General
Preferred name
CONESSINE
Synonyms
Conessinum ()
Wrightine ()
Roquessine ()
Neriine ()
Konessin ()
CONESSINE HYDROBROMIDE ()
NSC-119994 ()
CONESINA ()
Conessine dihydrobromide ()
Conessine hbr ()
P&D ID
PD019682
CAS
546-06-5
Tags
available
natural product
drug candidate
Drug indication
Discovery agent
Drug Status
investigational
Max Phase
2.0
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)
DESCRIPTION
Conessine is an alkaloid obtained from the bark and seeds of Holarrhena antidysenterica trees. It binds with high affinity to rat and human histamine H3 receptors in radio-ligand binding assays, acting as a receptor antagonist . H3 antagonists are being researched as potential drugs for the treatment of neurodegenerative conditions and for their stimulant and nootropic effects. For example, is in clinical trial for Parkinson's disease, narcolepsy, cataplexy and excessive daytime sleepiness.
(GtoPdb)
PRICE
76
DESCRIPTION
Conessine is a naturally occurring steroidal dibasic alkaloid with a rigid steroid-based skeleton. It is found in a number of plant species from the apocynaceae family. It is a selective, specific and potent histamine H3 receptor antagonist. It has high selectivity for both rat and human histamine H3 receptors. It has a poor rate of CNS clearance. It also binds to the human α2C4 adrenergic receptor. It has anti-malarial activity and displays in vitro antiplasmodial activity. It is used as a treatment for amoebic dysentery. It was developed by Abbott.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Conessine (Conessinum), a steroidal alkaloid isolated from Holarrhena floribunda, interacts with the histamine H3 receptor and has anti-malarial activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
13
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
31
Molecular Weight
356.32
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
1
Ring Count
5
Aromatic Ring Count
0
cLogP
4.81
TPSA
6.48
Fraction CSP3
0.92
Chiral centers
8.0
Largest ring
6.0
QED
0.62
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Anti-infection
Apoptosis
Metabolic Enzyme/Protease
Neuronal Signaling
NF-κB
Recommended Cell Concentration
1 uM
Target
Bacterial
FOXO
Histamine Receptor
MDM-2/p53
Parasite
H3 receptor
Source data
