Melis M R, Stancampiano R, Argiolas A
Bernard B. Brodie Department of Neuroscience, University of Cagliari, Italy.
Eur J Pharmacol. 1992 Sep 10;220(1):43-8. doi: 10.1016/0014-2999(92)90009-s.
The effect of excitatory amino acid receptor antagonists, (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5, 10-imine hydrogen maleate ((+)-MK-801), (+/-)-3-(2-carboxy-piperazin-4-yl)-propyl-1-phosphonic acid (CPP), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and (+/-)-2-amino-4-phosphonobutanoic acid (AP-4), on penile erection and yawning induced by subcutaneous apomorphine (80 micrograms/kg), intracerebroventricular (i.c.v.) oxytocin (30 ng) and adrenocorticotropin (ACTH)-(1-24) (10 micrograms) was studied in male rats. Intraperitoneal (0.1-0.4 mg/kg) and i.c.v. (10-50 micrograms) (+)-MK-801 prevented dose dependently the penile erection and yawning induced by the three drugs. The (+)-MK-801 effect coincided with the appearance of head weaving, body rolling, hyperlocomotion and ataxia. Haloperidol (0.5 mg/kg i.p.) antagonized the prevention by (+)-MK-801 of oxytocin responses. Penile erection but not yawning was also prevented by high, but not low doses of CPP and CNQX, which impaired motor performance, AP-4 was ineffective at all doses tested. The above compounds were ineffective when injected into the paraventricular nucleus of the hypothalamus, the brain area where apomorphine and oxytocin act to induce penile erection and yawning. The results suggest that excitatory amino acid transmission is not involved in the expression of penile erection and yawning induced by the above compounds.
研究了兴奋性氨基酸受体拮抗剂（5R，10S）-（+）-5-甲基-10，11-二氢-5H-二苯并[a，d]环庚烯-5，10-亚胺马来酸氢盐（（+）-MK-801）、（±）-3-（2-羧基哌嗪-4-基）-丙基-1-膦酸（CPP）、6-氰基-7-硝基喹喔啉-2，3-二酮（CNQX）和（±）-2-氨基-4-膦酰基丁酸（AP-4）对皮下注射阿扑吗啡（80微克/千克）、脑室内（i.c.v.）注射催产素（30纳克）和促肾上腺皮质激素（ACTH）-（1-24）（10微克）诱导的雄性大鼠阴茎勃起和打哈欠的影响。腹腔注射（0.1-0.4毫克/千克）和脑室内注射（10-50微克）（+）-MK-801剂量依赖性地阻止了这三种药物诱导的阴茎勃起和打哈欠。（+）-MK-801的作用与头部摆动、身体翻滚、活动亢进和共济失调的出现同时发生。氟哌啶醇（0.5毫克/千克腹腔注射）拮抗了（+）-MK-801对催产素反应的阻止作用。高剂量而非低剂量的CPP和CNQX也阻止了阴茎勃起，但不影响打哈欠，且损害运动表现，AP-4在所有测试剂量下均无效。当将上述化合物注射到下丘脑室旁核（阿扑吗啡和催产素诱导阴茎勃起和打哈欠的脑区）时，它们没有效果。结果表明，兴奋性氨基酸传递不参与上述化合物诱导的阴茎勃起和打哈欠的表达。
