Inhibitory presynaptic imidazoline receptors on sympathetic nerves in the rabbit aorta differ from I1- and I2-imidazoline binding sites

The involvement of imidazoline receptors in modulation of noradrenaline release was investigated in the rabbit aorta preincubated with [³H]noradrenaline and superfused with physiological salt solution containing cocaine, corticosterone and propranolol.After blockade of ₂-autoreceptors by rauwolscine, the electrically evoked tritium overflow was inhibited by various imidazolines and guanidines. The rank order of potency was BDF 7579 (4-chloro-2-isoindolinyl) guanidine) BDF 6143 (4-chloro-2-(2-imidazolin-2-ylamino)-isoindoline] > BDF 6100 [2-(2-imidazolin2-y-lamino)-isoindoline] > clonidine > ST587 (2-(2-chloro-5-trifluoromethylphenylimino) imidazolidine nitrate) cirazoline > tolazoline > idazoxan > phentolamine. Comparison of the potencies of these drugs with those previously found for the presynaptic imidazoline receptors in the rabbit pulmonary artery revealed a very good correlation. In contrast, no positive correlation was found with their affinities for the I₁-and I₂-imidazoline binding sites in bovine adrenal medullary membranes and with their lipophilicity (log P values). The electrically evoked tritium overflow was also inhibited by the recently identified endogenous imidazoline receptor ligand agmatine, but was not affected by amiloride. In further series of experiments, the ability of putative antagonist at presynaptic imidazoline receptors to counteract the inhibitory effect of imidazoline derivatives was determined. Amiloride, imidazole-4-acetic acid and 1-benzylimidazole did not attenuate the inhibitory effect of BDF 6143 on the electrically evoked tritium overflow. In contrast, rauwolscine antagonized the inhibitory effect of various imidazolines; rauwolscine was clearly less potent in antagonizing the effect of clonidine, BDF 6143 and cirazoline (apparent pA₂ 6.48–7.32) than in antagonizing that of oxymetazoline and moxonidine (apparent pA₂ 8.33 and 8.12, respectively). In a final series of experiments, BDF 6143 (under the conditions applied a selective agonist at presynaptic imidazoline receptors) proved to be considerably less potent in inhibiting tritium overflow evoked by high K⁺ than by electrical stimulation, whereas moxonidine (in rabbit aorta a selective agonist at presynaptic ₂-adrenoceptors) exhibited similar potency in inhibiting the overflow evoked by both methods of stimulation.It is concluded that noradrenaline release in the rabbit aorta is inhibited via both ₂-autoceptors and presynaptic imidazoline receptors which can be activated by the endogenous imidazoline receptor ligand agmatine. The occurrence of such an ₂-adrenoceptor-independent mechanism is compatible with the ability of K⁺ ions to attenuate the inhibitory effect of an imidazoline receptor agonist but not of an ₂-adrenoceptor agonist, since susceptibility to K⁺ ions has been suggested to be a typical feature of imidazoline recognition sites. The presynaptic imidazoline receptor in rabbit aorta appears to be identical with the previously characterized presynaptic imidazoline receptor in rabbit pulmonary artery, but differs clearly from the I₁ and I₂ binding sites in the bovine adrenal medulla.     

野罂粟生物碱单体心血管效应的构效关系

目的：观察野罂粟总生物碱中八种生物碱单体心血管应的构效关系。方法：采用离体实验观察单体对ＫＣｌ所致兔胸主动脉环收缩的影响,并以Ｖｅｒ 作对照。结果：野罂粟碱（ｎｕｄｉｃａｕｌｉｎｅ,Ⅰ）、瑞芙热米定（ｒｅｆｒａｍ ｉｄｉｎｅ,Ⅱ）、黑龙辛甲醚（ａｍ ｕｒｅｎｓｉｎｉｎｅ,Ⅳ）、黑龙辛（ａｍ ｕｒｅｎｓｉｎｅ,Ⅴ）、野罂粟醇（ａｍ ｕｒｏｌｉｎｅ,Ⅵ）和七号生物碱（Ⅶ）均可使ＫＣｌ量－ 效曲线不平行右移,最大反应压低,其ＩＣ５０分别为０．２０,０．８０,０．１６,０．６０,０．６０,０．１６ｍ ｍ ｏｌ·Ｌ－ １。结论：野罂粟碱类（Ⅱ,Ⅳ,Ⅴ,Ⅶ）对经ＰＤＣ钙内流抑制效果较强,其中以Ⅱ作用最强;原阿朴菲类（Ⅵ,ⅧＡ,Ｘ）的抑制作用较弱     

