Tìm theo
BL-1020
Thuốc Gốc
Small Molecule
BL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine).
Dược Lực Học : Extensive preclinical testing of BL-1020 has shown it to have a positive safety and pharmacokinetic profile. BL-1020 reduces dopamine activity while avoiding the side affects associated with unmitigated dopamine blockade. In animal models of schizophrenia, BL-1020 reduces behaviors characteristic of psychosis and causes minimal or no impairment of movement, the most severe side effect of classic antipsychotic drugs. Biochemical testing confirms that BL-1020 works via the mechanism previously established for classic antipsychotics. BL-1020 is structurally and mechanistically distinct from the atypical antipsychotics and is not anticipated to trigger diabetes or elevated cholesterol. Preliminary studies do not reveal toxicity.
Cơ Chế Tác Dụng : BL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine). In radioligand binding studies, BL-1020 displayed strong interaction with dopamine receptors especially D2L and D2S (Ki of 0.27 nM and 0.17 nM respectively), the serotonin receptor 5-HY2a (Ki 0.25 nM) as well as moderate interaction with the GABAA receptor (Ki 3.29 microK).
Dược Động Học :
▧ Absorption :
Orally available.
▧ Metabolism :
BL-1020, after oral administration, crosses the blood brain barrier intact and is metabolized to GABA and perphenazine.
Chỉ Định : Investigated for use/treatment in schizophrenia and schizoaffective disorders.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05687
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