An enhancer of several neurotransmitters

Linopirdine – 1 mg

Brand:
Cayman
CAS:
105431-72-9
Storage:
-20
UN-No:
Non-Hazardous - /

Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 µM.{31443,31441} Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release.{31444} Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory.{31445} Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV).{31442}  

 

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Description

An enhancer of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate by blocking M-type K+ current (IC50 = 2.4 µM); also acts as an agonist of TRPV1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV)

Formal name: 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one

Synonyms:  DuP-996

Molecular weight: 391.5

CAS: 105431-72-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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