| |
SH-SY5Y
|
SHβ
2
AR4
|
|---|
Agonist:
|
log(K
i
)
|
log(EC
50
)
|
log(EC
50
)
|
|---|
EPI | -7.38 ± .04 | -8.83 ± .06 | -8.22 ± 0.21 |
UK 14,304 | -7.38 ± .12 | -7.22 ± .36 | -7.72 ± 0.77 |
Oxymetazoline (OXY) | -8.85a | -8.35 ± .47 | N.D. |
Isoproterenol | N.A. | N.A. | -7.02 ± 0.28 |
Antagonist:
|
log(K
i
)
|
K
i
Ratio with OXY
| |
Rauwolscine | -8.82 ± .15 | 1.07 | N.A |
Yohimbine | -8.56 ± .17 | 1.95 | N.A |
Prasozin | -6.98a | 74.4 | N.A |
- Binding inhibition and cAMP accumulation studies were performed as described in Methods. The values of the apparent affinity constants Log(K
i
) for each competitor were derived from their IC50 values (n = 3–9) using the equation of Cheng and Prusoff [40]. The Log(EC50) values (concentration of the drug that produces 50% of the maximal inhibitory/stimulatory effect of that drug) were calculated by nonlinear regression analysis of the agonist concentration-response curves (n = 3–9) of each agonist. aValues from Kazmi and Mishra [24]. N.D., not determined; N.A., not applicable.
