Van der Laan J W
Pharmacol Biochem Behav. 1987 Feb;26(2):265-9. doi: 10.1016/0091-3057(87)90116-x.
B-HT920 is known to be a selective alpha 2-adrenoceptor agonist, and has been used in a study on morphine-withdrawal in rats. In accordance with other alpha 2-agonists B-HT920 was found to potentiate "jumping" and to reduce "body shakes." However, B-HT920 did not suppress body weight loss. Furthermore, it induced strong salivation and prevented ptosis (described for the alpha 1-adrenergic agonist ST-587). Rearing and locomotor activity appeared to be enhanced, an effect shared by dopamine-agonist lisurid. The effects of B-HT920 have been specified using the alpha-adrenergic antagonists yohimbine and prazosin and the dopamine antagonist haloperidol. Yohimbine could not antagonize any of the actions of B-HT920. However the increase in rearing and locomotion was blocked by haloperidol. The induction of salivation was prevented by prazosin. Pretreatment with prazosin showed a decrease in the loss of body weight caused by B-HT920, while pretreatment with yohimbine showed that B-HT920 induced an increased loss in body weight. These data suggest that B-HT920 under certain conditions exerts dopamine-agonistic actions in stimulating locomotor activity and alpha 1-adrenergic actions in inducing salivation and enhanced loss of body weight.
已知B-HT920是一种选择性α2-肾上腺素能受体激动剂,已被用于大鼠吗啡戒断的研究。与其他α2-激动剂一样,发现B-HT920可增强“跳跃”并减少“身体颤抖”。然而,B-HT920并未抑制体重减轻。此外,它会引起强烈的唾液分泌,并防止上睑下垂(α1-肾上腺素能激动剂ST-587也有此作用描述)。竖毛和运动活动似乎增强,多巴胺激动剂利舒脲也有此作用。使用α-肾上腺素能拮抗剂育亨宾和哌唑嗪以及多巴胺拮抗剂氟哌啶醇确定了B-HT920的作用。育亨宾不能拮抗B-HT920的任何作用。然而,氟哌啶醇可阻断竖毛和运动活动的增加。哌唑嗪可防止唾液分泌的诱导。哌唑嗪预处理显示B-HT920引起的体重减轻减少,而育亨宾预处理显示B-HT920导致体重减轻增加。这些数据表明,B-HT920在某些条件下在刺激运动活动方面发挥多巴胺激动作用,在诱导唾液分泌和增强体重减轻方面发挥α1-肾上腺素能作用。