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Identification
NameBL-1020
Accession NumberDB05687
TypeSmall Molecule
GroupsInvestigational
DescriptionBL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine).
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationInvestigated for use/treatment in schizophrenia and schizoaffective disorders.
Structured Indications Not Available
PharmacodynamicsExtensive 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 actionIn 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).
TargetKindPharmacological actionActionsOrganismUniProt ID
D(2) dopamine receptorProteinunknownNot AvailableHumanP14416 details
5-hydroxytryptamine receptor 2AProteinunknownNot AvailableHumanP28223 details
Related Articles
AbsorptionOrally available.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

BL-1020, after oral administration, crosses the blood brain barrier intact and is metabolized to GABA and perphenazine.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
5'-Deoxy-5'-MethylthioadenosineThe serum concentration of BL-1020 can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine.Experimental
AcebutololBL-1020 may increase the hypotensive activities of Acebutolol.Approved
AlfentanilBL-1020 may increase the hypotensive activities of Alfentanil.Approved, Illicit
AlphacetylmethadolBL-1020 may increase the hypotensive activities of Alphacetylmethadol.Experimental, Illicit
AlprenololBL-1020 may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminum phosphateAluminum phosphate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AmodiaquineThe serum concentration of BL-1020 can be increased when it is combined with Amodiaquine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Amoxapine.Approved
Aop200704BL-1020 may increase the hypotensive activities of Aop200704.Investigational
ArotinololBL-1020 may increase the hypotensive activities of Arotinolol.Approved
ArtemetherThe serum concentration of BL-1020 can be increased when it is combined with Artemether.Approved
ArtemisininThe serum concentration of BL-1020 can be increased when it is combined with Artemisinin.Investigational
ArtesunateThe serum concentration of BL-1020 can be increased when it is combined with Artesunate.Approved
AtenololBL-1020 may increase the hypotensive activities of Atenolol.Approved
AtovaquoneThe serum concentration of BL-1020 can be increased when it is combined with Atovaquone.Approved
BefunololBL-1020 may increase the hypotensive activities of Befunolol.Experimental
BetaxololBL-1020 may increase the hypotensive activities of Betaxolol.Approved
Betulinic AcidThe serum concentration of BL-1020 can be increased when it is combined with Betulinic Acid.Investigational
BevantololBL-1020 may increase the hypotensive activities of Bevantolol.Approved
BezitramideBL-1020 may increase the hypotensive activities of Bezitramide.Experimental, Illicit, Withdrawn
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
BisoprololBL-1020 may increase the hypotensive activities of Bisoprolol.Approved
BopindololBL-1020 may increase the hypotensive activities of Bopindolol.Approved
BucindololBL-1020 may increase the hypotensive activities of Bucindolol.Investigational
BufuralolBL-1020 may increase the hypotensive activities of Bufuralol.Experimental, Investigational
BupranololBL-1020 may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineBL-1020 may increase the hypotensive activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolBL-1020 may increase the hypotensive activities of Butorphanol.Approved, Illicit, Vet Approved
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CarfentanilBL-1020 may increase the hypotensive activities of Carfentanil.Illicit, Vet Approved
CarteololBL-1020 may increase the hypotensive activities of Carteolol.Approved
CarvedilolBL-1020 may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololBL-1020 may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of BL-1020 can be increased when it is combined with Chloroquine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when BL-1020 is combined with Citalopram.Approved
ClomipramineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Clomipramine.Approved, Vet Approved
CodeineBL-1020 may increase the hypotensive activities of Codeine.Approved, Illicit
DapoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Dapoxetine.Investigational
DapsoneThe serum concentration of BL-1020 can be increased when it is combined with Dapsone.Approved, Investigational
DextromoramideBL-1020 may increase the hypotensive activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneBL-1020 may increase the hypotensive activities of Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineBL-1020 may increase the hypotensive activities of Dezocine.Approved
DihydroartemisininThe serum concentration of BL-1020 can be increased when it is combined with Dihydroartemisinin.Approved
DihydrocodeineBL-1020 may increase the hypotensive activities of Dihydrocodeine.Approved, Illicit
DihydroetorphineBL-1020 may increase the hypotensive activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineBL-1020 may increase the hypotensive activities of Dihydromorphine.Experimental, Illicit
DiphenoxylateBL-1020 may increase the hypotensive activities of Diphenoxylate.Approved, Illicit
DoxycyclineThe serum concentration of BL-1020 can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEBL-1020 may increase the hypotensive activities of DPDPE.Investigational
EscitalopramThe risk or severity of adverse effects can be increased when BL-1020 is combined with Escitalopram.Approved, Investigational
EsmololBL-1020 may increase the hypotensive activities of Esmolol.Approved
EthylmorphineBL-1020 may increase the hypotensive activities of Ethylmorphine.Approved, Illicit
EtoperidoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Etoperidone.Approved
EtorphineBL-1020 may increase the hypotensive activities of Etorphine.Illicit, Vet Approved
FenfluramineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fenfluramine.Illicit, Withdrawn
FentanylBL-1020 may increase the hypotensive activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fluvoxamine.Approved, Investigational
HalofantrineThe serum concentration of BL-1020 can be increased when it is combined with Halofantrine.Approved
