1‐(Arylalkyl)quinolizidine Derivatives and Thio‐Isosteric Analogues as Ligands for Sigma Receptors | Zendy

Sparatore Anna | Zendy; Novelli Federica | Zendy; Sparatore Fabio | Zendy

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1‐(Arylalkyl)quinolizidine Derivatives and Thio‐Isosteric Analogues as Ligands for Sigma Receptors

Author(s) -

Sparatore Anna,

Novelli Federica,

Sparatore Fabio

Publication year - 2004

Publication title -

helvetica chimica acta

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.74

H-Index - 82

eISSN - 1522-2675

pISSN - 0018-019X

DOI - 10.1002/hlca.200490055

Subject(s) - chemistry , thio , quinolizidine , stereochemistry , pentazocine , receptor , sigma receptor , intrinsic activity , biochemistry , pharmacology , alkaloid , agonist , medicine , morphine

A set of 1‐(arylalkyl)quinolizidines, isosteric thioanalogues, and variously functionalized congeners were synthesized (see 1 – 25 ) and tested for affinity to sigma 1 and sigma 2 receptor subtypes, by displacing [ 3 H]‐ (+)‐pentazocine and [ 3 H]DTG from guinea pig brain and rat brain preparations, respectively. All compounds exhibited a good affinity for the σ 1 subtype, with subnanomolar K i values for the best of them, while only modest or poor affinity for the σ 2 subtype was observed ( Tables 1 and 2 ). Some structureactivity relationships were put forward.

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