Fanestil D D, Vaughn D A
Am J Physiol. 1979 May;236(5):C221-4. doi: 10.1152/ajpcell.1979.236.5.C221.
The organic cation 2,4,6-triaminopyrimidine (TAP) produced inhibition of short-circuit current (SCC) when added to either the mucosal or serosal surface of the isolated urinary bladder of the toad. Fifty percent inhibition was produced by 10(-3) M TAP in the mucosal solution at pH 6.8 when the mucosal [Na+] was 113 mM. The actions of TAP resemble those produced by amiloride in several ways: a) inhibition of SCC by mucosal application is rapid; b) the mucosal inhibition is fully reversible; c) high concentrations in the serosal solutions produce irreversible inhibition; and d) the concentration required to produce 50% inhibition from the mucosal side is reduced when mucosal [Na+] is reduced. It is postulated that mucosal application of TAP and amiloride inhibit short-circuit current in high-resistance epithelia via action at a common locus.
当向蟾蜍离体膀胱的黏膜或浆膜表面添加有机阳离子2,4,6-三氨基嘧啶(TAP)时,会产生短路电流(SCC)抑制作用。当黏膜溶液中pH为6.8且黏膜[Na⁺]为113 mM时,10⁻³ M TAP在黏膜溶液中可产生50%的抑制作用。TAP的作用在几个方面类似于氨氯吡脒产生的作用:a)通过黏膜给药对SCC的抑制作用迅速;b)黏膜抑制作用完全可逆;c)浆膜溶液中的高浓度会产生不可逆抑制;d)当黏膜[Na⁺]降低时,从黏膜侧产生50%抑制所需的浓度会降低。据推测,TAP和氨氯吡脒经黏膜给药通过作用于共同位点来抑制高电阻上皮中的短路电流。