Chiral arylpyrrolidinols: preparation and biological profile.
The preparation and biological evaluation of a new class of arylpyrrolidinols is reported. The antinociceptive activity was evaluated in vivo with the hot plate test (HPT) and formalin test (FT), excluding any involvement on motor coordination with the rota-rod test (RRT). The nociceptive behavior in the late phase of FT (representative of chronic pain) suggests an involvement of the antiinflammatory process and it is clearly influenced by the stereochemical features, being the eutomer of phenylpyrrolidinols, the (2R,3S) enantiomer. Despite this, a specific mechanism of action is not yet clarified.
Collina
Simona
S
Dipartimento di Chimica Farmaceutica, Università di Pavia, Viale Taramelli, 12, I-27100 Pavia, Italy. simona.collina@unipv.it
Rossi
Daniela
D
Loddo
Guya
G
Barbieri
Annalisa
A
Lanza
Enrica
E
Linati
Laura
L
Alcaro
Stefano
S
Gallelli
Andrea
A
Azzolina
Ornella
O
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D018360:Crystallography, X-Ray; D008297:Male; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement / Q000187:drug effects; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*
D000700:Analgesics; D011759:Pyrrolidines