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EnglishAs analogues of some conformationally restricted spiropiperidine derivatives which are endowed with high affinity for σ1 receptor, a set of 16 spiro[1,2,4-benzotriazine-3(4H),4'-(1'-substituted)piperidines] and congeneric compounds was prepared and tested for affinity to σ1 receptor subtype. All N-arylalkyl substituted derivatives exhibited high affinity for the relevant receptor, with Ki in the low nanomolar range. Affinity for σ2 subtype (assayed only for a few representative compounds) was from one to three order of magnitude lower. Spiro[1,2,4-benzotriazine-3(4H),4'-(1'-benzyl)piperidine] (2), with a ratio Kiσ2/Kiσ1/7000 should represent the most selective s1 ligand so far described.
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| Titolo: | Spiro[1,2,4-benzotriazine-3(4H),4’-(1’-substituted)-piperidines] and related compounds as ligands for sigma receptors |
| Autori: | |
| Data di pubblicazione: | 2002 |
| Rivista: | |
| Abstract: | As analogues of some conformationally restricted spiropiperidine derivatives which are endowed with high affinity for σ1 receptor, a set of 16 spiro[1,2,4-benzotriazine-3(4H),4'-(1'-substituted)piperidines] and congeneric compounds was prepared and tested for affinity to σ1 receptor subtype. All N-arylalkyl substituted derivatives exhibited high affinity for the relevant receptor, with Ki in the low nanomolar range. Affinity for σ2 subtype (assayed only for a few representative compounds) was from one to three order of magnitude lower. Spiro[1,2,4-benzotriazine-3(4H),4'-(1'-benzyl)piperidine] (2), with a ratio Kiσ2/Kiσ1/7000 should represent the most selective s1 ligand so far described. |
| Handle: | http://hdl.handle.net/11567/211741 |
| Appare nelle tipologie: | 01.01 - Articolo su rivista |
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