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Binding of the Imidazoline UK-14, 304, a Putative Full Alpha 2-adrenoceptor Agonist, to Rat Cerebral Cortex Membranes

Binding of the Imidazoline UK-14, 304, a Putative Full Alpha 2-adrenoceptor Agonist, to Rat Cerebral Cortex Membranes

D J Loftus, J M Stolk, D C U'Prichard

Life Sci. 1984 Jul 2;35(1):61-9.

PMID: 6146086

Abstract:

The aryl imidazoline compound UK-14, 304 (5-bromo-6-[2-imidazolin-2-yl-amino]-quinoxaline) is a potent and selective alpha 2-adrenoceptor agonist with full intrinsic activity, unlike other imidazolines. We examined the characteristics of high specific activity (84 Ci/mmol) [3H]UK-14, 304 binding to rat cerebral cortex membranes. [3H]UK-14, 304 specific binding was enhanced by Mn2+ ion, and associated and dissociated moderately rapidly at 25 degrees C. Norepinephrine-displaceable binding was saturable and monophasic, with a KD of 1.4 nM, in agreement with rate and competition experiments, and a Bmax of 200 fmol/mg protein. Competition studies revealed that binding was alpha 2-adrenoceptor-specific, with yohimbine being 12 times more potent than prazosin. [3H]UK-14, 304 appeared to label predominantly the R(H) state of the brain alpha 2-adrenoceptor, as judged by the high affinity of catecholamine and imidazoline agonists (IC50, 1-13 nM), and the relatively low affinity of yohimbine and rauwolscine (IC50, 100-300 nM), at the binding site. [3H]UK-14, 304 compares favorably with other alpha 2-adrenoceptor ligands because of its high affinity and specific activity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP59803984	UK 14,304		59803-98-4	Price

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