James S, Chapple C R, Phillips M I, Greengrass P M, Davey M J, Turner-Warwick R T, Milroy E J, Burnstock G
Department of Anatomy and Developmental Biology, University College London, England.
J Urol. 1989 Aug;142(2 Pt 1):438-44. doi: 10.1016/s0022-5347(17)38780-3.
Radioligand receptor binding and autoradiography were used to characterize, localize and compare alpha-1 and alpha-2 adrenoceptors and muscarinic cholinergic receptor populations in human benign prostatic hyperplastic tissue. The binding of selective alpha-1 and alpha-2 ligands, [3H]-prazosin and [3H]-UK 14,304, to homogenates of human central and peripheral prostate was saturable and of high affinity. Scatchard analysis produced an equilibrium dissociation constant (KD) of 0.51 +/- 0.10 nM for alpha-1 adrenoceptors, and 2.34 +/- 0.40 nM for alpha-2 adrenoceptors. The mean densities, Bmax, of alpha-1 and alpha-2 adrenoceptors identified in the human adenomatous prostate were 65.9 +/- 12.9 and 36.1 +/- 7.0 fmoles/mg. protein respectively. Receptor autoradiography was used to examine the distribution of muscarinic cholinergic receptors [( 3H]-QNB), alpha-1 adrenoceptors [( 3H]-prazosin]), and alpha-2 adrenoceptors [( 3H]-rauwolscine) on consecutive sections of benign hyperplastic prostatic tissue. Although both subtypes of adrenoceptor were seen in the stromal component of the hyperplastic prostate, there was a substantial predominance of alpha-1 adrenoceptors. A densitometric computer-assisted analysis was performed on the autoradiographic slides to determine the mean ratio of specific alpha-1: alpha-2 adrenoceptors in the stromal compartment of the hyperplastic tissue. The ratio, expressed as % grain occupancy/unit area, was 3.9 +/- 0.75, which is in agreement with a functional alpha-1 adrenoceptor predominance shown in previous studies. Although sparsely distributed in the stroma, a dense alpha-2 adrenoceptor population was seen in association with blood vessels, and in close proximity to the base of some of the [3H]-QNB-labelled prostatic glandular epithelial cells.(ABSTRACT TRUNCATED AT 250 WORDS)
采用放射性配体受体结合和放射自显影技术,对人良性前列腺增生组织中的α-1和α-2肾上腺素能受体以及毒蕈碱胆碱能受体群体进行表征、定位和比较。选择性α-1和α-2配体[³H] - 哌唑嗪和[³H] - UK 14,304与人中枢和外周前列腺匀浆的结合具有饱和性且亲和力高。Scatchard分析得出α-1肾上腺素能受体的平衡解离常数(KD)为0.51±0.10 nM,α-2肾上腺素能受体的平衡解离常数为2.34±0.40 nM。在人腺瘤性前列腺中鉴定出的α-1和α-2肾上腺素能受体的平均密度Bmax分别为65.9±12.9和36.1±7.0 fmol/mg蛋白质。利用受体放射自显影技术,在良性增生性前列腺组织的连续切片上检测毒蕈碱胆碱能受体([³H] - QNB)、α-1肾上腺素能受体([³H] - 哌唑嗪)和α-2肾上腺素能受体([³H] - 萝芙木碱)的分布。尽管在增生性前列腺的基质成分中都能看到两种亚型的肾上腺素能受体,但α-1肾上腺素能受体占主导地位。对放射自显影片进行密度计计算机辅助分析,以确定增生组织基质区中特异性α-1:α-2肾上腺素能受体的平均比例。以每单位面积的颗粒占有率百分比表示的比例为3.9±0.75,这与先前研究中显示的功能性α-1肾上腺素能受体优势一致。虽然在基质中分布稀疏,但在血管附近以及一些[³H] - QNB标记的前列腺腺上皮细胞基部附近可以看到密集的α-2肾上腺素能受体群体。(摘要截短于250字)