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Linopirdine

Catalog No. T15758   CAS 105431-72-9
Synonyms: DuP 996

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.

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Linopirdine Chemical Structure
Linopirdine, CAS 105431-72-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 36.00
2 mg In stock $ 51.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
25 mg In stock $ 239.00
50 mg In stock $ 413.00
100 mg In stock $ 590.00
200 mg In stock $ 853.00
500 mg In stock $ 1,270.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 M-type K+ current:2.4 μM
In vitro Linopirdine is a well known blocker of voltage-gated potassium channels from the Kv7 (or KCNQ) family that generate the so called M current in mammalian neurons. Kv7 subunits are also expressed in pain-sensing neurons in dorsal root ganglia, in which they modulate neuronal excitability. Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1), another ion channel expressed in nociceptors and involved in pain signaling. Linopirdine induces increases in intracellular calcium concentration in human embryonic kidney 293 (HEK293) cells expressing TRPV1, but not TRPA1 and TRPM8 or in wild-type HEK293 cells. Linopirdine also activates an inward current in TRPV1-expressing HEK293 cells that is almost completely blocked by the selective TRPV1 antagonist capsazepine. At low concentrations linopirdine sensitizes both recombinant and native TRPV1 channels to heat, in a manner that is not prevented by the Kv7-channel opener flupirtine. Linopirdine exerts an excitatory action on mammalian nociceptors not only through inhibition of the M current but also through activation of the capsaicin receptor TRPV1[4].
In vivo Linopirdine (i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently enhances MAP by up to 15%[2].
Synonyms DuP 996
Molecular Weight 391.46
Formula C26H21N3O
CAS No. 105431-72-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 110 mg/mL (281 mM), sonification is recommended.

TargetMolReferences and Literature

1. Schnee ME, et al. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998 Aug;286(2):709-17. 2. Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8. 3. Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40.

Related compound libraries

This product is contained In the following compound libraries:
Potassium Channel Blocker Library ReFRAME Related Library Ion Channel Inhibitor Library Anti-Cancer Compound Library NO PAINS Compound Library Orally Active Compound Library Inhibitor Library Human Metabolite Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Linopirdine 105431-72-9 Membrane transporter/Ion channel TRP/TRPV Channel Potassium Channel Kv7 enhancing DuP996 inhibit TRP Channel Inhibitor Transient receptor potential channels DuP 996 KcsA current acetylcholine DuP-996 Channels orally TRPV1 KCNQ M-type cognition inhibitor

 

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