The Journal of pharmacy and pharmacology, 61(7), 901-910 (2009-07-11)
alpha(2)-Adrenergic and mu-opioid receptors belong to the rhodopsin family of G-protein coupled receptors and mediate antinociceptive effects via similar signal transduction pathways. Previous studies have revealed direct functional interactions between both receptor systems including synergistic and additive effects. To evaluate
One subtype of imidazoline receptors (IR1) is similar to alpha 2-adrenoceptors (alpha 2 AR) based on their high affinity for clonidine and related imidazoline compounds. On the other hand, IR1 possess low affinity for norepinephrine (NE) and other catecholamines. Imidazoline
The binding properties of p-[125I]iodoclonidine [( 125I]PIC) to human platelet membranes and the functional characteristics of PIC are reported. [125I]PIC bound rapidly and reversibly to platelet membranes, with a first-order association rate constant (kon) at room temperature of 8.0 +/-
The Journal of pharmacology and experimental therapeutics, 279(2), 694-702 (1996-11-01)
To identify selective compounds for nonadrenergic I1-imidazoline receptors (I1), the affinities of 22 ligands for [125I]p-iodoclonidine binding have been compared at human platelet I1-imidazoline binding sites (analyzed under norepinephrine mask of alpha-2 AR) and at human alpha-2A, alpha-2B and alpha-2C
Imidazoline binding sites are labeled by [3H]clonidine (I1) or by [3H]idazoxan (I2). I2-sites are mitochondrial. The subcellular localization of I1-sites in brain is unknown. Crude membranes from bovine rostral ventrolateral medulla (RVLM) were further purified by discontinuous sucrose density gradient.
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