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Table 2 Affinity of norepinephrine for the mutated alpha-2C adrenergic receptors expressed in CHO cells.

From: Down-regulation of the alpha-2C adrenergic receptor: involvement of a serine/threonine motif in the third cytoplasmic loop

Clone

Ki, nM

Slope factor

n

Wild-type (SSTS)

184 ± 9

0.79

3

SSVA

90 ± 4*

0.73

3

AAVA

71 ± 5*

0.65

3

  1. Ki values were derived based on a single-site model and are the geometric means of three independent inhibition experiments, each done in duplicate. The slope factor was determined in a separate analysis based on a variable slope model. The data were not consistently better fit by a two-site model than a one-site model for any of the three clones. The concentration of [3H]rauwolscine was 0.12 ± 0.01 nM. *Significantly different (p < 0.05) than wild-type based on a t-test of the pKi values.