Table 2.

Affinity estimates for CCK-receptor antagonists competition studies using [³H]-JB93182 as radiolabel at the CCK_2S and CCK_2L receptors

	CCK2S receptor			CCK2L receptor			Literature values
Compound	pKI	nH	n	pKI	nH	n	pKI
CCK2-receptor selective
YM022	9.94±0.09	1.25±0.12	5	10.28±0.06	0.96±0.04	4	9.73a
YM220	9.32±0.09	0.85±0.09	5	9.66±0.06	1.01±0.22	3	9.72b
PD-134,308	8.86±0.04	0.90±0.01*	4	8.80±0.11	0.83±0.02*	3	8.35c
PD-140,376	8.82±0.07	1.06±0.06	4	9.12±0.06	0.74±0.07*	3	nd
R-L-365,260	7.98±0.07	0.97±0.03	3	7.64±0.05	0.95±0.06	4	8.48b
S-L-365,260	6.33±0.06	1.58±0.28	3	6.37±0.04	1.48±0.28	3	nd
JB93182	8.94±0.06	1.02±0.08	5	9.02±0.09	1.12±0.04	4	nd
L-740,093	9.34±0.04	0.93±0.02*	3	9.56±0.11	0.84±0.08 *	3	9.72d
CCK1-receptor selective
SR27897	6.68±0.04	1.23±0.07	4	7.04±0.13	1.29±0.39	4	nd
L-364,718	6.54±0.22	1.18±0.10	4	6.79±0.11	1.34±0.34	3	6.82d
2-NAP	4.90±0.05	1.62±0.10	3	4.70±0.05	1.60±0.31	3	nd
Agonist
CCK-8S	9.05±0.04	0.76±0.03*	3	9.27±0.02	0.89±0.10	3	9.92d

nd = not determined.

^*Significantly different from unity.

References: ^aBlaker et al. (1998);

^bTakinami et al. (1997);

^cDenyer et al. (1994);

^dBeinborn et al. (1998).