Ferrari F, Baggio G
Eur J Pharmacol. 1982 Jul 9;81(2):321-6. doi: 10.1016/0014-2999(82)90451-4.
N-n-Propyl-norapomorphine (NPA), a potent dopamine (DA) receptor stimulant, in doses from 0.4 to 80 micrograms/kg i.p. produced a dose-related sexual stimulant effect characterized by recurrent episodes of penile erection (PE). The number of episodes and percentage of responding subjects were proportional to the dose. However, above the maximal effective dose, the effect decreased in a dose-related fashion until beyond 2.5 mg/kg even the natural occurrence of PE was suppressed. Morphine (5 mg/kg), as well as haloperidol (0.3 mg/kg), prevented NPA stimulation. Naloxone, which per se caused a modest increase in PE, markedly potentiated the stimulant effect of low doses of NPA, reversing the inhibitory component of higher doses. We suggest that NPA stimulation of DNA receptors causes release of opiate peptides, dampening the sexual stimulant response. The combination of DA receptor stimulants with naloxone might offer a new possibility for erection defect therapy.
N-正丙基去甲阿扑吗啡(NPA)是一种强效多巴胺(DA)受体兴奋剂,腹腔注射剂量为0.4至80微克/千克时,会产生与剂量相关的性兴奋作用,其特征为阴茎勃起(PE)反复发作。发作次数和有反应的受试者百分比与剂量成正比。然而,超过最大有效剂量后,该作用呈剂量相关方式下降,直至超过2.5毫克/千克,甚至自然发生的阴茎勃起也受到抑制。吗啡(5毫克/千克)以及氟哌啶醇(0.3毫克/千克)可阻止NPA的刺激作用。纳洛酮本身会使阴茎勃起略有增加,它能显著增强低剂量NPA的兴奋作用,逆转高剂量的抑制作用。我们认为,NPA对多巴胺受体的刺激会导致阿片肽释放,从而减弱性兴奋反应。多巴胺受体兴奋剂与纳洛酮联合使用可能为勃起功能障碍治疗提供新的可能性。