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Molecular Pharmacology

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Abstract

Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.

A L Wilson, S W Womble, C Prakash, E J Cragoe Jr, I A Blair and L E Limbird
Molecular Pharmacology August 1992, 42 (2) 175-179;
A L Wilson
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S W Womble
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C Prakash
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E J Cragoe Jr
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I A Blair
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L E Limbird
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Abstract

Two novel amiloride analogs have been synthesized during the course of efforts to develop a photoaffinity label for the amiloride allosteric domain on alpha 2-adrenergic receptors. One of these, 5-[N-2'-aminoethyl-N'-isopropyl]amiloride-N-[4"-azidosalicylamide] (A-EIA-AS), markedly accelerates the rate of dissociation of [3H]yohimbine from affinity-purified alpha 2-adrenergic receptors, an assay for allosteric modulation of receptor-adrenergic ligand interactions. In contrast, this agent does not appreciably inhibit Na+/H+ exchange, measured as 5-(N-ethyl-N-isopropyl)amiloride (EIA)-inhibitable 22Na+ uptake into cultured renal epithelial cells. A second analog, 5-[N-2'-(4"-azidosalicylamidino)ethyl-N'- isopropyl]amiloride (ASA-EIA), does not foster an accelerated rate of dissociation of [3H]yohimbine binding from the alpha 2 receptor but does block the ability of A-EIA-AS to do so, suggesting that ASA-EIA and A-EIA-AS interact at a common binding site. Interestingly, the ability of EIA to accelerate [3H]yohimbine dissociation is not blocked by ASA-EIA, a finding that may indicate that EIA and A-EIA-AS allosterically modulate alpha 2 receptor-ligand interactions via distinct or nonoverlapping binding sites.

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Molecular Pharmacology
Vol. 42, Issue 2
1 Aug 1992
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Abstract

Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.

A L Wilson, S W Womble, C Prakash, E J Cragoe, I A Blair and L E Limbird
Molecular Pharmacology August 1, 1992, 42 (2) 175-179;

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Abstract

Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.

A L Wilson, S W Womble, C Prakash, E J Cragoe, I A Blair and L E Limbird
Molecular Pharmacology August 1, 1992, 42 (2) 175-179;
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