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哌唑嗪而非KMD-3213或利血平诱导大鼠α-1肾上腺素能受体上调。

Alpha-1 adrenoceptor up-regulation induced by prazosin but not KMD-3213 or reserpine in rats.

作者信息

Zhang Li, Taniguchi Takanobu, Tanaka Takashi, Shinozuka Kazumasa, Kunitomo Masaru, Nishiyama Masahiko, Kamata Koji, Muramatsu Ikunobu

机构信息

Department of Pharmacology, School of Medicine, Fukui Medical University, Matsuoka, Fukui 910-1193, Japan.

出版信息

Br J Pharmacol. 2002 Apr;135(7):1757-64. doi: 10.1038/sj.bjp.0704639.

DOI:10.1038/sj.bjp.0704639
PMID:11934817
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1573304/
Abstract
  1. We have investigated the effects of chronic administration of prazosin (a subtype-nonspecific alpha-1 AR antagonist), KMD-3213 (an alpha-1A AR subtype-specific antagonist) and reserpine (a catecholamine depletor) on the density of alpha-1 AR subtypes in various rat tissues (liver, kidney, submaxillary gland, heart and spleen). 2. Administration of prazosin (2 mg kg(-1) day(-1), i.p.) for 2 weeks did not affect K(D) values for [(3)H]-prazosin or [(3)H]-KMD-3213 of alpha-1 ARs in five rat tissues tested. However, it caused 52% up-regulation of alpha-1B AR in the spleen, and 84% and 107% up-regulation of alpha-1A- and alpha-1B ARs, respectively, in the heart. Although major subtypes of alpha-1 AR are alpha-1A AR in the submaxillary gland, alpha-1B AR in the liver, and alpha-1A and alpha-1B ARs in the kidney, these tissues showed no up-regulation. The mRNA levels of alpha-1 AR subtypes were not affected by prazosin administration in any tissue tested. 3. Neither administration of KMD-3213 (2 mg kg(-1) day(-1), i.p.) nor reserpine (0.5 - 1 mg kg(-1) day(-1), i.p.) for 2 weeks caused any change in either the binding affinity for [(3)H]-prazosin or [(3)H]-KMD-3213 or the density of the alpha-1 AR subtypes in the five rat tissues. 4. Neither prazosin nor KMD-3213 treatment reduced the noradrenaline content in the five rat tissues, in contrast to reserpine treatment, which markedly reduced it. 5. The findings of the present study demonstrated that up-regulation of alpha-1 AR is selectively caused by prazosin treatment in some tissues but neither by KMD-3213 treatment nor by chemical denervation with reserpine. These results suggest that up-regulation of alpha-1 ARs is not caused by a simple blockade of sympathetic tone.
摘要
  1. 我们研究了长期给予哌唑嗪（一种非亚型特异性α-1肾上腺素能受体拮抗剂）、KMD-3213（一种α-1A肾上腺素能受体亚型特异性拮抗剂）和利血平（一种儿茶酚胺耗竭剂）对大鼠各种组织（肝脏、肾脏、颌下腺、心脏和脾脏）中α-1肾上腺素能受体亚型密度的影响。2. 以2 mg·kg⁻¹·天⁻¹的剂量腹腔注射哌唑嗪2周，对所检测的五种大鼠组织中α-1肾上腺素能受体与[³H] - 哌唑嗪或[³H] - KMD-3213的解离常数（K(D)值）没有影响。然而，它使脾脏中的α-1B肾上腺素能受体上调了52%，使心脏中的α-1A和α-1B肾上腺素能受体分别上调了84%和107%。虽然颌下腺中α-1肾上腺素能受体的主要亚型是α-1A肾上腺素能受体，肝脏中是α-1B肾上腺素能受体，肾脏中是α-1A和α-1B肾上腺素能受体，但这些组织均未出现上调。在所检测的任何组织中，哌唑嗪给药均未影响α-1肾上腺素能受体亚型的mRNA水平。3. 以2 mg·kg⁻¹·天⁻¹的剂量腹腔注射KMD-3213 2周或腹腔注射利血平（0.5 - 1 mg·kg⁻¹·天⁻¹）2周，对大鼠五种组织中[³H] - 哌唑嗪或[³H] - KMD-3213的结合亲和力或α-1肾上腺素能受体亚型的密度均未引起任何变化。4. 与利血平治疗显著降低去甲肾上腺素含量相反，哌唑嗪和KMD-3213治疗均未降低大鼠五种组织中的去甲肾上腺素含量。5. 本研究结果表明，α-1肾上腺素能受体的上调是由哌唑嗪治疗在某些组织中选择性引起的，而不是由KMD-3213治疗或利血平化学去神经支配引起的。这些结果表明，α-1肾上腺素能受体的上调不是由交感神经张力的简单阻断所致。

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