Neuron 1993 Dec 01;116:1013-21. doi: 10.1016/0896-6273(93)90215-d.

Molecular localization of regions in the L-type calcium channel critical for dihydropyridine action.

???displayArticle.abstract???
Sensitivity to dihydropyridines (DHPs) is a distinct characteristic that differentiates L-type Ca2+ channels from T-, N-, and P-type Ca2+ channels. To identify regions necessary for the functional effects of DHPs, chimeric Ca2+ channels were constructed in which portions of motif III or motif IV of a DHP-insensitive brain Ca2+ channel, BI-2, were introduced into the DHP-sensitive cardiac L-type Ca2+ channel. The resultant chimeric Ca2+ channels were expressed in Xenopus oocytes, and the effects of a DHP agonist and antagonist were studied. The results show that the linker region between S5 and S6 in motif IV of the L-type Ca2+ channel is a major site for DHP action. The DHP agonist and antagonist molecules interact with distinct sites on the alpha 1 subunit of the L-type Ca2+ channel. The data further show that the SS2-S6 region of motif III is not involved in DHP action but may be an important structural component of inactivation.

???displayArticle.pubmedLink??? 8274273
???displayArticle.link??? Neuron
???displayArticle.grants??? [+]

Species referenced: Xenopus
Genes referenced: btnl2 dhps dpys