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.
Bova, S., Saponara, S., Rampa, A., Gobbi, S., Cima, L., Fusi, F., et al. (2009). Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile. JOURNAL OF MEDICINAL CHEMISTRY, 52(5), 1259-1262 [10.1021/jm801589x].
Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile
SAPONARA, SIMONA;FUSI, FABIO;SGARAGLI, GIAN PIETRO;
2009-01-01
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.
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https://hdl.handle.net/11365/2503
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