A partial agonist for α4β2 subunit-containing nAChRs (EC50 = 0.18 µM); selective for α4β2 over α2β4

TC 2559 (fumarate) – 10 mg

Brand:
Cayman
CAS:
212332-35-9
Storage:
-20
UN-No:
Non-Hazardous - /

TC 2559 is a CNS-selective partial agonist for α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) with an EC50 value of 0.18 µM for calcium signaling in HEK293 cells expressing human recombinant nAChRs.{46064,46065} It is selective for α4β2 over α2β4, α4β4, α3β4, α3β2, and α7 subunit-containing nAChRs (EC50s = 14, 12.5, >30, >100, and >100 µM, respectively). It increases dopamine cell firing in the rat ventral tegmental area (VTA) in vitro. TC 2559 increases spontaneous inhibitory postsynaptic currents (sIPSCs) in dorsal horn neurons, indicating an enhancement of inhibitory synaptic transmission, an effect that is blocked by the α4β2 subunit-containing nAChR antagonist DHβE.{46066} It reduces formalin-induced paw-licking time in mice when administered at doses of 3 and 10 mg/kg and increases paw withdrawal latency in a rat model of chronic constriction injury when administered at a dose of 3 mg/kg. TC 2559 (3 and 6 µmol/kg) also reverses cognitive deficits induced by scopolamine in rats, increasing step-through latency in a passive avoidance task.{46064}  

 

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Description

A partial agonist for α4β2 subunit-containing nAChRs (EC50 = 0.18 µM); selective for α4β2 over α2β4, α4β4, α3β4, α3β2, and α7 subunit-containing nAChRs (EC50s = 14, 12.5, >30, >100, and >100 µM, respectively); increases dopamine cell firing in the rat VTA in vitro; enhances inhibitory synaptic transmission in dorsal horn neurons via α4β2 subunit-containing nAChRs; reduces formalin-induced paw-licking time in mice at 3 and 10 mg/kg; reverses scopolamine-induced cognitive deficits in rats in a step-through passive avoidance test at 3 and 6 µmol/kg

Formal name: 4-(5-ethoxy-3-pyridinyl)-N-methyl-3-buten-1-amine, difumaric acid

Synonyms: 

Molecular weight: 438.4

CAS: 212332-35-9

Purity: ≥95%

Formulation: A solid

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

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