Pranzatelli M R
Department of Neurology, College of Physicians and Surgeons, Columbia University, New York, NY 10032.
Neurosci Lett. 1990 Jul 17;115(1):74-80. doi: 10.1016/0304-3940(90)90520-j.
DOI (1-(2,5-dimethoxy-4-iodophenyl aminopropane)-2) has recently been suggested as a selective 5-HT2 receptor agonist, but its behavioral effects have not been previously reported. In naive rats, DOI induced dose-dependent shaking behavior, the novel behavior 'skin jerks' (paraspinal muscle contractions), and forepaw tapping of the 'serotonin syndrome'. These behaviors had a similar dose-response and time course and were blocked by the 5-HT2/5-HT1C antagonists mianserin, ritanserin, and methysergide. Skin jerks, unlike other behaviors, were not blocked by 1-propranolol or phenoxybenzamine, drugs with little activity at 5-HT2/5-HT1C sites. Differences in the pharmacology and neuroanatomy between skin jerks and shaking behavior suggest that the 5-HT1C receptor may participate in skin jerks and the 5-HT2 receptor in shaking behavior, but drug coaffinities for 5-HT2 and 5-HT1C receptors require further investigation.
DOI(1-(2,5-二甲氧基-4-碘苯基氨基丙烷)-2)最近被认为是一种选择性5-HT2受体激动剂,但此前尚未报道其行为效应。在未接触过该药物的大鼠中,DOI诱发剂量依赖性的颤抖行为、新出现的行为“皮肤抽搐”(椎旁肌收缩)以及“血清素综合征”的前爪轻拍。这些行为具有相似的剂量反应和时间进程,并被5-HT2/5-HT1C拮抗剂米安色林、利坦色林和麦角酰二乙胺阻断。与其他行为不同,皮肤抽搐不会被1-普萘洛尔或苯氧苄胺阻断,这两种药物在5-HT2/5-HT1C位点活性较低。皮肤抽搐和颤抖行为在药理学和神经解剖学上的差异表明,5-HT1C受体可能参与皮肤抽搐,而5-HT2受体参与颤抖行为,但药物对5-HT2和5-HT1C受体的亲和力需要进一步研究。