多塞平对离体兔基底动脉环和隐动脉环的作用

目的：观察多塞平（ｄｏｘｅｐｉｎ，Ｄｏｘ）对兔脑血管的作用．方法：采用离体兔基底动脉和隐动脉动脉环离体实验方法．结果：多塞平抑制ＫＣｌ４５．６ｍｍｏｌ·Ｌ－１和５羟色胺１０μｍｏｌ·Ｌ－１诱发的兔基底动脉环和隐动脉环收缩，其拮抗ＣａＣｌ２量效反应的ｐＤ２值分别为５．２８±０．４０和４．７６±０．１４（ｎ＝６，Ｐ＜００１）．多塞平５．８μｍｏｌ·Ｌ－１抑制在无Ｃａ２＋液中去甲肾上腺素引起的隐动脉环收缩，多塞平３０μｍｏｌ·Ｌ－１对无Ｃａ２＋液中去甲肾上腺素和恢复正常Ｃａ２＋液（１．２５ｍｍｏｌ·Ｌ－１）引起的隐动脉环收缩均有抑制作用．结论：与隐动脉环相比较，多塞平对基底动脉环具有选择性抑制作用     

双氢杨梅树皮素对兔胸主动脉条平滑肌收缩反应的影响

用兔胸主动脉条研究双氢杨梅树皮素对去甲肾上腺素，ＫＣｌ和ＣａＣｌ２所致兔胸主动脉条收缩反应量效曲线的影响。双氢杨梅树皮素能显著地抑制ＮＥ，ＫＣｌ和ＣａＣｌ２所致兔胸主动脉条的收缩，量效曲线右移，最大反应降低，对高Ｋ＾＋兔胸动脉条收缩的抑制作用明显大于ＮＥ所致兔胸主动脉条收缩的抑制作用。     

海群生对豚鼠离体气管条平滑肌收缩的影响

目的研究海群生（枸橼酸乙胺嗪,ＤＥＣ）对豚鼠离体气管条平滑肌收缩反应的影响及其作用机制。方法取气管条放入３７℃浴管的Ｋｒｅｂｓ溶液中,分别在浴液中加入药物,测定ＫＣＩ和５－羟色胺（５－ＨＴ）收缩气管条的作用和量效反应以及ＤＥＣ和维拉帕米对ＫＣｌ和５－ＨＴ作用的影响。结果ＤＥＣ能使ＫＣＩ或５－ＨＴ引起的气管条平滑肌收缩显著抑制,其ＩＣ５０值分别为５．０３ｍｍｏｌ·Ｌ－１和９．５４ｍｍｏｌ·Ｌ－１,与维拉帕米的作用相似。ＤＥＣ使ＫＣｌ和５－ＨＴ的量效曲线右移,最大反应降低,呈非竞争性拮抗,其ｐＤ２值分别为１．５５４和１．８５１,并对细胞内Ｃａ２＋释放和细胞外Ｃａ２＋内流引起的收缩有抑制作用。结论ＤＥＣ可抑制ＫＣｌ和５－ＨＴ引起的气管条平滑肌收缩,其机制可能是通过其钙拮抗作用所致。     

阿托品对兔局部脑缺血Ca2+积累和细胞水肿的作用

阿托品对兔局部脑缺血Ｃａ２＋积累和细胞水肿的作用吕爱刚胡香杰贾丹辉张贵卿可君（河南医科大学药理学教研室，郑州４５００５２）阿托品（ａｔｒｏｐｉｎｅ，Ａｔｒ）为一典型的Ｍ受体阻断剂，近年研究表明它可以选择性对抗ＫＣｌ和ＣａＣｌ２对兔基底动脉收缩作用，其...     

