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A - Bungarotoxin

Acetylcholine nicotinic (LGIC) Na+, K+ and Ca2 + conductance Nicotine, suxamethonium Tubocurarine, a-conotoxins, a-bungarotoxin... [Pg.1172]

Peptides in the a-conotoxin family are inhibitors of nicotinic acetylcholine receptors. They were first isolated from C. geographus venom as components which cause paralysis in mice and fish when injected intraperitoneally (27). Early physiological experiments (28) indicated that a-conotoxins GI, GII, and GIA (see Table III) all act at the muscle end plate region. Mini end-plate potentials and end plate potentials evoked in response to nerve stimulation are inhibited in the presence of a-conotoxins in the nM to pM range. a-Conotoxin GI was subsequently shown to compete with rf-tubocurarine and a-bungarotoxin for the acetylcholine receptor (29). [Pg.271]

Radioiodinated derivatives have been prepared to define more closely the target site of a-conotoxins on the acetylcholine receptor (R. Myers, unpublished data). In membrane preparations from Torpedo electroplax, photoactivatable azidosalicylate derivatives of a-conotoxin GIA preferentially label the p and 7 subunits of the acetylcholine receptor. However, when the photoactivatable derivative is cross-linked to detergent solubilized acetylcholine receptor (AChR), only the 7 subunit is labeled. Since snake a-neurotoxins mainly bind to the a subunits of AChR and a-conotoxins compete directly with a-bungarotoxin, the cross-linking results above are both intriguing and problematic. [Pg.271]

Beta-bungarotoxin, a protein in cobra snake venom, also binds to cholinergic nerves to stop ACh release while a-bungarotoxin (from the same source) binds firmly to peripheral postsynaptic nicotinic receptors. The combined effect ensures the paralysis of the snake s victim. [Pg.121]

The nAChR subtypes vary in response to pharmacological manipulation. The a7 receptors have a low affinity for nicotine and are sensitive to a-bungarotoxin (a-BTX) antagonism, whereas the heteromeric nAChRs are not.14 The p2 containing (p2 asterisk denotes the presence of additional subunits) nAChRs have the highest affinity for nicotine binding and some selectivity for antagonism... [Pg.24]

Mixture of neurotoxins that block the acetylcholine receptors. The /3-bungarotoxin is a pre-synaptic neural toxin, a-bungarotoxin is a postsynaptic neural toxin, and K-bungarotoxin is specific to the neuronal receptors in ganglions. They are obtained from the venom of the banded krait (Bungarus multicinctus). [Pg.471]

S. L. Pearce and E. Hawrot, Intrinsic fluorescence of binding-site fragments of the nicotinic acetylcholine receptor Perturbations produced upon binding a-bungarotoxin, Biochemistry 29, 10649-10659 (1990). [Pg.63]

Figure 7,13. AChR dusters on a rat rayotube in culture, visualized with (A) rhodamine anti-43K protein (B) fluorescein-labeled a-bungarotoxin (corresponding field) (C) rhodamine-labeled anti-vinculin and (D) fluorescein-labeled g-bungarotoxin (corresponding field). The antibodies were gifts from R. Bloch. University of Maryland Medical School. Note that AChR and 43K tend to aggregate in the same regions, whereas AChR and vinculin appear to exdude each other. Additional photographs are in Ref. 107. Figure 7,13. AChR dusters on a rat rayotube in culture, visualized with (A) rhodamine anti-43K protein (B) fluorescein-labeled a-bungarotoxin (corresponding field) (C) rhodamine-labeled anti-vinculin and (D) fluorescein-labeled g-bungarotoxin (corresponding field). The antibodies were gifts from R. Bloch. University of Maryland Medical School. Note that AChR and 43K tend to aggregate in the same regions, whereas AChR and vinculin appear to exdude each other. Additional photographs are in Ref. 107.
Anand R, Peng X, BaUesta 11, Lindstrom 1 (1993) Pharmacological characterization of a-bungarotoxin-sensitive acetylcholine receptors immunoisolated from chick retina Contrasting preoperties of al and a8 subunit-containing subtypes. Mol Pharmacol 44 1046-1050... [Pg.105]

