General
Preferred name
RITANSERIN
Synonyms
R 55667 ()
Ritanserin ()
Tiserton ()
RITANSERINA ()
R-55667 ()
RITANSERINE ()
NSC-758470 ()
R 55,667 ()
TISERTON ()
P&D ID
PD000984
CAS
87051-43-2
Tags
available
drug candidate
Drug indication
Anxiety disorder
cocaine dependence
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic ¦Á1, Adrenergic ¦Á2 receptors[1].
PRICE 78
DESCRIPTION Selective non-peptide OX1 antagonist (Tocris Bioactive Compound Library)
DESCRIPTION Potent 5-HT2 antagonist (Tocriscreen Plus)
DESCRIPTION Potent 5-HT2 serotonin receptor antagonist which passes the blood-brain barrier (LOPAC library)
DESCRIPTION Potent 5-HT2 antagonist (Tocriscreen Total)
DESCRIPTION Ritanserin is a potent and long-acting 5-HT2 receptor antagonist (Ki = 0.39 nM) with high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively). (BOC Sciences Bioactive Compounds)
DESCRIPTION Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM. (TargetMol Bioactive Compound Library)
Cell lines
4
Organisms
4
Compound Sets
21
BOC Sciences Bioactive Compounds
ritanserin-cas-87051-43-2-item-78677
Cayman Chemical Bioactives
21374
ChEMBL Drugs
CHEMBL267777
Concise Guide to Pharmacology 2023/24
97
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12693
DrugMAP
DM0X36Y
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0000422
Guide to Pharmacology
97
Ki Database
RITANSERIN
LOPAC library
MedChem Express Bioactive Compound Library
HY-10791
NPC Screening Collection
ReFrame library
TargetMol Bioactive Compound Library
T16759
The Spectrum Collection
Tocris Bioactive Compound Library
1955
Tocriscreen Plus
1955
Tocriscreen Total
External IDs
31
Properties
(calculated by RDKit )
Molecular Weight
477.17
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
5.48
TPSA
37.61
Fraction CSP3
0.26
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Selectivity
5-HT2/5-HT1C
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Primary Target
Non-selective 5-HT2
MOA
Antagonist
serotonin receptor antagonist
Target
ADRA1A, ADRA1B, ADRA1D, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
5-HT2
D2
dopamine
H1 receptor
α1-adrenergic receptor
α2 receptor
Recommended Cell Concentration
100 nM
Source data