Andén N E, Nilsson H, Ros E, Thornström U
Acta Pharmacol Toxicol (Copenh). 1983 Jan;52(1):51-6. doi: 10.1111/j.1600-0773.1983.tb01075.x.
B-HT 920 at low doses inhibited the accumulation of DOPA following treatment with reserpine and a DOPA decarboxylase inhibitor in the dopamine-, but not in the noradrenaline-predominant regions of the rat brain. B-HT 933 selectively inhibited this DOPA accumulation in the noradrenaline-predominant regions. These effects of B-HT 920 and B-HT 933 were completely antagonized by haloperidol and yohimbine, respectively. The rat motor activity was reduced by B-HT 920 and it was restored following apomorphine. B-HT 933 decreased the motor activity by a yohimbine-sensitive mechanism. The results indicate that B-HT 920 can selectively and potently stimulate the dopamine autoreceptors whereas B-HT 933 can selectively stimulate the noradrenaline autoreceptors.
低剂量的B-HT 920可抑制利血平和多巴脱羧酶抑制剂处理后大鼠脑中多巴胺占优势区域(而非去甲肾上腺素占优势区域)内多巴的蓄积。B-HT 933可选择性抑制去甲肾上腺素占优势区域内的这种多巴蓄积。B-HT 920和B-HT 933的这些作用分别被氟哌啶醇和育亨宾完全拮抗。B-HT 920可降低大鼠的运动活性,而阿扑吗啡可使其恢复。B-HT 933通过一种对育亨宾敏感的机制降低运动活性。结果表明,B-HT 920可选择性且强效地刺激多巴胺自身受体,而B-HT 933可选择性刺激去甲肾上腺素自身受体。