General
Preferred name
RILMENIDINE
Synonyms
Rilmenidine hemifumarate ()
Rilmenidine Phosphate ()
Rilmenidine (hemifumarate) ()
Rilmenidine (phosphate) ()
Hyperium ()
Rilmenidina ()
Rilmenidine-d4 ()
P&D ID
PD002612
CAS
207572-68-7
85409-38-7
54187-04-1
85047-14-9
Tags
available
drug
Drug indication
Hypertension
Drug Status
approved
investigational
Max Phase
4.0
First approval
1987
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 Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [1][2][3].
PRICE 86
DESCRIPTION Rilmenidine is an oxazoline compound, that is reported to exhibit selectivity for I1 imidazoline receptors (binding sites) compared to cerebral α2-adrenoceptors . (GtoPdb)
DESCRIPTION Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
DESCRIPTION Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [1][2][3].
DESCRIPTION α2 agonist. Also I1 ligand (Tocriscreen Total)
DESCRIPTION alpha2 antagonist. Also I2 ligand (Tocris Bioactive Compound Library)
DESCRIPTION Rilmenidine hemifumarate, a centrally acting antihypertensive agent, is an I1-imidazoline binding site selective ligand and α2-adrenoceptor agonist. Rilmenidine targets the nonadrenergic imidazoline-binding site I1 receptor with a Ki value of 7.1 nM and demonstrates weaker affinity for the I2 receptor with a Ki value of 5.2 µM. (BOC Sciences Bioactive Compounds)
DESCRIPTION Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used for the treatment of hypertension. (BOC Sciences Bioactive Compounds)
DESCRIPTION Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used to treat hypertension. (TargetMol Bioactive Compound Library)
DESCRIPTION Selective I1 imidazoline receptor agonist. (LOPAC library)
Cell lines
1
Organisms
0
Compound Sets
26
AdooQ Bioactive Compound Library
A14256
BOC Sciences Bioactive Compounds
rilmenidine-hemifumarate-cas-207572-68-7-item-101621
rilmenidine-phosphate-cas-85409-38-7-item-84-392273
Cayman Chemical Bioactives
16988
32879
31691
ChEMBL Approved Drugs
CHEMBL289480
ChEMBL Drugs
CHEMBL289480
Drug Repurposing Hub
DrugBank
DB11738
DrugBank Approved Drugs
DB11738
DrugCentral
2381
DrugCentral Approved Drugs
2381
DrugMAP
DM13PQW
DrugMAP Approved Drugs
DM13PQW
DrugMatrix
Guide to Pharmacology
13356
Ki Database
rilmenidine
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL289480
MedChem Express Bioactive Compound Library
HY-100490B
HY-100490
HY-100490A
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
Selleckchem Bioactive Compound Library
rilmenidine-phosphate
TargetMol Bioactive Compound Library
T6641
Tocris Bioactive Compound Library
0790
Tocriscreen Total
ZINC Tool Compounds
ZINC000000009708
External IDs
66
Properties
(calculated by RDKit )
Molecular Weight
180.13
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
0
cLogP
1.15
TPSA
33.62
Fraction CSP3
0.9
Chiral centers
0.0
Largest ring
5.0
QED
0.71
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
I1
Pathway
Apoptosis
Autophagy
GPCR/G protein
Neuroscience
Neuronal Signaling
Primary Target
Adrenergic ?2 Receptors
MOA
Agonist
Imidazoline I1 Receptor Agonists
adrenergic receptor agonist, imidazoline receptor agonist
Member status
member
Indication
hypertension
Target
ADRA2A
Imidazoline Receptor
Adrenergic Receptor
I1-imidazoline receptor
Source data