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.

S. Bova, S. Saponara, A. Rampa, S. Gobbi, L. Cima, F. Fusi, et al. (2009). Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile. JOURNAL OF MEDICINAL CHEMISTRY, 52, 1259-1262 [10.1021/jm801589x].

Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile

RAMPA, ANGELA;GOBBI, SILVIA;BISI, ALESSANDRA
2009

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.
2009
S. Bova, S. Saponara, A. Rampa, S. Gobbi, L. Cima, F. Fusi, et al. (2009). Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile. JOURNAL OF MEDICINAL CHEMISTRY, 52, 1259-1262 [10.1021/jm801589x].
S. Bova; S. Saponara; A. Rampa; S. Gobbi; L. Cima; F. Fusi; G. Sgaragli; M. Cavalli; C. de los Rios; J. Striessnig; A. Bisi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/75673
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