Add time:09/03/2019         Source:sciencedirect.com

L-657, 743 (MK-912), a highly potent and selective α2-adrenoceptor antagonist was tritiated to a high specific activity and its binding characteristics to brain tissue were determined. The specific binding of [3H]L-657, 743 to rat cerebrocortex was saturable, reversible, and dependent on tissue concentration. In saturation studies, [3H]L-657, 743 binding was resolved into two high affinity components exhibiting Kd values of 86 pM and 830 pM with densities of 82 fmol/mg protein and 660 fmol/mg protein, respectively. Based on the binding potencies of a variety of compounds with differing receptor selectivities, the sites labeled by [3H]L-657, 743 were characteristic of α2-adrenoceptors. In contrast to α2-antagonists, α2-agonists displayed shallow competition curves. In the presence of 100 μM GTP, Gpp(NH)p or 150 mM NaCl, the competition curve for epinephrine was shifted to the right, whereas that for yohimbine was unaffected. In studies utilizing human cerebrocortical tissue, [3H]L-657, 743 also bound with high affinity to sites characteristic of α2-adrenoceptors.

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