Chen DN, Patrick JW (1997) The a-bungarotoxin-binding nicotinic acetylcholine receptor from rat brain contains only the a7 subunit, J Biol Chem 272 24024-24029 Clarke PBS, Schwartz RD, Paul SM, Pert CB, Pert A (1985) Nicotinic binding in rat brain autoradiographic comparison of [ H]acetylcholine, [ H]nicotine, and [ I]-alpha-bungarotoxin, J Neurosci 5 1307-1315... [Pg.106]

Deneris ES, Boulter J, SwansonLW, Patrick , Heinemann S (1989) P3 A new member of nicotinic acetylcholine receptor gene family is expressed in brain, J Biol Chem 264 6268-6272 Drisdel RC, Green WN (2000) Neuronal a-bungarotoxin receptors are a7 homomers, J Neurosci 20 133-139... [Pg.106]

Frazier CJ, Buhler AV, Weiner JL, Dunwiddie TV (1998) Synaptic potentials mediated by a-bungarotoxin-sensitive nicotinic receptors in rat hippocampal interneurons. J Neurosci 18 8228-8235... [Pg.107]

Keyser KT, Britto ERG, Schoepfer R, Whiting P Cooper J, Conroy W, Brozozowska-Prechtl A, Karten HJ, Lindstrom J (1993) Three subtypes of a-bungarotoxin-sensitive nicotinic acetylcholine receptors are expressed in chick brain. J Neurosci 13 442-452 Khiroug S, Harkness PC, Lamb PW, Sudweeks S, Khiroug L, Millar NS, Yakel JL (2002) Rat nicotinic ACh receptor al and fil subunits co-assemble to form functional heteromeric nicotinic receptor channels. J Physiol 540 425 34... [Pg.108]

Marks Ml, Collins AC (1982) Characterization of nicotine binding in mouse brain and comparison with the binding of a-bungarotoxin and quinuclidinyl benzilate. Mol Pharmacol 22 554-564 Marks Ml, Burch JB, Collins AC (1983) Effects of chronic nicotine infusion on tolerance development and nicotinic receptors. J Pharmacol Exp Ther 226 817-825 Marks Ml, Stitzel JA, Romm E, Wehner JM, Collins AC (1986) Nicotinic binding sites in rat and mouse brain comparison of acetylchohne, nicotine, and alpha-bungarotoxin. Mol Pharmacol 30 427 36... [Pg.109]

Orr-Urtreger A, Goldner FM, Saeki M, Lorenzo 1, Goldberg L, deBiasis M, Dani JA, Patrick JW, Beaudet AL (1997) Mice deficient in the a7 neuronal nicotinic acetylchohne receptor lack a-bungarotoxin binding sites and hippocampal fast nicotinic currents. J Neurosci 17 9165-9171... [Pg.109]

Paton WDM, Zaimis EJ (1949) The pharmacological actions of polymethylene bistrimethylammo-nium salts. Br J Pharmacol Chemother 4 381 00 Patrick J, Stallcup WB (1977) a-Bungarotoxin binding and cholinergic receptor function on a rat sympathetic nerve line. J Biol Chem 252 8629-8633 Patrick J, Boulter J, Deneris E, Wada K, Wada E, Connolly J, Swanson L, Heinemann S (1989) Structure and function of neuronal nicotinic acetylcholine receptors deduced from cDNA clones. Prog Brain Res 79 27-33... [Pg.110]

Schoepfer R, Conroy WG, Whiting P, Gore M, Lindstrom J (1990) Brain a-bungarotoxin binding protein cDNAs and MAbs reveal subtypes of this branch of the ligand-gated ion channel gene superfamily. Neuron 5 35 8... [Pg.111]

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