不同方法制作犬腹主动脉瘤模型的比较

目的：探讨用于检验带膜记忆合金支架血管腔内搭桥治疗动脉瘤的模型。方法：分别以实验动物腹直肌后鞘、Ｄａｃｒｏｎ补片、不同口径的Ｄａｃｒｏｎ人血管及球囊导管材料,采用四种不同手术方法制作腹主动脉瘤模型。结果：１１例动物１０例模型制作成功,１例死亡,１月后造影检查发现９例的动脉瘤模型形态满意,１例动脉脉瘤扩张程度较差。结论;以腹阗甩垢鞘为材料制作动脉瘤模型具有取材方便,操作简便、不易漏血、无异物反应的优     

戈米辛J和异型南五味子丁素对大鼠胸主动脉的作用

目的研究由南五味子属药用植物分离的戈米辛Ｊ（ｇｏｍｉｓｉｎＪ,ＧＪ）和异型南五味子丁素（ｈｅｔｅｒｏｃｌｉｔｉｎＤ,ＨＤ）对血管平滑肌的作用。方法采用离体大鼠胸主动脉标本,观察他们对高钾去极化收缩和对ＣａＣｌ２、ＮＡ量效曲线的影响。结果ＧＪ和ＨＤ能抑制ＫＣｌ所致的收缩,其ＩＣ５０（９５％可信限）分别为３．８（２．４～５．９）和７．５（１．４～３９）μｍｏｌ／Ｌ;ＧＪ和ＨＤ能使ＣａＣｌ２量效曲线右移,最大效应降低,其ｐＤ′２值分别为５．１３±０．０７和４．７７±０．１８;ＧＪ和ＨＤ也可使ＮＡ量效曲线右移和最大效应降低,其ｐＤ′２值分别为３．７２±０．２３和３．３１±０．２７。结论ＧＪ和ＨＤ能抑制ＫＣｌ、ＣａＣｌ２和ＮＡ产生的血管收缩,而且对ＣａＣｌ２的致缩作用强于对ＮＡ的收缩作用,提示他们具有钙拮抗活性。     

多脏器微栓塞病细胞综合征动物实验模型──定义、判断标准、发生机制及其与临床的关系

利用健康杂交犬制作了多脏器微栓塞病细胞综合征（ＰＯＭＳ）模型,观察在不同时限、不同组织器官造成的病理生理改变。从中发现,钳夹腹主动脉阻断血流后,其供血器官都发生了ＲＯＭＳ,且不同器官的功能与结构损害有发生时间和程度的不同,但均有不同程度的微栓塞形成趋势,这有助对“多脏器衰竭”概念认识的深化。     

多沙唑嗪及其手性对映体对离体兔血管α_1 受体的拮抗特性(英文)

目的　分析α1 肾上腺素受体阻断药多沙唑嗪手性对映体对兔胸主动脉和颈总动脉的选择性作用 ,以探讨作为良性前列腺增生症治疗药物的可能性。方法　测定去甲肾上腺素 (NE)诱发兔离体胸主动脉和颈总动脉收缩反应 ,并采用Schild作图法计算rac 多沙唑嗪、R 多沙唑嗪和S 多沙唑嗪的pA2 值。结果　在兔胸主动脉和颈总动脉 ,0 .0 3 ,0 .1和 0 .3μmol·L-1 的rac 多沙唑嗪、R 多沙唑嗪和S 多沙唑嗪均使NE诱发的血管收缩反应量效曲线平行右移 ,Emax不变 ;由Schild作图法计算得到的多沙唑嗪及其手性对映体的斜率值 ,经统计学分析符合竞争性拮抗。3种拮抗剂pA2 值的强度顺序为 :R 多沙唑嗪 >rac 多沙唑嗪 >S 多沙唑嗪。结论　与多沙唑嗪及其手性对映体对人前列腺组织作用的报道结果不同 ,S 多沙唑嗪对兔胸主动脉和颈总动脉α1 肾上腺素受体拮抗作用的选择性显著低于rac 多沙唑嗪和R 多沙唑嗪     

