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A study of cannabinoid receptor ligands revealed the following Haunch equation f

ID: 1066459 • Letter: A

Question

A study of cannabinoid receptor ligands revealed the following Haunch equation for variation of substituent Log 1/C = 2.51 pi + 0.14sigma + 7.66 Explain how the substituent X will influence the binding affinity of the ligand and what chemical properties (e.g. electronic, hydrophilic...) are most important at this position in the molecule. Would you expect the amino analogue (X = NH2) to exhibit higher or lower affinity than the chloro analogue (X = Cl)? Calculate the theoretical IC_50 values for the NH2 and Cl analogues.

Explanation / Answer

ans a) if X is Cl then it will increase binding ability of ligand by balancing electon pulling force .

ans b) amino analogue have lower affinity than Cl

reason Cl is more Electronegative than NH2