Solution structure of the calcium channel antagonist ω-conotoxin GVIA
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چکیده
منابع مشابه
Opioid Receptor-Mediated Inhibition of v-Conotoxin GVIA-Sensitive Calcium Channel Currents in Rat Intracardiac Neurons
Adams, David J. and Carlo Trequattrini. Opioid receptor-medinized the effects of these substances in rabbit (Weitzell et ated inhibition of v-conotoxin GVIA-sensitive calcium channel al. 1984) and canine heart (Musha et al. 1989). currents in rat intracardiac neurons. J. Neurophysiol. 79: 753–762, Endogenous opioid peptides were found in rat and guinea 1998. Modulation of depolarization-activat...
متن کاملOpioid receptor-mediated inhibition of omega-conotoxin GVIA-sensitive calcium channel currents in rat intracardiac neurons.
Modulation of depolarization-activated ionic conductances by opioid receptor agonists was investigated in isolated parasympathetic neurons from neonatal rat intracardiac ganglia by using the whole cell perforated patch clamp technique. Met-enkephalin (10 muM) altered the action potential waveform, reducing the maximum amplitude and slowing the rate of rise and repolarization but the afterhyperp...
متن کاملBrain voltage-sensitive calcium channel subtypes differentiated by omega-conotoxin fraction GVIA.
We have studied the voltage-activated influx of Ca2+ into synaptosomes. Rapid 45Ca2+ influx into synaptosomes, measured at 1 sec, was blocked by predepolarization and by low concentrations of cadmium (IC50, 1 microM), as anticipated for voltage-sensitive calcium channels (VSCCs). However, fluxes were insensitive to dihydropyridine drugs that block or activate VSCCs, including nitrendipine, Bay ...
متن کاملω-Conotoxin GVIA Mimetics that Bind and Inhibit Neuronal Cav2.2 Ion Channels
The neuronal voltage-gated N-type calcium channel (Ca(v)2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and tested using three experimental measures of calcium channel blockade. These consisted of a ¹²⁵I-ω-conotoxin GVIA displacement assay, a fluorescen...
متن کاملThree-dimensional solution structure of the calcium channel antagonist omega-agatoxin IVA: consensus molecular folding of calcium channel blockers.
The three-dimensional solution structure of omega-agatoxin IVA, which is a specific blocker of the P-type calcium channel isolated from funnel web spider venom and has a molecular mass of 5.2 kDa, was determined by two dimensional 1H NMR spectroscopy, combined with simulated annealing calculations. On the basis of 563 experimental constraints, including 516 distance constraints obtained from th...
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ژورنال
عنوان ژورنال: Protein Science
سال: 1993
ISSN: 0961-8368,1469-896X
DOI: 10.1002/pro.5560021005