Structural features important for sigma 1 receptor binding.
J Med Chem
; 37(8): 1214-9, 1994 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-8164264
ABSTRACT
Two problems that have hampered sigma receptor research are (i) a lack of high-affinity agents and (ii) the recent identification of multiple populations of sigma receptors (i.e., sigma 1 and sigma 2 sites). Recently, several high-affinity sigma ligands have been identified, and the term superpotent sigma ligands has been coined to describe agents with Ki values of < 1 nM. We have previously shown that appropriately N-substituted phenylalkylamines bind at sigma receptors with high affinity. In the present investigation, we examine the structure-affinity relationships of these phenylalkylamine derivatives for sigma 1 binding and describe some of the first superpotent sigma 1 ligands. A binding model was developed to account for the structural features of the phenylalkylamines that appear to be important for the interaction of these agents with sigma 1 sites.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores sigma
/
Aminas
Limite:
Animals
Idioma:
En
Ano de publicação:
1994
Tipo de documento:
Article