Anti-muscarinic activity of a family of C11N5 compounds isolated from Agelas sponges.
In a search for potential target sites for C11N5 compounds obtained from marine sponges of the genus Agelas we evaluated their interaction with muscarinic acetylcholine receptors from rat brain membranes. In competition experiments with 3H-QNB these compounds displayed the following rank order of potency: sceptrin greater than oroidin greater than or equal to dibromosceptrin greater than or equal to clathrodin. Sceptrin (50 microM) was shown to be a competitive inhibitor of 3H-QNB binding as revealed by Scatchard analysis. The results demonstrate the ability of these compounds to interact with multiple target molecules in the micromolar range.
Rosa
R
R
Department of Chemistry, University of Puerto Rico, San Juan.
Silva
W
W
Escalona de Motta
G
G
Rodríguez
A D
AD
Morales
J J
JJ
Ortiz
M
M
D000470:Alkaloids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000648:ultrastructure; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D010276:Parasympatholytics / Q000737:chemistry / Q000302:isolation & purification* / Q000378:metabolism; D011161:Porifera / Q000737:chemistry*; D011758:Pyrroles / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000378:metabolism
D000470:Alkaloids; D010276:Parasympatholytics; D011758:Pyrroles; D011976:Receptors, Muscarinic; C077212:dibromosceptrin; C077211:clathrodin; C077210:sceptrin; C077209:oroidin