碘杂环化合物IHC-66对离体子宫平滑肌的作用

本文观察了碘杂环化合物IHC-66对离体子宫平滑肌的作用,发现IHC-66可兴奋大鼠、豚鼠离体子宫平滑肌,但对离体兔子宫的兴奋作用不规律。同时观察了消炎痛对IHC-66兴奋子宫平滑肌作用的影响,结果表明,浴管内加入消炎痛20μg/ml,可拮抗IHC-66对豚鼠子宫的兴奋作用。     

六种甾体化合物对离体胎盘滋养层、蜕膜和卵巢颗粒细胞的影响

本文为探讨NET,NETO,NET-AC,NETO-AC,NGT和NGTO的抗着床原理,以体外培养方法研究了这六种甾体药物对离体人胎盘滋养层、蜕膜和大鼠离体卵巢颗粒细胞的形态学的直接影响。实验结果发现,当培养液内加入NET,NET-AC和NGT时对上述细胞无明显影响;当培养液内加入NETO,NETO-AC及NGTO的浓度为50μg/ml及100μg/ml时,在胎盘滋养层细胞培养过程中,可见细胞生长受抑制,细胞被破坏,其中以NGTO 100μg/ml作用更为明显。当NETO及NETO-AC的浓度为100μg/ml及NGTO的浓度为50μg/ml和100μg/ml时对离体蜕膜细胞也有损坏作用。六种甾体药物对大鼠离体卵巢颗粒细胞均无明显作用。     

皂苷提取物宫血宁缩宫作用与细胞外钙内流关系的研究

目的探讨皂苷类提取物宫血宁引起的大鼠离体子宫收缩作用与细胞外钙内流的关系。方法应用离体子宫张力测定法,观察不同Ca2+浓度及Ca2+通道阻滞剂对宫血宁引起的大鼠离体子宫收缩作用的影响。结果无钙的台氏平衡液中,宫血宁的浓度从25μg/ml增至200μg/ml都不能引起大鼠离体子宫节律性收缩;在半钙和全钙的台氏平衡液中宫血宁能引起大鼠离体子宫节律性收缩,并与宫血宁的剂量呈显著正相关;Ca2+通道阻滞剂能明显抑制宫血宁和缩宫素引起的子宫收缩,但同缩宫素相比,宫血宁引起的子宫收缩对Ca2+通道阻滞剂更敏感。结论皂苷类提取物宫血宁的缩宫作用依赖于细胞外钙的存在,其作用机制可能是通过促进平滑肌细胞外钙内流来实现的。     

怀牛膝总皂甙对离体大鼠子宫的兴奋作用及机理研究

研究表明，怀牛膝总皂甙（ＡＢＳ０．１～０．４ｍｇ／ｍｌ）对离体大鼠子宫产生明显的浓度依赖性兴奋作用，５－ＨＴ（１０μｇ／ｍｌ）可明显增强ＡＢＳ的作用。ＡＢＳ和５－ＨＴ均使高Ｋ＋去极化后的高体大鼠子宫产生依细胞内Ｃａ２＋性和依细胞外Ｃａ２＋性收缩；氯两嗪（０．５μｇ／ｍｌ）或氟丙嗪（０．４μｇ／ｍｌ）和消炎痛（２０μｇ／ｍｌ）合用均明显拮抗ＡＢＳ的作用。     

雪莲多糖对离体大鼠子宫的作用

雪莲是菊科青木香属多年生草本植物。古籍记载,有除寒、状阳、调经、止血等作用。近年研究证明雪莲煎剂有抗炎、加强蟾蜍心肌收缩力、降低兔血压、抑制兔回肠活动、兴奋离体和在体兔子宫、终止小鼠和家兔早期妊娠等作用。我院化学教研室从雪南省德钦县产的水母雪莲花(Saussurea medusa Maxim.)中分离出多糖单一组分,已证明对小鼠有明显的终止妊娠作用。本文研究了雪莲多糖(简称SPS)对各期离体大鼠子宫的作用。并观察前列腺素E_2(PGE_2)和消炎痛对雪莲多糖兴奋子宫作用的影响。     

