Characteristics of [125I]omega-conotoxin MVIIA binding to rat neocortical membranes.
[125I]omega-Conotoxin MVIIA (omega-CTM) binding to N-type voltage-sensitive calcium channels (VSCCs) was characterized using rat neocortical membranes. [125I]omega-CTM bound rapidly and with high affinity; these parameters were similar to binding using omega-conotoxin GVIA ([125I]omega-CTG). Unlike [125I]omega-CTG, however, [125I]omega-CTM readily dissociated from its binding site. Monovalent and divalent cations, polyamines, and aminoglycosides inhibited [125I]omega-CTM binding. Since [125I]omega-CTM appears to bind to the same site as [125I]omega-CTG in mammalian neurons, the reversibility of [125I]omega-CTM binding makes this ligand preferable for equilibrium binding analyses.
Stoehr
S J
SJ
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48106-1047.
Dooley
D J
DJ
D000595:Amino Acid Sequence; D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology; D015220:Calcium Channels / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism*; D006801:Humans; D008297:Male; D008566:Membranes / Q000378:metabolism; D008969:Molecular Sequence Data; D009355:Neomycin / Q000494:pharmacology; D009474:Neurons / Q000378:metabolism; D010455:Peptides / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013096:Spermine / Q000494:pharmacology; D020866:omega-Conotoxin GVIA; D020960:omega-Conotoxins
D002121:Calcium Channel Blockers; D015220:Calcium Channels; D010455:Peptides; D020960:omega-Conotoxins; D013096:Spermine; C078452:ziconotide; D020866:omega-Conotoxin GVIA; D009355:Neomycin