| Literature DB >> 19203272 |
Sergio Bova1, Simona Saponara, Angela Rampa, Silvia Gobbi, Lorenzo Cima, Fabio Fusi, Giampietro Sgaragli, Maurizio Cavalli, Cristobal de los Rios, Jörg Striessnig, Alessandra Bisi.
Abstract
L-Type Ca(2+) channels (LTCCs) play a key role in the regulation of vascular smooth muscle contraction, and substances that interfere with their function (Ca(2+) channel blockers) are widely used in the therapy of hypertension. Here, we report anthracene-maleimide derivatives as new LTCC blockers. Among these, 3, lacking intracellular effects, was investigated in more detail. The results show that 3 binds preferentially to inactivated LTCCs, directly interacting with the pore-forming subunit of the channel.Entities:
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Year: 2009 PMID： 19203272 DOI： 10.1021/jm801589x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446