Hedlund H, Andersson K E
J Auton Pharmacol. 1985 Mar;5(1):81-8. doi: 10.1111/j.1474-8673.1985.tb00568.x.
The contractile and relaxant effects of drugs which interact with adreno- and muscarinic receptors were investigated in isolated tissue from the human corpus cavernosum urethrae (CC) and the cavernous artery (Acc). Isolated CC preparations were contracted in a concentration-dependent fashion by noradrenaline (NA), phenylephrine and clonidine in the mentioned order of potency. Prazosin was 300 times more active than rauwolscine in inhibiting NA-induced contractions. In segments of the isolated Acc, clonidine was more potent than NA and phenylephrine, and prazosin and rauwolscine were about equieffective in inhibiting NA-induced contractions. Prazosin was more effective than rauwolscine in CC strips, and rauwolscine more effective than prazosin in Acc segments in inhibiting the noradrenergically mediated part of electrically induced contractions. Isoprenaline, prenalterol and procaterol each relaxed NA-contracted CC preparations in a concentration-dependent way; this effect was blocked by propranolol. Isoprenaline had no relaxant action in Acc segments. Neither acetylcholine (ACh) nor carbachol produced contraction in CC and Acc preparations. ACh, but particularly carbachol, had potent relaxant effects in NA-contracted CC preparations. This effect of ACh and carbachol was blocked by scopolamine. Relaxant, but less potent effects of the muscarinic receptor agonists were found in the Acc segments. It is suggested that there are important differences between penile arteries and erectile tissue proper in the response to adrenoreceptor and muscarinic receptor active drugs. The contractile effect of NA seems to be mediated mainly by alpha 1-adrenoreceptors in the CC and by alpha 2-adrenoreceptors in the Acc. It cannot be excluded that muscarinic receptor-mediated relaxation of NA-contracted CC preparations can be of importance for penile tumescence and erection.
研究了与肾上腺素能和毒蕈碱受体相互作用的药物对人尿道海绵体(CC)和海绵体动脉(Acc)离体组织的收缩和舒张作用。离体CC制剂以浓度依赖性方式依次被去甲肾上腺素(NA)、去氧肾上腺素和可乐定收缩。哌唑嗪在抑制NA诱导的收缩方面比萝芙木碱活性高300倍。在离体Acc节段中,可乐定比NA和去氧肾上腺素更有效,哌唑嗪和萝芙木碱在抑制NA诱导的收缩方面效果大致相同。在CC条带中,哌唑嗪比萝芙木碱更有效,而在Acc节段中,萝芙木碱在抑制电诱导收缩的去甲肾上腺素能介导部分方面比哌唑嗪更有效。异丙肾上腺素、普瑞特罗和丙卡特罗均以浓度依赖性方式舒张NA收缩的CC制剂;这种作用被普萘洛尔阻断。异丙肾上腺素在Acc节段中无舒张作用。乙酰胆碱(ACh)和卡巴胆碱在CC和Acc制剂中均未产生收缩作用。ACh,尤其是卡巴胆碱,在NA收缩的CC制剂中具有强效舒张作用。ACh和卡巴胆碱的这种作用被东莨菪碱阻断。在Acc节段中发现了毒蕈碱受体激动剂的舒张作用,但效力较低。提示阴茎动脉和勃起组织本身在对肾上腺素能受体和毒蕈碱受体活性药物的反应上存在重要差异。NA的收缩作用似乎主要由CC中的α1肾上腺素能受体和Acc中的α2肾上腺素能受体介导。不能排除毒蕈碱受体介导的NA收缩的CC制剂舒张对阴茎肿胀和勃起可能具有重要意义。