General
Preferred name
LINOPIRDINE
Synonyms
Linopirdine dihydrochloride ()
Dup-996 ()
DuP 996 ()
2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)- ()
Linopirdina ()
P&D ID
PD002692
CAS
113168-57-3
105431-72-9
Tags
available
drug
Drug indication
Attention deficit hyperactivity disorder
Cognitive impairment
Drug Status
approved
experimental
investigational
Max Phase
2.0
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)
DESCRIPTION
Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 ¦ÌM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue[1][2][3].
PRICE
107
DESCRIPTION
Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 ??M). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.
DESCRIPTION
Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents
(Tocris Bioactive Compound Library)
DESCRIPTION
KV7 (KCNQ) channel blocker
(Tocriscreen Plus)
DESCRIPTION
KCNQ channel blocker
(Tocriscreen Total)
DESCRIPTION
Linopirdine dihydrochloride is a blocker of KV7 voltage-gated potassium channels. It can block KV7.1 + 7.3 (KCNQ2 + 3) / M-currents with IC50 value from 4 to 7 μM and KV7.1 homomeric channels with IC50 value of 8.9 μM.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Stimulates release of acetylcholine and other neurotransmitters; cognitive enhancer
(LOPAC library)
DESCRIPTION
Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
3
Compound Sets
26
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
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
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMatrix
Guide to Pharmacology
LOPAC library
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
391.17
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
4.88
TPSA
46.09
Fraction CSP3
0.12
Chiral centers
0.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Target
M-type K+ current
Potassium Channel
TRP Channel
TRPV1
KCNQ2, KCNQ3, KCNQ4, KCNQ5
Primary Target
Voltage-gated Potassium (KV) Channels
MOA
Blocker
Acetylcholine Release Enhancers
potassium channel blocker
Member status
member
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Source data