氟哌啶醇季铵盐衍生物对猪冠状动脉螺旋条件作用机制的探讨

目的：研究氟哌啶醇季铵盐衍生物Ｆ２对猪冠状动脉的作用及其作用机制。方法：采用去内皮的猪冠状动脉螺旋条,观察在有钙和无钙的Ｋｒｅｂｓ液中,不同浓度（０．１～１００μｍｏｌ／Ｌ）Ｆ２对预先用３０ｍｍｏｌ／Ｌ ＫＣｌ诱导冠状动脉螺旋条收缩曲线的影响,以及１０μｍｏｌ／Ｌ格列苯脲（ｇｉｌｂｅｎｃｈａｍｉｄｅ,Ｇｌｉ）对１００μｍｏｌ／Ｌ Ｆ２对抗ＫＣｌ诱导的冠状动脉条收缩作用的影响。结果：在含钙的Ｋｒｅｂｓ液中,０．１～１００μｍｏｌ／Ｌ Ｆ２均量效依赖地抑制３０ｍｍｏｌ／Ｌ ＫＣｌ诱导的冠状动脉螺旋条收缩,在无钙的Ｋｒｅｂｓ液中,１００μｍｏｌ／ＬＦ２对３０ｍｍｏｌ／Ｌ ＫＣｌ诱导的冠状动脉螺旋条收缩曲线无影响;１０μｍｏｌ／Ｌ格列苯脲不能恢复１００μｍｏｌ／ＬＦ２对抗ＫＣｌ诱导的冠状动脉条的收缩作用。结论：Ｆ２可能     

甘草酸三铵盐对兔胸注动脉条收缩反应的影响

甘草酸三铵盐（ＴＡＧＡ）非竞争性对抗去甲肾上腺素（ＮＡ）和氯化钾（ＫＣｌ）对离休兔胸主动脉条的收缩效应，ＰＤ２（ＮＡ）＝６．２４２６±０．３５０８，ＰＤ’２（ＴＡＧＡ）＝１．７８４４±０．３６４５。ＴＡＧＡ同时促进低浓度ＫＣｌ（１０ｍＭｏｌ／Ｌ）收缩动脉条件作用，表现为双向作用。ＴＡＧＡ使ＮＡ所致动脉条收缩发生舒张，且作用持久。在给ＫＣｌ之前，先给ＴＡＧＡ，ＴＡＧＡ抑制ＫＣｌ的收缩作用。     

粉防己碱对犬多种血管平滑肌的作用

观察了粉防己碱（Ｔｅｔ）对犬离体冠状动脉，脑基底动脉和肠系膜动脉平滑肌的作用。Ｔｅｔ３０μｍｏｌ·Ｌ－１对ＫＣｌ２０及６０ｍｍｏｌ·Ｌ－１去极化犬冠状动脉呈非内皮依赖性松弛。给格列本脱后，Ｔｅｔ仍可使冠状动脉松弛７４．５％．Ｔｅｔ可使ＫＣｌ所致冠状劝脉收缩的量效曲线右移，最大反应降低，ｐＤ２为４．４其－ｌｇＥＣ５０与其松弛苯福林引起的大肠系膜劝脉收缩的－ｌｇＥＣ５０相近，均为４．１Ｔｅｔ对ＫＣｌ所致犬基底动脉的收缩有明显松弛作风     

DDPH对多种介质所致豚鼠离体气管平滑肌收缩的影响

目的：研究ＤＤＰＨ对多种介质引起的豚鼠离体气管平滑肌收缩的影响。方法：离体器官平滑肌实验法。结果：不同剂量的ＤＤＰＨ可非竞争性抑制Ｈｉｓｔ，ＡＣｈ及Ｃａ＾２＋的作用，使它们的量效曲线非平行右移，最大反应变低，其ｐＤ’２值分别为４．０９，３．９５，３．９５。ＤＤＰＨ还抑制Ｋ＾＋所致气管平滑肌收缩，但作用较维拉帕米弱，它们的ＩＣ５０值分别为１１．７５和１．５８μｍｏｌ／Ｌ。结论：ＤＤＰＨ通过非竞争性Ｃ     

