Abstract
Imidazoline and guanidinium α 2 -adrenergic aggonists such as clonidine and guanabenz are used as centrally mediating antihypertensive drugs. However, we showed that in human and rabbit kidney, this class of molecules recognized not only α 2 -adrenergic receptors but also a previously unknown membrane protein, the imidazoline-guanidinium receptive site (IGRS). Through pharmacological and biochemical studies, we demonstrated that IGRS is recognized by imidazoline and guanidinium derivatives, insensitive to catecholamine, physically distinct from α 2 -adrenergic receptors, localized in the basolateral membranes and, mainly, in mitochondria, and regulated by K + in vitro
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