General
Preferred name
AZELNIDIPINE
Synonyms
Azelnidipine D7 ()
CS-905 D7 ()
CS 905 ()
UR-12592 ()
Calblock ()
Azelnidipine ()
P&D ID
PD008993
CAS
123524-52-7
Tags
available
drug
Drug Status
investigational
approved
Max Phase
Phase 3
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)
PHARMACODYNAMICS
Azelnidipine is a vasodilator that induces a gradual decrease in blood pressure in hypertensive patients. Unlike other members of its drug class, azelnidipine does not induce reflex tachycardia due to vasodilation. This is likely due to the fact that it elicits a gradual fall in blood pressure; ; It also exhibits a prolonged hypotensive effect and has been shown to have a strong anti-arteriosclerotic action in vessels due to its high affinity for vascular tissue and antioxidative activity [A31944]. ; ; Clinical studies have demonstrated that azelnidipine markedly reduced heart rate and proteinuria in hypertensive patients by inhibiting sympathetic nerve activity. Azelnidipine has also been confirmed to have cardio-protective, neuroprotective, and anti-atherosclerotic properties, and has also been found to prevent insulin resistance [A31944].
ABSORPTION
Oral ingestion of azelnidipine demonstrates rapid and dose-dependent absorption [L1382].;
METABOLISM
Like most members of its class, azelnidipine primarily undergoes first-pass hepatic metabolism. Azelnidipine is metabolized by hepatic cytochrome P450 (CYP) 3A4 and has no active metabolite product. It may interact with other drugs or compounds that are substrates for this enzyme. ; ; Azelnidipine is lipophilic and has a potent affinity for membranes of vascular smooth muscle cells [L1382].
TOXICITY
As with any calcium channel blocker toxicity, bradycardia and hypotension may result from overdose. The treatment of patients with bradycardia and hypotension begins with supportive therapy and atropine, however, patients with severe toxicity do not have an adequate response and must be managed more aggressively. ; ; Calcium plays an imperative role in myocardial contractility, automaticity and vascular tone. Administration of exogenous calcium is of benefit in cases of toxicity [L1384].
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
5
Compound Sets
15
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMatrix
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
22
Molecular Weight
582.25
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
2
Rotatable Bonds
9
Ring Count
5
Aromatic Ring Count
3
cLogP
4.69
TPSA
137.03
Fraction CSP3
0.27
Chiral centers
1.0
Largest ring
6.0
QED
0.21
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Calcium Channel
Ca channel blocker
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Member status
member
MOA
Calcium Channel Blockers
Source data
