Structure-activity relationship studies with (+/-)-nantenine derivatives for alpha1-adrenoceptor antagonist activity.

@article{Indra2002StructureactivityRS,
  title={Structure-activity relationship studies with (+/-)-nantenine derivatives for alpha1-adrenoceptor antagonist activity.},
  author={Bachtiar Indra and Kimihiro Matsunaga and Osamu Hoshino and Masaji Suzuki and Hiromichi Ogasawara and Yasushi Ohizumi},
  journal={European journal of pharmacology},
  year={2002},
  volume={437 3},
  pages={173-8}
}
A series of (+/-)-nantenine derivatives of the natural aporphine alkaloids was synthesized and examined for a blocking action on alpha1-adrenoceptors in rat aorta and A10-cells. The potency of these derivatives was compared with that of an aporphine-related compounds (+)-boldine, an alpha1-adrenoceptor antagonist. Among nine (+/-)-nantenine derivatives having different substituents at N-6, C-1, or C-4 of the aporphine skeleton, (+/-)-domesticine had the most powerful alpha1-adrenoceptor… CONTINUE READING

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