TABLE 2.
| ||||||||
---|---|---|---|---|---|---|---|---|
Compound | R1 | R2 | R3 | R4 | Agonist Effect (% maximum) |
EC50 (μM) |
Antagonist Effect (%maximum) |
IC50 (μM) |
1 | H | NH2 | H | OH | 21% | 1.28 | 77% | 4.19 |
2 | H | NH2 | H | OCH3 | 35% | 12.9 | 65% | 12.4 |
3 | H | NH2 | H | H | 12% | 6.26 | 87% | 5.76 |
4 | Cl | NH2 | H | H | 19% | 0.651 | 80% | 2.01 |
5 | SCH3 | NH2 | H | H | 22% | 0.550 | 77% | 2.11 |
6 | H | NH2 | Br | H | 0% | 100% | 36.7 | |
7 | H | NHCH3 | H | H | 0% | 99% | 0.330 | |
(MRS 219) | ||||||||
8 | H | NHCH2CH3 | H | H | 0% | 100% | 1.08 | |
9 | H | NH(CH2)2CH3 | H | H | 0% | <20% | ||
10 | H | NHCOC6H6 | H | H | 0% | 0% | ||
11 | H | N(CH3)2 | H | H | 0% | 70% | 46.7 | |
12 | H | Cl | H | H | <10% | <10% | ||
13 | H | OH | H | H | 0% | <20% | ||
14 | H | SCH3 | H | H | 0% | 78% | 29.1 |