BL-1020
Identification
- Name
- BL-1020
- Accession Number
- DB05687
- Type
- Small Molecule
- Groups
- Investigational
- Description
BL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine).
- Synonyms
- Not Available
- Categories
- UNII
- Not Available
- CAS number
- Not Available
- Weight
- Not Available
- Chemical Formula
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in schizophrenia and schizoaffective disorders.
- Pharmacodynamics
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.
- Mechanism of action
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).
Target Actions Organism UD(2) dopamine receptor Not Available Human U5-hydroxytryptamine receptor 2A Not Available Human - Absorption
Orally available.
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
BL-1020, after oral administration, crosses the blood brain barrier intact and is metabolized to GABA and perphenazine.
- Route of elimination
- Not Available
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction 2,5-Dimethoxy-4-ethylamphetamine BL-1020 may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine. 2,5-Dimethoxy-4-ethylthioamphetamine BL-1020 may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine. 3,4-Methylenedioxyamphetamine The risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with BL-1020. 4-Bromo-2,5-dimethoxyamphetamine BL-1020 may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine. Acebutolol The serum concentration of Acebutolol can be increased when it is combined with BL-1020. Acetazolamide The risk or severity of adverse effects can be increased when Acetazolamide is combined with BL-1020. Alaproclate The risk or severity of adverse effects can be increased when BL-1020 is combined with Alaproclate. Alfentanil The risk or severity of hypotension and central nervous system depression can be increased when BL-1020 is combined with Alfentanil. Alimemazine The risk or severity of adverse effects can be increased when Alimemazine is combined with BL-1020. Almasilate Almasilate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. - Food Interactions
- Not Available
References
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Schizoaffective Disorders / Schizophrenic Disorders 1 2 Completed Treatment Schizophrenic Disorders 1 2, 3 Terminated Treatment Cognitive Effect on Schizophrenic Patients / Schizophrenic Disorders 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Taxonomy
- Classification
- Not classified
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
Drug created on November 18, 2007 11:27 / Updated on October 01, 2018 14:02