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Acylating phencyclidines irreversibly enhance brain calcium antagonist binding
Pharmacology, Biochemistry, and Behavior
|July 1, 1986
Summary
Phencyclidine (PCP) derivatives like FOURPHIT irreversibly bind to calcium channels, unlike PCP itself. This irreversible interaction offers a new tool for studying PCP
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- Phencyclidine (PCP) is known to allosterically modulate dihydropyridine calcium antagonist binding sites.
- Previous studies indicated reversible interactions of PCP with these sites.
Purpose of the Study:
- To investigate the irreversible interaction of phencyclidine derivatives with dihydropyridine calcium antagonist binding sites.
- To explore the potential of FOURPHIT as a tool for studying PCP interactions.
Main Methods:
- Treatment of mouse forebrain synaptosomal membranes with FOURPHIT and METAPHIT.
- Measurement of [3H]nitrendipine binding affinity.
- Assessment of the effects of phencyclidine on FOURPHIT-induced changes.
Main Results:
- FOURPHIT caused a concentration-dependent, irreversible increase in [3H]nitrendipine apparent affinity.
- METAPHIT also irreversibly increased affinity but was less potent than FOURPHIT.
- Phencyclidine blocked the irreversible affinity increase induced by FOURPHIT.
- FOURPHIT altered interactions of cations and diltiazem with the binding site.
Conclusions:
- FOURPHIT irreversibly interacts with the same sites as PCP.
- FOURPHIT serves as a valuable tool for probing PCP's behavioral and biochemical interactions with dihydropyridine calcium antagonist binding sites.