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离体人前列腺中的α-肾上腺素能受体和毒蕈碱受体

Alpha-adrenoceptors and muscarinic receptors in the isolated human prostate.

作者信息

Hedlund H, Andersson K E, Larsson B

出版信息

J Urol. 1985 Dec;134(6):1291-8. doi: 10.1016/s0022-5347(17)47714-7.

Abstract

Prostatic specimens of adenomatous tissue (PA) were obtained from the lateral lobe of the prostate in patients with benign prostatic hyperplasia (BPH). Non-hyperplastic specimens of the outer prostatic tissue (PC) were taken from the dorsal part of the prostate in patients undergoing cystourethrectomy. Effects of alpha-adrenoceptor and muscarinic receptor active drugs were studied. Noradrenaline (NA) and the alpha 1-adrenoceptor agonist phenylephrine induced concentration-dependent contractions in PC and PA preparations. The alpha 2-adrenoceptor agonist clonidine was without effect on PC but contracted PA preparations; it was less potent and had less intrinsic activity than phenylephrine. In PC and PA strips, the alpha 1-adrenoceptor antagonist prazosin was more effective than the alpha 2-adrenoceptor antagonist rauwolscine to inhibit NA-induced contractions. Prazosin, but not rauwolscine, inhibited electrically induced contractions in PC strips. The muscarinic receptor agonists acetylcholine and carbachol were without effect in PC and PA preparations. In both PC and PA preparations, clonidine decreased and rauwolscine increased the electrically elicited 3H-efflux after pre-loading of the tissues with 3H-noradrenaline. Carbachol and scopolamine were without consistent effects. In radioligand receptor binding experiments, the occurrence of alpha 1- and alpha 2-adrenoceptor binding sites was demonstrated; the ratio between alpha 1- and alpha 2-adrenoceptor binding sites was 3/2 in PC, but 2/3 in PA tissue. By autoradiography, muscarinic receptors were found to be localized exclusively to the glandular epithelium, consistent with the lack of contractile effects of muscarinic receptor active drugs on PC and PA preparations. Our results thus suggest that the main alpha-adrenoceptor function in human prostatic smooth muscle is of the alpha 1-type and that muscarinic receptors in the prostate are involved in processes other than control of smooth muscle contraction.

摘要

从良性前列腺增生(BPH)患者的前列腺侧叶获取腺瘤组织前列腺标本(PA)。从接受膀胱尿道切除术患者的前列腺背侧获取前列腺外组织非增生标本(PC)。研究了α - 肾上腺素能受体和毒蕈碱受体活性药物的作用。去甲肾上腺素(NA)和α1 - 肾上腺素能受体激动剂去氧肾上腺素在PC和PA制剂中诱导浓度依赖性收缩。α2 - 肾上腺素能受体激动剂可乐定对PC无作用,但使PA制剂收缩;其效力低于去氧肾上腺素,内在活性也较小。在PC和PA条带中,α1 - 肾上腺素能受体拮抗剂哌唑嗪比α2 - 肾上腺素能受体拮抗剂利血平更有效地抑制NA诱导的收缩。哌唑嗪而非利血平抑制PC条带中的电诱导收缩。毒蕈碱受体激动剂乙酰胆碱和卡巴胆碱在PC和PA制剂中无作用。在PC和PA制剂中,用3H - 去甲肾上腺素预加载组织后,可乐定降低而利血平增加电诱发的3H - 外流。卡巴胆碱和东莨菪碱无一致作用。在放射性配体受体结合实验中,证明了α1和α2 - 肾上腺素能受体结合位点的存在;PC中α1与α2 - 肾上腺素能受体结合位点的比例为3/2,但PA组织中为2/3。通过放射自显影,发现毒蕈碱受体仅定位于腺上皮,这与毒蕈碱受体活性药物对PC和PA制剂缺乏收缩作用一致。因此,我们的结果表明,人前列腺平滑肌中的主要α - 肾上腺素能受体功能是α1型,并且前列腺中的毒蕈碱受体参与平滑肌收缩控制以外的过程。

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