Synthesis and σ receptor affinity of spiro[[2]benzopyran-1,1′-cyclohexanes] with an exocyclic amino moiety in the 3′-position-Reference-Cited by-同舟云学术

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Synthesis and σ receptor affinity of spiro[[2]benzopyran-1,1′-cyclohexanes] with an exocyclic amino moiety in the 3′-position

Published:2021 Issue:2 Volume:12 Page:237-244
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Kronenberg Elisabeth¹²³,Weber Frauke¹²³,Schepmann Dirk¹²³^ORCID,Wünsch Bernhard¹²³^ORCID

Affiliation:

1. Institut für Pharmazeutische und Medizinische Chemie der Westfälischen Wilhelms-Universität Münster

2. D-48149 Münster

3. Germany

Abstract

Novel spirocyclic σ₁ ligands with defined distances between the basic amino moiety and the phenyl rings were designed, synthesized and pharmacologically evaluated, in order to analyze the structural features crucial for high σ₁ affinity.

Funder

Deutsche Forschungsgemeinschaft

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/MD/D0MD00307G

Reference47 articles.

1. Naloxone-inaccessible sigma receptor in rat central nervous system.

2. Naltrexone fails to antagonize the σ effects of PCP and SKF 10,047 in the dog

3. Evidence for a multi-site model of the rat brain σ receptor

4. Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling

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