided.

Disclosed is a method of administering a Kv7 channel activator, or a pharmaceutically acceptable salt thereof, to a human without developing adverse events typically associated with antiepileptic drugs in the human. Also disclosed is a method of treating a medical condition in a patient without developing an adverse event typically associated with an antiepileptic drug, the method comprising administering to the patient in need of such treatment a therapeutically effective amount of a Kv7 channel activator or a pharmaceutically acceptable salt thereof.

The invention relates to the technical field of treatment drug monitoring, in particular to a method for simultaneously determining the concentration of multiple antiepileptic drugs in plasma. Comprising the following steps: S1, preparing a standard working solution; s2, preparing an internal standard solution; s3, mixing the standard working solution with blank plasma, adding an internal standard solution, centrifuging, and detecting to obtain a chromatogram of a standard solution; s4, based on the chromatogram, taking the ratio of the peak area of the anti-epileptic drug to the peak area of the corresponding internal standard substance as a vertical coordinate Y, taking the ratio of the concentration of the anti-epileptic drug to the concentration of the corresponding internal standard substance as a horizontal coordinate X, and fitting to obtain a standard curve equation; s5, preparing a plurality of groups of quality control working solutions, and verifying the standard curve equation obtained in the step S4; and S6, uniformly mixing the blood to be detected with the internal standard solution, centrifuging, detecting the supernate, and calculating the concentration of the antiepileptic drug in the plasma. The method can realize simultaneous, accurate and quantitative detection of multiple antiepileptic drugs in blood.

A genetically-modified rat having a PKHD1L1 gene with a point or other mutation and a construction method thereof are disclosed. A CRISPR / Cas9 system knocks the PKHD1L1 gene into a rat source, and a codon changes from TTA to TCA to construct the mutant PKHD1L1 gene. The genetically-modified rat can be applied to epilepsy pathogenesis studies and design and testing of new anti-epileptic drugs. Methods for detecting abnormal cortical excitability and detecting an epileptic phenotype of an animal can use the genetically-modified rat. A somatosensory evoked potential is used to detect whether the genetically-modified rat has an abnormal cortical excitability phenotype, so as to confirm whether the rat can be a successful model for testing anti-epileptic drugs. The method can detect abnormal cortical excitability and verify the effectiveness of anti-epileptic drugs or treatments.

This application relates to the field of analytical detection technology, specifically to sample pretreatment methods, kits, and detection methods for the detection of antiepileptic drugs. The sample pretreatment method for the detection of antiepileptic drugs in this application includes one or more of the following antiepileptic drugs: valproic acid, carbamazepine, phenytoin, levetiracetam, lamotrigine, and phenobarbital. The sample pretreatment method includes the following steps: mixing magnetic beads with an activation solution to prepare a magnetic bead suspension; mixing the sample to be tested, the magnetic bead suspension, and an internal standard solution, and separating the supernatant and the magnetic bead complex after magnetic adsorption treatment; adding an eluent to the magnetic bead complex, and collecting the magnetic bead-target complex after elution treatment; adding an elution buffer to the magnetic bead-target complex, and collecting the supernatant after elution treatment for detection. The above sample pretreatment method is simple to operate, time-saving, and low-cost, providing key technical support for the efficient quantitative detection of antiepileptic drugs.

The invention relates to the technical field of antiepileptic drugs, in particular to a sulfur-containing piperidine ether aryl derivative as well as a preparation method and application thereof, and the structural general formula of the sulfur-containing piperidine ether aryl derivative is as shown in formula (I), in the formula (I), R is selected from H, 2-Cl, 3-Cl and 4-Cl; n = 1 or 2. The sulfur-containing piperidine ether aryl derivative provided by the invention has remarkable histamine H3 receptor antagonistic activity and shows an anti-convulsion characteristic, so that the sulfur-containing piperidine ether aryl derivative can be used as an anti-epileptic compound.

The invention belongs to the technical field of biological medicine, and particularly relates to preparation of a novel high-selectivity KV7.2 opener and application of the novel high-selectivity KV7.2 opener in antiepileptic drugs. A series of KV7.2-targeted small-molecule inhibitors are designed and synthesized, and the small-molecule inhibitors can enhance the current of a potassium ion channel KV7.2, accelerate channel activation and delay the inactivation process of the channel. The small molecule has a remarkable potential for treating epilepsy, shows efficient anti-epileptic activity in three classic epilepsy models for simulating human comprehensive attack and drug-refractory focal attack, is remarkably superior to positive control RTG, can be used for preparing anti-epileptic drugs and has a wide application prospect.