Name: 2,3-Dichloro-5-iodopyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,3-Dichloro-5-iodopyridine, is researched, Molecular C5H2Cl2IN, CAS is 97966-01-3, about Synthesis and Structure-Activity Relationships of 3,8-Diazabicyclo[4.2.0]octane Ligands, Potent Nicotinic Acetylcholine Receptor Agonists. Author is Frost, Jennifer M.; Bunnelle, William H.; Tietje, Karin R.; Anderson, David J.; Rueter, Lynne E.; Curzon, Peter; Surowy, Carol S.; Ji, Jianquo; Daanen, Jerome F.; Kohlhaas, Kathy L.; Buckley, Michael J.; Henry, Rodger F.; Dyhring, Tino; Ahring, Philip K.; Meyer, Michael D..
A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (hα4β2) and in a rat model of persistent nociceptive pain (formalin model). Numerous analogs in this series exhibit picomolar affinity in radioligand binding assays and nanomolar agonist potency in functional assays, placing them among the most potent nAChR ligands known for the hα4β2 receptor. The 3,8-diazabicyclo[4.2.0]octanes (1R,6S)-I [R = H, Cl, Me, R1 = Cl; R = Br, Cn, R1 = Br] and (1S,6R)-I [R = H, R1 = Cl] exhibit equivalent or greater affinity for the hα4β2 receptor relative to epibatidine, and like epibatidine, many exhibit robust analgesic efficacy in the rat formalin model of persistent pain.
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