An α2-adrenergic receptor agonist
Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.
[3H]Brimonidine (UK 14304) is a full agonist at alpha 2-adrenergic receptors. [3H]Brimonidine (UK 14304) labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site [1-3].
参考文献:
[1]. Andorn, A.C., M.A. Carlson, and R.C. Gilkeson, Specific [3H]UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha 2-adrenergic selectivity and differing affinities for GTP. Life Sci, 1988. 43(22): p. 1805-12.
[2]. Cambridge, D., UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol, 1981. 72(4): p. 413-5.
[3]. Chopin, P., F.C. Colpaert, and M. Marien, Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J Pharmacol Exp Ther, 1999. 288(2): p. 798-804.
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