眼镜蛇毒直接溶解因子对兔主动脉条Ca^2＋动员的影响

在无Ｃａ＾２＋Ｋｒｅｂｓ液中，ＤＬＦ引起兔主动脉条明显收缩，加入ＣａＣｌ２能使收缩进一步增强，这些反应可被普鲁卡因抑制。用苯福林耗竭胞内Ｃａ＾２＋池后，ＤＬＦ不再引起收缩反应。ＤＬＦ引起兔主动脉环＾４５Ｃａ＾２＋外溢与内流。硝苯地平与维拉帕米能明显抑制ＤＬＦ的＾４５Ｃａ＾２＋内流作用。结果提示ＤＬＦ可能通过开放电位依赖性Ｃａ＾２＋通道引起Ｃａ＾２＋内流，并促进Ｃａ＾２＋从苯福林敏感的胞内Ｃａ＾２＋     

苦参碱对大鼠输精管的作用与激活钙通道的关系

哌唑嗪（１０μｍｏｌ·Ｌ＾－１），硝苯地平（５０ｎｍｏｌ·Ｌ＾－１）可竞争性拮抗苦参碱收缩大鼠离体输精管，ｐＡ２值分别为５．１和９．２９。维拉帕米（１μｍｏｌ·Ｌ＾－１）可非竞争性拮抗苦参碱，ｐＤ２为６．０７。苦参碱可增强ＣａＣｌ２和ＫＣｌ收缩输精管的作用，对ＫＣｌ的增强作用更显。提示苦参碱是一钙通道激动剂。     

艾叶油的呼吸系统药理研究-Ⅱ,抗过敏作用

目的：本文研究艾叶油的抗过敏作用。方法：采用致敏豚鼠气管ＳｃｈｕｌｔｚＤａｌｅ 反应,组胺或氨甲酰胆碱引起的豚鼠气管收缩,大鼠被动皮肤过敏,５羟色胺引起的大鼠皮肤毛细血管通透性增强,豚鼠肺组织释放过敏性慢反应物质（ＳＲＳＡ） ,ＳＲＳＡ 收缩豚鼠回肠等试验。结果：艾叶油抑制致敏豚鼠气管ＳｃｈｕｌｔｚＤａｌｅ 反应（ＩＣ５０ ：９８ ．６ｍｇ／Ｌ） ;１００ｍｇ／Ｌ 明显降低组胺或氨甲酰胆碱引起的豚鼠气管收缩ｐＤ２ 值;明显抑制大鼠被动皮肤过敏（ＩＤ５０ ：０ ．２２ｇ／ｋｇ） 和５羟色胺引起的大鼠皮肤毛细血管通透性增强反应（ＩＤ５０ ：０ ．５２ｇ／ｋｇ） ;抑制豚鼠肺组织释放ＳＲＳＡ（ＩＣ５０ ：４９ ．７ｍｇ／Ｌ） ;拮抗ＳＲＳＡ 对豚鼠回肠的收缩（ＩＣ５０ ：３４ ．９ｍｇ／Ｌ） 。结论：艾叶油具有抗过敏作用,对呼吸道过敏反应有保护作用,是其治疗支气管哮喘和慢性气管炎作用机制之一     

葛缕酮的气道扩张作用和呼吸道抗过敏作用

目的观察留兰香油中葛缕酮的气道扩张作用和对呼吸道介质的影响。方法用豚鼠药物引喘法、豚鼠离体气管片法、致敏豚鼠肺组织ＳＲＳ Ａ释放和拮抗ＳＲＳ Ａ、致敏豚鼠离体气管Ｓｃｈｕｌｔｚ Ｄａｌｅ反应法检测。结果葛缕酮对豚鼠药物性哮喘具有保护作用,灌胃给药延长５０％剂量为７６ｍｇ·ｋｇ－１,气雾给药为６３ｇ·Ｌ－１;对豚鼠离体气管有直接松弛作用,ｐＤ２值为４２７±００８,并有抗氨甲酰胆碱作用;能抑制致敏豚鼠肺组织ＳＲＳ Ａ的释放,ＩＣ５０为１８ｍｇ·Ｌ－１,拮抗ＳＲＳ Ａ收缩回肠的ＩＣ５０为２７ｍｇ·Ｌ－１,并能抑制致敏豚鼠离体气管的Ｓｃｈｕｌｔｚ Ｄａｌｅ反应。结论葛缕酮具有气道扩张作用和呼吸道抗过敏作用。     

Inhibition of calcium channels by harmaline and other harmala alkaloids in vascular and intestinal smooth muscles.

