Abstract
To characterize the conformational requirements of the anterior pituitary dopamine (DA) receptor, we have examined the PRL-suppressive effects of two semirigid DA agonists of the 2-aminotetralin series: 2-amino-5,6-dihydroxy-1,2,3,4-tetrahydronaphthalene (A-5.6-DTN), an a-rotamer, and 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (A-6,7-DTN), the corresponding β-rotamer. In vivo studies were conducted on conscious, estrogen-primed male rats bearing indwelling right atrial catheters; in vitro studies utilized isolated rat anterior pituitary cells in 4-day primary culture. Both compounds exhibited full agonist activity in both systems, as judged by dose-response curves parallel to that of DA and identical maximal PRL suppression. In vivo A-5,6-DTN was equipotent to DA, and A-6,7-DTN was 8 times as potent as DA. The effects of all three agonists were unaltered by phentolamine or propranolol and were attenuated to a similar extent by haloperidol. The in vitro potency ratios were A-6,7-DTN:DA:A-5,6-DTN =...
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