Andersen M B, Fuxe K, Werge T, Gerlach J
Sct. Hans Hospital, Research Institute of Biological Psychiatry, DK-4000 Roskilde, Denmark.
Behav Pharmacol. 2002 Dec;13(8):639-44. doi: 10.1097/01.fbp.0000047148.28986.67.
The adenosine A2A receptor agonist CGS 21680 has shown effects similar to dopamine antagonists in behavioural assays in rats predictive for antipsychotic activity, without induction of extrapyramidal side-effects (EPS). In the present study, we examined whether this functional dopamine antagonism and lack of EPS in rodents could also be observed in non-human primates. We investigated the effects of CGS 21680 on behaviours induced by D-amphetamine and (-)-apomorphine in EPS-sensitized Cebus apella monkeys. CGS 21680 was administered s.c. in doses of 0.01, 0.025 and 0.05 mg/kg, alone and in combination with D-amphetamine and (-)-apomorphine. The monkeys were videotaped after drug administration and the tapes were rated for EPS and psychosis-like symptoms. CGS 21680 decreased apomorphine-induced behavioural unrest, arousal (0.01-0.05 mg/kg) and stereotypies (0.05 mg/kg) while amphetamine-induced behaviours (unrest, stereotypies, arousal) were unaffected. EPS were not observed at any dose. At 0.05 mg/kg CGS 21680 produced vomiting. The two lower doses did not produce observable side-effects. Though the differential effect on amphetamine- and apomorphine-induced behaviours is intriguing, CGS 21680 showed a functional anti-dopaminergic effect in Cebus apella monkeys without production of EPS. This further substantiates that adenosine A2A receptor agonists may have potential as antipsychotics with atypical profiles.
腺苷A2A受体激动剂CGS 21680在预测抗精神病活性的大鼠行为试验中显示出与多巴胺拮抗剂相似的作用,且不会诱发锥体外系副作用(EPS)。在本研究中,我们检测了在非人类灵长类动物中是否也能观察到这种在啮齿动物中的功能性多巴胺拮抗作用及缺乏EPS的情况。我们研究了CGS 21680对EPS致敏的僧帽猴中由D-苯丙胺和(-)-阿扑吗啡诱导的行为的影响。CGS 21680以0.01、0.025和0.05 mg/kg的剂量皮下给药,单独给药以及与D-苯丙胺和(-)-阿扑吗啡联合给药。给药后对猴子进行录像,并对录像带进行EPS和类精神病症状评分。CGS 21680减少了阿扑吗啡诱导的行为不安、觉醒(0.01 - 0.05 mg/kg)和刻板行为(0.05 mg/kg),而苯丙胺诱导的行为(不安、刻板行为、觉醒)未受影响。在任何剂量下均未观察到EPS。CGS 21680在0.05 mg/kg时引起呕吐。两个较低剂量未产生可观察到的副作用。尽管对苯丙胺和阿扑吗啡诱导行为的差异效应很有趣,但CGS 21680在僧帽猴中显示出功能性抗多巴胺能作用且未产生EPS。这进一步证实腺苷A2A受体激动剂可能具有作为非典型抗精神病药物的潜力。