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.

Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile / S. Bova; S. Saponara; A. Rampa; S. Gobbi; L. Cima; F. Fusi; G. Sgaragli; M. Cavalli; C. de los Rios; J. Striessnig; A. Bisi. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 52:(2009), pp. 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
Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile / S. Bova; S. Saponara; A. Rampa; S. Gobbi; L. Cima; F. Fusi; G. Sgaragli; M. Cavalli; C. de los Rios; J. Striessnig; A. Bisi. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 52:(2009), pp. 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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