新型磷酸吡哆醛-5'-磷酸衍生物PPNDS能有效拮抗P2X(1)受体的激活。
The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors.
作者信息
Lambrecht G, Rettinger J, Bäumert H G, Czeche S, Damer S, Ganso M, Hildebrandt C, Niebel B, Spatz-Kümbel G, Schmalzing G, Mutschler E
机构信息
Department of Pharmacology, Biocentre Niederursel, University of Frankfurt, Geb. N260, Marie-Curie-Str. 9, D-60439, Frankfurt, Germany.
出版信息
Eur J Pharmacol. 2000 Jan 17;387(3):R19-21. doi: 10.1016/s0014-2999(99)00834-1.
Pyridoxal-5'-phosphate-6-(2'-naphthylazo-6'-nitro-4',8'-disulfonat e) (PPNDS) potently antagonized P2X(1) receptor-mediated responses in rat vas deferens (pK(B)=7.43) and Xenopus laevis oocytes (pIC(50)=7. 84). It showed lower (up to 20,000-fold) inhibitory potency on ecto-nucleotidase in Xenopus oocytes and on P2Y(1) receptors in guinea-pig ileum (pA(2)=6.13). PPNDS did not interact with alpha(1A)-adrenoceptors, adenosine A(1) and A(2B), histamine H(1) and muscarinic M(3) receptors. Thus, PPNDS is a novel, specific P2 receptor antagonist and represents the pyridoxal-5'-phosphate derivative with the highest potency at P2X(1) receptors.
磷酸吡哆醛-5'-磷酸-6-(2'-萘基偶氮-6'-硝基-4',8'-二磺酸盐)(PPNDS)能有效拮抗大鼠输精管中P2X(1)受体介导的反应(pK(B)=7.43)以及非洲爪蟾卵母细胞中的反应(pIC(50)=7.84)。它对非洲爪蟾卵母细胞中的外切核苷酸酶以及豚鼠回肠中的P2Y(1)受体的抑制效力较低(高达20000倍)(pA(2)=6.13)。PPNDS不与α(1A)-肾上腺素能受体、腺苷A(1)和A(2B)、组胺H(1)和毒蕈碱M(3)受体相互作用。因此，PPNDS是一种新型的特异性P2受体拮抗剂，是在P2X(1)受体上效力最高的磷酸吡哆醛-5'-磷酸衍生物。
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