Pichler L, Kobinger W
Naunyn Schmiedebergs Arch Pharmacol. 1981 Sep;317(2):180-2. doi: 10.1007/BF00500078.
The influence of two alpha-adrenoceptor agonists, clonidine and B-HT 920, on motor activity was tested in mice. Both, clonidine and B-HT 920 (2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo-[4,5-d]-azepine) in the dose range 30--300 micrograms/kg s.c. effectively inhibited exploratory activity. On the other hand only clonidine, which stimulates alpha 2- and alpha 1-adrenoceptors increased locomotor activity in mice treated with reserpine (5 mg/kg) and apomorphine (3 mg/kg) in the doses of 0.3 and 1 mg/kg i.p. The highly selective alpha 2-agonist B-HT 920 was ineffective under these conditions up to 30 mg/kg i.p. It is concluded, that in mice "sedative" alpha-adrenoceptors are of the alpha 2- and "excitatory" of the alpha 1-type.
在小鼠中测试了两种α-肾上腺素能受体激动剂可乐定和B-HT 920对运动活性的影响。可乐定和B-HT 920(2-氨基-6-烯丙基-5,6,7,8-四氢-4H-噻唑并-[4,5-d]-氮杂卓)皮下注射剂量在30 - 300微克/千克范围内均能有效抑制探索性活动。另一方面,仅可乐定,它能刺激α2和α1肾上腺素能受体,腹腔注射0.3和1毫克/千克剂量可增加用利血平(5毫克/千克)和阿扑吗啡(3毫克/千克)处理的小鼠的运动活性。在这些条件下,高达腹腔注射30毫克/千克剂量时,高选择性α2激动剂B-HT 920无效。得出结论,在小鼠中,“镇静性”α-肾上腺素能受体为α2型,“兴奋性”为α1型。