General
Preferred name
SILODOSIN
Synonyms
KMD 3213 ()
KAD 3213 ()
KAD 3213, KMD 3213 ()
Rapilif ()
Urief ()
KMD-3213 ()
Kso-0400 ()
Urorec ()
Silodal ()
KAD-3213 ()
Silodyx ()
Rapaflo ()
Silodosin-d4 ()
P&D ID
PD009321
CAS
160970-54-7
1426173-86-5
Tags
natural product
drug
available
Approved by
EMA
FDA
First approval
2008
Drug Status
approved
Drug indication
Benign prostatic hyperplasia
Max Phase
Phase 4
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)
ABSORPTION
Quickly absorbed and has a bioavailability of 32% at 8mg/day (therapeutic dose).; When 8 mg of silodosin is taken once daily with food, the pharmacokinetic parameters are as follows: ; Cmax = 61.6 ± 27.54 ng/mL;; Tmax = 2.6 ± 0.90 hours; ; AUC (0h-24h) = 373 ngâ¢hr/ml. ; The AUC of its metabolite, KMD3213G, is four times greater than silodosin.
ROE
Fecal (54.9%); ; Renal (33.5%)
HALF-LIFE
Silodosin = 13.3 ± 8.07 hours;; KMD-3213G = 24 hours;
DESCRIPTION
Silodosin an α1-adrenoceptor antagonist with selectivity for prostate adrenoceptors (mainly the α1A subtype).
(GtoPdb)
MOA
Benign prostate hyperplasia (BPH), or an enlarged prostate, is a condition found only in men and is characterized by a non-cancerous enlargement of the prostate gland. Symptoms of BPH include urinary difficulty, urinary frequency and an inability to complete bladder emptying. Silodosin is highly uroselective for the alpha (1A) receptors located in the prostate, [urethrea and bladder trigone in the lower urinary tract]. Blocking these receptors relaxes the smooth muscles, resulting in an improvement in urine flow and a reduction in BPH symptoms. The selective binding of silodosin to the alpha (1A) receptors is substantially greater than the binding to the cardiovascular-associated alpha (1B) receptors and thereby maximizes target organ activity while minimizing the potential for blood pressure effects. [Watson Pharmaceutical Inc. Press release] Silodosin is alpha 1A-adrenoceptor selective antagonist which inhibits sympathetic nerve stimulation and relaxation of smooth muscle tone in the lower urinary tract which relieves the pressure from contraction of smooth muscle. The reduction of intraurethral pressure improves voiding and storage issues associated with BPH. ; ; ; ;
DESCRIPTION
Selective GPR55 agonist; also promotes NSC proliferation and differentiation
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
26
Axon Medchem Screening Library
ChEMBL Approved Drugs
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
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
VGSC-DB
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
34
Molecular Weight
495.23
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
13
Ring Count
3
Aromatic Ring Count
2
cLogP
3.07
TPSA
97.05
Fraction CSP3
0.48
Chiral centers
1.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Anti-infection
Neuronal Signaling
Target
??-adrenergic receptor
ADRA1A, ADRA1B, ADRA1D
a1A antagonist
Adrenergic Receptor
Bacterial
Primary Target
Adrenergic ?1 Receptors
MOA
Antagonist
Adrenergic Receptor antagonist
Indication
benign prostatic hyperplasia (BPH)
VGSC Target
Nav1.5
Source data
