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Pharmacological characteristics of adrenoceptors in SH-SH5Y and SHβ2AR4 cells. |
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| SH-SY5Y |
SHβ2AR4 |
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|
|
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| Agonist: |
log(Ki) |
log(EC50) |
log(EC50) |
|
|
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| 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 |
|
|
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| Antagonist: |
log(Ki) |
Ki 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(Ki) 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. | |||
Bawa-Khalfe et al. BMC Pharmacology 2007 7:16 doi:10.1186/1471-2210-7-16 |
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