Binding affinities (Ki; micromolar) for selected compounds at α adrenergic receptors
Values for α1A-, α1B-, and α2B-receptors determined by NovaScreen Biosciences, using their standard protocols as described for Table 3. Values for α2A and α2B receptors were conducted at Alcon and are the mean of at least three experiments ± S.E.M. where appropriate.
Compound | α1Aa | α1Bb | α2Ac [IC50] | α2Bd | α2Cc [IC50] |
|---|---|---|---|---|---|
| 5-MeODMT | >10 | >10 | 13.5 ± 1.40 | ∼1 | 6.93 ± 3.63 |
| 5-HOAMT | >10 | >10 | 29.6 ± 3.62 | >10 | 10.4 ± 3.36 |
| 5-MeOAMT | >10 | >10 | 21.2 ± 12.3 | >1 | >10 |
| R-DOI | >10 | >10 | >10 | 2.11 | 10.1 ± 0.60 |
| Apraclonidine | 0.033 ± 0.005 | 0.195 ± 0.069 | |||
| Brimonidine |
|
| 0.027 ± 0.005 |
| 0.434 ± 0.088 |