Abstract
Human cerebrocortical synaptic terminals elicited concentration-dependent Ca2+ transients after Ap5A (diadenosine pentaphosphate) and ATP stimulation, with EC50 values of 23.44 +/- 3.70 microM and 11.48 +/- 2.12 microM, respectively. The lack of cross-desensitisation and the selective antagonism by Ip5I (diinosine pentaphosphate), suggests the activation of a dinucleotide receptor by Ap5A, and a P2X receptor by ATP. Ap5A Ca2+ transients were partially abolished by omega-conotoxin GVI-A (53%), suggesting the participation of a N-type Ca2+ channel in the dinucleotide response. ATP effect on Ca2+ entry was abolished by nicardipine (44%) and by omega-conotoxin GVI-A (52%), suggesting the participation of L- and N-type Ca2+ channels. These data suggest that Ap5A and ATP activate dinucleotide and P2X receptors, respectively, in human brain synaptic terminals.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine Triphosphate / pharmacology
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Animals
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Binding, Competitive
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Calcium / pharmacology
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Calcium Channel Blockers / pharmacology
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Cerebral Cortex / physiology*
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Dinucleoside Phosphates / pharmacology
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Humans
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In Vitro Techniques
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Inosine Nucleotides / pharmacology
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Membrane Potentials / drug effects
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Nicardipine / pharmacology
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Nickel / pharmacology
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Presynaptic Terminals / drug effects
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Presynaptic Terminals / metabolism
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Presynaptic Terminals / physiology*
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Purinergic P2 Receptor Antagonists
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Pyridoxal Phosphate / analogs & derivatives
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Pyridoxal Phosphate / pharmacology
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Rabbits
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Receptors, Purinergic P1 / drug effects
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Receptors, Purinergic P1 / metabolism*
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Receptors, Purinergic P2 / metabolism*
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Synaptosomes / drug effects
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Synaptosomes / physiology
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Vasoconstrictor Agents / pharmacology
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Venoms / pharmacology
Substances
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Calcium Channel Blockers
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Dinucleoside Phosphates
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Inosine Nucleotides
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P1
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Receptors, Purinergic P2
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Vasoconstrictor Agents
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Venoms
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pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
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P(1),P(5)-di(adenosine-5'-)pentaphosphate
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Pyridoxal Phosphate
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Nickel
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Adenosine Triphosphate
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Nicardipine
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Calcium