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On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity.
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ABSTRACT:
SUBMITTER: Stefanucci A
PROVIDER: S-EPMC6453917 | biostudies-literature | 2019 Apr
REPOSITORIES: biostudies-literature
Publications
On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity.
Scientific reports 20190408 1
Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a Cu<sup>I</sup>-catalyzed azide-alkyne cycloaddition, with the aim of improving in vivo analgesic efficacy versus DPDPE. NOVA2 showed good affinity and selectivity for the μ-opioid receptor (K<sub>I</sub> of 59.2 nM, EC<sub>50</sub> of 12.9 nM, E<sub>Max</sub> of 87.3%), and long lasting anti-nociceptive effects in mice w ...[more]