Sigma receptor binding profile of a series of analgesic tropane derivatives.
The binding profile on sigma receptor subtypes of a family of tropane derivatives, previously studied as analgesic and nootropic drugs, is reported. The results show that the sigma receptors are not involved in the enhancement of acetylcholine release and of the consequent analgesic activity of this class of drugs. Structure-affinity relationships for sigma receptor subtypes are discussed. They lead to the identification of a few useful leads for further development of potent sigma ligands within the series.
Prezzavento
Orazio
O
Dipartimento di Scienze Framaceutiche, Università di Firenze, Firenze, Italy.
Gualtieri
Fulvio
F
Marrazzo
Agostino
A
Romanelli
Maria Novella
MN
Ronsisvalle
Giuseppe
G
Teodori
Elisabetta
E
D000700:Analgesics / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001923:Brain Chemistry; D006168:Guinea Pigs; D011485:Protein Binding; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014326:Tropanes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
D000700:Analgesics; D017480:Receptors, sigma; D014326:Tropanes