RJR 2429 dihydrochloride
Potent nAChR agonist that displays selectivity for α4β2 (Ki = 1 nM) and α1βγδ subtypes (EC50 values are 297 and 55 nM respectively). Induces dopamine release from striatal neurons (EC50 = 2 nM) and inhibits ion flux in thalamic neurons (IC50 = 154 nM). Also putative α3β4 agonist that potentiates catecholamine release.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 261.19. Batch specific molecular weights may vary from batch to batch due to solvent 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||3.83 mL||19.14 mL||38.29 mL|
|5 mM||0.77 mL||3.83 mL||7.66 mL|
|10 mM||0.38 mL||1.91 mL||3.83 mL|
|50 mM||0.08 mL||0.38 mL||0.77 mL|
References are publications that support the products' biological activity.
Bencherif et al (1998) The heterocyclic substituted pyridine derivative (±)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors. J.Pharmacol.Exp.Ther. 284 886 PMID: 9495846
Bhatti et al (2008) Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands. J.Org.Chem. 73 3497 PMID: 18363376
Yokotani et al (2002) Characterization of functional nicotinic acetylcholine receptors involved in catecholamine release from isolated rat adrenal gland. Eur.J.Pharmacol. 446 83 PMID: 12098588
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Literature in this Area
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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.