General
Preferred name
APRACLONIDINE
Synonyms
p-Aminoclonidine hydrochloride ()
Aminoclonidine, p ()
p-AMINOCLONIDINE ()
Apraclonidine (hydrochloride) ()
Pharmaprojects No. 1758 ()
APRACLONIDINE HYDROCHLORIDE ()
ALO 2145 ()
Apraclonidine HCl ()
Iopidine HCl,ALO 2145 ()
Iopidine ()
Aplonidine hydrochloride ()
AL02145 ()
AL-02145 ()
P&D ID
PD009614
CAS
66711-21-5
73218-79-8
Tags
available
drug
Approved by
FDA
First approval
1987
Drug Status
approved
Drug indication
Intra ocular pressure reduction
Adrenergic (alpha12-agonist)
Max Phase
Phase 4
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 Apraclonidine is a derivative which acts as sympathomimetic α2-adrenoceptor agonist. (GtoPdb)
DESCRIPTION alpha2 Adrenoceptor agonist (LOPAC library)
DESCRIPTION Apraclonidine is an α2-adrenergic receptor (α2-AR) agonist and structural analog of clonidine. It is used for the treatment of post-surgical elevated intraocular pressure. It inhibits noradrenaline-stimulated contraction in guinea pig ileum with EC50s of 7.59 nM and rabbit vas deferens with EC50s of 6.76 nM. (BOC Sciences Bioactive Compounds)
DESCRIPTION Apraclonidine is a clonidine derivative with relatively selective alpha-2-adrenergic agonistic activity. It is an α2 adrenergic receptor agonist and a weak α1 adrenergic receptor agonist. It enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction. It is a sympathomimetic used in glaucoma therapy. It was developed by Alcon and has been listed. (BOC Sciences Bioactive Compounds)
Compound Sets
28
Cayman Chemical Bioactives
ChEMBL Approved 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
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
ZINC Tool Compounds
External IDs
52
Properties
(calculated by RDKit )
Molecular Weight
244.03
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
1
Ring Count
2
Aromatic Ring Count
1
cLogP
1.95
TPSA
62.44
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
6.0
QED
0.66
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Selectivity
alpha2
Member status
member
MOA
alpha2-Adrenoceptor Agonists
Adrenergic Receptor agonist
Indication
glaucoma, intraocular pressure
Target
ADRA1A, ADRA2A, ADRA2B, ADRA2C
Adrenergic Receptor
Therapeutic Class
Antiglaucomic Agents
Pathway
GPCR/G protein
Neuronal Signaling
Solubility
Soluble in DMSO, ethanol, methanol.
Soluble in DMSO, not in water
Source data