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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Okada F, Saito H, Matsuki N

Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

Br J Pharmacol. 1995 Mar;114(5):931-4. doi: 10.1111/j.1476-5381.1995.tb13293.x.

The effects of (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOl), a 5-hydroxytryptamine 5-HT2A/5-HT2C receptor agonist, on motion- and cisplatin-induced emesis were studied in Suncus murinus. Subcutaneous injection of DOl, 30 min prior to the emetic stimuli, dose-dependently blocked the emesis induced by motion sickness and cisplatin (20 mg kg-1, i.p.) with estimated ID50 values of 640 and 780 micrograms kg-1, respectively. 2. alpha-Methyl-5-hydroxytryptamine (alpha-Me-5-HT), a peripheral 5-HT2A/5-HT2C receptor agonist, had no effect on motion- and cisplatin-induced emesis. 3. The antiemetic effects of DOl on motion- and cisplatin-induced emesis were attenuated by preadministration of ketanserin, a selective 5-HT2A receptor antagonist. 4. The present results suggest an inhibitory role for central 5-HT2 receptors in the emetic reflex mechanism and that a 5-HT2 receptor agonist may be a useful tool to investigate the involvement of 5-HT receptors in the emetic reflex.

研究了5-羟色胺5-HT2A/5-HT2C受体激动剂（±）-1-（2,5-二甲氧基-4-碘苯基）-2-氨基丙烷（DOI）对小家鼠运动和顺铂诱导呕吐的影响。在催吐刺激前30分钟皮下注射DOI，剂量依赖性地阻断晕动病和顺铂（20毫克/千克，腹腔注射）诱导的呕吐，估计ID50值分别为640和780微克/千克。2. α-甲基-5-羟色胺（α-Me-5-HT），一种外周5-HT2A/5-HT2C受体激动剂，对运动和顺铂诱导的呕吐没有影响。3. DOI对运动和顺铂诱导呕吐的止吐作用被选择性5-HT2A受体拮抗剂酮色林预先给药所减弱。4. 目前的结果表明中枢5-HT2受体在呕吐反射机制中起抑制作用，并且5-HT2受体激动剂可能是研究5-HT受体参与呕吐反射的有用工具。

Okada F, Saito H, Matsuki N

Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

Br J Pharmacol. 1995 Mar;114(5):931-4. doi: 10.1111/j.1476-5381.1995.tb13293.x.

The effects of (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOl), a 5-hydroxytryptamine 5-HT2A/5-HT2C receptor agonist, on motion- and cisplatin-induced emesis were studied in Suncus murinus. Subcutaneous injection of DOl, 30 min prior to the emetic stimuli, dose-dependently blocked the emesis induced by motion sickness and cisplatin (20 mg kg-1, i.p.) with estimated ID50 values of 640 and 780 micrograms kg-1, respectively. 2. alpha-Methyl-5-hydroxytryptamine (alpha-Me-5-HT), a peripheral 5-HT2A/5-HT2C receptor agonist, had no effect on motion- and cisplatin-induced emesis. 3. The antiemetic effects of DOl on motion- and cisplatin-induced emesis were attenuated by preadministration of ketanserin, a selective 5-HT2A receptor antagonist. 4. The present results suggest an inhibitory role for central 5-HT2 receptors in the emetic reflex mechanism and that a 5-HT2 receptor agonist may be a useful tool to investigate the involvement of 5-HT receptors in the emetic reflex.

研究了5-羟色胺5-HT2A/5-HT2C受体激动剂（±）-1-（2,5-二甲氧基-4-碘苯基）-2-氨基丙烷（DOI）对小家鼠运动和顺铂诱导呕吐的影响。在催吐刺激前30分钟皮下注射DOI，剂量依赖性地阻断晕动病和顺铂（20毫克/千克，腹腔注射）诱导的呕吐，估计ID50值分别为640和780微克/千克。2. α-甲基-5-羟色胺（α-Me-5-HT），一种外周5-HT2A/5-HT2C受体激动剂，对运动和顺铂诱导的呕吐没有影响。3. DOI对运动和顺铂诱导呕吐的止吐作用被选择性5-HT2A受体拮抗剂酮色林预先给药所减弱。4. 目前的结果表明中枢5-HT2受体在呕吐反射机制中起抑制作用，并且5-HT2受体激动剂可能是研究5-HT受体参与呕吐反射的有用工具。