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PRX-07034

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

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Data Packages
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Identification

Generic Name
PRX-07034
DrugBank Accession Number
DB05993
Background

Not Available

Type
Small Molecule
Groups
Investigational
Structure
Similar Structures
Weight
Average: 490.44
Monoisotopic: 489.125583
Chemical Formula
C21H29Cl2N3O4S
Synonyms
Not Available
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Pharmacology

Indication

Investigated for use/treatment in alzheimer's disease, obesity, and schizophrenia and schizoaffective disorders.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

PRX-07034 is a novel, highly selective, small-molecule antagonist of a specific G-protein coupled receptor (GPCR) known as 5-HT6 being developed for the treatment of obesity, Alzheimer's disease and cognitive impairment associated with schizophrenia.

PRX-07034 has also been shown to enhance cognitive function in preclinical animal models of memory impairment through a dual mechanism of action.It has an effect on both the acetylcholine and glutamate neurotransmitter systems in the brain, which makes it a potentially complementary therapy to cholinesterase inhibitors, a class of drugs approved for the treatment of Alzheimer's disease.

TargetActionsOrganism
A5-hydroxytryptamine receptor 6
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
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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.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
336H22ETCG
CAS number
903580-39-2
InChI Key
PILCQJJJAFRKHO-UHFFFAOYSA-N
InChI
InChI=1S/C21H28ClN3O4S.ClH/c1-14(17-11-15(22)12-19(28-2)21(17)29-3)24-18-13-16(25-9-7-23-8-10-25)5-6-20(18)30(4,26)27;/h5-6,11-14,23-24H,7-10H2,1-4H3;1H
IUPAC Name
N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methanesulfonyl-5-(piperazin-1-yl)aniline hydrochloride
SMILES
Cl.COC1=C(OC)C(=CC(Cl)=C1)C(C)NC1=CC(=CC=C1S(C)(=O)=O)N1CCNCC1

References

General References
Not Available
ChemSpider
52083411
Wikipedia
PRX-07034

Clinical Trials

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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
PropertyValueSource
Water Solubility0.0431 mg/mLALOGPS
logP3.2ALOGPS
logP2.29Chemaxon
logS-4ALOGPS
pKa (Strongest Acidic)14.33Chemaxon
pKa (Strongest Basic)8.63Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count7Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area79.9 Å2Chemaxon
Rotatable Bond Count7Chemaxon
Refractivity122.2 m3·mol-1Chemaxon
Polarizability47.29 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
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 6
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen (PubMed:35714614, PubMed:36989299, PubMed:37327704, PubMed:8522988). Also has a high affinity for tricyclic psychotropic drugs (By similarity). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:35714614). HTR6 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity (PubMed:35714614, PubMed:37327704). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of mTOR signaling (PubMed:23027611)
Specific Function
G protein-coupled serotonin receptor activity
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Drug created at November 18, 2007 18:29 / Updated at August 26, 2024 19:22