吡喹酮及其对映异构体对离体大鼠心房肌生理特性的影响

吡喹酮(praziquantel,PQT)对心肌生理特性的影响有立体选择性。(-)-PQT对离体大鼠左心房的正性肌力作用的效能和强度均比(+)-PQT和(±)-PQT小。用维拉帕米可明显减弱PQT及其对映异构体的正性肌力作用。在浓度为100μmol/1时,PQT及其对映异构体对离体大鼠右心房均有负性频率作用,而当30μmol/1时仅(+)-PQT对频率有明显影响。它们尚可诱发右心房心律失常,其发生率以(+)-PQT最高,(-)-PQT最低,(±)-PQT居中。(+)-和(±)-PQT可明显缩短左房不应期。(+)-PQT还可明显降低左房自律性,而(-)-PQT对不应期,自律性均无影响。     

紫贻贝水提取物对大鼠离体子宫、平滑肌的作用

本文首次报道了紫贻贝水提取液对大鼠离体子宫、平滑肌的作用及其作用机制。结果表明:①贻贝水提取液对大鼠离体子宫有明显收缩作用,对场刺激输精管引起的收缩有明显增强作用,而这些收缩作用可被α—受体阻断剂酚妥拉明所对抗与阻断。②对大鼠离体胃条与回肠平滑肌有松弛作用,而这种松弛作用也可被α—受体阻断剂酚妥拉明所对抗与阻断。③对蟾蜍血管灌注则流量减少从47±11dr/min降至24±7dr/min,(P<0.05),故表明紫贻贝水提取液对大鼠离体子宫呈收缩作用,而这种作用是由于兴奋了α—受体的结果。     

甲巯丙脯酸增强消心痛引起的冠脉扩张

用离体大鼠心脏模型研究甲巯丙脯酸对消心痛(ISDN)引起血管扩张反应的影响,并与半胱胺酸(无血管紧张素转移酶活性的含巯基化合物)和Ramiprilate(不含巯基的血管紧张素转移酶抑制剂)进行疗效比较.将雄性大鼠的离体心脏随机分为4组,每组6个,按Langendorff方法在60mmHg恒压下灌注,平衡后,离体心脏分别用不同药物灌注,每次灌注10min,再清洗10min.A组用8μg/ml甲巯丙脯酸或40μg/ml     

二甲基氨氯吡咪对正常大鼠离体心功能的影响

目的研究二甲基氨氯吡咪(dimethylamiloride,DMA)对正常大鼠离体心功能的影响及特点。方法采用Langendorff心脏灌流方法观察DMA对正常大鼠离体心脏功能的影响。结果①在Langendorff灌流的大鼠心脏,DMA(2.5~20μmol/L)能增强正常大鼠离体心脏功能。2.5μmol/L DMA对心功能各项指标左室收缩压(LVSP)-左室舒张压(LVDP)、左室压最大上升速率(+dp/dtmax)、左室压最大下降速度(-dp/dtmax)的增强幅度分别为8.17%、5.22%、10.15%;5μmol/L DMA的增强幅度分别为7.59%、8.84%、10.93%,;10μmol/LDMA的增强幅度分别为9.27%、10.53%、11.48%;20μmol/L DMA的增强幅度分别为8.37%、11.19%、13.31%。②在离体心脏,DMA在用药2 min后明显起效,6 min时作用达高峰,之后作用逐渐减弱,10 min作用消失。结论DMA(2.5~20μmol/L)能增强正常大鼠离体心功能,产生正性肌力作用。     

N-(3’,4’,5’-三甲氧基肉桂酰)邻氨基苯甲酸对抗原诱发的离体豚鼠回肠收缩、大鼠肥大细胞脱颗粒及组胺释放的影响

实验证明 N-(3′,4′,5′-三甲氧基肉桂酰)邻氨基苯甲酸(TOA)管内浓度80μg/ml 能明显抑制抗原诱发的主动致敏豚鼠离体回肠收缩。TOA 管内浓度25和50μg/ml 能显著抑制亲同种细胞抗体介导的大鼠肠系膜肥大细胞脱颗粒和腹腔肥大细胞组胺释放。     

