Linopirdine

SKU: orb1308125

Description

Linopirdine (DuP 996) is a selective M-type potassium channel (Kv7/KCNQ) inhibitor and a TRPV1 agonist. This orally active cognitive enhancer stimulates the release of acetylcholine and other neurotransmitters, making it a useful research tool for studying synaptic transmission and cognitive function in both in vitro and in vivo neurological models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	105431-72-9
MW	391.46
Purity	99.92%
Formula	C₂₆H₂₁N₃O
SMILES	O=C1N(c2ccccc2C1(Cc1ccncc1)Cc1ccncc1)c1ccccc1
Target	TRP/TRPV Channel,Potassium Channel
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.22 mM);DMSO:110 mg/mL (281 mM)

Bioactivity

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Target IC50	K+ current, M-type:2.4 μM
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%.
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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DuP 996, DuP996, DuP-996, current, cognition, Channels, acetylcholine, enhancing, Inhibitor, Linopirdine, Kv7, KcsA, KCNQ, inhibit, M-type, M-type K+ current, orally, PotassiumChannel, Potassium Channel, TRP Channel, Transient receptor potential channels, TRPV1, TRPV Channel, TRPVChannel, TRPChannel

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Compound Identifiers

PubChem CID

3932 ↗

Key Properties

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No computed properties available.

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Linopirdine (orb1308125)

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CAS Number:	113168-57-3
MW:	427.93
Formula:	C₂₆H₂₂ClN₃O

Linopirdine

Description

Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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