Guanabenz, guanochlor, guanoxan and idazoxan bind with high affinity to non-adrenergic sites in pig kidney membranes.

Abstract:

:[3H]Idazoxan is a labelled ligand that is frequently used to study alpha 2-adrenoceptors in the central nervous system. In pig kidney membranes, [3H]idazoxan labelled high-affinity binding sites (Kd = 1.5 nM) that were not alpha 2-adrenoceptors and which recognized clonidine with low affinity. This new class of binding sites was recognized by amiloride derivatives; however, it is not likely that these sites are the well-known targets of amiloride in the kidney: the Na+/H+ exchanger and the epithelium Na+ channel. These binding sites may be the normal target of a series of imidazolidines derivatives (guanabenz, guanochlor, guanoxan), which are known for their antihypertensive properties.

journal_name

Eur J Pharmacol

authors

Vigne P,Lazdunski M,Frelin C

doi

10.1016/0014-2999(89)90503-7

subject

Has Abstract

pub_date

1989-01-31 00:00:00

pages

295-8

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(89)90503-7

journal_volume

160

pub_type

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