The in vitro pharmacological profile of KR31080, a nonpeptide AT1 receptor antagonist

Summary— KR31080 (2-butyl-5-methyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b] pyridine) is a potent inhibitor of angiotensin type 1 (AT₁) receptors in rabbit aorta and human recombinant AT₁ receptors. In the isolated rabbit thoracic aorta, KR31080 caused a nonparallel shift to the right of the concentration-response curves to angiotensin II (All) with decreased maximal response (pD'₂ = 10.1 ± 0.1), but had no effect on the contractile response induced by norepinephrine. KR31080 inhibited specific [¹²⁵I]AII binding to rabbit aortic membranes (AT, receptors) and [¹²⁵I][Sar¹, Ile⁸]AII binding to human recombinant AT₁ receptors in a concentration-dependent manner with IC₅₀ values of 0.84 ± 0.08 nM and 1.92 ± 0.15 nM, respectively, but did not inhibit specific [¹²⁵I)AII binding to bovine cerebellum membranes (ÀT₂ receptors). In the Scatchard analysis, KR31080 interacted with rabbit aortic AT₁ receptors in a competitive manner, similar to losartan. These results demonstrate that KR31080 is a potent and AT₁ selective angiotensin receptor antagonist which exerts a competitive antagonism in the [¹²⁵I]AII binding assay and insurmountable AT₁ receptor antagonism in the functional study.     

Constraints on Social Activities of Care-Givers: A Sociological Perspective

Newer policies of community care for those with disabilities have resulted in the home becoming the usual site of care. Policy makers must now give attention to the needs of those at home giving this care. This article explores the constraints on sociability opportunities of 73 mothers who were caring for children with disabilities. These opportunities are often built into leisure pursuits for women without caring responsibilities. However, choice of out-of-house leisure activity was circumscribed for the mothers in this study and their reported leisure activities revolved around home and neighbourhood. Even these sites offered limited scope for sociability because of the way in which caring affected domestic space and because of the characteristics of the modern Australian suburb. It is argued in this paper that personal time and personal domestic space are needed by care-givers so their sociability needs can be fulfilled. An understanding of the constraints imposed by use of the home as a place of care may make possible the planning of a rearrangement of domestic space to increase sociability opportunities for carers.     

Anatomic bases of tongue flaps

Summary The morphological structure of the lingual a. was studied in 50 dissected and 14 vascular cast specimens. The course of this artery is divided into 4 segments: the original segment, the segment within hyoglossus, the ascending and the horizontal segments of the deep lingual a. The root of the tongue is supplied by 2 to 3 root branches of the lingual a., the ascending palatine a. and the tonsillar a. The body of the tongue is nourished on average by 25 arterial branches from the deep lingual a. The ventral surface of the tongue, as well as the sublingual gland and the floor of the mouth, is supplied by the sublingual a. The termination of the lingual a. anastomoses with the submental branch of the facial a. to form the lingual frenal a. Except for a submucous arterial network on the dorsum of the tongue, all blood vessels are separated completely by the lingual septum, through which arterial anastomoses (2.0 mm in diameter) can be found occasionally.This work was supported by the National Natural Science Fund     

小儿内伤头痛辨治

74例小儿慢性头痛经辨证治疗,显效80.95%,好转16.67%,无效2.38%。痰浊头痛二陈汤或半夏白术天麻汤加减;肾虚头痛,杞菊地黄汤加减;淤血头痛,补阳还五汤;气血虚头痛八珍汤加减。指出了小儿内伤头痛的病因病机,并指出脑电图,脑阻抗血流图、CT、甲皱微循环可做为此病的诊断及疗效指标。     

长江北三角洲抗倭碑文的史料意义

长江北三角平原上所遗存的二十余种记及明代倭患和抗倭战争的古代的碑石文献 ,在数量上据全国各抗倭战区所存的同类文献之首。在内容上 ,对补充旧史的阙失、订正传误、佐证史实、深化研究也有诸多帮助 ,尤其是对廓正对倭寇与倭患问题的认识有着积极的意义     

Enucleation combined with orbital implants for malignant melanoma of the uvea

Advanced malignant melanomas of the uvea unsuited for an eye salvaging approach require enucleation of the tumor containing eye. A series of 68 patients is reported who underwent enucleation combined with insertion of a spherical dura-encased implant after 30 Gray pre-irridiation therapy of the orbit. Postoperative results with special attention to cosmetic outcome and motility of the prosthesis suggest that the insertion of an orbital implant should be preferred to the enucleation with no implant.     

经尿道前列腺电切气化术治疗前列腺增生568例报告

目的 :进一步探讨前列腺增生 (BPH)的有效手术新方法。方法 :采用经尿道前列腺电切术和气化术治疗BPH患者 5 6 8例。结果 :疗效满意 ,术后 3～ 6个月随访 ,国际前列腺症状评分 (IPSS) 8.5± 1.5分 ;最大尿流率 (Q max) 2 0 .5± 4 .5ml s,剩余尿量 2 9.1± 14 .2ml,未出现严重并发症。结论 :将电切和气化相结合行经尿道前列腺切除术是一种安全性高、并发症少、疗效确切的新手术方法 ,具有操作易掌握、出血少、速度快、安全可靠等优点。     

经T管窦道网篮取石治疗胆道残余结石

目的：采用非手术方法治疗胆道残余结石，方法：应用介入方法经T管窦道网蓝取石，结果：治疗39例。取得了满意的疗效。成功率达92．3％，结论：经T管窦道网蓝取石治疗胆道残余结石，是一种简便，安全、有效的治疗方法。     

以病人选择医生为契机 全力推进人事分配制度改革

介绍了邯郸市中心医院在病人选医生中,努力完善制度,提高素质,深化内容,并以此为突破口,建立了灵活、高效的人事分配制度.用较为低廉的医疗费用,为人民群众提供了较好的医疗服务.     

甲状腺切除术中喉返神经损伤的预防

目的：探讨降低喉返神经损伤的方法。方法：2005年9月-2007年1月共有375例甲状腺手术患者，对其喉返神经损伤进行分析。结果：375例病人中有5例喉返神经损伤，其中甲状腺腺瘤3例，桥本甲状腺炎1例，甲状腺癌1例，损伤后立即行喉镜检查示声带处于外展位。给予营养神经治疗，15 d-3个月后完全恢复，喉镜检查示声带正常。结论：喉返神经损伤可以预防，关键是术者应熟悉喉返神经的解剖结构和变异，熟悉其与周围组织及血管的关系，要有手术区域的组织结构特别是喉返神经走行的“立体影像”。