Affinity ligands, classification

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Two very similar molecules are two different physical objects [40], Hence, chemical/ structural comparison of similarity is a subtle and relative concept that acquires significance in a well-defined reference physical context. In other words, it is necessary to define in what respect and to what extent two different molecules are similar. Molecular series of specific and selective ligands interacting, in vitro and in equilibrium conditions, with a specific receptor constitute a sophisticated example of chemical similarity-diversity classification. This classification is based on the experimental binding affinity (AG°) values that quantify a particular molecular recognition phenomenon, which is, essentially, a noncovalent process [41]. This implies,... 

Receptor Ligand Receptor affinity (fiM) EC50 on G-bead6 (/tM) Max receptor on G-beadc (No. per bead) Classification 4... 

A classification scheme has been suggested. Those receptors that bind the (-F )-6,7-benzomorphans, such as (-F)-NANM and (-F )-Pentazocine, with high affinity and those which bind these ligands with low affinity are designed as CT, and CTj respectively (Quirion et al., 1992). Other sites with a distinct pharmacological profile versus the previously defined subtypes appear to exist. A series of l-phenyl-3-aminotetralines (PATs), exemplified by Hj-PAT was found to stimulate tyrosine hydroxylase activity and dopamine synthesis through interaction with a novel aj receptor (Wyrick and Booth, 1995). 

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