This article is cited in 7 papers

Communications

Synthesis of an allosteric modulator of ionotropic glutamate receptors

M. I. Lavrov^ab, O. V. Stroganov^cd, V. L. Zamoyski^b, V. V. Grigoriev^ab, M. E. Zapolskiy^d, S. V. Sysolyatin^e, V. V. Malykhin^e, V. N. Surmachev^e, V. A. Palyulin<sup>ab

a</sup> Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation
^c N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russian Federation
^d QM Pharma LLC, Skolkovo Innovation Center, Moscow, Russian Federation
^e Institute for Problems of Chemical & Energetic Technologies, Siberian Branch of the Russian Academy of Sciences, Biysk, Russian Federation

Abstract: Synthesis of 6-[4-methoxy-3-(pyrrolidin-1-ylmethyl)benzyl]-1,11-dimethyl-3,6,9-triazatricyclo[7.3.1.13,11]tetradecane-4,8,12-trione has been carried out and optimized. In vitro studies using electrophysiological patch clamp technique have revealed a negative effect of this compound on kainateinduced currents in Purkinje neurons in a wide range of concentrations from 10⁻¹¹ to 10⁻⁶m.

Keywords: 3,7-diazabicyclo[3.3.1]nonane, AMPA receptor, negative allosteric modulator, NAM, patch clamp.

Language: English

DOI: 10.1016/j.mencom.2020.03.008

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