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Displacement activity of some natural cularine alkaloids at striatal3H-SCH 23 390 and3H-raclopride binding sites |
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| Authors: | P. Protais D. Cortes J. -L. Pons S. Lopez M. C. Villaverde L. Castedo |
| Affiliation: | (1) Laboratoire de Physiologie (Pharmacochimie), U.F.R. de Médecine-Pharmacie, Université de Rouen, B.P. 97, F-76 803 Saint Etienne Rouvray cedex, (France);(2) Laboratoire de Pharmacognosie (Pharmacochimie), U.F.R. de Médecine-Pharmacie, Université de Rouen, B.P. 97, F-76 803 Saint Etienne Rouvray cedex, (France);(3) Laboratoire de Microbiologie (Pharmacochimie), U.F.R. de Médecine-Pharmacie, Université de Rouen, B.P. 97, F-76 803 Saint Etienne Rouvray cedex, (France);(4) Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad de Santiago, E-15 706 Santiago de Compostela, (Spain) |
| Abstract: | Five natural cularines isolated from the aerial parts ofSarcocapnos crassifolia (Fumariaceae) and a cularioid isolated from the bark ofGuatteria ouregou (Annonaceae) were tested for their ability to displace3H-SCH 23 390 and3H-raclopride from their striatal binding sites. Celtisine, breoganine and cularidine were able to inhibit the binding at D-1 and D-2 dopaminergic sites at nanomolar concentrations. Other alkaloids were active at micromolar concentrations. These data suggest that the presence of an oxepine system in the isoquinoline skeleton could lead to compounds which would be very active and possibly selective at dopaminergic receptor sites. |
| Keywords: | Cularines isoquinoline alkaloids 3H-SCH 23 390 3H-raclopride dopamine D-1/D-2 receptors |
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