HeroinBL-1020 may increase the hypotensive activities of Heroin.Approved, Illicit
HydrocodoneBL-1020 may increase the hypotensive activities of Hydrocodone.Approved, Illicit
HydromorphoneBL-1020 may increase the hypotensive activities of Hydromorphone.Approved, Illicit
HydroxychloroquineThe serum concentration of BL-1020 can be increased when it is combined with Hydroxychloroquine.Approved
IndalpineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Indalpine.Investigational, Withdrawn
IndenololBL-1020 may increase the hypotensive activities of Indenolol.Withdrawn
KetobemidoneBL-1020 may increase the hypotensive activities of Ketobemidone.Approved
LabetalolBL-1020 may increase the hypotensive activities of Labetalol.Approved
LevobunololBL-1020 may increase the hypotensive activities of Levobunolol.Approved
Levomethadyl AcetateBL-1020 may increase the hypotensive activities of Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when BL-1020 is combined with Levomilnacipran.Approved
LevorphanolBL-1020 may increase the hypotensive activities of Levorphanol.Approved
LofentanilBL-1020 may increase the hypotensive activities of Lofentanil.Illicit
Lu AA21004The risk or severity of adverse effects can be increased when BL-1020 is combined with Lu AA21004.Investigational
LumefantrineThe serum concentration of BL-1020 can be increased when it is combined with Lumefantrine.Approved
MagaldrateMagaldrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Withdrawn
Magnesium carbonateMagnesium carbonate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MefloquineThe serum concentration of BL-1020 can be increased when it is combined with Mefloquine.Approved
MethadoneBL-1020 may increase the hypotensive activities of Methadone.Approved
Methadyl AcetateBL-1020 may increase the hypotensive activities of Methadyl Acetate.Approved, Illicit
MetipranololBL-1020 may increase the hypotensive activities of Metipranolol.Approved
MetoprololBL-1020 may increase the hypotensive activities of Metoprolol.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when BL-1020 is combined with Milnacipran.Approved
MizoribineThe serum concentration of BL-1020 can be increased when it is combined with Mizoribine.Investigational
MorphineBL-1020 may increase the hypotensive activities of Morphine.Approved, Investigational
NadololBL-1020 may increase the hypotensive activities of Nadolol.Approved
NalbuphineBL-1020 may increase the hypotensive activities of Nalbuphine.Approved
NormethadoneBL-1020 may increase the hypotensive activities of Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Olanzapine.Approved, Investigational
OpiumBL-1020 may increase the hypotensive activities of Opium.Approved, Illicit
OxprenololBL-1020 may increase the hypotensive activities of Oxprenolol.Approved
OxycodoneBL-1020 may increase the hypotensive activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneBL-1020 may increase the hypotensive activities of Oxymorphone.Approved, Investigational, Vet Approved
ParoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Paroxetine.Approved, Investigational
PenbutololBL-1020 may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineBL-1020 may increase the hypotensive activities of Pentazocine.Approved, Vet Approved
PethidineBL-1020 may increase the hypotensive activities of Pethidine.Approved
PindololBL-1020 may increase the hypotensive activities of Pindolol.Approved
PiritramideBL-1020 may increase the hypotensive activities of Piritramide.Investigational
PractololBL-1020 may increase the hypotensive activities of Practolol.Approved
PrimaquineThe serum concentration of BL-1020 can be increased when it is combined with Primaquine.Approved
ProguanilThe serum concentration of BL-1020 can be increased when it is combined with Proguanil.Approved
PropranololBL-1020 may increase the hypotensive activities of Propranolol.Approved, Investigational
PyrimethamineThe serum concentration of BL-1020 can be increased when it is combined with Pyrimethamine.Approved, Vet Approved
PyronaridineThe serum concentration of BL-1020 can be increased when it is combined with Pyronaridine.Investigational
QuinacrineThe serum concentration of BL-1020 can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of BL-1020 can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of BL-1020 can be increased when it is combined with Quinine.Approved
RadicicolThe serum concentration of BL-1020 can be increased when it is combined with Radicicol.Experimental
RemifentanilBL-1020 may increase the hypotensive activities of Remifentanil.Approved
SertralineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Sertraline.Approved
SinefunginThe serum concentration of BL-1020 can be increased when it is combined with Sinefungin.Experimental
SotalolBL-1020 may increase the hypotensive activities of Sotalol.Approved
SufentanilBL-1020 may increase the hypotensive activities of Sufentanil.Approved, Investigational
SulfadoxineThe serum concentration of BL-1020 can be increased when it is combined with Sulfadoxine.Approved
SulfametopyrazineThe serum concentration of BL-1020 can be increased when it is combined with Sulfametopyrazine.Approved, Withdrawn
tafenoquineThe serum concentration of BL-1020 can be increased when it is combined with tafenoquine.Investigational
TapentadolBL-1020 may increase the hypotensive activities of Tapentadol.Approved
ThiopentalThe risk or severity of adverse effects can be increased when BL-1020 is combined with Thiopental.Approved, Vet Approved
TimololBL-1020 may increase the hypotensive activities of Timolol.Approved
TramadolBL-1020 may increase the hypotensive activities of Tramadol.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Trazodone.Approved, Investigational
TrimethoprimThe serum concentration of BL-1020 can be increased when it is combined with Trimethoprim.Approved, Vet Approved
VilazodoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Vortioxetine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Zimelidine.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot 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
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
Comments
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Drug created on November 18, 2007 11:27 / Updated on August 17, 2016 12:24