A-84,543 Explained

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A-84543 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It is widely used in scientific research into the structure and function of this receptor subtype and has been the lead compound for the development of a large family of related derivatives.^{[1] [2] [3] [4]}

Notes and References

1. Abreo MA, Lin NH, Garvey DS, Gunn DE, Hettinger AM, Wasicak JT, Pavlik PA, Martin YC, Donnelly-roberts DL, Anderson DJ, Sullivan JP, Williams M, Arneric SP, Holladay MW . 6 . Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors . Journal of Medicinal Chemistry . 39 . 4 . 817–25 . February 1996 . 8632405 . 10.1021/jm9506884 .
2. Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts DL, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW . 6 . Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist . Bioorganic & Medicinal Chemistry Letters . 8 . 3 . 249–54 . February 1998 . 9871663 . 10.1016/S0960-894X(98)00019-5 .
3. Wei ZL, Xiao Y, Yuan H, Baydyuk M, Petukhov PA, Musachio JL, Kellar KJ, Kozikowski AP . 6 . Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits . Journal of Medicinal Chemistry . 48 . 6 . 1721–4 . March 2005 . 15771418 . 10.1021/jm0492406 .
4. Carreras J, Avenoza A, Busto JH, Peregrina JM . Synthesis of azabicyclo[2.2.n]alkane systems as analogues of 3-[1-methyl-2-(S)-pyrrolidinyl- methoxy]pyridine (A-84543) . The Journal of Organic Chemistry . 72 . 8 . 3112–5 . April 2007 . 17371077 . 10.1021/jo0700732 .