Selection binding

Neurotropic and antistress properties of 2,4-dimethylpyrido[l, 2-u]pyr-imidinium perchlorate were compared with those of piracetam (95MI7). AH-Pyrido[l,2-u]pyrimidin-4-one binds selectively to rat A3 receptors with a A", value of 48/xM. No affinities were observed to rat Ai and A2 receptors (96MI17). 4-Oxo-4//-pyrido[l,2-u]pyrimidine-3-carboxylic acid and -3-carbonitrile did not exhibit significant antibacterial activities (97MI6). 

For the cycloaddition reaction in Scheme 4.6 it was found that 3-bromocam-phor, for example, can bind selectively to one enantiomer of the complex [12] and that if the reaction was performed in the presence of the racemic catalyst 8 and 3-bromocamphor, cis-3 was isolated with up to 80% ee compared to 95% ee for the reaction catalyzed by (J )-8b. 

The VACM-1 receptor is a membrane-associated protein with a single putative transmembrane domain that binds selectively AVP (XD — 2 nM), but cannot discriminate between VXR and V2R analogues. It is expressed in endothelial and medullary collecting duct cells and upon stimulation by AVP. It induces a mobilization of cytosolic-free Ca2+, decreases cAMP production and inhibits cellular growth via MAPK phosphorylation and p53 expression. The mechanism of action and physiological functions of this new receptor are not well understood, but it seems to participate in the regulation of AVP induced signal transduction pathways or of a yet unidentified peptide. 

Phe-Pro-Phe-D-Trp-Lys-Thr]. This study also yielded compounds with an enhanced binding selectivity, in this case, for the hsst2 receptor [37]. 

Another possible target for toxins are the receptors for neurotransmitters since such receptors are vital, especially for locomotion. In vertebrates the most strategic receptor is that for acetylcholine, the nicotinic receptor. In view of the breadth of action of the various conotoxins it is perhaps not surprising that alpha-conotoxin binds selectively to the nicotinic receptor. It is entirely possible that similar blockers exist for the receptors which are vital to locomotion in lower species. As mentioned previously, lophotoxin effects vertebrate neuromuscular junctions. It appears to act on the end plate region of skeletal muscle (79,59), to block the nicotinic receptor at a site different from the binding sites for other blockers (81). 

These agents bind selectively to a region of the SOS ribosomal subunit close to that of chloramphenicol and erythromycin. They block elongation of the peptide chain by inhibition of peptidyl transferase. 

The concept of immunoassay was first described in 1945 when Landsteiner suggested that antibodies could bind selectively to small molecules (haptens) when they were conjugated to a larger carrier molecule. This hapten-specific concept was explored by Yalow and Berson in the late 1950s, and resulted in an immunoassay that was applied to insulin monitoring in humans. This pioneering work set the stage for the rapid advancement of immunochemical methods for clinical use. 

Selectivity at formation of a respective inclusion compound and its thermal stability behavior might differ (cf. Tables 1 and 2), since for both representations different processes should be taken into consideration. Formation of a crystal inclusion compound is normally controlled by kinetics, whereas the thermal stability (decomposition property) is a result of thermodynamics. Thus, we speak of formation selectivity , on the one hand, and of binding selectivity , on the other. 

Binding to P-tubulin. The anthelmintic benzimidazoles, such as thiabendazole and albendazole, are drugs that bind selectively to nematode... 

Meng F, Ueda Y, FIoversten MT et al. Mapping the receptor domains critical for the binding selectivity of d-opioid receptor ligands. Eur J Pharmacol 1996 311 285-292. 

Flajolet, M., Rakhilin, S., Wang, H. et al. Protein phosphatase 2C binds selectively to and dephosphorylates metabotropic glutamate receptor 3. Proc. Natl Acad. Sci. U.S.A. 16006-16011,2003. 

Varenicline is a partial agonist that binds selectively to nicotinic acetylcholine receptors with a greater affinity than nicotine, thus producing an attenuated response compared to that of nicotine. Its place in therapy has not been established. 

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