ArticleBritish journal of pharmacology2004
Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 56 citations in OpenAlex.
- The transdiagnostic use of worry and rumination to avoid negative emotional contrasts following negative events: A momentary assessment study.Journal of anxiety disorders · 2023Article
- CaInternational journal of molecular sciences · 2022Review
- Analgesic effect of a broad-spectrum dihydropyridine inhibitor of voltage-gated calcium channels.Pflugers Archiv : European journal of physiology · 2015Article
- Dissecting fibrosis: therapeutic insights from the small-molecule toolbox.Nature reviews. Drug discovery · 2015Review
- 1,4-Dihydropyridine derivatives with T-type calcium channel blocking activity attenuate inflammatory and neuropathic pain.Pflugers Archiv : European journal of physiology · 2015Article
- Characterization of novel cannabinoid based T-type calcium channel blockers with analgesic effects.ACS chemical neuroscience · 2015Article
- Synthesis and evaluation of 1,4-dihydropyridine derivatives with calcium channel blocking activity.Pflugers Archiv : European journal of physiology · 2014Article
- A molecular signature of tissues with pacemaker activity in the heart and upper urinary tract involves coexpressed hyperpolarization-activated cation and T-type Ca2+ channels.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2014Article
- Identification of L- and T-type Ca2+ channels in rat cerebral arteries: role in myogenic tone development.American journal of physiology. Heart and circulatory physiology · 2013Article
- 1,4-dihydropyridines: the multiple personalities of a blockbuster drug family.Translational medicine @ UniSa · 2012Article
- Modulation of subthalamic T-type Ca(2+) channels remedies locomotor deficits in a rat model of Parkinson disease.The Journal of clinical investigation · 2011Article
- T-type calcium channels and vascular function: the new kid on the block?The Journal of physiology · 2011Review
- Effect of efonidipine on TGF-β1-induced cardiac fibrosis through Smad2-dependent pathway in rat cardiac fibroblasts.Journal of pharmacological sciences · 2011Article
- Dihydropyridine-insensitive calcium currents contribute to function of small cerebral arteries.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2010Article
- Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs.The Journal of pharmacology and experimental therapeutics · 2009Article
- Review
- A selective T-type Ca2+ channel blocker R(-) efonidipine.Naunyn-Schmiedeberg's archives of pharmacology · 2008Article
- Review
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Efonidipine, a derivative of dihydropyridine Ca(2+) antagonist, is known to block both L- and T-type Ca(2+) channels. It remains to be clarified, however, whether efonidipine affects other voltage-dependent Ca(2+) channel subtypes such as N-, P/Q- and R-types, and whether the optical isomers of efonidipine have different selectivities in blocking these Ca(2+) channels, including L- and T-types. To address these issues, the effects of efonidipine and its R(-)- and S(+)-isomers on these Ca(2+) channel subtypes were examined electrophysiologically in the expression systems using Xenopus oocytes and baby hamster kidney cells (BHK tk-ts13). Efonidipine, a mixture of R(-)- and S(+)-isomers, exerted blocking actions on L- and T-types, but no effects on N-, P/Q- and R-type Ca(2+) channels. The selective blocking actions on L- and T-type channels were reproduced by the S(+)-efonidipine isomer. By contrast, the R(-)-efonidipine isomer preferentially blocked T-type channels. The blocking actions of efonidipine and its enantiomers were dependent on holding potentials. These findings indicate that the R(-)-isomer of efonidipine is a specific blocker of the T-type Ca(2+) channel.
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