Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards sigma(1)- and sigma(2)-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.
Rossi
Daniela
D
Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Urbano
Mariangela
M
Pedrali
Alice
A
Serra
Massimo
M
Zampieri
Daniele
D
Mamolo
Maria Grazia
MG
Laggner
Christian
C
Zanette
Caterina
C
Florio
Chiara
C
Schepmann
Dirk
D
Wuensch
Bernard
B
Azzolina
Ornella
O
Collina
Simona
S
D000475:Alkenes / Q000737:chemistry / Q000494:pharmacology; D000588:Amines / Q000737:chemistry* / Q000494:pharmacology*; D000605:Amino Alcohols / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006168:Guinea Pigs; D006841:Hydrocarbons, Aromatic / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D008958:Models, Molecular; D011485:Protein Binding; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000475:Alkenes; D000588:Amines; D000605:Amino Alcohols; D006841:Hydrocarbons, Aromatic; D008024:Ligands; D011957:Receptors, Opioid; D017480:Receptors, sigma