利凡诺对豚鼠子宫兴奋作用机制的初步研究

利凡诺是常用的中孕引产药。但它对实验动物子宫的作用并不完全一致。对豚鼠子宫以兴奋为主,而对家兔、大和小白鼠子宫则有时兴奋,有时抑制,兴奋与抑制的比例并无显著差别。这些结果提示利凡诺可能不是直接作用于子宫而是通过间接机制。本文采用豚鼠     

Effect of urethane on synaptic and amino acid-induced excitation in isolated spinal cord preparations

Urethane (50 mM) produced a non-selective antagonism of depolarizations evoked by excitant amino acids or carbachol recorded from ventral roots of isolated spinal cord preparations of the frog or immature rat. Depolarizing responses to substance P or eledoisin-related-peptide were either unaffected or potentiated by this concentration of urethane. The threshold level for depression of dorsal to ventral root transmission was 10 mM urethane and transmission was completely blocked at 70-100 mM urethane. It is suggested that post-junctional blockade of the actions of excitant amino acids may be important in the anaesthetic action of urethane.     

大子蒿对下丘脑—垂体—肾上腺皮质系统的影响

Pharmacological effects of Tibetan medical plant Artemisia sieversiana on the hypothalamo-pituitary-adrenocortical axis are reported in present paper.The alcoholic (60%) extract of A. sieversiana (AEAS) injected intraperitoneally at 460 mg/kg in rats enhanced significantly the levels of corticosterone of the peripheral and adrenal venous plasma from 41±1.8 to 78±2.1 μg/100ml and from 1220±64 to 2020±56μg/ml (mean+SE) respectively. Administrations of AEAS at 3 g/kg orally or 460 mg/kg/day ip (for 6 days) also produced a marked increase. However, the increase was not detected in hypophysectomized rats. The effect of AEAS could be blocked completely by morphine in combination with pentobarbital, but not by pentobarbital alone, nor by prior injection of dexamethasone, chlorpromazine or cortisone acetate in rats under pentobarbital sodium anesthesia.We also demonstrated that in the same doses AEAS (ip) markedly increased the 5-HT content in the diencephalon of rats but not the 5-HIAA and NE contents. The action of AEAS which had been shown to result in the activation of the pituitary-adrenocortical system, was not abolished by prior treatment with reserpine at 4 mg/kg, but was completly blocked by the injection of atropine (250 μg) into the lateral ventricle of the brain. In intact rats AEAS produced a decrease of the amount of GABA in the diencephalon and significant increase of glutamine levels, while in adrenolectomized rats the effects were reversed.It is considered that the antiphlogistic effects of AEAS are due to its activation of ACh and 5-HT system and inhibition of GABA in the hypothalamus. Through the regulative action of the neurotransmitters, CRF is further activated, and, finally, it leads to the serial response of the pituitary-adrenocortical system.     

Effect of methysergide and indomethacin on the anaphylactic contraction of the rat isolated uterus (Schultz-Dale response)

The anaphylactic contraction (Schultz-Dale response) of the isolated uterus from actively sensitized rats was partially suppressed by methysergide, 1.5 mug/ml. Although the inhibitory effect of indomethacin, 3.5 mug/ml, was only slight, the combination of indomethacin and methysergide abolished the response almost completely. These observations indicate that, although serotonin must be the primary mediator of tha anaphylactic uterine response, prostaglandin is also involved. Metiamide, a histamine H2-receptor antagonist, 10 mug/ml, did not affect the anaphylactic response, suggesting that histamine was not released in amounts sufficient to counteract the uterine contracting mediators.     

Factors involved in the time course of response to acetylcholine in mesenteric arteries from spontaneously hypertensive rats.

