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Title: Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma

Abstract

Propionyl-L-carnitine (PC) protects perfused rat hearts against damage by ischemia-reperfusion. Activation of L-type calcium channel play a role on ischemia-reperfusion damage. Therefore, we studied the effect of PC on some properties of L-type calcium channels in an in vitro preparation from human myocardium sarcolemma (from patients with idiopathic dilated cardiomyopathy). Binding of the L-type calcium channel blockers isradipine ({sup 3}H)-PN 200-110 (PN) to plasma membrane preparations revealed a single population of binding sites (total number: Bmax = 213 +/- 34 fM/mg protein and affinity: Kd = 152 +/- 19 nM; n = 6). The characteristics of these binding sites were evaluated in the presence and in the absence of Ca{sup 2}{sup +} and of calcium blockers (D-888, a verapamillike drug, and diltiazem). Incubation in a Ca{sup 2}{sup +}-containing buffer increased the affinity of PN binding sites. Binding sites for PN were modulated by organic calcium channel blockers; in competition isotherms at 37{degree}C, D-888 (desmethoxyverapamil) decreased the PN binding, whereas diltiazem increased it. These results strongly suggest that the site labelled by PN is the voltage-operated calcium channel of the human myocardium. The addition of PC (1 mM) to plasma membranes labelled with PN at 37{degree}C decreased the affinity of themore » binding; this effect was counteracted by the addition of Ca{sup 2}{sup +} to the medium. This result was consistent with a competition between Ca{sup 2}{sup +} and PC. The effect of PC incubation at 4{degree}C was the opposite; at this temperature PC increased the affinity of the binding sites and the effect was obscured by Ca{sup 2}{sup +}.« less

Authors:
; ;  [1]
  1. Servizio di Endocrinologia, Milano, (Italy)
Publication Date:
OSTI Identifier:
5545200
Resource Type:
Journal Article
Journal Name:
Cardiovascular Drugs and Therapy; (USA)
Additional Journal Information:
Journal Volume: 5 Suppl 1; Journal ID: ISSN 0920-3206
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; CARNITINE; BIOLOGICAL FUNCTIONS; ISCHEMIA; PATHOGENESIS; PORINS; BIOCHEMICAL REACTION KINETICS; AFFINITY; CALCIUM; CELL MEMBRANES; HEART; IN VITRO; MAN; MYOCARDIUM; OXADIAZOLES; PERFUSED ORGANS; RECEPTORS; TRACER TECHNIQUES; TRITIUM COMPOUNDS; ALKALINE EARTH METALS; AMINO ACIDS; ANEMIAS; ANIMALS; AZOLES; BODY; CARBOXYLIC ACIDS; CARDIOVASCULAR DISEASES; CARDIOVASCULAR SYSTEM; CELL CONSTITUENTS; DISEASES; ELEMENTS; HEMIC DISEASES; HETEROCYCLIC COMPOUNDS; HYDROGEN COMPOUNDS; HYDROXY ACIDS; ISOTOPE APPLICATIONS; KINETICS; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; METALS; MUSCLES; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC OXYGEN COMPOUNDS; ORGANS; PRIMATES; PROTEINS; REACTION KINETICS; SYMPTOMS; VASCULAR DISEASES; VERTEBRATES; VITAMIN B GROUP; VITAMINS; 550901* - Pathology- Tracer Techniques

Citation Formats

Bevilacqua, M, Vago, T, and Norbiato, G. Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma. United States: N. p., 1991. Web. doi:10.1007/BF00128241.
Bevilacqua, M, Vago, T, & Norbiato, G. Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma. United States. https://doi.org/10.1007/BF00128241
Bevilacqua, M, Vago, T, and Norbiato, G. 1991. "Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma". United States. https://doi.org/10.1007/BF00128241.
@article{osti_5545200,
title = {Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma},
author = {Bevilacqua, M and Vago, T and Norbiato, G},
abstractNote = {Propionyl-L-carnitine (PC) protects perfused rat hearts against damage by ischemia-reperfusion. Activation of L-type calcium channel play a role on ischemia-reperfusion damage. Therefore, we studied the effect of PC on some properties of L-type calcium channels in an in vitro preparation from human myocardium sarcolemma (from patients with idiopathic dilated cardiomyopathy). Binding of the L-type calcium channel blockers isradipine ({sup 3}H)-PN 200-110 (PN) to plasma membrane preparations revealed a single population of binding sites (total number: Bmax = 213 +/- 34 fM/mg protein and affinity: Kd = 152 +/- 19 nM; n = 6). The characteristics of these binding sites were evaluated in the presence and in the absence of Ca{sup 2}{sup +} and of calcium blockers (D-888, a verapamillike drug, and diltiazem). Incubation in a Ca{sup 2}{sup +}-containing buffer increased the affinity of PN binding sites. Binding sites for PN were modulated by organic calcium channel blockers; in competition isotherms at 37{degree}C, D-888 (desmethoxyverapamil) decreased the PN binding, whereas diltiazem increased it. These results strongly suggest that the site labelled by PN is the voltage-operated calcium channel of the human myocardium. The addition of PC (1 mM) to plasma membranes labelled with PN at 37{degree}C decreased the affinity of the binding; this effect was counteracted by the addition of Ca{sup 2}{sup +} to the medium. This result was consistent with a competition between Ca{sup 2}{sup +} and PC. The effect of PC incubation at 4{degree}C was the opposite; at this temperature PC increased the affinity of the binding sites and the effect was obscured by Ca{sup 2}{sup +}.},
doi = {10.1007/BF00128241},
url = {https://www.osti.gov/biblio/5545200}, journal = {Cardiovascular Drugs and Therapy; (USA)},
issn = {0920-3206},
number = ,
volume = 5 Suppl 1,
place = {United States},
year = {Fri Feb 01 00:00:00 EST 1991},
month = {Fri Feb 01 00:00:00 EST 1991}
}