Down-regulation of alpha 2-adrenoceptor subtypes.

To characterize further the alpha 2-adrenoceptor subtypes in terms of their regulation, monolayers of cells expressing either the alpha 2A (CHO-A2AR cells) or alpha 2C (OK cells) subtype were preincubated with norepinephrine for various times and the extent of receptor down-regulation was assessed. Exposure to 30 microM norepinephrine caused a similar time course and extent of down-regulation (approximately 50%) in both cells lines. The extent of down-regulation caused by 0.3 microM norepinephrine in OK cells was similar to that with 30 microM norepinephrine in CHO-A2AR cells, although the time course was somewhat slower. Reversal of the down-regulation of the alpha 2-adrenoceptor caused by 30 microM norepinephrine was more rapid in the CHO-A2AR than in the OK cell. With 0.3 microM norepinephrine, reversal of down-regulation of the alpha 2-adrenoceptor in the OK cell was slightly faster than that of the CHO-A2AR cell with 30 microM norepinephrine. These data indicate that although norepinephrine is more potent in causing down-regulation of the alpha 2C (OK cells) as compared to the alpha 2A subtype (CHO-A2AR cells), the time courses for down-regulation and its reversal are similar for the two subtypes.