NAV

YKP-1358

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
YKP-1358
DrugBank Accession Number
DB06109
Background

YKP1358 is a novel serotonin (5-HT2A) and dopamine (D2) antagonist that has demonstrated potent activity in animals that relates to both positive and negative symptoms of schizophrenia. In addition, the YKP1358 pharmacological profile suggests a very low potential for extrapyramidal side effects.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
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Pharmacology

Indication

Investigated for use/treatment in schizophrenia and schizoaffective disorders.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

serotonin (5-HT2A) and dopamine (D2) antagonist.

TargetActionsOrganism
U5-hydroxytryptamine receptor 2ANot AvailableHumans
UDopamine D2 receptor
antagonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when YKP-1358 is combined with 1,2-Benzodiazepine.
AcenocoumarolThe risk or severity of adverse effects can be increased when YKP-1358 is combined with Acenocoumarol.
AcetazolamideThe risk or severity of CNS depression can be increased when Acetazolamide is combined with YKP-1358.
AcetophenazineThe risk or severity of CNS depression can be increased when Acetophenazine is combined with YKP-1358.
AgomelatineThe risk or severity of CNS depression can be increased when YKP-1358 is combined with Agomelatine.
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Lim KS, Kwon JS, Jang IJ, Jeong JM, Lee JS, Kim HW, Kang WJ, Kim JR, Cho JY, Kim E, Yoo SY, Shin SG, Yu KS: Modeling of brain D2 receptor occupancy-plasma concentration relationships with a novel antipsychotic, YKP1358, using serial PET scans in healthy volunteers. Clin Pharmacol Ther. 2007 Feb;81(2):252-8. [Article]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Details1. 5-hydroxytryptamine receptor 2A
Kind
Protein
Organism
Humans
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
Details2. Dopamine D2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
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
References
  1. Lim KS, Kwon JS, Jang IJ, Jeong JM, Lee JS, Kim HW, Kang WJ, Kim JR, Cho JY, Kim E, Yoo SY, Shin SG, Yu KS: Modeling of brain D2 receptor occupancy-plasma concentration relationships with a novel antipsychotic, YKP1358, using serial PET scans in healthy volunteers. Clin Pharmacol Ther. 2007 Feb;81(2):252-8. [Article]

Drug created at November 18, 2007 18:30 / Updated at June 12, 2020 16:52