Rosenzweig-Lipson S, Bergman J
Harvard University, Department of Psychology, Cambridge, MA 02138.
Eur J Pharmacol. 1994 Aug 1;260(2-3):237-41. doi: 10.1016/0014-2999(94)90343-3.
Observational procedures were used to compare the behavioral effects of dopamine D1 receptor antagonists and partial dopamine D1 receptor agonists in squirrel monkeys. The dopamine D1 receptor antagonists SCH 39166 ((-)-trans-6-7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N- methyl-5H-benzo(d)naphtho-(2,1-b)azepine) and BW 737C89 ([S]-6-chloro-1-[2,5-dimethoxy-4-propylbenzyl]-7- hydroxy-2-methyl-1,2,3,4-tetrahydroisoquinoline) produced dose-related increases in the duration of static and unusual postures, indicative of catalepsy. R-SKF 38393 (R(+)-7,8- dihydroxy-1-phenyl-2,3,4,5-tetrahydro-[1H]-3-benzazepine) and SKF 75670 (7,8-dihydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-[1H]-3- benzazepine), which are considered partial dopamine D1 receptor agonists, also consistently produced dose-related increases in catalepsy-associated behavior and had effects comparable in magnitude to those of dopamine D1 receptor antagonists. In contrast, the higher efficacy D1 agonists SKF 81297 (6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-[1H]-3- benzazepine) and SKF 82958 (6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-3-allyl-[1H]-3- benzazepine) did not produce catalepsy-associated behavior at any dose tested. The results indicate that dopamine D1 agonists differ with respect to cataleptogenic activity, possibly reflecting differences in intrinsic activity.
采用观察程序比较多巴胺D1受体拮抗剂和部分多巴胺D1受体激动剂对松鼠猴的行为影响。多巴胺D1受体拮抗剂SCH 39166（（-）-反式-6,7,7a,8,9,13b-六氢-3-氯-2-羟基-N-甲基-5H-苯并[d]萘并[2,1-b]氮杂卓）和BW 737C89（[S]-6-氯-1-[2,5-二甲氧基-4-丙基苄基]-7-羟基-2-甲基-1,2,3,4-四氢异喹啉）可使静态和异常姿势的持续时间呈剂量依赖性增加，提示有僵住症。R-SKF 38393（R（+）-7,8-二羟基-1-苯基-2,3,4,5-四氢-[1H]-3-苯并氮杂卓）和SKF 75670（7,8-二羟基-3-甲基-1-苯基-2,3,4,5-四氢-[1H]-3-苯并氮杂卓）被认为是部分多巴胺D1受体激动剂，它们也始终使僵住症相关行为呈剂量依赖性增加，且其作用强度与多巴胺D1受体拮抗剂相当。相比之下，高效能D1激动剂SKF 81297（6-氯-7,8-二羟基-1-苯基-2,3,4,5-四氢-[1H]-3-苯并氮杂卓）和SKF 82958（6-氯-7,8-二羟基-1-苯基-2,3,4,5-四氢-3-烯丙基-[1H]-3-苯并氮杂卓）在任何测试剂量下均未产生僵住症相关行为。结果表明，多巴胺D1激动剂在致僵住症活性方面存在差异，这可能反映了内在活性的差异。
