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RJR 2429 is a nicotinic acetylcholine receptor (AChR) agonist.1 It is selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells). RJR 2429 induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland when used at a concentration of 100 µM.2,3 It inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM).2
WARNING This product is not for human or veterinary use.
1. Synthesis of 2-
2. The heterocyclic substituted pyridine derivative (+/-
3. Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). Bioorg. Med. Chem. Lett. 24(24), 5801-5804 (2014).