On the kaliotoxin and dendrotoxin binding sites on rat brain synaptosomes

Citation
N. Tricaud et al., On the kaliotoxin and dendrotoxin binding sites on rat brain synaptosomes, TOXICON, 38(12), 2000, pp. 1749-1758
Citations number
26
Categorie Soggetti
Pharmacology & Toxicology
Journal title
TOXICON
ISSN journal
00410101 → ACNP
Volume
38
Issue
12
Year of publication
2000
Pages
1749 - 1758
Database
ISI
SICI code
0041-0101(200012)38:12<1749:OTKADB>2.0.ZU;2-5
Abstract
The toxic polypeptides alpha- beta-, gamma- and delta-dendrotoxin (DTX), kn own to be potent blockers of voltage-dependent potassium channels of the K nu 1 family, were purified from the venom of the green mamba Dendroaspis an gusticeps. Their binding behaviour to synaptosomal membranes of rat brain w as analysed and compared with that of kaliotoxin (KTX), in a competition as say using [I-125] KTX. alpha-DTX and delta-DTX were found to compete with r adioiodinated-KTX (IC50 of 8 pM and 0.2 nM respectively), whereas gamma-DTX did not. Several minor components that competed with radioiodinated-KTX bi nding were identified and characterised chemically and biologically. (C) 20 00 Elsevier Science Ltd. All rights reserved.