Appel J B, Callahan P M
Department of Psychology, University of South Carolina, Columbia 29208.
Eur J Pharmacol. 1989 Jan 2;159(1):41-6. doi: 10.1016/0014-2999(89)90041-1.
In order to further evaluate the extent to which particular 5-HT receptor subtypes (5-HT1, 5-HT2) might be involved in the behavioral effects of hallucinogenic drugs, rats were trained to discriminate mescaline (10 mg/kg i.p.) from saline and were given substitution (generalization) and combination (antagonism) tests with putatively selective serotonergic and related neuroactive compounds. The mescaline cue generalized to relatively high doses of the 5-HT2 agonists, 2,5-dimethoxy-4-methylamphetamine (DOM), LSD and psilocybin; the extent of generalization to 5-HT1 agonists (8-hydroxy-2-[diethylamino]tetralin (8-OHDPAT), RU-24969 and 8-hydroxy-2-[di-n-propylamino]tetralin (TFMPP] was unclear. Combinations of the training drug and sufficiently high doses of 5-HT2 antagonists (ketanserin, LY-53857, pirenperone) were followed by saline-lever responding; less selective central 5-HT (metergoline), and DA (SCH-23390, haloperidol) antagonists, did not block the mescaline cue. These data suggest that 5-HT2 receptors are involved in the stimulus properties of mescaline.
为了进一步评估特定的5-羟色胺（5-HT）受体亚型（5-HT1、5-HT2）可能参与致幻药物行为效应的程度，训练大鼠区分腹腔注射10毫克/千克的三甲氧苯乙胺与生理盐水，并给予其替代（泛化）和联合（拮抗）测试，使用假定具有选择性的血清素能及相关神经活性化合物。三甲氧苯乙胺线索泛化到相对高剂量的5-HT2激动剂，2,5-二甲氧基-4-甲基苯丙胺（DOM）、麦角酸二乙胺（LSD）和裸盖菇素；对5-HT1激动剂（8-羟基-2-[二乙氨基]四氢化萘（8-OHDPAT）、RU-24969和8-羟基-2-[二正丙氨基]四氢化萘（TFMPP））的泛化程度尚不清楚。训练药物与足够高剂量的5-HT2拮抗剂（酮色林、LY-53857、哌仑西平）联合使用后，大鼠出现生理盐水杠杆反应；选择性较低的中枢5-HT拮抗剂（麦角乙脲）和多巴胺拮抗剂（SCH-23390、氟哌啶醇）并未阻断三甲氧苯乙胺线索。这些数据表明，5-HT2受体参与了三甲氧苯乙胺的刺激特性。
