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Publications [#274189] of Edward D. Levin

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Papers Published

  1. Yenugonda, VM; Xiao, Y; Levin, ED; Rezvani, AH; Tran, T; Al-Muhtasib, N; Sahibzada, N; Xie, T; Wells, C; Slade, S; Johnson, JE; Dakshanamurthy, S; Kong, H-S; Tomita, Y; Liu, Y; Paige, M; Kellar, KJ; Brown, ML (2013). Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.. Journal of Medicinal Chemistry, 56(21), 8404-8421. [24047231], [doi]
    (last updated on 2019/12/06)

    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 1 (VMY-2-95) binds with high affinity and potently desensitizes α4β2 nAChRs. At a dose of 3 mg/kg, compound 1 significantly reduced rat nicotine self-administration. The overall results support further characterizations of compound 1 and its analogues in preclinical models of nicotine addiction and perhaps other disorders involving nAChRs.

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