Design, Synthesis and Discovery of Picomolar Selective α4β2 Nicotinic Acetylcholine Receptor Ligands was written by Yenugonda, Venkata M.;Xiao, Yingxian;Levin, Edward D.;Rezvani, Amir H.;Tran, Thao;Al-Muhtasib, Nour;Sahibzada, Niaz;Xie, Teresa;Wells, Corinne;Slade, Susan;Johnson, Joshua E.;Dakshanamurthy, Sivanesan;Kong, Hye-Sik;Tomita, York;Liu, Yong;Paige, Mikell;Kellar, Kenneth J.;Brown, Milton L.. And the article was included in Journal of Medicinal Chemistry in 2013.Name: 3-Fluoro-5-iodoaniline This article mentions the following:
Developing novel and selective compounds that desensitize α4β2 nicotinic acetylcholine receptors (nAChRs) could provide new effective treatments for nicotine addiction, as well as other disorders. Here we report a new class of nAChR ligands that display high selectivity and picomolar binding affinity for α4β2 nicotinic receptors. The novel compounds have Ki values in the range of 0.031-0.26 nM and properties that should make them good candidates as drugs acting in the CNS. The selected lead compound I (VMY-2-95) binds with high affinity and potently desensitizes α4β2 nAChRs. At a dose of 3 mg/kg, compound I significantly reduced rat nicotine self-administration. The overall results support further characterizations of compound I and its analogs in preclin. models of nicotine addiction and perhaps other disorders involving nAChRs. In the experiment, the researchers used many compounds, for example, 3-Fluoro-5-iodoaniline (cas: 660-49-1Name: 3-Fluoro-5-iodoaniline).
3-Fluoro-5-iodoaniline (cas: 660-49-1) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Iodo alkanes participate in a variety of organic synthesis reactions, which include the SimmonsSmith reaction (cyclopropanation using iodomethane), Williamson ether synthesis, Wittig reaction, Grignard reaction, alkyl coupling reactions, and Wurtz reaction.Name: 3-Fluoro-5-iodoaniline
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com