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and itching. Argiotoxin antagonizes the actions of the neurotransmitter glutamate, blocks the functioning of ion channel and affects the synaptic transmission of preys. These toxins, like all the other low-molecular-weight toxins, have a huge potential to be used in neurochemical studies to develop
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toxins (Arg 636, Arg 630, Arg 658, Arg 744, Arg 759, Arg 373, Arg 728, Arg 723, ...) show a close similarity in their structures; the subtle differences between them are chemical points, such as N-methyl groups, molecular masses or lysine residues that are determined in a certain position in their
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Scott, R. H.; Thatcher, N. M.; Ayar, A.; Mitchell, S. J.; Pollock, J.; Gibson, M. T.; Duce, I. R.; Moya, E.; Blagbrough, I. S. (1998-12-01). "Extracellular or intracellular application of argiotoxin-636 has inhibitory actions on membrane excitability and voltage-activated currents in cultured rat
642:
Poulsen, Mette H.; Lucas, Simon; Bach, Tinna B.; Barslund, Anne F.; Wenzler, Claudius; Jensen, Christel B.; Kristensen, Anders S.; Strømgaard, Kristian (2013-02-14). "Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors".
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in the central nervous system of mammals and the insects' glutamic receptor (it has been characterized as an opposite of homomeric and heteromeric glutamate-activated receptor channels ). It has been seen that it can also inhibit the following receptors:
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is a mollusc involved in one of the many ionic experiments. To begin with, neurons of molluscan pedal ganglia were isolated and transferred to a special chamber with saline solution and regulated temperature. Then, the observation was based on routine
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T. Moe, Scott; Smith, Daryl L.; Yongwei Chien, Eric; L.Raszkiewiez, Joanna; D. Artman, Linda; L. Mueller, Alan (October 1997). "Design, Synthesis, and
Biological Evaluation of Spider Toxin (Argiotoxin-636) Analogs as NMDA Receptor Antagonists".
686:
Verdoni, Marion; Roudaut, Hermine; De
Pomyers, Harold; Gigmes, Didier; Bertin, Denis; Luis, José; Bengeloune, Abd Haq; Mabrouk, Kamel (2016-08-27). "ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors".
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Argiotoxins studies have been particularly made to discover the relation between inhibition, receptors, and ionic channels. Researchers have specifically pursued the blocking of receptors on invertebrates, rather than on vertebrates.
388:
Adams, ME; Carney, RL; Enderlin, FE; Fu, ET; Jarema, MA; Li, JP; Miller, CA; Schooley, DA; Shapiro, MJ (1987). "Structures and biological activities of three synaptic antagonists from orb weaver spider venom".
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This same toxin is demonstrated to be a good regulator for melanogenesis without cytotoxicity. That's why ArgTX-636 is playing a leading role in the research of cosmetic products against hyper pigmentation.
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ArgTX-636 can also work as an analgesic due to some peripheral actions. Thanks to its action as inhibitor on gtutamate-activated channels it could work as an anti convulsant.
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Argiotoxins are classified into three different categories according to its chromophore's nature: the argiopine type, the argiopinine type and the pseudoargiopinine type.
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This spider's venom shows varied action mechanisms that affect the different parts of the nervous impulse transmission chain. As mentioned above, Argiotoxins are
227:. It is thought that polyamine toxins' inhibition is both use and voltage dependent. What is more, they bind within the pore of the open channels they inhibit.
134:
polyamine. The polyamine is connected to the asparagine's α-carboxyl group. The amino group of this aminoacid is linked to 2,4-dihydroxyphenyl acetic acid.
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Fleming, James J.; England, Pamela M. (2010-02-15). "Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands".
302:, a freshwater crustacean, has followed a similar protocol to this study. In this case, the analysis was made of the stomach muscles and using the
531:
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Argiopinines: (4-hydroxyindol-3-yl) acetic acid is carried as the chromophore. These molecules are: Arg-630, Arg-658, Arg-659, Arg-744, Arg-759.
310:
187:
313:, mass spectrometry, UV data and amino acid analysis are the elements that allow identifying diverse argiotoxins due to their spectrum.
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A complete synthesis strategy of argiotoxin and derivatives was developed in order to make biological tests in different living beings.
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A noted type of argiotoxin, the Arg-636, which molecular formula is C29H52N10O6 , has a molecular weight of 636.78658 g/mol. It has a
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A lot of attention is drawn to the pharmacological uses of polyamine toxins. They are highly valuable due to their high affinity for
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The most relevant example for the strategies mentioned above is the
Argiotoxin-636. This is a polyamine toxin isolated from the
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technique. Electrical measurements were obtained from the evaluation of neurons response to various substances (argiopines).
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Argiotoxin could even be used as a tool for analyzing the subunit composition of AMPA receptors in native membranes.
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technique. The research findings were obtained taking into account the bursts of openings of excitatory channels.
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Pseudoargiopinines: They contain a (indol-3-yl) acetic acid. This group is composed of: Arg-373, Arg-728, Arg-743.
