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Affinity of fentanyl and its derivatives for the sigma(1)-receptor

Lipinski, Piotr F. J. and Szűcs, Edina and Jaronczyk, Malgorzata and Kosson, Piotr and Benyhe, Sándor (2019) Affinity of fentanyl and its derivatives for the sigma(1)-receptor. MEDCHEMCOMM, 10 (7). pp. 1187-1191. ISSN 2040-2503

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Abstract

Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the sigma(1) receptor. The parent compound is a rather poor binder (IC50 = 4973 nM), but its close derivatives (benzylfentanyl or p-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity.

Item Type: Article
Subjects: Q Science / természettudomány > QH Natural history / természetrajz > QH301 Biology / biológia > QH3011 Biochemistry / biokémia
SWORD Depositor: MTMT SWORD
Depositing User: MTMT SWORD
Date Deposited: 22 Nov 2019 12:23
Last Modified: 22 Nov 2019 12:23
URI: http://real.mtak.hu/id/eprint/103633

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