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Anti-muscarinic activity of a family of C11N5 compounds isolated fromAgelas sponges |
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| Authors: | R Rosa W Silva G Escalona de Motta A D Rodríguez J J Morales M Ortiz |
| Institution: | (1) Department of Chemistry, University of Puerto Rico, Blvd del Valle 201, 00901 San Juan, Puerto Rico, USA;(2) Department of Pharmacology, Universidad Central del Caribe, School of Medicine, Blvd del Valle 201, 00901 San Juan, Puerto Rico, USA;(3) Institute of Neurobiology, Medical Sciences Campus, University of Puerto Rico, Blvd del Valle 201, 00901 San Juan, Puerto Rico, USA |
| Abstract: | In a search for potential target sites for C11N5 compounds obtained from marine sponges of the genusAgelas we evaluated their interaction with muscarinic acetylcholine receptors from rat brain membranes. In competition experiments with3H-QNB these compounds displayed the following rank order of potency: sceptrin>oroidin dibromosceptrinclathrodin. Sceptrin (50  M) was shown to be a competitive inhibitor of3H-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. |
| Keywords: | Marine sponges muscarinic receptor sceptrin oroidin dibromosceptrin clathrodin |
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