Amiloride analogs

An amiloride analog that inhibits Na+/H+ ion exchangers and is under consideration for the prevention of post-ischemic damage. 

Among the organic derivates, amiloride analogs were the first to be described as powerful inhibitors of NCX activity when the antiporter operates either in the forward or the reverse mode of operation (Fig. 5). These... 

Huot et al. [38] used affinity chromatography to identify and partially purify an amiloride-binding protein with characteristics of the renal brush border Na /H exchanger. The high-affinity amiloride analog A35 (5-A-(3-aminophenyl)amiloride) was coupled to Sepharose CL-4B through a triglycine spacer. Rabbit renal brush border membranes were solubilized with 0.6% Triton X-100, incubated with the... 

Subsequently, proteolytic fragments of the rabbit renal 25-kDa amiloride-binding protein were micro-sequenced and found to have high sequence homology with rat and human NAD(P)H quinone oxidoreductase. Indeed, enzymatic assays revealed that renal brush border membrane vesicles contain significant NADPH quinone oxidoreductase activity. Presumably NAD(P)H quinone oxidoreductase coincidentally binds amiloride analogs with the same rank order as the Na /H exchanger [39]. 

Wilson AL, Womble SW, Prakash C, Cragoe EJ Jr, Blair IA, Limbird LE. Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+ /H exchange. Mol Pharmacol 1992 42 175-179. 

Hoare SR, Strange PG. Regulation of D2 dopamine receptors by amiloride and amiloride analogs. Mol Pharmacol 1996 50 1295-1308. 

Wilson, A. L., Guyer, C. A., Cragoe, E. J., and Limbird, L. E. (1990). The hydrophobic tryptic core of the porcine alpha 2-adrenergic receptor retains allosteric modulation of binding by Na+, H+, and 5-amino-substituted amiloride analogs. J. Biol. Chem. 265, 17318-17322. 

In C3H10T1/2 cells, the proton release induced by ferricyanide is insensitive to amiloride analogs. The rate of H+ release is also very low to the extent that it is equal to or less than the electron transport (Table 3). Therefore, the proton movement from these cells may be based on anisotropic oxidation-reduction of... 

Wilson AL, Seibert K, Brandon S, Cragoe EJ Jr, Limbird LE. Monovalent cation and amiloride analog modulation of adrenergic ligand binding to the... 

Muramoto, K., Sugiyama, S., Cragoe, E.J. and Imae, Y. (1994). Successive inactivation of the force-generating units of sodium-driven bacterial flagellar motors by a photoreactive amiloride analog. /. Biol. Chetn. 269, 3374—3380. 

Probes for the Na" channel and the Na /H antiporter amiloride analogs Na /K -ATPase ouabain probes Probes for channels and carriers glibenclamide conjugates for the ATP-dependent channel, apamin probes for small-conductance Ga -activated channels. 

Amiloride Analogs as Inhibitors of the Urokinase-type Plasminogen Activator [93,94]... 

Figure 9 1 Amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA).

Matthews, H., Tyndall, J., and Kelso, M.J. Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA). Bioorganic and Medicinal Chemistry Letters, 21 (22), 6760-6766. 

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