TABLE 3

Affinities (Ki values in radioligand displacement study), potencies (EC50 values in [35S]GTPγS binding assay), and relative intrinsic activities (RIA; [35S]GTPγS binding assay) of pyrazole-derived partial agonists for the rat nicotinic acid receptor

Embedded ImageEmbedded Image
R1R2KiEC50RIAR1KiEC50RIA
μM%μM%
Nicotinic acid0.0330.74100C6H5-CH2-1.38750
HH0.592285C6H5-(CH2)2-1.6N.D.N.D.
i-C3H7H0.682268C6H5-(CH2)3-6.3N.D.n.d.
C3H7H0.145.1703Cl-C6H4-CH2-0.504739
C4H9H0.0722.3814Cl-C6H4-CH2-3.6N.D.N.D.
-C3H6-0.167.0564-CH3-C6H4-CH2-20N.D.N.D.
-C4H8-3.565474-OCH3-C6H4-CH2-66N.D.N.D.
  • N.D., not determined.