DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME TETRAAMINES RELATEDTO METHOCTRAMINE AND 4-DAMP

Authors
MELCHIORRE C MINARINI A SPAMPINATO S TUMIATTI V
Citation
C. Melchiorre et al., DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME TETRAAMINES RELATEDTO METHOCTRAMINE AND 4-DAMP, Bioorganic & medicinal chemistry letters, 5(8), 1995, pp. 785-790
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
8
Year of publication
1995
Pages
785 - 790
Database
ISI
SICI code
0960-894X(1995)5:8<785:DSABOS>2.0.ZU;2-5
Abstract
Three novel tetraamines (1-3) related to methoctramine were designed, and their biological profiles at muscarinic receptor subtypes were ass essed by binding assays. It turned out that the constrained analogue s pirotramine (3, FC 15-94) of 4-DAMP has an affinity profile better tha n that of pirenzepine owing to a high affinity for muscarinic M(1) rec eptors and a significantly lower affinity for the M(2), M(3) and M(4) subtypes.