NNC 55-0396 [(1S, 2S)-2-(2-(N-[(3-benzimidazol-2-yl) propyl]-N-methylamino) ethyl)-6-fluoro-1, 2, 3, 4-tetrahydro-1-isopropyl-2-naphtyl cyclopropanecarboxylate …

L Huang, BM Keyser, TM Tagmose, JB Hansen… - … of Pharmacology and …, 2004 - ASPET
Mibefradil is a Ca2+ channel antagonist that inhibits both T-type and high-voltage-activated
Ca2+ channels. We previously showed that block of high-voltage-activated channels by …

Towards selective antagonists of T‐type calcium channels: design, characterization and potential applications of NNC 55‐0396

M Li, JB Hansen, L Huang, BM Keyser… - Cardiovascular drug …, 2005 - Wiley Online Library
ABSTRACT NNC 55‐0396 is a structural analog of mibefradil (Ro 40‐5967) that inhibits
both T‐type and high‐voltage‐activated (HVA) Ca2+ channels with a higher selectivity for T …

Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels

C Jiménez, E Bourinet, V Leuranguer, S Richard… - …, 2000 - Elsevier
The voltage gated calcium channel family is a major target for a range of therapeutic drugs.
Mibefradil (Ro 40–5967) belongs to a new chemical class of these molecules which differs …

Actions of Mibefradil, Efonidipine and Nifedipine Block of Recombinant T- and L-Type Ca2+ Channels with Distinct Inhibitory Mechanisms

TS Lee, T Kaku, S Takebayashi, T Uchino, S Miyamoto… - Pharmacology, 2006 - karger.com
We compared detailed efficacy of efonidipine and nifedipine, dihydropyridine analogues,
and mibefradil using recombinant T-and L-type Ca2+ channels expressed separately in …

Inhibition of T-type and L-type calcium channels by mibefradil: physiologic and pharmacologic bases of cardiovascular effects

V Leuranguer, ME Mangoni, J Nargeot… - Journal of …, 2001 - journals.lww.com
Ca 2+ channel antagonists of the dihydropyridine, benzothiazepine, and phenylalkylamine
classes have selective effects on L-type versus T-type Ca 2+ channels. In contrast …

High affinity interaction of mibefradil with voltage‐gated calcium and sodium channels

P Eller, S Berjukov, S Wanner, I Huber… - British journal of …, 2000 - Wiley Online Library
Mibefradil is a novel Ca2+ antagonist which blocks both high‐voltage activated and low
voltage‐activated Ca2+ channels. Although L‐type Ca2+ channel block was demonstrated …

Mibefradil block of cloned T-type calcium channels

RL Martin, JH Lee, LL Cribbs, E Perez-Reyes… - … of Pharmacology and …, 2000 - ASPET
Mibefradil is a tetralol derivative chemically distinct from other calcium channel antagonists.
It is a very effective antihypertensive agent that is thought to achieve its action via a higher …

Contrasting biophysical and pharmacological properties of T-type and R-type calcium channels

AD Randall, RW Tsien - Neuropharmacology, 1997 - Elsevier
In contrast to other kinds of voltage-gated Ca2+ channels, the underlying molecular basis of
T-type and R-type channels is not well-understood. To facilitate comparisons with cloned …

Mibefradil (Ro 40-5967): the first selective T-type Ca2+ channel blocker

SI Ertel, JP Clozel - Expert opinion on investigational drugs, 1997 - Taylor & Francis
Mibefradil is a novel Ca2+ antagonist acting on both L-and T-type Ca2+ channels, with a ten-
fold selectivity for T-type Ca2+ channels. It belongs to a chemical class different from other …

A mibefradil metabolite is a potent intracellular blocker of L-type Ca2+ currents in pancreatic β-cells

S Wu, M Zhang, PA Vest, A Bhattacharjee, L Liu… - Journal of Pharmacology …, 2000 - ASPET
It has been shown that mibefradil (Ro 40-5967) exerts a selective inhibitory effect on T-type
Ca2+ currents, although at higher concentrations it can antagonize high voltage-activated …