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EnglishL-Type Ca2+ channels (LTCCs) play a key role in the regulation of vascular smooth muscle contraction, and substances that interfere with their function (Ca2+ 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 poreforming subunit of the channel.
| Titolo: | Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile |
| Autore/i: | S. Bova; S. Saponara; RAMPA, ANGELA; GOBBI, SILVIA; L. Cima; F. Fusi; G. Sgaragli; M. Cavalli; C. de los Rios; J. Striessnig; BISI, ALESSANDRA |
| Autore/i Unibo: | |
| Anno: | 2009 |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm801589x |
| Abstract: | L-Type Ca2+ channels (LTCCs) play a key role in the regulation of vascular smooth muscle contraction, and substances that interfere with their function (Ca2+ 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 poreforming subunit of the channel. |
| Data prodotto definitivo in UGOV: | 2009-03-30 18:59:00 |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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