85:
family, which contains more than 100 different chemical structures of closely related toxins. Acylpolyamines are
261:'s venom. However, there are still some difficulties, as ArgTX-636 cannot distinguish the different subtypes of
845:"Different types of glutamate receptors in isolated and identified neurons of the mollusc Planorbarius corneus"
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174:, are harmless to humans, although in certain cases the bite of argiotoxin spiders can produce mild
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788:"Argiopine blocks glutamate-activated single-channel currents on crayfish muscle by two mechanisms"
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238:. It has not been developed yet, although it is thought that it could be a great procedure in
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Elin, E.A.; de Macedo, B.F.; Onoprienko, V.V.; Osokina, N.E.; Tijomirova., O.B. (June 1992).
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which has highly functional polar groups: free phenolic OH and amine and guanidine residues.
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Argiotoxin can be classified, according to the 1980s classification of spider venoms, as a
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Other experiments use spectroscopy in order to analyse and differentiate these molecules.
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spider family. This type of spider is found in almost every area of the world.
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Argiopine: contains 2,4-dihydroxyphenylacetic acid. It is also named Arg-636.
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that are found only in the venom glands of spiders at a picomolar level.
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130:) connected to a -NH (CH)3 NH (C ~) 3NH (CH) 5-NH- one through a
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Structural parts of the acylpolyamine toxins from spider venoms
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Behaviour of argiotoxins at the junction of nerve and muscle
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Its structure was established using spectroscopy 1H, C-RMN,
503:. No. Biochemical composition of Arg-636. 24 June 2005
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The effects of argiotoxin, when it enters an organism by a
786:
Antonov, S M; Dudel, J; Franke, C; Hatt, H (1989-12-01).
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Bolshakov VYu; Gapon, S A; Magazanik, L G (1991-08-01).
155:{ 5 - amino ] propylamino ) propylamino ] pentyl }
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219:(argiotoxin has higher potency at NMDA receptors),
179:novel drugs of neurotherapeutic applications.
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467:"Síntesis de la Argiopina (Argiotoxin-636)"
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206:group can effectively inhibit certain
45:The orb-weaver spiders, also known as
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689:Bioorganic & Medicinal Chemistry
598:Bioorganic & Medicinal Chemistry
428:. Springer Reference. pp. 3–20.
371:Taylor & Francis, 1994; page 7.
141:, and elemental aminoacid analysis.
126:It also possesses arginine (free NH
183:Mechanism of action of argiotoxins
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225:nicotine acetylcholine receptors
905:. Academic Press. 1994-06-17.
861:10.1113/jphysiol.1991.sp018654
804:10.1113/jphysiol.1989.sp017887
645:Journal of Medicinal Chemistry
444:. Academic Press. 1994-06-17.
424:Gopalakrishnakone, P. (2016).
263:ionotropic glutamate receptors
232:ionotropic glutamate receptors
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749:10.1016/s0028-3908(98)00144-0
234:, important drug targets for
119:It is a low-molecular-weight
403:10.1016/0006-291X(87)90930-2
284:Referring to invertebrates,
276:Experiments with argiotoxins
369:Neurotoxins in Neurobiology
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902:Chemistry and Pharmacology
441:Chemistry and Pharmacology
849:The Journal of Physiology
792:The Journal of Physiology
701:10.1016/j.bmc.2016.08.023
610:10.1016/j.bmc.2009.12.072
208:ligand-gated ion channels
151:of 0. Its IUPAC name is:
242:and in the treatment of
567:10.1023/a:1011988317683
555:Pharmaceutical Research
522:Parchas, G.; Goula, M.
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166:Effects and properties
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62:Chemical structure of
497:"Argiopine (Arg-636)"
298:In addition to that,
236:psychiatric disorders
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107:Biochemical structure
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19:represent a class of
938:at Wikimedia Commons
287:Planorbarius corneus
87:neurotoxic compounds
977:Invertebrate toxins
244:Alzheimer's disease
471:Revista de Química
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26:isolated from the
934:Media related to
743:(12): 1563–1578.
737:Neuropharmacology
695:(22): 5685–5692.
657:10.1021/jm301602d
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367:K F Tipton (ed).
139:mass spectrometry
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798:: 569–587.
320:structure.
304:patch clamp
172:spider bite
159:{ amino }
17:Argiotoxins
972:Polyamines
962:Guanidines
946:Categories
936:Argiotoxin
538:2016-10-15
507:15 October
481:15 October
377:013614991X
355:References
349:Neurotoxin
344:Delucemine
121:neurotoxin
869:0022-3751
855:: 15–35.
812:0022-3751
757:0028-3908
709:1464-3391
665:1520-4804
618:1464-3391
197:polyamine
153:(2S) - N-
64:argiopine
51:Araneidae
21:polyamine
773:39483719
731:sensory
717:27647371
673:23320429
626:20096591
583:22419144
324:See also
300:crayfish
176:swelling
47:araneids
967:Phenols
887:1654412
878:1180096
830:2482886
821:1190022
765:9886679
733:neurons
575:9487543
501:pubchem
411:3689366
221:kainate
202:. This
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200:toxins
24:toxins
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79:toxin
907:ISBN
883:PMID
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661:ISSN
622:PMID
614:ISSN
571:PMID
509:2016
483:2016
446:ISBN
407:PMID
373:ISBN
311:HPLC
217:NMDA
213:AMPA
36:and
873:PMC
857:doi
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816:PMC
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