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).

TargetActionsOrganism
UD(2) dopamine receptorNot AvailableHuman
U5-hydroxytryptamine receptor 2ANot AvailableHuman
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
DrugInteraction
2,5-Dimethoxy-4-ethylamphetamineBL-1020 may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineBL-1020 may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with BL-1020.
4-Bromo-2,5-dimethoxyamphetamineBL-1020 may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with BL-1020.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with BL-1020.
AlaproclateThe risk or severity of adverse effects can be increased when BL-1020 is combined with Alaproclate.
AlfentanilThe risk or severity of hypotension and central nervous system depression can be increased when BL-1020 is combined with Alfentanil.
AlimemazineThe risk or severity of adverse effects can be increased when Alimemazine is combined with BL-1020.
AlmasilateAlmasilate 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

General References
Not Available
External Links
PubChem Substance
347910192
Wikipedia
BL-1020

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2CompletedTreatmentSchizophrenic Disorders1
2, 3TerminatedTreatmentCognitive Effect on Schizophrenic Patients / Schizophrenic Disorders1

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