F90927: a new member in the class of cardioactive steroids

Keller, Markus; Pignier, Christophe; Egger, Marcel; Niggli, Ernst (2007). F90927: a new member in the class of cardioactive steroids. Cardiovascular drug reviews, 25(3), pp. 210-20. New York, N.Y.: Raven Press 10.1111/j.1527-3466.2007.00014.x

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F90927 is a newly developed cardioactive drug with a steroid-like structure. It acts directly and agonistically on the cardiac L-type Ca2+ channel by shifting its voltage-dependent activation toward more negative potentials. This leads to an increased influx of Ca2+ and, therefore, to a stronger contraction; however, no arrhythmias occur. Calcium current stimulation can already be observed at nanomolar concentrations, but higher concentrations of F90927 elevate intracellular Ca2+ concentration, causing a reduction of the myocardial compliance and an increased diastolic blood pressure. Vessels also react to F90927 and contract in its presence. Binding of F90927 with the L-type Ca2+ channel presumably occurs in the vicinity of the transmembrane domains III and IV of the alpha1 subunit. F90927 exhibits no use dependence and interacts with Ca2+ channel inhibitors of all three known classes of channel modulators (dihydropyridines, phenylalkylamines, and benzothiazepines), suggesting that it is a member of a new class of Ca2+ channel modulators. Due to its adverse effects on blood pressure and vessel contraction, F90927 is not an ideal drug candidate. It has, however, some unique properties, which makes it a promising tool to study the function of the L-type Ca2+ channel.

Item Type:	Journal Article (Original Article)
Division/Institute:	04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Physiology
UniBE Contributor:	Niggli, Ernst
ISSN:	0897-5957
ISBN:	17919256
Publisher:	Raven Press
Language:	English
Submitter:	Factscience Import
Date Deposited:	04 Oct 2013 14:53
Last Modified:	05 Dec 2022 14:16
Publisher DOI:	10.1111/j.1527-3466.2007.00014.x
PubMed ID:	17919256
Web of Science ID:	000249953700002
URI:	https://boris.unibe.ch/id/eprint/22290 (FactScience: 33900)