WO2025262072 - NEURONAL DRUG SCREENING METHOD AND NEW APPLICATIONS FOR DILAZEP AND PENBUTOLOL

National phase entry is expected:
Publication Number WO/2025/262072
Publication Date 26.12.2025
International Application No. PCT/EP2025/066963
International Filing Date 17.06.2025
Title **
[English] NEURONAL DRUG SCREENING METHOD AND NEW APPLICATIONS FOR DILAZEP AND PENBUTOLOL
[French] PROCÉDÉ DE CRIBLAGE DE MÉDICAMENT NEURONAL ET NOUVELLES APPLICATIONS POUR DILAZEP ET PENBUTOLOL
Applicants **
MIĘDZYNARODOWY INSTYTUT BIOLOGII MOLEKULARNEJ I KOMÓRKOWEJ
INSTYTUT BIOLOGII DOŚWIADCZALNEJ IM. MARCELEGO NENCKIEGO POLSKIEJ AKADEMII NAUK
INSTYTUT FARMAKOLOGII IM. JERZEGO MAJA POLSKIEJ AKADEMII NAUK
Inventors
MLOSTEK, Magdalena
URBAŃSKA, Małgorzata
JAWORSKI, Jacek
KNAPSKA, Ewelina
MEYZA, Ksenia
BOGUSZEWSKI, Paweł
HAMED, Adam
SZEWCZYK, Bernadeta
POCHWAT, Bartłomiej
Priority Data
P.448932   21.06.2024   PL
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting1902
EPO Filing, Examination, Granting8163
Japan Filing, Examination, Granting1892
South Korea Filing, Examination, Granting1499
USA Filing, Examination, Granting5940
MasterCard Visa
Total: 19,396
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Abstract[English] The present invention relates to the field of drug development and neuropharmacology. One aspect of this invention involves a method for screening substances that increase the stability of excitatory synaptic connections under destabilizing conditions. This method entails exposing a tested compound to an in vitro differentiated neuron culture along with a destabilization compound, followed by incubation with the test compound. Subsequently, a postsynaptic parameter is measured in the neurons, and this measurement is compared to that of neurons not exposed to the tested substance. This high-content screening system represents a significant advancement in neuropharmacology and drug discovery, offering automated and high-throughput capabilities for assessing the effects of chemical compounds on neuronal connections in vitro. Another aspect of the invention pertains to the use of dilazep, penbutolol, and their salts for alleviating and treating symptoms associated with depressive disorders.[French] La présente invention concerne le domaine de la mise au point de médicaments et de la neuropharmacologie. Un aspect de la présente invention concerne un procédé de criblage de substances qui augmentent la stabilité de connexions synaptiques excitatrices dans des conditions de déstabilisation. Ce procédé consiste à exposer un composé testé à une culture de neurones différenciés in vitro conjointement avec un composé de déstabilisation, suivi d'une incubation avec le composé de test. Ensuite, un paramètre post-synaptique est mesuré dans les neurones, et cette mesure est comparée à celle de neurones non exposés à la substance testée. Ce système de criblage à haute teneur représente une avancée considérable dans la neuropharmacologie et la découverte de médicaments, offrant des capacités automatisées et à haut débit pour évaluer les effets de composés chimiques sur des connexions neuronales in vitro. Un autre aspect de l'invention concerne l'utilisation de dilazep, de penbutolol, et de leurs sels pour soulager et traiter des symptômes associés à des troubles dépressifs.

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