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ABT 089 dihydrochloride is a high affinity and selective α4β2 partial agonist (Ki = 16 nM). Exhibits >1000-fold and >10,000-fold selectivity for α4β2 over α1β1γ1 and α7 receptors respectively. Neuroprotective against glutamate-induced toxicity in rat cortical neurons in vitro. Enhances cognitive performance in vivo. Orally bioavailable and brain penetrant.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 265.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.77 mL||18.86 mL||37.71 mL|
|5 mM||0.75 mL||3.77 mL||7.54 mL|
|10 mM||0.38 mL||1.89 mL||3.77 mL|
|50 mM||0.08 mL||0.38 mL||0.75 mL|
References are publications that support the biological activity of the product.
Rueter et al (2004) ABT-089: pharmacological properties of a neuronal nicotinic acetylcholine receptor agonist for the potential treatment of cognitive disorders. CNS Drug Rev. 10 167 PMID: 15179445
Sullivan et al (1997) ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties. J.Pharmacol.Exp.Ther. 283 235 PMID: 9336329
Decker et al (1997) ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys. J.Pharmacol.Exp.Ther. 283 247 PMID: 9336330
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.