The time course of the response to prolonged application of acetylcholine in mesenteric arteries from stroke-prone spontaneously hypertensive rats (SHRSP) and Wistar Kyoto rats (WKY) was compared. Only a relaxing response, which was blocked by N(omega)-nitro-L-arginine (L-NOARG), was observed after the prolonged application of a low concentration of acetylcholine (10(-8) M) in both preparations; the response was impaired in SHRSP preparations. Prolonged application of a high concentration of acetylcholine (10(-5) M) induced a second contractile response after a first relaxing response in SHRSP preparations under basal conditions and in WKY preparations in the presence of L-NOARG. This contractile response was attenuated by indomethacin. In the presence of a combination of apamin and charybdotoxin, the relaxing response to the high concentration of acetylcholine was reduced and a contractile response, which was abolished by indomethacin, appeared. In the presence of all of these blockers, a contractile response, which was blocked by cyclo(D-alpha-aspartyl-L-propyl-D-valyl-L-leucyl-D-tryptophyl) (BQ-123), was observed in preparations from WKY but not in preparations from SHRSP. Results indicate that prolonged application of acetylcholine in rat mesenteric arteries induces the release of endothelium-derived relaxing, contracting, hyperpolarizing factors and endothelin-1, and that the mode of action differs between preparations from WKY and SHRSP.     

Marine toxins from the Pacific—IX Some effects of ciguatoxin on isolated mammalian atria

Ciguatoxin produced an initial negative inotropic and chronotropic effect which was followed by a positive inotropic and chronotropic effect on the isolated rat atria. The initial depression could be effectively blocked by atropine (1 × 10⁻⁷ g per ml), and partially blocked by hexamethonium or hemicholinium-3 (2 × 10⁻⁵ g per ml). The positive inotropic and chronotropic action of ciguatoxin was reduced by pretreating the atria with MJ-1999 (1 × 10⁻⁶ g per ml) or guanethidine (1 × 10⁻⁶ g per ml). Abolition of the response to ciguatoxin could also be accomplished with a single dose of 2 mg per kg of reserpine given to the rat 24 hr before isolating the heart. It is not yet possible to correlate inotropic and chronotropic effects of the toxin with the release of catecholamines, but it seems likely that excitatory effect of the toxin may be elicited by a release of catecholamines from their stores.     

古罗酸伯喹对豚鼠心肌生物电活动的作用

用细胞内微电极技术,发现古罗酸伯喹6μg/ml使心肌细胞AP之V_(max)降低(p相似文献   

反相高效液相色谱法测定栀子及其制剂中栀子苷的含量

目的 :建立以反相高效液相色谱法测定栀子及其制剂中栀子苷含量的方法。方法 :以KromasilC18 为色谱柱 ,乙腈 -水(10∶90)为流动相 ,检测波长为238nm。结果 :栀子苷的线性范围为0 596μg～2 98μg(r=0 9997)。栀子全果、栀子皮、栀子仁、加味逍遥丸和清开灵注射液中栀子苷含量分别为41 8、12 3、67 3、4 26mg/g和0 316mg/ml,栀子、加味逍遥丸和清开灵注射液的平均回收率与相对标准差分别为99 35 %、0 52 % ;99 51%、0 72 % ;99 57 %、0 73 %。结论 :本法操作简便 ,测定结果准确 ,精密度和稳定性良好 ,可用于栀子及其制剂中栀子苷的含量测定。     

In vivo method for quantitation of anti-platelet potency of drugs

Summary Aortic strips from atherosclerotic rabbits or Achilles tendons from healthy rabbits were superfused with blood (3 ml/min) from anaesthetized and heparinized cats, while blood was returned to the venous system of animals. The superfused tissues gained in weight because of deposition of platelet thrombi on their surface. This gain in weight was continuously monitored and quantified. Forty minutes after intravenous administration of indomethacin (14 mg/kg), aspirin (7 mg/kg) or nictindole (2 mg/kg) the formation of platelet deposits was reduced by half. Three hours after i.v. administration of each drug at a dose of 20 mg/kg the remaining anti-platelet activities were 92% for aspirin, 59% for indomethacin and 18% for nictindole as compared to their antithrombotic action, which was recorded 40 min after their administration. Thrombogenesis was also prevented by a direct infusion of nictindole (50 ng/ml) or indomethacin (2000 ng/ml) into a stream of superfusing blood. Thereby our method enables us to quantify in vivo anti-aggregating potency of drugs, to estimate the duration of this action, and to compare their in vitro and in vivo aggregation-inhibitory activities.