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.
Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-DAMP / Melchiorre C.; Minarini A.; Spampinato S.; Tumiatti V.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 5:8(1995), pp. 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.
