title: T-type calcium channel blockers - new and notable.
abstract: Since cloning of the T-type or Ca(V)3.n calcium channel family in 1998-1999 much progress was made in investigation of their regulation. Most effective metal Ca(V)3 channel blockers are trivalent cations from lanthanide group together with transition metals La(3+) and Y(3+). Divalent cations Zn(2+), Cu(2+) and Ni(2+) inhibit Ca(V)3.2 channels more efficiently than Ca(V)3.1 and Ca(V)3.3 channels via second high-affinity binding site including histidine H191 specific for the Ca(V)3.2 channel. Dihydropyridines and phenylalkylamines in addition to block of L-type calcium channel can inhibit Ca(V)3 channels in clinically relevant concentration.
authors: Institute of Molecular Physiology and Genetics, Slovak Academy of Sciences, Bratislava, Slovak Republic. lubica.lacinova@savba.sk
authors: L'ubica
authors: L
authors: Lacinová
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000737:chemistry / Q000378:metabolism*; D002412:Cations; D003300:Copper / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D009532:Nickel / Q000737:chemistry; D015032:Zinc / Q000737:chemistry
chemical_list: C121855:CACNA1G protein, human; C479952:CACNA1H protein, human; C469757:CACNA1I protein, human; D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D002412:Cations; D003300:Copper; D009532:Nickel; D015032:Zinc