Three novel tetraamines (1-3) related to methoctramine were designed, and their biological profiles at muscarinic receptor subtypes were assessed by binding assays. It turned out that the constrained analogue spirotramine (3, FC 15-94) of 4-DAMP has an affinity profile better than that of pirenzepine owing to a high affinity for muscarinic M(1) receptors and a significantly lower affinity for the M(2), M(3) and M(4) subtypes.
Melchiorre C., Minarini A., Spampinato S., Tumiatti V. (1995). Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-DAMP. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 5(8), 785-790 [10.1016/0960-894X(95)00113-8].
Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-DAMP
Melchiorre C.
;Minarini A.;Spampinato S.;Tumiatti V.
1995
Abstract
Three novel tetraamines (1-3) related to methoctramine were designed, and their biological profiles at muscarinic receptor subtypes were assessed by binding assays. It turned out that the constrained analogue spirotramine (3, FC 15-94) of 4-DAMP has an affinity profile better than that of pirenzepine owing to a high affinity for muscarinic M(1) receptors and a significantly lower affinity for the M(2), M(3) and M(4) subtypes.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
