각종 Purinergic Receptor Blocker Peptide Toxin
본문
화학 합성의 각종 Purinergic Receptor Blocker Peptide Toxin
Acetylcholine receptor 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
Purotoxin 1
Purotoxin1 (PT-1) is a peptide originally isolated from the Central Asian spider Geolycosa sp. It was shown to inhibit
selectively P2X3 receptor channels at a 100 nM concentration. Studies were carried-out on cultured rat DRG neurons.
Patch-clamp experiments did not show any inhibitory effect of PT-1 on voltage-gated channels (potentials range tested
from -100 to 20 mV), neither on TRPV1 (after activation with 500 nM capsaicin). The selectivity of PT-1 for P2X3 was
highlighted by activating this receptor with 10 µM ATP and 100 µM α, β Methylene-ATP. Indeed, unlike P2X3, P2X2 and heterodimer P2X2/3 are known to be not sensitive to such concentrations. Moreover, P2X3, P2X2, and P2X2/3 are the only known ATP-sensitive receptors expressed in plasma membranes of DRG neurons. So, the observed effect seems to be well related to a selective inhibition of P2X3. P2X3-mediated current was fully inhibited with 100 nM PT-1, making it
the most potent and selective ligand for P2X3.
P2X3 receptors are known to be implicated in pain mechanisms. Behavioral experimentations carried-out on rat pain
models using 0.5 nmol PT-1 injected intraplantar showed to reduce nociception. This anti-nociceptive effect is
comparable to A-317491 compound (Abbott's drug) with an amount of almost 3 orders of magnitude lower.
Details
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AA sequence: |
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Gly-Tyr-Cys3-Ala-Glu-Lys-Gly-Ile-Arg-Cys10-Asp-Asp-Ile-His-Cys15-Cys16-Thr-Gly-Leu-Lys-Cys21-Lys-Cys23-Asn-Ala-Ser-Gly-Tyr-Asn-Cys30-Val-Cys32-Arg-Lys-Lys-NH2 |
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(Disulfide bridges: Cys3-Cys16; Cys10- Cys21; Cys15-Cys32; Cys23-Cys30 |
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Length (aa): |
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35 |
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Formula: |
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C155H248N50O48S8 |
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Molecular Weight: |
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3834.59 Da |
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Appearance: |
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White lyophilized solid |
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Solubility: |
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Water and saline buffer |
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CAS number: |
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- |
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Source: |
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Synthetic |
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Purity |
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> 97 % |
References
1. Kabanova NV, et al. (2012) Modulation of P2X3 receptors by spider toxins. Biochim Biophys Acta. PubMed link
2. G. A. Savchenko, et al. (2010) Purinergic Membrane Receptors as Targets for the Effect of Purotoxin 1, a Component of
Venom of Spiders from the Geolycosa Genus. Neurophysiology.
3. E.V. Grishin, et al. (2010) Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.
3. E.V. Grishin, et al. (2010) Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.
Ordering informations
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Catalog No. |
Product Name |
Size |
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011PUR001 |
Purotoxin 1 |
0.1 mg, 0.5 mg
& 1.0 mg |
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
▣ 관련 페이지 ; Smartox Biotechnology
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