巴曲酶的扩血管作用及其机制探讨

目的研究巴曲酶对血管张力的影响及其可能机制。方法离体大鼠主动脉环测定张力，主动脉薄片孵育测定ＮＯ生成、血管一氧化氮合酶（ＮＯＳ）活性与Ｌ－精氨酸（Ｌ－Ａｒｇ）转运。结果巴曲酶（０．１～２０Ｂｕ·Ｌ－１）浓度依赖性扩张大鼠离体主动脉环，去内皮血管对巴曲酶的舒张反应明显低于内皮完整血管（Ｐ＜０．０１），最大舒张反应分别为４０．１％±２１．９％和８８．１％±４．２％（Ｐ＜０．０１）。巴曲酶（１０Ｂｕ·Ｌ－１）刺激孵育主动脉产生ＮＯ－２增加１２８％（Ｐ＜０．０１），固有型ＮＯＳ（ｃＮＯＳ）和总ＮＯＳ（ｔＮＯＳ）活性分别增加２．０倍和４０．０％（Ｐ值均小于０．０１），诱导型ＮＯＳ（ｉＮＯＳ）活性无显著变化（Ｐ＞０．０５）。血管壁对Ｌ－Ａｒｇ的转运呈高和低亲和两种方式，巴曲酶（１０Ｂｕ·Ｌ－１）可使其最大转运速率Ｖｍａｘ分别增加８３．８％和４７．４％（Ｐ＜０．０１）。结论巴曲酶的内皮依赖的扩血管作用通过Ｌ－Ａｒｇ／ＮＯ途径，巴曲酶增加血管壁Ｌ－Ａｒｇ的转运和激活ＮＯＳ，使ＮＯ生成增加     

Follow-up of patients with previous treatment for coarctation of the thoracic aorta: comparison between contrast-enhanced MR angiography and fast spin-echo MR imaging

Regular follow-up is required in patients with previous intervention for coarctation of the aorta to detect recoarctation or aneurysm formation. In this study we describe the findings encountered on routine follow-up exams and we compare the use of contrast-enhanced 3D MR angiography (CE MRA) with fast spin-echo MRI (FSE) to study the thoracic aorta after previous intervention. In 51 consecutive patients previously treated for aortic coarctation, 74 MR studies of the thoracic aorta were performed during a 2-year period using CE MRA and FSE MRI. The thoracic aorta was evaluated for abnormalities of course, caliber, shape, and pathology of side branches. The CE MRA and FSE MRI studies were evaluated side by side by consensus of two reviewers evaluating which MR technique depicted the abnormalities of the thoracic aorta the best. Of 74 exams, six clinically important abnormalities were found: four aneurysms and two restenoses. Two small pseudoaneurysms were missed on the FSE studies. Contrast-enhanced MRA was judged to visualize aortic abnormalities better than FSE (47 of 74 MR studies) especially for the transverse aortic arch, coarctation site, left subclavian artery, and aortic arch configuration. For the ascending aorta and distal descending aorta, CE MRA and FSE performed equally well. Aortic diameters measured at four levels in the first 18 MRI studies showed no significant differences in diameter when measured by FSE or CE MRA (p = not significant). Clinically important abnormalities, such as aneurysm formation and restenosis, can be present years after treatment for aortic coarctation. In the regular follow-up of these patients, CE MRA may provide additional diagnostic information compared with FSE and should be included as part of the routine exam. Received: 3 April 2000; Revised: 5 July 2000; Accepted: 7 July 2000     

MR diagnosis of a congenital abnormality of the thoracic aorta with an aneurysm of the right subclavian artery presenting as a Horner's syndrome in an adult

Congenital abnormality of the aortic arch is a diagnosis made most of the time incidentally in childhood, unless dysphagia or respiratory disorders occur before. A case of a complex aortic arch anomaly with an aneurysm of the right subclavian artery presenting as an isolated Horner's syndrome in an adult is reported herein. Magnetic resonance imaging led to this very unusual diagnosis. Received: 17 March 1999; Revised: 15 July 1999; Accepted: 13 August 1999     

Histological findings after angioplasty using conventional balloon, radiofrequency thermal balloon, and stent for experimental aortic coarctation

Abstract Background : Use of balloon angioplasty or stent implantation has been reported to be effective in relieving coarctation of the aorta. However, restenosis frequently occurs after balloon angioplasty for native aortic coarctation in small infants, and sometimes develops after stent implantation because of vessel growth. The causes of restenosis remain uncertain. The purpose of this study was to assess the histologic differences in vascular responses to angioplasty using conventional balloon, radiofrequency thermal balloon (RFTB), or stent for experimental aortic coarctation. Methods : The authors surgically created an aortic coarctation model using 14 puppies. Angioplasty using conventional balloon, RFTB, or stent was performed 1 month after the initial operation. At the acute or chronic phase after angioplasty, the animals were killed and histologic studies were performed. Results : More vascular injuries were noted in the specimens from animals undergoing conventional angioplasty than in those with RFTB or stent. However, neointimal hyperplasia was seen more often after RFTB or stent because of the proliferation of smooth muscle cells from the tunica media, caused by secretion of growth factors. Apoptosis reached a peak 1?2 weeks after angioplasty, regardless of the type of intervention. Conclusions : The authors conclude that angioplasty with RFTB or stent can provide relatively small injuries in the vessel wall for aortic coarctation, but care must be taken to prevent restenosis caused by intimal hyperplasia, because neointima hyperplasia is more frequent after RFTB or stent.