General
Preferred name
NAFTOPIDIL
Synonyms
Naftopidil hydrochloride ()
Naftopidil dihydrochloride ()
KT-611 2HCl ()
Naftopidil DiHCl ()
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3- ()
KT-611 hydrochloride ()
BM-15275 hydrochloride ()
KT-611 ()
BM-15275 ()
Naftopidil (Flivas) ()
Flivas, KT-611, Avishot,BM-15275 ()
Naftopidil (hydrochloride) ()
NSC-759293 ()
Flivas ()
Naftopidil-d5 ()
P&D ID
PD000224
CAS
57149-07-2
1164469-60-6
57149-08-3
2747918-58-5
Tags
available
drug
Approved by
PMDA
First approval
1998
1999
Drug indication
Hypertension
hyperplasia
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 29
DESCRIPTION Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human ¦Á1a-, ¦Á1b- and ¦Á1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
DESCRIPTION Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective ??1-adrenergic receptor antagonist or ??-blocker.
PRICE 29
DESCRIPTION Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and ??1-adrenergic receptor antagonist with IC50 of 0.1 ??M and 0.2 ??M, respectively.
PRICE 107
DESCRIPTION Naftopidil hydrochloride (BM-15275 hydrochloride) is a selective alpha1-adrenoceptor antagonist with Ki of 3.7 nM, 20 nM and 1.2 nM for the cloned human ??1a-adrenoceptor, ??1b-adrenoceptor and ??1d-adrenoceptor, respectively. Naftopidil hydrochloride has antiproliferative effects.
DESCRIPTION Naftopidil is a selective alpha1-adrenoceptor antagonist, with antiproliferative effects. Naftopidil has been investigated for the treatment of Disorder of Urinary Stent. (Enamine Bioactive Compounds)
DESCRIPTION Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker. (TargetMol Bioactive Compound Library)
DESCRIPTION alpha1 Adrenoceptor antagonist; antihypertensive (LOPAC library)
DESCRIPTION Naftopidil DiHCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. (BOC Sciences Bioactive Compounds)
DESCRIPTION Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. (TargetMol Bioactive Compound Library)
DESCRIPTION Non-selective opioid antagonist (Tocris Bioactive Compound Library)
DESCRIPTION alpha1 antagonist (Tocriscreen Plus)
DESCRIPTION α1 antagonist (Tocriscreen Total)
DESCRIPTION Naftopidil hydrochloride is an α1-adrenoceptor antagonist with only weak antagonism at post-junctional α2 receptors. Used as a potent, persistent antihypertensive and vasodilator. Clinical formulations of naftopidil are used in the treatment of benign prostatic hyperplasia in Japan. Naftopidil also exhibits antiproliferative activity, inhibiting the growth of androgen-sensitive LNcaP cells and androgen-insensitive PC-3 cancer cell lines with IC50 values of 22.2 and 33.2 µM, respectively. (BOC Sciences Bioactive Compounds)
DESCRIPTION Naftopidil hydrochloride (BM-15275 hydrochloride) is a selective alpha1-adrenoceptor antagonist with Ki of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, respectively. Naftopidil hydrochloride has antiproliferative effects. (TargetMol Bioactive Compound Library)
Cell lines
8
Organisms
3
Compound Sets
28
AdooQ Bioactive Compound Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
External IDs
55
Properties
(calculated by RDKit )
Molecular Weight
392.21
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
3
cLogP
3.41
TPSA
45.17
Fraction CSP3
0.33
Chiral centers
1.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Selectivity
alpha1
Target
5-HT1A
Adrenergic Receptor
α1-adrenergic receptor
α1-adrenoceptor
α1A-adrenergic receptor
α1B-adrenergic receptor
α1D-adrenergic receptor
Primary Target
Adrenergic ?1 Receptors
MOA
Antagonist
alpha1D-Adrenoceptor Antagonists
Member status
member
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Solubility
DMSO to 100 mM
Source data