Effects of harmaline and other harmala alkaloids on the contractions induced in the vascular smooth muscle of rabbit aorta and intestinal smooth muscle of taenia isolated from guinea-pig caecum were examined. In rabbit isolated aorta, harmaline inhibited the sustained contraction induced by 65.4 mM K+ with an IC50 (concentration needed for 50% inhibition) of 4.6 X 10(-5) M. This inhibitory effect on high K+-induced contraction was antagonized by raising the concentration of external Ca2+ but not by Bay K 8644, a Ca2+ channel facilitator. Harmaline also inhibited the sustained contraction induced by noradrenaline (10(-6) M) with an IC50 of 7.6 X 10(-5) M. The inhibitory effects on noradrenaline-induced contractions were not antagonized by raising the external Ca2+ concentrations or by Bay K 8644. In guinea-pig taenia, harmaline inhibited the 45.4 mM K+-induced contraction with an IC50 of 6.8 X 10(-5) M and the carbachol (10(-6) M)-induced contraction with an IC50 of 7.0 X 10(-5) M. The inhibitory effects on both high K+- and carbachol-induced contractions were antagonized by raising the external Ca2+ concentrations but not by Bay K 8644. Harmaline, at the concentrations needed to inhibit the muscle contraction, inhibited the increase in 45Ca2+ uptake induced by high K+, noradrenaline and carbachol in aorta and taenia. Harmaline did not change the cellular Na+ and ATP contents in resting and high K+ stimulated taenia. Other harmala alkaloids also inhibited the contractions in these smooth muscles.(ABSTRACT TRUNCATED AT 250 WORDS)     

Antispasmodic Activity of SJ-200 (Himcospaz): An Herbal Preparation

SJ-200 (Himcospaz), an herbal preparation, was investigated for antispasmodic activity on gastrointestinal smooth muscles of guinea pig, rats, rabbits and mice. SJ-200 dosedependently inhibited acetylcholine, histamine and barium chloride-induced contraction of guinea pig ileum. It inhibited spontaneous contraction of rabbit and rat colon. Oxytocin-induced contraction of rat uterus was also inhibited. Oral administration of SJ-200 dose-dependently reduced gastric emptying in rats and intestinal transit in mice. All these findings suggest the non-specific antispasmodic activity of SJ-200 in experimental models.     

茶碱沙丁胺醇缓释片对变应性哮喘作用的研究

茶碱和沙丁胺醇伍用对卵蛋白致敏豚鼠离体气管平滑肌、肺条在抗原攻击时引起的收缩反应，均有明显抑制作用．ＩＣ５０分别为９２～２３０μｇｍＬ－１和５９～２２９μｇ·ｍＬ １．茶碱／沙丁胺醇３种剂量（１２０ｍｇ／０１６ｍｇ·ｋｇ－１，２４０ｍｇ／０３２ｍｇ·ｋｇ－１，４８０ｍｇ／０６４ｍｇ·ｋｇ－１）灌胃给药明显延长过敏性哮喘豚鼠引喘潜伏期及减少致敏麻醉豚鼠的肺溢流量增加．     

Species differences in inhibitory effect of Li+ on high K+-induced contraction in the ileal longitudinal smooth muscle

