Table 2.
Compared properties of R(−) and S(+) sopromidine at the recombinant rH3(445) and rH3(413) receptor isoforms and at the rat H3 autoreceptor
R(−) sopromidine | S(+) sopromidine | |||||
---|---|---|---|---|---|---|
Condition | rH3(445) receptor | rH3(413) receptor | H3 autoreceptora | rH3(445) receptor | rH3(413) receptor | H3 autoreceptora |
Alone | Full agonist (EC50= 79 ± 34 nM) | Partial agonist (EC50= 91 ± 78 nM) | nd | Inverse agonist (EC50= 180 ± 90 nM) | Inverse agonist (EC50= 340 ± 92 nM) | nd |
With histamine | No effect (Ki > 100 µM) | Antagonist (Ki= 63 ± 40 nM) | Antagonist (Ki= 56 ± 22 nM) | Antagonist (Ki= 250 ± 120 nM) | Antagonist (Ki= 220 ± 100 nM) | Antagonist (Ki= 45 ± 11 nM) |
Values from Arrang et al. (1985a). The values at the two isoforms are derived from data shown in Figure 4.
nd, not determined.