High-affinity ligand/receptor

High Affinity Ligand/Receptor Complex, Heavy PM, Actin-associated, Desensitized... 

Williamson PTE. Sohd-state NMR for the analysis of high-affinity ligand/receptor interactions. Concepts Magn. Reson. 2009 34A 144-172. 

For reasons that are not yet clear, skeletal muscle transverse (T)-tubule membranes contain 50-100-fold more high affinity DHP receptors than any other source yet identified [43,45]. Transverse tubule membranes contain 30-70 pmol/mg protein of DHP receptors that bind [ H]PN 200-100 with a of 0.1-0.2nM. The strategy utilized for the purification of L-type channels was similar to that used for the purification of other high affinity ligand binding proteins, and its success was predicted from the prior use of such an approach for the purification of other ion channels [54,55]. Thus the L-type channels were purified as high affinity DHP receptors, with the anticipation that the purified component(s) would constitute functional Ca channels. 

Several bis-heterocyclopyridines have been previously demonstrated to have various central nervous system effects <1996CHEC-II(8)967>. Pyrrolo[l, 2- ]thieno[3,2-f ]pyrazines have been demonstrated to be high-affinity ligands for 5-HT3 receptors <1996JME2068>. Pyrazolo[4,3- ]pyrrolo[ l,2-tf]pyrazines have moderate antibacterial and antifungal activity <2005M217>. 

The cysteine motifs in this polydnavirus gene family are structurally analogous to the cysteine motifs of the >-conotoxins. The a>-conotoxins are high-affinity ligands with different receptor specificity for voltage-sensitive ion channels (64, 65). The mature w-conotoxins have three... 

We were greatly surprised to find that (27) was approximately 100-times more potent (RVN p 2 9.9) than the N-linked imidazole (15). A radiola-belled form of this high-affinity ligand, [ HjGR 65630 (28), has been used to demonstrate the existence and distribution of 5-HT3 receptors in brain tissue from several species, including man [62]. 

Dihydrotestosterone is the preferred (high affinity) ligand for the androgen receptor and is formed by reduction of testosterone catalyzed by the enzyme steroid 50C-reductase. 

C.S. Dence, C.S. John, W.D. Bowen, M.J. Welch, Synthesis and evaluation of [F-18] labeled benzamides High affinity sigma receptor ligands for PET imaging, Nucl. Med. Biol. 24 (1997) 333-340. 

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