General
Preferred name
KETANSERIN
Synonyms
KETANSERIN TARTRATE ()
Ketanserinum ()
R41468 ()
KJK 945 tartrate ()
KJK-945 tartrate ()
KJK945 tartrate ()
Ketanserin tartrate hydrate ()
Ketanserin (tartrate) ()
R41468 tartrate ()
R41468, Ketanserinum ()
[3H]ketanserin ()
R 49945 ()
Perketan ()
Sufrexal ()
Ketanserina ()
KJK 945 ()
Serepress ()
NSC-758959 ()
R-41468 ()
R-49945 ()
R-41,468 ()
Ketanserine ()
P&D ID
PD000921
CAS
83846-83-7
74050-98-9
Tags
available
drug
First approval
1985
Drug indication
diabetic foot
Hypertension
Drug Status
approved
investigational
Max Phase
3.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE
29
DESCRIPTION
Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 ¦ÌM).
DESCRIPTION
Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 ¦ÌM).
PRICE
29
DESCRIPTION
Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and ??1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.
DESCRIPTION
Ketanserin is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Ketanserin is a specific 5-hydroxytryptamine receptor 2a (5-HT2A) serotonin receptor antagonist. It is used as an antihypertensive drug.
(Enamine Bioactive Compounds)
DESCRIPTION
Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Selective M4 antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective 5-HT2 serotonin receptor blocker
(LOPAC library)
DESCRIPTION
Selective 5-HT2A antagonist. Also antagonist at 5-HT1D
(Tocriscreen Total)
DESCRIPTION
Ketanserin tartrate is the tartrate salt of ketanserin, which is a potent and selective serotonin (5-HT) receptor antagonist. It is selective for 5-HT2 with IC50 value of 6.3 nM and Ki value of 2.1 nM, but has no activity at 5-HT1 receptors. It is used in nutrient-sensitized screening for drugs that shift energy metabolism from mitochondrial respiration to glycolysis. It could prevent some diseases ranging from cancer to ischemic injury. It induces dose-dependent inhibition of contractile responses to 5-HT in isolated canine basilar, rat caudal artery, carotid, gastrosplenic arteries, coronary and so on. It reduces nicotine self-administration in rats, supporting an unexpected involvement of serotonin in nicotine addiction. It significantly decreases blood pressure variability (BPV) and hypertensive organ damage in spontaneously hypertensive rats. It may be used to treat hypertension in early-onset preeclampsia.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
4
Compound Sets
35
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
64
Molecular Weight
395.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
2.42
TPSA
75.17
Fraction CSP3
0.32
Chiral centers
0.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
5-HT2
Target
5-HT2A
α1-adrenergic receptor
serotonin
ADRA1A, ADRA1B, ADRA1D, DRD1, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR7, SLC18A1, SLC18A2
5-HT2A antagonist
5-HT Receptor
Potassium Channel
5-HT2C (Human)
5-HT2C (Rat)
Pathway
Autophagy
GPCR/G protein
Membrane Transporter/Ion Channel
Neuroscience
Neuronal Signaling
Primary Target
5-HT2A Receptors
MOA
Antagonist
5-HT2 Antagonists
serotonin receptor antagonist
Member status
member
Indication
hypertension
Therapeutic Class
Antihypertensive Agents
Source data
