Purotoxin-1
Selective inhibitor of P2X3 receptors
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產(chǎn)品名稱: Purotoxin-1
Selective inhibitor of P2X3 receptors
產(chǎn)品型號(hào): 011PUR001-00100
產(chǎn)品展商: 其他品牌
產(chǎn)品文檔: 無相關(guān)文檔
簡單介紹
Purotoxin-1
Selective inhibitor of P2X3 receptors
的詳細(xì)介紹
Purotoxin-1
Selective inhibitor of P2X3 receptors
Purotoxin-1 (PT-1) is a peptide originally isolated from the Central Asian spider Geolycosa sp. Purotoxin-1 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 Purotoxin-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 Purotoxin-1, making it the most potent and selective ligand for P2X3.
Therapeutic interest : pain
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.
