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mM Ca2+ (mm + ca2+)

Distribution by Scientific Domains

Medical Sciences	50%

Selected Abstracts

Dynamics of P2X7 receptor pore dilation: Pharmacological and functional consequences

DRUG DEVELOPMENT RESEARCH, Issue 2-3 2001
I.P. Chessell
Abstract The biophysical and functional properties of the human P2X7 receptor, expressed recombinantly in HEK-293 cells or natively in THP-1 pro-monocytic cells, were investigated in the context of pore dilation and externalisation of mature interleukin 1, (IL1,). In HEK-293 cells, the agonist 2,- and 3,-O-(4-benzoylbenzoyl)-ATP (BzATP) caused concentration-dependent inward currents (EC50 59 ,M) and with prolonged application this agonist caused a gradual increase in inward current culminating in a plateau. This increase in current was associated with pore dilation, determined by intracellular accumulation of YO-PRO-1. BzATP displayed increased potency at the pore-dilated form of the P2X7 receptor (EC50 17 ,M), and positive correlations between apparent receptor density and speed of pore dilation were observed. A monoclonal antibody selectively blocked current mediated by the naïve receptor, while currents through pore-dilated receptors were not significantly affected, which together suggest a conformational change at the level of the receptor during the dilation event. The release of mature IL1, from THP-1 cells was independent of P2X7 -mediated cell lysis, as determined by study of lactate dehydrogenase release. Moreover, using conditions designed to minimise pore dilation (using buffers containing 2 mM Ca2+ and 1 mM Mg2+), BzATP caused significant release of IL1,, but without concomitant YO-PRO-1 accumulation, indicating pore dilation is not required for IL1, release. In addition, short (4-min) incubation of THP-1 cells with BzATP (terminated by enzymatic degradation of BzATP using apyrase) resulted in significant quantities of IL1, release some 60 min later, suggesting commitment of cells to release IL1, can be triggered with only brief receptor ligation. These findings suggest that receptor expression and ligation time are critical factors for selecting multiple functional states of P2X7. Drug Dev. Res. 53:60,65, 2001. © 2001 Wiley-Liss, Inc. [source]

The Effect of Carbachol and ,-Bungarotoxin on the Frequency of Miniature Endplate Potentials at the Frog Neuromuscular Junction

EXPERIMENTAL PHYSIOLOGY, Issue 2 2000
Ela Bukharaeva
The effects of an acetylcholine analogue, carbachol (CCh), and a purified irreversible nicotinic antagonist, ,-bungarotoxin (BTX), on the frequency of the miniature endplate potentials (mEPPs) at the neuromuscular junction of the frog were tested at 20 and 10°C. CCh (5 ± 10-6 m) reduced the frequency of mEPPs to about 60%; this reduction was not affected by 1 ± 10-7 g ml-1 BTX. BTX also reversibly decreased the mEPP frequency by 40%, but not in the presence of CCh or in Ringer solution with 0 or 8 mM Ca2+. The present data show that BTX, which inhibits a class of nicotinic ACh receptors, does not block the decrease of mEPP frequency evoked by CCh and can itself suppress the frequency of spontaneous quantal release. [source]

Monetite (CaHPO4) Synthesis in Ethanol at Room Temperature

JOURNAL OF THE AMERICAN CERAMIC SOCIETY, Issue 12 2009
A. Cuneyt Tas
A straightforward process was developed to synthesize monetite (CaHPO4, dicalcium phosphate anhydrous) powders at room temperature (21°±1°C) in ethanol solutions. The process reported here constitutes an alternative to well-publicized monetite synthesis procedures based on the dehydration of brushite (CaHPO4·2H2O, dicalcium phosphate dihydrate) powders either in acidic, hot (70°,95°C) aqueous solutions or in drying ovens (200°,225°C). Submicrometer monetite powders were synthesized in ethanol (ethyl alcohol) solutions containing small aliquots of concentrated H3PO4 (orthophosphoric acid, 85%). Precipitated CaCO3 (calcium carbonate, calcite form) powders with submicrometer particles were simply stirred in the above solutions in glass bottles for 3 h. The starting Ca/P molar ratio in the synthesis bottles was 0.50. Monetite powders obtained with a stacked-nanosheets particle texture did not contain any unreacted CaCO3. Monetite powders were also found to have the ability to completely transform into apatitic (apatite-like) calcium phosphate powders when soaked in calcium-containing saline solutions (i.e., 142 mM Na+, 5 mM K+, and 50 mM Ca2+ in water) for 6 days at 37°C. [source]

Lindane (,-Hexachlorocyclohexane) Induces Internal Ca2+ Release and Capacitative Ca2+ Entry in Madin-Darby Canine Kidney Cells

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 4 2000
Cheng-Hsien Lu
The effect of lindane (,-hexachlorocyclohexane), an organochlorine pesticide, on Ca2+ mobilization in Madin-Darby canine kidney cells was examined by fluorimetry using fura-2 as a Ca2+ indicator. Lindane (5,200 ,M) increased [Ca2+]i concentration-dependently. The [Ca2+]i signal comprised an immediate initial rise followed by a persistent phase. Ca2+ removal inhibited the [Ca2+]i signal by reducing both the initial rise and the sustained phase. This implies lindane-triggered Ca2+ influx and Ca2+ release. In Ca2+ -free medium, 0.15 mM lindane increased [Ca2+]i after pretreatment with carbonylcyanide m-chlorophenylhydrazone (CCCP; 2 ,M), a mitochondrial uncoupler, and two endoplasmic reticulum Ca2+ pump inhibitors, thapsigargin and cyclopiazonic acid. Conversely, pretreatment with lindane abolished CCCP- and thapsigargin-induced Ca2+ release. This suggests that 0.15 mM lindane released Ca2+ from the endoplasmic reticulum, mitochondria and other stores. La3+ (1 mM) partly inhibited 0.1 mM lindane-induced [Ca2+]i increase, confirming that lindane induced Ca2+ influx. Addition of 3 mM Ca2+ increased [Ca2+]i after pretreatment with 0.15 mM lindane for 750 sec. in Ca2+ -free medium, which indicates lindane-induced capacitative Ca2+ entry. Lindane (0.15 mM)-induced Ca2+ release was not reduced by inhibiting phospholipase C with 2 ,M U73122, but was inhibited by 70% by the phospholipase A2 inhibitor aristolochic acid (40 ,M). [source]