The effects of Li+ substitution for external Na+ in the medium on a 60 mN KCl (60K+)-induced contraction were compared in the ileal longitudinal smooth muscles isolated from monkey, rabbit, guinea pig and rat. Li+ substitution inhibited the 60K+-induced contraction in the ileum of all the animal species. Greater inhibitory effect was observed with the increase in external Li+ concentration and the increase in incubation period with Li+. Intracellular Li+ contents of these muscles also increased with the increase in external Li+ concentration and the incubation period. Thus, a good correlation was obtained between Li+-induced inhibition of 60K+-induced contraction and the increase in Li+ content. However, close examination revealed that the contraction in monkey and rat ileum was inhibited by much lower Li+ accumulation than that in guinea pig and rabbit ileum, suggesting the existence of species difference in the sensitivity of the ileal smooth muscle to the inhibitory effect of Li+ substitution, and a mechanism for the species differences in the inhibitory action of Li+-substitution was discussed.     

阿司匹林铜对离体兔主动脉血管条收缩的影响(英文)

目的:观察阿司匹林铜对离体免胸主动脉血管平滑肌的作用。方法:取免胸主动脉条,观察阿司匹林铜对去甲肾上腺素(NE)、KCl、CaCl_2诱导收缩作用的影响。结果:证实阿司匹林铜和对照物硫酸铜拮抗NE诱导的兔胸主动脉条收缩,IC_(50)分别为31nmol/L和0.29μmol/L,而阿司匹林本身没有拮抗作用。阿司匹林铜对KCl、CaCl_2诱导的收缩没有影响。在去内皮细胞兔胸主动脉条上,观察到相同的作用。结论:阿司匹林铜具有较强的拮抗NE诱导离体兔胸主动脉条收缩的作用,但不能拮抗KCl、CaCl_2诱导的收缩,提示阿司匹林铜通过阻断受体调控钙通道,舒张血管平滑肌。     

Calcium antagonism of enpiperate on isolated rabbit aorta strips and guinea pig ileum

Enpiperate, 4-(3, 5)-exocydopropyl-N-methylpiperidyl diphenyl hydroxy acetate, was synthesized in China. It has been shown to have no effect on the normal tension of rabbit aorta strips or contractions induced by NE. It inhibited the contraction of high K+-depolarized rabbit aorta strips at concentrations of 3.8 and 10.9 mumol/L. The same effect was seen on isolated guinea pig ileum, at a concentration of 10.9 mumol/L, which was depolarized by Ca2+ free high K+ Locke-Ringer's solution and the contraction was extragenous Ca2+ dependent. The inhibition was overcome by increasing the extracellular Ca2+ concentration. In the presence of EDTA (0.1 mmol/L), the NE induced intracellular Ca2+ dependent contraction was inhibited by enpiperate (3.8, 10.9 mumol/L), although no significant difference was found between enpiperate and papaverine. It is suggested that enpiperate is a calcium antagonist and that the antagonism is carried out by blocking the potential dependent calcium channel (PDC) in the membrane of vascular smooth muscles. A intracellular calcium antagonistic action may also be involved.     

Prompt effect of progesterone on the adrenergic response of smooth muscles

The contractile effects of epinephrine on the uterus and ductus deferens of the rabbit and the ductus deferens of the monkey were inhibited by the preincubation with progesterone (6.4 X 10(-5) M) for 1 or 3 min in Locke-Ringer solution. Epinephrine relaxed the guinea pig uterus and taenia caecum. The relaxant effects were enhanced by preincubation with progesterone. Their effects were in a dose-dependent manner. There was no apparent change in the number and affinity of alpha-adrenergic receptors in the uterus of rabbits and the ductus deferens of guinea pigs during the incubation with progesterone. Progesterone has no direct effect on alpha-adrenergic receptors. All smooth muscles yielded reproducible contractile reactions to Ca2+ when maintained in depolarizing Tyrode's solution containing K+ (40 mmol/l). Their concentration-response curves were inhibited by preincubation with progesterone (6.4 X 10(-5) M), and they were shifted to the right in a concentration-dependent manner. Established Ca2+-induced contractions were rapidly relaxed by the addition of progesterone (6.4 X 10(-5) M). It suggests that progesterone directly affects the plasma membrane and inhibits the voltage-dependent Ca2+ channel and then inhibits smooth muscle contraction.