Two constrained analogues (4a and 4b) of both 4-DAMP (1) and spiro-DAMP (2) were designed, and their biological profiles at muscarinic receptor subtypes were assessed by functional and binding assays. It turned out that these constrained analogues display a modest, if any, M2/M3 selectivity ratio. However, most interestingly, they proved to be highly selective for muscarinic M1 receptors. © 1995.
Tumiatti V., Santi S., Recanatini M., Minarini A., Melchiorre C., Chiarini A., et al. (1995). Design, synthesis and biological activity of some 4-DAMP- related compounds. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 5(20), 2325-2330 [10.1016/0960-894X(95)00403-G].
Design, synthesis and biological activity of some 4-DAMP- related compounds
Tumiatti V.;Santi S.;Recanatini M.;Minarini A.;Melchiorre C.;Chiarini A.;Budriesi R.
1995
Abstract
Two constrained analogues (4a and 4b) of both 4-DAMP (1) and spiro-DAMP (2) were designed, and their biological profiles at muscarinic receptor subtypes were assessed by functional and binding assays. It turned out that these constrained analogues display a modest, if any, M2/M3 selectivity ratio. However, most interestingly, they proved to be highly selective for muscarinic M1 receptors. © 1995.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
