Damer S, Niebel B, Czeche S, Nickel P, Ardanuy U, Schmalzing G, Rettinger J, Mutschler E, Lambrecht G
Department of Pharmacology, Biocentre Niederursel, University of Frankfurt, Frankfurt/M., Germany.
Eur J Pharmacol. 1998 May 29;350(1):R5-6. doi: 10.1016/s0014-2999(98)00316-1.
8,8'-(Carbonylbis(imino-4, 1 -phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis(1,3, 5-naphthalenetrisulfonic acid) (NF279) antagonized P2X receptor-mediated contractions in rat vas deferens, evoked by alpha,beta-methylene ATP (10 microM; pIC50=5.71) without affecting responses mediated via alpha1A-adrenoceptors, adenosine A1 and A2B receptors, histamine H1, muscarinic M3 and nicotinic receptors. The low inhibitory potency of NF279 on P2Y receptors in guinea-pig taenia coli (pA2=4.10) and at ecto-nucleotidases in folliculated Xenopus laevis oocytes (IC50 > 100 microM) indicates that NF279 is a novel specific and selective P2X receptor antagonist.
8,8'-（羰基双（亚氨基-4,1-亚苯基羰基亚氨基-4,1-亚苯基羰基亚氨基））双（1,3,5-萘三磺酸）（NF279）可拮抗大鼠输精管中由α,β-亚甲基ATP（10微摩尔；pIC50 = 5.71）诱发的P2X受体介导的收缩，且不影响通过α1A-肾上腺素能受体、腺苷A1和A2B受体、组胺H1、毒蕈碱M3和烟碱样受体介导的反应。NF279对豚鼠结肠带中P2Y受体的低抑制效力（pA2 = 4.10）以及对卵泡化非洲爪蟾卵母细胞中外核苷酸酶的抑制效力（IC50 > 100微摩尔）表明NF279是一种新型的特异性和选择性P2X受体拮抗剂。
